Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 20 de 39
Filtrar
1.
J Pak Med Assoc ; 72(9): 1760-1765, 2022 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-36280971

RESUMO

OBJECTIVE: To characterize human liver tissues by demonstrating the ability of machine vision, and to propose a new auto-generated report based on texture analysis that may work with co-occurrence matrix statistics. METHODS: The retrospective study was conducted at Bahawal Victoria Hospital (BVH), Bahawalpur, Pakistan, and comprised clinically verified computed tomography imaging data between October 2018 and September 2020. The image samples and related data were used to segregate classes 1-4. Appropriate image classes belonging to the same disease were trained to confirm the abnormalities in liver tissues using supervised learning methods, principal component analysis, linear discriminant analysis, and non-linear discriminant analysis. Robust and reliable texture features were investigated by generating testing classes. Overall performance of the presented machine vision approach was analyzed using four parameters; precision, recall/sensitivity, F1-score, and accuracy. Statistical analysis was done using B11 software. RESULTS: There were 312 image samples from 71 patients; 51(71.8%) males and 20(28.2%) females. Among the patients, 19(26.7%) had abscess, 15(21.1%) had metastatic disease, 23(32.4%) had tumour necrosis, 6(8.5%) had vascular disorder, and 8(11.3%) were normal. Principal component analysis, linear discriminant analysis, and non-linear discriminant analysis showed high >97.86% values, but the discrimination rate was 100% for class 4. CONCLUSIONS: Abnormalities in the human liver could be discriminated and diagnosed by texture analysis techniques using second-order statistics that may assist the radiologist and medical physicists in predicting the severity and proliferation of abnormalities in liver diseases.


Assuntos
Algoritmos , Tomografia Computadorizada por Raios X , Masculino , Feminino , Humanos , Estudos Retrospectivos , Tomografia Computadorizada por Raios X/métodos , Fígado/diagnóstico por imagem , Análise de Componente Principal
2.
Transp Policy (Oxf) ; 108: 21-33, 2021 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-36568479

RESUMO

Travel behavior has been affected around the world since the eruption of corona virus disease (COVID-19). Several industries including transportation industry have been hard hit by the pandemic. As the virus is transmitted through close contact with infected people, number of outdoor trips has reduced causing roads and public transport to be less crowded than before. In order to develop transport-related policies for the post COVID-19 world, it is necessary to explore how the pandemic has affected the travel behavior pattern. This study explored the influence of the COVID-19 pandemic on travel pattern and mode preferences in Pakistan using a questionnaire survey. The results showed significant shift in primary traveling purpose from work and studying to shopping during the pandemic. Number of trips performed for non-commuting purposes were also significantly different before and during the pandemic. A significant modal shift from motorbike to non-motorized modes of travel was found for distances less than 5 km. For longer distances, people shifted from public transport to private car. These findings suggest that past policies regarding different modes may be revisited in the post COVID-19 world. The statistical tests performed on the factors affecting mode choices indicated that the respondents put more priority on pandemic-related items such as infection concern, social distance, hand sanitizers' availability, and cleanliness, etc., during the pandemic. The findings of this study will certainly help in shaping up the policies for the post COVID-19 world especially in the developing countries.

3.
J Pak Med Assoc ; 70(11): 2039-2042, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-33341855

RESUMO

The present research study was done to determine the correlation between antibiotic susceptibility and drug prescription patterns in empirical treatment of uropathogenic Escherichia coli (E. coli) in two hospitals of district Muzaffarabad, Azad Kashmir, Pakistan. One hundred uropathogenic E. coli clinical isolates were collected from UTI patients who attended the Combined Military Hospital (CMH) and Abbas Institute of Medical Sciences (AIMS), district Muzaffarabad, AJK. All isolates were subjected to antibiotic susceptibility against seven commonly prescribed antibiotics by Kirby-Bauer disk diffusion method. However, all the E. coli isolates were susceptible to Imipenem. Eight percent and 10% of isolates from CMH and AIMS were found to be resistant against Nitrofurantoin drug respectively. Similarly, 94% and 74% isolates from CMH and 60% and 64% isolates from AIMS were found to be resistant against Co-trimoxazole and Coamoxiclave, respectively. Pipemedic acid resistance was also detected in 76% and 60% isolates from AIMS and CMH, respectively. Ciprofloxacin resistance was also observed in 54% and 36% isolates from AIMS and CMH, respectively. The finding of the study revealed that both hospitals have different drug susceptibility pattern against uropathogenic E. coli, which may be associated with patterns of drug prescription in empirical treatment of urinary tract infections. There is a vital need for appropriate development of hospital-specific antibiograms to determine appropriate empiric therapy of urinary tract infections.


Assuntos
Infecções por Escherichia coli , Infecções Urinárias , Escherichia coli Uropatogênica , Antibacterianos/farmacologia , Antibacterianos/uso terapêutico , Prescrições de Medicamentos , Farmacorresistência Bacteriana Múltipla , Infecções por Escherichia coli/tratamento farmacológico , Infecções por Escherichia coli/epidemiologia , Humanos , Testes de Sensibilidade Microbiana , Paquistão/epidemiologia , Infecções Urinárias/tratamento farmacológico , Infecções Urinárias/epidemiologia
4.
Bioorg Chem ; 85: 33-48, 2019 04.
Artigo em Inglês | MEDLINE | ID: mdl-30599411

RESUMO

Diabetes is one of the pre-dominant metabolic disorders all over the world. It is the prime reason of mortality and morbidity due to hyperglycemia which is link with numerus obstacles. Delaying absorption and digestion of carbohydrate has great therapeutic impact for governing postprandial hyperglycemia. Consequently, alpha glucosidase is one of the potential therapeutic approaches that reduce absorption of glucose and delay carbohydrate digestion hence maintaining blood glucose level. In this regard we have synthesized benzothiazole based oxadiazole in search of potent anti-diabetic agent as α-glucosidase Inhibitors. Benzothiazole based oxadiazole derivatives 1-23 have been synthesized, characterized by 1HNMR, 13CNMR, and MS and evaluated for α-glucosidase Inhibition. All analogs exhibited a varying degree of α-glucosidase inhibitory activity with IC50 values ranging in between 0.5 ±â€¯0.01-30.90 ±â€¯0.70 µM when compared with the standard acarbose (IC50 = 866.30 ±â€¯3.20 µM). Structure activity relationship has been established for all compounds. Molecular docking studies were performed to predict the binding interaction of the compounds with the active site of enzyme.


Assuntos
Benzotiazóis/química , Inibidores de Glicosídeo Hidrolases/química , Benzotiazóis/síntese química , Benzotiazóis/metabolismo , Domínio Catalítico , Inibidores de Glicosídeo Hidrolases/síntese química , Inibidores de Glicosídeo Hidrolases/metabolismo , Simulação de Acoplamento Molecular , Estrutura Molecular , Ligação Proteica , Saccharomyces cerevisiae/enzimologia , Relação Estrutura-Atividade , alfa-Glucosidases/química , alfa-Glucosidases/metabolismo
5.
Bioorg Med Chem ; 26(1): 152-160, 2018 01 01.
Artigo em Inglês | MEDLINE | ID: mdl-29183662

RESUMO

Bisindolylmethane thiosemicarbazides 1-18 were synthesized, characterized by 1H NMR and ESI MS and evaluated for urease inhibitory potential. All analogs showed outstanding urease inhibitory potentials with IC50 values ranging between 0.14 ±â€¯0.01 to 18.50 ±â€¯0.90 µM when compared with the standard inhibitor thiourea having IC50 value 21.25 ±â€¯0.90 µM. Among the series, analog 9 (0.14 ±â€¯0.01 µM) with di-chloro substitution on phenyl ring was identified as the most potent inhibitor of urease. The structure activity relationship has been also established on the basis of binding interactions of the active analogs. These binding interactions were identified by molecular docking studies.


Assuntos
Inibidores Enzimáticos/farmacologia , Indóis/farmacologia , Semicarbazidas/farmacologia , Urease/antagonistas & inibidores , Canavalia/enzimologia , Relação Dose-Resposta a Droga , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/química , Indóis/química , Modelos Moleculares , Estrutura Molecular , Semicarbazidas/química , Relação Estrutura-Atividade , Urease/metabolismo
6.
Bioorg Chem ; 79: 323-333, 2018 09.
Artigo em Inglês | MEDLINE | ID: mdl-29803079

RESUMO

Thymidine phosphorylase is an enzyme involved in pyrimidine salvage pathway that is identical to platelet-derived endothelial cell growth factor (PD-ECGF) and gliostatin. It is enormously up regulated in a variety of solid tumors. Furthermore, surpassing of TP level protects tumor cells from apoptosis and helps cell survival. Thus TP is identified as a prime target for developing novel anticancer therapies. A new class of exceptionally potent isatin based oxadiazole (1-30) has been synthesized and evaluated for thymidine phosphorylase inhibitory potential. All analogs showed potent thymidine phosphorylase inhibition when compared with standard 7-Deazaxanthine, 7DX (IC50 = 38.68 ±â€¯1.12 µM). Molecular docking study was performed in order to determine the binding interaction of these newly synthesized compounds, which revealed that these synthesized compounds established stronger hydrogen bonding network with active site of residues as compare to the standard compound 7DX.


Assuntos
Desenho de Fármacos , Inibidores Enzimáticos/farmacologia , Isatina/farmacologia , Simulação de Acoplamento Molecular , Oxidiazóis/farmacologia , Timidina Fosforilase/antagonistas & inibidores , Relação Dose-Resposta a Droga , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/química , Humanos , Isatina/química , Estrutura Molecular , Oxidiazóis/síntese química , Oxidiazóis/química , Proteínas Recombinantes/metabolismo , Software , Relação Estrutura-Atividade , Timidina Fosforilase/metabolismo
7.
Bioorg Chem ; 78: 201-209, 2018 08.
Artigo em Inglês | MEDLINE | ID: mdl-29597114

RESUMO

α-Glucosidase is a catabolic enzyme that regulates the body's plasma glucose levels by providing energy sources to maintain healthy functioning. 2-Amino-thiadiazole (1-13) and 2-amino-thiadiazole based Schiff bases (14-22) were synthesized, characterized by 1H NMR and HREI-MS and screened for α-glucosidase inhibitory activity. All twenty-two (22) analogs exhibit varied degree of α-glucosidase inhibitory potential with IC50 values ranging between 2.30 ±â€¯0.1 to 38.30 ±â€¯0.7 µM, when compare with standard drug acarbose having IC50 value of 39.60 ±â€¯0.70 µM. Among the series eight derivatives 1, 2, 6, 7, 14, 17, 19 and 20 showed outstanding α-glucosidase inhibitory potential with IC50 values of 3.30 ±â€¯0.1, 5.80 ±â€¯0.2, 2.30 ±â€¯0.1, 2.70 ±â€¯0.1, 2.30 ±â€¯0.1, 5.50 ±â€¯0.1, 4.70 ±â€¯0.2, and 5.50 ±â€¯0.2 µM respectively, which is many fold better than the standard drug acarbose. The remaining analogs showed good to excellent α-glucosidase inhibition. Structure activity relationship has been established for all compounds. The binding interactions of these compounds were confirmed through molecular docking.


Assuntos
Inibidores de Glicosídeo Hidrolases/farmacologia , Simulação de Acoplamento Molecular , Tiadiazóis/farmacologia , alfa-Glucosidases/metabolismo , Relação Dose-Resposta a Droga , Inibidores de Glicosídeo Hidrolases/síntese química , Inibidores de Glicosídeo Hidrolases/química , Humanos , Estrutura Molecular , Relação Estrutura-Atividade , Tiadiazóis/química
8.
Bioorg Chem ; 72: 323-332, 2017 06.
Artigo em Inglês | MEDLINE | ID: mdl-28505547

RESUMO

Natural products are the main source of motivation to design and synthesize new molecules for drug development. Designing new molecules against ß-glucuronidase inhibitory is utmost essential. In this study indole analogs (1-35) were synthesized, characterized using various spectroscopic techniques including 1H NMR and EI-MS and evaluated for their ß-glucuronidase inhibitory activity. Most compounds were identified as potent inhibitors for the enzyme with IC50 values ranging between 0.50 and 53.40µM, with reference to standard d-saccharic acid 1,4-lactone (IC50=48.4±1.25µM). Structure-activity relationship had been also established. The results obtained from docking studies for the most active compound 10 showed that hydrogen bond donor features as well as hydrogen bonding with (Oε1) of nucleophilic residue Glu540 is believed to be the most importance interaction in the inhibition activity. It was also observed that hydroxyl at fourth position of benzylidene ring acts as a hydrogen bond donor and interacts with hydroxyl (OH) on the side chain of catalysis residue Tyr508. The enzyme-ligand complexed were being stabilized through electrostatic π-anion interaction with acid-base catalyst Glu451 (3.96Å) and thus preventing Glu451 from functioning as proton donor residue.


Assuntos
Glucuronidase/antagonistas & inibidores , Glicoproteínas/farmacologia , Indóis/farmacologia , Relação Dose-Resposta a Droga , Glucuronidase/metabolismo , Glicoproteínas/síntese química , Glicoproteínas/química , Humanos , Indóis/síntese química , Indóis/química , Estrutura Molecular , Relação Estrutura-Atividade
9.
Bioorg Chem ; 74: 30-40, 2017 10.
Artigo em Inglês | MEDLINE | ID: mdl-28750203

RESUMO

Discovery of α-glucosidase inhibitors has been actively pursued with the aim to develop therapeutics for the treatment of type-II diabetes mellitus and the other carbohydrate mediated disease. In continuation of our drug discovery research on potential antidiabetic agents, we synthesized novel tris-indole-oxadiazole hybrid analogs (1-21), structurally characterized by various spectroscopic techniques such as 1H NMR, EI-MS, and 13C NMR. Elemental analysis was found in agreement with the calculated values. All compounds were evaluated for α-glucosidase inhibiting potential and showed potent inhibitory activity in the range of IC50=2.00±0.01-292.40±3.16µM as compared to standard acarbose (IC50=895.09±2.04µM). The pharmacokinetic predictions of tris-indole series using descriptor properties showed that almost all compounds in this series indicate the drug aptness. Detailed binding mode analyses with docking simulation was also carried out which showed that the inhibitors can be stabilized by the formation of hydrogen bonds with catalytic residues and the establishment of hydrophobic contacts at the opposite side of the active site.


Assuntos
Diabetes Mellitus Tipo 2/tratamento farmacológico , Inibidores de Glicosídeo Hidrolases/farmacologia , Hipoglicemiantes/farmacologia , Indóis/farmacologia , Simulação de Acoplamento Molecular , Oxidiazóis/farmacologia , alfa-Glucosidases/metabolismo , Diabetes Mellitus Tipo 2/metabolismo , Inibidores de Glicosídeo Hidrolases/síntese química , Inibidores de Glicosídeo Hidrolases/química , Humanos , Hipoglicemiantes/síntese química , Hipoglicemiantes/química , Indóis/química , Oxidiazóis/química
10.
Bioorg Chem ; 74: 179-186, 2017 10.
Artigo em Inglês | MEDLINE | ID: mdl-28826047

RESUMO

α-Amylase is a target for type-2 diabetes mellitus treatment. However, small molecule inhibitors of α-amylase are currently scarce. In the course of developing small molecule α-amylase inhibitors, we designed and synthesized thiadiazole quinoline analogs (1-30), characterized by different spectroscopic techniques such as 1HNMR and EI-MS and screened for α-amylase inhibitory potential. Thirteen analogs 1, 2, 3, 4, 5, 6, 22, 23, 25, 26, 27, 28 and 30 showed outstanding α-amylase inhibitory potential with IC50 values ranges between 0.002±0.60 and 42.31±0.17µM which is many folds better than standard acarbose having IC50 value 53.02±0.12µM. Eleven analogs 7, 9, 10, 11, 12, 14, 15, 17, 18, 19 and 24 showed good to moderate inhibitory potential while seven analogs 8, 13, 16, 20, 21 and 29 were found inactive. Our study identifies novel series of potent α-amylase inhibitors for further investigation. Structure activity relationship has been established.


Assuntos
Inibidores Enzimáticos/farmacologia , Quinolinas/farmacologia , Tiadiazóis/farmacologia , alfa-Amilases/antagonistas & inibidores , Animais , Relação Dose-Resposta a Droga , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/química , Simulação de Acoplamento Molecular , Estrutura Molecular , Quinolinas/síntese química , Quinolinas/química , Relação Estrutura-Atividade , Suínos , Tiadiazóis/síntese química , Tiadiazóis/química , alfa-Amilases/metabolismo
11.
Bioorg Chem ; 72: 248-255, 2017 06.
Artigo em Inglês | MEDLINE | ID: mdl-28482265

RESUMO

Twenty five derivatives of indole carbohydrazide (1-25) had been synthesized. These compounds were characterized using 1H NMR and EI-MS, and further evaluated for their α-amylase inhibitory potential. The analogs (1-25) showed varying degree of α-amylase inhibitory potential. ranging between 9.28 and 599.0µM when compared with standard acarbose having IC50 value 8.78±0.16µM. Six analogs, 25 (IC50=9.28±0.153µM), 22 (IC50=9.79±0.43µM), 4 (IC50=11.08±0.357µM), 1 (IC50=12.65±0.169µM), 8 (IC50=21.37±0.07µM) and 14 (IC50=43.21±0.14µM) showed potent α-amylase inhibition as compared to the standard acarbose (IC50=8.78±0.16µM). All other analogs displayed good to moderate inhibitory potential. Structure-activity relationship was established through the interaction of the active compounds with enzyme active site with the help of docking studies.


Assuntos
Inibidores de Glicosídeo Hidrolases/farmacologia , Indóis/farmacologia , alfa-Amilases/antagonistas & inibidores , Relação Dose-Resposta a Droga , Inibidores de Glicosídeo Hidrolases/síntese química , Inibidores de Glicosídeo Hidrolases/química , Humanos , Indóis/síntese química , Indóis/química , Estrutura Molecular , Relação Estrutura-Atividade , alfa-Amilases/metabolismo
12.
Bioorg Chem ; 74: 1-9, 2017 10.
Artigo em Inglês | MEDLINE | ID: mdl-28719801

RESUMO

A new library of 2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl aryl ether derivatives (1-23) were synthesized and characterized by EI-MS and 1H NMR, and screened for their α-amylase inhibitory activity. Out of twenty-three derivatives, two molecules 19 (IC50=0.38±0.82µM) and 23 (IC50=1.66±0.14µM), showed excellent activity whereas the remaining compounds, except 10 and 17, showed good to moderate inhibition in the range of IC50=1.77-2.98µM when compared with the standard acarbose (IC50=1.66±0.1µM). A plausible structure-activity relationship has also been presented. In addition, in silico studies was carried out in order to rationalize the binding interaction of compounds with the active site of enzyme.


Assuntos
Inibidores Enzimáticos/farmacologia , Éter/farmacologia , Imidazóis/farmacologia , Simulação de Acoplamento Molecular , alfa-Amilases/antagonistas & inibidores , Animais , Relação Dose-Resposta a Droga , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/química , Éter/síntese química , Éter/química , Imidazóis/síntese química , Imidazóis/química , Estrutura Molecular , Relação Estrutura-Atividade , Suínos , alfa-Amilases/metabolismo
13.
J Pak Med Assoc ; 67(2): 225-232, 2017 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-28138176

RESUMO

OBJECTIVE: To provide optimised pulse sequence and imaging protocols for contrast-to-noise ratio and for tissues that have different signal intensities in magnetic resonance imaging. METHODS: A tissue equivalent material, ferrous benzoic xylenol orange gel, was prepared using gelatine, ferrous ammonium sulfate, sulfuric acid, xylenol orange tetrasodium salt and benzoic acid. The gel was irradiated using 6MV photons from a Varian Clinac 600C linear accelerator, with a dose of 5, 10, 15, 20 and 25 gray. Experimental variations in imaging parameters were performed in echo time and repetition time. The quantitative analysis consisted of contrast-to-noise ratio. RESULTS: Conventional spin echo and fast spin echo were equivalent for the tissues of comparable signal intensities and for entities moderate difference between signal intensities. Conventional spin echo provided remarkable contrast for tissues where signal intensity difference was extremely high in T1, T2-weighted study. An appropriate inversion time of fast fluid attenuated inversion recovery made it significant to measure contrast between tissues where signal intensity difference was the smallest and ordinary. CONCLUSIONS: Choice of pulse sequence and parameters played a vital role in developing fine image contrast.


Assuntos
Processamento de Imagem Assistida por Computador/métodos , Imageamento por Ressonância Magnética/métodos , Imagens de Fantasmas , Humanos
14.
J Pak Med Assoc ; 67(11): 1764-1766, 2017 11.
Artigo em Inglês | MEDLINE | ID: mdl-29171579

RESUMO

The aim of this note is to assess the common clinical features of paediatric multiple sclerosis (PMS) in Pakistan. For this purpose, 150 MS patients with the age range of (1-72) years and mean age (34.2±11.09) years were studied during the period 2010 to 2015 from MRI centers of Pakistan. We found 15 paediatric MS cases which had clinical course relapsing-remitting MS (11), secondary-progressive MS (3) and primary-progressive MS (1). Revised McDonald criteria 2010 of MRI was used to disseminate lesions in space and time. Sensory symptoms were found 27% in PMS patients and contributed brain area of corpus callosum, brain stem, periventricle, basal ganglia, white matter and cerebellum. Optic neuritis was the second clinical feature and its prevalence was reported 20% in paediatric patients. In conclusion, Paediatric multiple sclerosis is predicted 10 % with mean age 11.2 years in Pakistan. Sensory and optic neuritis are suggested the common clinical features of paediatric multiple sclerosis in Pakistan.


Assuntos
Esclerose Múltipla , Adolescente , Encéfalo/diagnóstico por imagem , Encéfalo/patologia , Criança , Estudos de Coortes , Feminino , Humanos , Imageamento por Ressonância Magnética , Masculino , Esclerose Múltipla/diagnóstico , Esclerose Múltipla/diagnóstico por imagem , Esclerose Múltipla/epidemiologia , Esclerose Múltipla/fisiopatologia , Paquistão/epidemiologia
15.
Bioorg Chem ; 60: 42-8, 2015 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-25955493

RESUMO

Isatin base Schiff bases (1-20) were synthesized, characterized by (1)H NMR and EI/MS and evaluated for α-glucosidase inhibitory potential. Out of these twenty (20) compounds only six analogs showed potent α-glucosidase inhibitory potential with IC50 value ranging in between 2.2±0.25 and 83.5±1.0µM when compared with the standard acarbose (IC50=840±1.73µM). Among the series compound 2 having IC50 value (18.3±0.56µM), 9 (83.5±1.0µM), 11 (3.3±0.25µM), 12 (2.2±0.25µM), 14 (11.8±0.15µM), and 20 (3.0±0.15µM) showed excellent inhibitory potential many fold better than the standard acarbose. The binding interactions of these active analogs were confirmed through molecular docking.


Assuntos
Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Isatina/análogos & derivados , Isatina/farmacologia , alfa-Glucosidases/metabolismo , Humanos , Simulação de Acoplamento Molecular , Saccharomyces cerevisiae/enzimologia , Bases de Schiff/química , Bases de Schiff/farmacologia , Relação Estrutura-Atividade
16.
Bioorg Chem ; 62: 15-21, 2015 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-26162519

RESUMO

A series of thiazole derivatives 1-21 were prepared, characterized by EI-MS and (1)H NMR and evaluated for α-glucosidase inhibitory potential. All twenty one derivatives showed good α-glucosidase inhibitory activity with IC50 value ranging between 18.23±0.03 and 424.41±0.94µM when compared with the standard acarbose (IC50, 38.25±0.12µM). Compound (8) (IC50, 18.23±0.03µM) and compound (7) (IC50=36.75±0.05µM) exhibited outstanding inhibitory potential much better than the standard acarbose (IC50, 38.25±0.12µM). All other analogs also showed good to moderate enzyme inhibition. Molecular docking studies were carried out in order to find the binding affinity of thiazole derivatives with enzyme. Studies showed these thiazole analogs as a new class of α-glucosidase inhibitors.


Assuntos
Inibidores de Glicosídeo Hidrolases/síntese química , Inibidores de Glicosídeo Hidrolases/farmacologia , Hidrazinas/síntese química , Hidrazinas/farmacologia , Simulação de Acoplamento Molecular , Fenóis/síntese química , Fenóis/farmacologia , Tiazóis/síntese química , Tiazóis/farmacologia , alfa-Glucosidases/efeitos dos fármacos , Acarbose/farmacologia , Proteínas de Saccharomyces cerevisiae/química , alfa-Glucosidases/química
17.
J Pak Med Assoc ; 65(5): 512-8, 2015 May.
Artigo em Inglês | MEDLINE | ID: mdl-26028386

RESUMO

OBJECTIVE: To investigate the practical impact of alteration of imaging parameters on signal-to-noise ratio for the most commonly used T1-weighted magnetic resonance sequences. METHODS: The study was conducted in the Department of Medical Physics, Ninewells Hospital and Medical School, Dundee, UK, in 2007. Magnetic resonance images of a tissue-equivalent material were generated with a set of T1 and T2 values. Experimental variations in the imaging parameters were performed in echo time and repetition time. Quantitative analysis consisted of signal-to-noise ratio. RESULTS: Percentage inaccuracy in signal-to-noise ratio was the result of inappropriate choice of parameters. We have investigated conventional spin echo, fast spin echo and fast fluid attenuated inversion recovery with one of corresponding percentage errors 28.68%, -36.65% and -40.34%, respectively. Conventional spin echo presented moderately low percentage error with the choice of repetition time and echo time. Factual error in fast spin echo was slightly higher than conventional spin echo. Fast fluid attenuated inversion recovery could create outstanding signal-to-noise ratio of high T1/T2 value phantoms in T1-weighted images. CONCLUSIONS: The role of repetition time and echo time in T1-weighted images was crucial to sustain the image quality.


Assuntos
Imageamento por Ressonância Magnética/métodos , Imagens de Fantasmas , Razão Sinal-Ruído , Humanos
18.
J Safety Res ; 89: 210-223, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38858045

RESUMO

INTRODUCTION: Aggressive behavior of drivers is a source of crashes and high injury severity. Aggressive drivers are part of the driving environment, however, excessive aggressive driving by fellow drivers may take the attention of the recipient drivers away from the road resulting in distracted driving. Such external distractions caused by the aggressive and discourteous behavior of other road users have received limited attention. These distractions caused by fellow drivers (DFDs) may agitate recipient drivers and ultimately increase crash propensity. Aggressive driving behaviors are quite common in South Asia and, thus, it is necessary to determine their contribution to distractions and crash propensity. METHOD: Our study aimed to evaluate the effects of DFDs using primary data collected through a survey conducted in Lahore, Pakistan. A total of 801 complete responses were obtained. Various hypotheses were defined to explore the associations between the latent factors such as DFDs, anxiety/stress (AS), anxiety-based performance deficits (APD), hostile behavior (HB), acceptability of vehicle-related distractions (AVRD), and crash propensity (CP). Structural Equation Modeling (SEM) was employed as a multivariate statistical technique to test these hypotheses. RESULTS: The results supported the hypothesis that DFDs lead to AS among recipient drivers. DFDs and AS were further found to have positive associations with APDs. Whereas, there was a significant negative association between DFD, AS, and AVRD. As hypothesized, DFD and AS had positive associations with CP, indicating that distractions caused by aggressive behaviors leads to stress and consequently enhances crash propensity. PRACTICAL APPLICATIONS: The results of this study provide a statistically sound foundation for further exploration of the distractions caused by the aggressive behaviors of fellow drivers. Further, the results of this study can be utilized by the relevant authorities to alter aggressive driving behaviors and reduce DFDs.


Assuntos
Acidentes de Trânsito , Direção Distraída , Humanos , Acidentes de Trânsito/estatística & dados numéricos , Acidentes de Trânsito/psicologia , Masculino , Feminino , Adulto , Direção Distraída/psicologia , Direção Distraída/estatística & dados numéricos , Pessoa de Meia-Idade , Paquistão , Condução de Veículo/psicologia , Condução de Veículo/estatística & dados numéricos , Agressão/psicologia , Inquéritos e Questionários , Análise de Classes Latentes , Adulto Jovem , Atenção
19.
Int J Occup Saf Ergon ; 30(2): 399-411, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38305082

RESUMO

Objectives. This research investigated the performance properties of protective gloves alongside improvement in thermo-physiological comfort properties. Methods. Knitted gloves prepared from filament stainless steel, filament Kevlar, staple spun Kevlar and filament glass were used in the core, while 100% viscose rayon and 50/50% polyester/viscose rayon were used in the sheath. Gloves were tested for cut resistance, tear resistance, puncture resistance and abrasion resistance as the prime focus, and thermo-physiological comfort properties were also tested. In this research, a multi-response optimization technique, i.e., principal component analysis, was applied to identify the best yarn combination for gloves based on the aforementioned properties. Thermal images were also taken in constant ambient conditions for temperature distribution maps across the hand's surface. Results. All of the results were evaluated statistically with analysis of variance, and concluded that the effects of the core yarn on thermo-physiological properties were less significant. Conclusion. The results revealed that samples having dual-core yarn exhibited better in terms of overall properties. The sample having dual-core filament Kevlar and staple spun Kevlar ranked the best. In addition, developed samples exhibited better comfort properties than the control sample.


Assuntos
Celulose , Luvas Protetoras , Teste de Materiais , Humanos , Estudos Prospectivos , Poliésteres , Aço Inoxidável , Análise de Componente Principal
20.
J Exp Zool A Ecol Integr Physiol ; 341(1): 41-47, 2024 01.
Artigo em Inglês | MEDLINE | ID: mdl-37877181

RESUMO

Bursa of Fabricius (BOF) is a unique immune organ of birds. It is the place where lymphocytes develop, differentiate and mature. Young chicken BOF is susceptible to infection and damage, and even atrophy, causing immune suppression, and bringing huge economic losses to chicken production. Therefore, studying the regulatory mechanism of chicken bursa development is of great practical significance for disease prevention and diagnosis. Jinhu silky chicken (JSC) is a local excellent breed in the Fujian Province of China and with strong disease resistance. However, studies on the disease resistance of JSC are scarce. This study aimed to provide a theoretical basis for reproduction and disease control of JSC. Developmental features of the structure and the IL-21-positive cell (IL-21 PC) distribution on the BOF in JSC were measured from 7 to 300 days of age. Bursas of chicken (n = 36) were taken at 7, 35, 70, 150, 240, and 300 days of age for preparation of paraffin sections and stained with hematoxylin-eosin (HE) and immunohistochemistry. The microstructure of JSC's BOF was similar to that of other poultry. The cortical-medullary boundary of the bursa nodule was not obvious at 7 days of age, but it was evident after 35 days of age. Before 70 days of age, IL-21 positive cells (PC) were scattered on the BOF. At 150 days of age, the number of IL-21 PC in the bursa were the highest and the nuclei were clear. The level of IL-21 PC gradually decreased with age. The BOF degenerated and disappeared in 300-day-old JSC. The histological structure of the BOF was similar to that of other poultry. IL-21 PC were widespread in the BOF at different ages, but the numbers were different.


Assuntos
Bolsa de Fabricius , Galinhas , Animais , Bolsa de Fabricius/patologia , Resistência à Doença
SELEÇÃO DE REFERÊNCIAS
Detalhe da pesquisa