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3.
Int J Surg ; 108: 106991, 2022 Nov 09.
Artigo em Inglês | MEDLINE | ID: mdl-36371061
4.
Artigo em Inglês | MEDLINE | ID: mdl-36266151

RESUMO

OBJECTIVE: The aim of this study was to compare TIMI flow after administering intracoronary (IC) medications through various routes for the treatment of slow flow/no-reflow during primary PCI. METHODS: Two independent parallel cohorts of the patients who underwent primary PCI for STEMI and developed slow/no-reflow were recruited. Selection of cohort was based on the route of administration of IC medications as proximal or distal. Post administration TIMI follow was compared between the two cohorts. RESULTS: A total of 100 patients were included in both, proximal and distal, cohort. Distribution of angiographic, clinical and demographic characteristics was not significant between the two cohorts except prevalence of hypertension, and diabetes mellitus. Frequency of hypertension, and diabetes mellitus were 45 % vs.70 %; p < 0.001 and 28 % vs. 44 %; p = 0.018 among patients in distal and proximal cohort respectively. Final TIMI III flow was achieved in significantly higher number of patients in distal cohort with the frequency of 88 % vs. 76 %; p = 0.027 as compared to proximal cohort. CONCLUSION: Administration of IC medication via distal route is observed to be more effective for the treatment of slow flow/no-reflow during primary PCI. Distal route via export catheter or perforated balloon technique should be preferred wherever feasible.

5.
Biochim Biophys Acta Rev Cancer ; 1877(5): 188786, 2022 09.
Artigo em Inglês | MEDLINE | ID: mdl-36058379

RESUMO

Deviant expressions of the tyrosine kinase AXL receptor are strongly correlated with a plethora of malignancies. Henceforth, the topic of targeting AXL is beginning to gain prominence due to mounting evidence of the protein's substantial connection to poor prognosis and treatment resistance. This year marked a milestone in clinical testing for AXL as an anti-carcinogenic target, with the start of the first AXL-branded inhibitor study. It is critical to emphasize that AXL is a primary and secondary target in various kinase inhibitors that have been approved or are on the verge of being approved while interpreting the present benefits and future potential effects of AXL suppression in the clinical setting. Several research arenas across the globe resolutely affirm the crucial significance of AXL receptors in the case study of several pathophysiologies including AML, prostate cancer, and breast cancer. This review endeavors to delve deeply into the biological, chemical, and structural features of AXL kinase; primary AXL inhibitors that target the enzyme (either purposefully or unintentionally); and the prospects and barriers for turning AXL inhibitors into a feasible treatment alternative. Furthermore, we analyse the co-crystal structure of AXL, which remains extensively unexplored, as well as the mutations of AXL that may be valuable in the development of novel inhibitors in the upcoming future and take a comprehensive look at the medicinal chemistry of AXL inhibitors of recent years.


Assuntos
Antineoplásicos , Neoplasias , Inibidores de Proteínas Quinases , Antineoplásicos/farmacologia , Antineoplásicos/uso terapêutico , Humanos , Neoplasias/tratamento farmacológico , Inibidores de Proteínas Quinases/farmacologia , Inibidores de Proteínas Quinases/uso terapêutico , Proteínas Proto-Oncogênicas , Receptores Proteína Tirosina Quinases
6.
Artigo em Inglês | MEDLINE | ID: mdl-35993476

RESUMO

BACKGROUND: PIM (Proviral Integration site for Moloney Murine Leukemia virus) kinases are members of the class of kinase family serine/ threonine kinases, which play a crucial role in cancer development. As there is no drug in the market against PIM-1, kinase has transpired as a budding and captivating target for discovering new anticancer agents targeting PIM-1 kinase. AIM: The current research pondered the development of new PIM-1 kinase inhibitors by applying a ligand-based and structure-based drug discovery approach involving 3D QSAR, molecular docking, and dynamics simulation. METHOD: In this study, association allying the structural properties and biological activity was undertaken using 3D-QSAR analysis. The 3D-QSAR model was generated with the help of 35 compounds from which the best model manifested an appreciated cross-validation coefficient (q2) of 0.8866 and conventional correlation coefficient (r2) of 0.9298, respectively and predicted correlation coefficient (r2 pred) was obtained as 0.7878. RESULT: The molecular docking analysis demonstrated that the analogs under analysis occupied the active site of PIM-1 kinase receptor and interactions with Lys67 in the catalytic region, Asp186 in the DFG motif, and Glu171 were noticed with numerous compounds. DISCUSSION: Furthermore, the molecular dynamics simulation study stated that the ligand portrayed the strong conformational stability within the active site of PIM-1 kinase protein, forming of two hydrogen bonds until 100 ns, respectively. CONCLUSION: Overall outcomes of the study revealed that applications of the ligand-based drug discovery approach and structure-based drug discovery strategy conceivably applied to discovering new PIM-1 kinase inhibitors as anticancer agents.

7.
Bioinorg Chem Appl ; 2022: 9459886, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35873731

RESUMO

Environmental problems with chemical and biological water pollution have become a major concern for society. Providing people with safe and affordable water is a grand challenge of the 21st century. The study investigates the photocatalytic degradation capabilities of hydrothermally prepared pure and Cu-doped ZnO nanoparticles (NPs) for the elimination of dye pollutants. A simple, cost-effective hydrothermal process is employed to synthesize the Cu-doped ZnO NPs. The photocatalytic dye degradation activity of the synthesized Cu-doped ZnO NPs is tested by using methylene blue (MB) dye. In addition, the parameters that affect photodegradation efficiency, such as catalyst concentration, starting potential of hydrogen (pH), and dye concentration, were also assessed. The dye degradation is found to be directly proportional to the irradiation time, as 94% of the MB dye is degraded in 2 hrs. Similarly, the dye degradation shows an inverse relation to the MB dye concentration, as the degradation reduced from 94% to 20% when the MB concentration increases from 5 ppm to 80 ppm. The synthesized cost-effective and environmentally friendly Cu-doped ZnO NPs exhibit improved photocatalytic activity against MB dye and can therefore be employed in wastewater treatment materials.

8.
Mol Carcinog ; 61(10): 941-957, 2022 10.
Artigo em Inglês | MEDLINE | ID: mdl-35856887

RESUMO

Dietary rice bran (RB) has shown capacity to influence metabolism by modulation of gut microbiota in individuals at risk for colorectal cancer (CRC), which warranted attention for delineating mechanisms for bidirectional influences and cross-feeding between the host and RB-modified gut microbiota to reduce CRC. Accordingly, in the present study, fermented rice bran (FRB, fermented with a RB responsive microbe Bifidobacterium longum), and non-fermented RB were fed as 10% w/w (diet) to gut microbiota-intactspf or germ-free micegf to investigate comparative efficacy against inflammation-associated azoxymethane/dextran sodium sulfate (AOM/DSS)-induced CRC. Results indicated both microbiota-dependent and independent mechanisms for RB meditated protective efficacy against CRC that was associated with reduced neoplastic lesion size and local-mucosal/systemic inflammation, and restoration of colonic epithelial integrity. Enrichment of beneficial commensals (such as, Clostridiales, Blautia, Roseburia), phenolic metabolites (benzoate and catechol metabolism), and dietary components (ferulic acid-4 sulfate, trigonelline, and salicylate) were correlated with anti-CRC efficacy. Germ-free studies revealed gender-specific physiological variables could differentially impact CRC growth and progression. In the germ-free females, the RB dietary treatment showed a ∼72% reduction in the incidence of colonic epithelial erosion when compared to the ∼40% reduction in FRB-fed micegf . Ex vivo fermentation of RB did not parallel the localized-protective benefits of gut microbial metabolism by RB in damaged colonic tissues. Findings from this study suggest potential needs for safety considerations of fermented fiber rich foods as dietary strategies against severe inflammation-associated colon tumorigenesis (particularly with severe damage to the colonic epithelium).


Assuntos
Bifidobacterium longum , Microbioma Gastrointestinal , Oryza , Animais , Azoximetano/toxicidade , Carcinogênese/patologia , Transformação Celular Neoplásica/patologia , Colo/patologia , Sulfato de Dextrana/toxicidade , Dieta , Modelos Animais de Doenças , Feminino , Inflamação/patologia , Camundongos , Camundongos Endogâmicos C57BL , Oryza/metabolismo
9.
J Med Case Rep ; 16(1): 262, 2022 Jul 05.
Artigo em Inglês | MEDLINE | ID: mdl-35787820

RESUMO

BACKGROUND: The I-gel is a second-generation supraglottic airway device that is built with a noninflatable elliptical gel material cuff and has a wide semirigid stem. The I-gel supralaryngeal seal has shown promising efficacy for both spontaneous and controlled ventilation under general anesthesia. The recommended, standard I-gel insertion technique is relatively challenging due to its shape and cuff size. Usually, the I-gel becomes entrapped at the oral cavity and requires excessive force to negotiate across the oropharynx, resulting in insertion resistance, tongue obstruction, insertion failure, and intraoral trauma. This case series evaluated a modified jaw thrust I-gel insertion technique because it is claimed to allow smooth and atraumatic I-gel placement in adults. CASE PRESENTATION: In this case series, ten male and female Indo-Aryan group of Asian patients aged 18-60 years were recruited for I-gel device placement through a modified jaw thrust technique for short to intermediate surgical duration in below-umbilical surgical procedures. Patient consent was obtained, and baseline vital signs such as electrocardiogram, noninvasive blood pressure, and peripheral oxygen saturation readings were recorded. Following preoxygenation, propofol 2 mg/kg was administered for anesthesia induction and nalbuphine 0.1 mg/kg for analgesia. In all patients, an I-gel was placed by the modified jaw thrust technique. The patient's demographics, number of attempts, I-gel insertion resistance, and insertion time duration were recorded. CONCLUSION: The findings showed a 100% first-attempt insertion rate along with negligible insertion resistance and convincing insertion time duration with modified jaw thrust I-gel insertion technique. However, a blood-stained I-gel was observed in one male patient at the time of removal. The patient's demographics such as age, weight, American Society of Anesthesiologists status, and surgical and anesthesia duration were found not to be significant. The modified jaw thrust I-gel insertion technique could be considered as an alternative in adults when difficulty is encountered with the standard I-gel insertion technique.


Assuntos
Anestesia Geral , Propofol , Adolescente , Adulto , Feminino , Humanos , Masculino , Pessoa de Meia-Idade
10.
Biomed Pharmacother ; 153: 113299, 2022 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-35750010

RESUMO

Neurodegenerative diseases and various other chronic ailments have gradually transformed into public-health issues. Neurodegenerative disorders are a range of progressive neural abnormalities characterized by cellular dysfunctions, neuronal structure, and function loss. Among many chronic disorders, oxidative stress, inflammation, mitochondrial dysregulation, and cellular alterations in the human body are considered the most prevalent diagnostic symptoms. They have a profound impact on patients' health and wellbeing. The disease's poor curability, high healthcare costs, and lethality are the principal reasons for approaching and exploring the conventional treatment's phytotherapeutic alternatives. Ginkgo biloba (Maidenhair tree) is a well-known and widely used herbal plant in the Ginkgoaceae family. Its phytochemical constituents, Flavonoids, and terpenes, have been identified as the primary ingredients of Ginkgo biloba leaf extracts. It has been widely used due to its therapeutic properties, including its neuroprotective, anti-dementia, antioxidant, anti-inflammatory, vasoactive, anti-psychotic, anti-neoplastic, and anti-platelet activity. In recent decades, plenty of Ginkgo-derived substances has been researched and elucidated to have significant therapeutic effects in numerous disease models. This review aims to provide a thorough understanding of the botanical basis for Ginkgo biloba, its usage as herbal medicine, and its pivotal role in functional foods. Additionally, the clinical significance of Ginkgo biloba, as observed in various research works and clinical investigations, is also emphasized, facilitating a better understanding of their molecular basis and application in many chronic diseases.


Assuntos
Ingredientes de Alimentos , Plantas Medicinais , Alimento Funcional , Ginkgo biloba , Humanos , Fitoterapia , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico
11.
Artigo em Inglês | MEDLINE | ID: mdl-35708082

RESUMO

Cyclin Dependent Kinase 9 (CDK9), which controls transcriptional elongation, is a promising pharmacological target for a variety of cancerous cells, specifically those characterized by transcriptional dysregulation. CDK9 promotes the pause or release of RNA polymerase II, a rate-limiting stage in normal transcriptional regulation that is often disturbed in cancers. New indications suggest that selective CDK9 antagonism may be beneficial in the treatment of some cancers. CDK9 modulators (inhibitors and degraders) have gotten a lot of attention recently, and many molecules are currently in clinical trials. In this review, the CDK9 antagonists under clinical and preclinical trials have been discussed, as well as the structure-activity relationship has been studied, which will help scientists generate more target-specific drug molecules in the future with less toxicity.

12.
Data Brief ; 42: 108315, 2022 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-35664656

RESUMO

Rotating machines as core component of an industry can effectively be monitored through vibration analysis. Considering the importance of vibration in industrial condition monitoring, this article reports and discusses triaxial vibration data for motor bearing faults detection and identification. The data is acquired using a MEMS based triaxial accelerometer and the National Instruments myRIO board. The bearing conditions include healthy bearing, bearings with inner race faults, and bearings with outer race faults. For each faulty bearing condition, the three-phase induction motor is operated under three different load conditions. The dataset can be used to assess performance of newly developed methods for effective bearing fault diagnosis. Mendeley Data. http://dx.doi.org/10.17632/fm6xzxnf36.2.

13.
Curr Top Med Chem ; 22(22): 1880-1896, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35761490

RESUMO

Alzheimer's disease (AD) is a severe progressive neurodegenerative condition that shows misfolding and aggregation of proteins contributing to a decline in cognitive function involving multiple behavioral, neuropsychological, and cognitive domains. Multiple epi (genetic) changes and environmental agents have been shown to play an active role in ER stress induction. Neurodegeneration due to endoplasmic reticulum (ER) stress is considered one of the major underlying causes of AD. ER stress may affect essential cellular functions related to biosynthesis, assembly, folding, and post-translational modification of proteins leading to neuronal inflammation to promote AD pathology. Treatment with phytochemicals has been shown to delay the onset and disease progression and improve the well-being of patients by targeting multiple signaling pathways in AD. Phytochemical's protective effect against neuronal damage in AD pathology may be associated with the reversal of ER stress and unfolding protein response by enhancing the antioxidant and anti-inflammatory properties of the neuronal cells. Hence, pharmacological interventions using phytochemicals can be a potential strategy to reverse ER stress and improve AD management. Towards this, the present review discusses the role of phytochemicals in preventing ER stress in the pathology of AD.


Assuntos
Doença de Alzheimer , Estresse do Retículo Endoplasmático , Humanos , Doença de Alzheimer/metabolismo , Neurônios/metabolismo , Transdução de Sinais , Compostos Fitoquímicos/farmacologia
14.
J Ayub Med Coll Abbottabad ; 34(2): 288-294, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35576288

RESUMO

BACKGROUND: Aim of this study was to perform quantitative evaluation of high thrombus burden (Grade ≥4) as an independent predictor of slow/no reflow phenomenon during primary percutaneous coronary interventions (PCI) of patients with ST-segment elevation myocardial infarction (STEMI). METHODS: In this analytical cross-sectional study we included consecutive patients who have undergone primary PCI for STEMI at a tertiary care cardiac center of the Pakistan. High thrombus burden was defined as angiographic thrombus grade ≥4. The thrombolysis in myocardial infarction (TIMI) flow rate < III was defined as slow/no reflow phenomenon. Results of multivariate logistic regression analysis for slow/no reflow phenomenon were reported as odds ratio (OR). RESULTS: This analysis included 747 patients, 78.2% (584) patients were male and mean age was 55.82±11.54 years. High thrombus burden was observed in 68.1% (509) of the patients. Slow/no reflow phenomenon was observed in 33.6% (251) which was more common among patients in high thrombus burden group, 39.7% (202/509) vs. 20.6% (49/238); p<0.001. Adjusted OR of thrombus Grade ≥ 4 was 2.33 [1.6 -3.39]; p<0.001. Other significant variables were female gender (1.51 [1.01 -2.27]; p=0.045), left ventricular end-diastolic pressure (LVEDP) ≥20 mmHg (2.34 [1.69 -3.26]; p<0.001), total lesion length ≥20 cm (1.54 [1.09-2.16]; p=0.014), and neutrophil count ≥8.8 cells/µL (1.72 [1.22 -2.43]; p=0.002). CONCLUSIONS: High thrombus burden (Grade ≥4) is a significant and an independent predictor of the slow/no reflow phenomenon. While predicting slow/no reflow phenomenon, thrombus burden should be given due importance along with other significant factors such as gender, LVEDP, lesion length, and neutrophil counts.


Assuntos
Fenômeno de não Refluxo , Intervenção Coronária Percutânea , Infarto do Miocárdio com Supradesnível do Segmento ST , Trombose , Adulto , Idoso , Angiografia Coronária/métodos , Estudos Transversais , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Fenômeno de não Refluxo/epidemiologia , Fenômeno de não Refluxo/etiologia , Intervenção Coronária Percutânea/métodos , Infarto do Miocárdio com Supradesnível do Segmento ST/cirurgia , Fatores de Tempo
15.
J Tradit Complement Med ; 12(3): 287-301, 2022 May.
Artigo em Inglês | MEDLINE | ID: mdl-35493312

RESUMO

Background and aim: Metabolic syndrome (MetS) is a complex disease of physiological imbalances interrelated to abnormal metabolic conditions, such as abdominal obesity, type II diabetes, dyslipidemia and hypertension. In the present pilot study, we investigated the nutraceutical bitter melon (Momordica charantia L) -intake induced transcriptome and metabolome changes and the converging metabolic signaling networks underpinning its inhibitory effects against MetS-associated risk factors. Experimental procedure: Metabolic effects of lyophilized bitter melon juice (BMJ) extract (oral gavage 200 mg/kg/body weight-daily for 40 days) intake were evaluated in diet-induced obese C57BL/6J male mice [fed-high fat diet (HFD), 60 kcal% fat]. Changes in a) serum levels of biochemical parameters, b) gene expression in the hepatic transcriptome (microarray analysis using Affymetrix Mouse Exon 1.0 ST arrays), and c) metabolite abundance levels in lipid-phase plasma [liquid chromatography mass spectrometry (LC-MS)-based metabolomics] after BMJ intervention were assessed. Results and conclusion: BMJ-mediated changes showed a positive trend towards enhanced glucose homeostasis, vitamin D metabolism and suppression of glycerophospholipid metabolism. In the liver, nuclear peroxisome proliferator-activated receptor (PPAR) and circadian rhythm signaling, as well as bile acid biosynthesis and glycogen metabolism targets were modulated by BMJ (p < 0.05). Thus, our in-depth transcriptomics and metabolomics analysis suggests that BMJ-intake lowers susceptibility to the onset of high-fat diet associated MetS risk factors partly through modulation of PPAR signaling and its downstream targets in circadian rhythm processes to prevent excessive lipogenesis, maintain glucose homeostasis and modify immune responses signaling.

16.
SAGE Open Med ; 10: 20503121221088106, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35387152

RESUMO

Objectives: No-reflow is a complication that frequently occurs after stenting during primary percutaneous coronary intervention. In this study, we focused on angiographic results and clinical outcomes after no-reflow in the left anterior descending (LAD) artery versus non-left anterior descending artery ST-elevation myocardial infarction (STEMI). Methods: In this prospective study, a total of 201 patients who had developed no-reflow during primary percutaneous coronary intervention were enrolled. The patients were divided into left anterior descending artery culprit and non-left anterior descending artery culprit groups. The primary endpoints were final thrombolysis in myocardial infarction flow, corrected thrombolysis in myocardial infarction frame count and final myocardial blush grade. Secondary endpoints were major adverse cardiovascular events in-hospital and at 1 month. Results: Out of the 201 patients, 60.19% had culprit left anterior descending artery. Pulse rate, baseline systolic and diastolic blood pressure, single-vessel disease, left ventricular ejection fraction <30%, baseline thrombolysis in myocardial infarction I flow and final thrombolysis in myocardial infarction II flow (24.8% vs 11.3%, p = .017), and thrombolysis in myocardial infarction frame count (28.17 ± 11.86 vs 24.38 ± 9.05, p = .016) were significantly higher in the left anterior descending artery group. In contrast, baseline Killip Class I, three-vessel disease, baseline thrombolysis in myocardial infarction II flow, final thrombolysis in myocardial infarction III flow (74.4% vs 87.5%, p = .024) and left ventricular ejection fraction >40% were significantly greater in the non-left anterior descending artery group. However, for both in-hospital and at 30 days, overall major adverse cardiovascular event was similar in the two groups. The demographics, clinical and medication profiles and the routes used to treat no-reflow were all comparable in both groups. Conclusions: No-reflow in left anterior descending artery ST-elevation myocardial infarction is associated with lower final thrombolysis in myocardial infarction III flow, higher thrombolysis in myocardial infarction frame count and relatively lower Grade III myocardial blush than non-left anterior descending artery ST-elevation myocardial infarction with subsequent lower left ventricular ejection fraction and a higher frequency of in-hospital heart failure and hospitalisation due to heart failure.

17.
Med Chem ; 18(10): 1060-1072, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35410619

RESUMO

BACKGROUND: Pyrazole is a component of a diversity of bioactive heterocyclic congeners with a broad-spectrum range of biological and pharmacological uses. Designing novel pyrazole and its analogues, revealing new routes for synthesizing this nucleus, exploring various potencies of that heterocycles, and looking for possible applications of pyrazoles are all becoming more important due to their numerous potential applications. OBJECTIVES: Pyrazole scaffolds have been proven to be successful as anti-viral and anti-inflammatory therapeutics against multiple targets like HSV-1, NNRTI, H1N1, CoX-1, and CoX-2. Due to this miscellany in the biotic area, this moiety has engrossed the consideration of many scientists to study chemistry and pharmacological profile. RESULTS: The review encompasses pyrazole having various scaffolds with multiple biological activities and attempts have also been made to correlate their structure-activity relationship. Multiple pyrazole correspondents have been synthesized as lead molecules and performed valuation for their actions. CONCLUSION: The incorporation of pyrazole with other pharmacophores in the molecule might lead to novel potent therapeutic agents that will further help in designing potent lead molecules.


Assuntos
Antivirais , Vírus da Influenza A Subtipo H1N1 , Anti-Inflamatórios , Desenho de Fármacos , Pirazóis , Relação Estrutura-Atividade
18.
Biochim Biophys Acta Rev Cancer ; 1877(3): 188725, 2022 05.
Artigo em Inglês | MEDLINE | ID: mdl-35367531

RESUMO

Cytosolic PIM kinases are the members of serine/ threonine family play a crucial role in the cancer progression and development. Overexpression of PIM kinases is observed in various types of cancers including prostate, hematological, pancreatic, breast carcinoma and likewise. PIM kinases have now been considered as limelight target for the discovery of new molecules as novel anticancer agents as no drug is in the market targeting PIM kinases. In the last two decades, numerous PIM kinase inhibitors have been developed and few of them were in clinical trial phases but could not pass the pipeline of the clinical trials. The present comprehensive review intends to cover biological and the structural aspects of PIM kinases and also medicinal chemistry of PIM inhibitors developed in recent years.


Assuntos
Antineoplásicos , Neoplasias , Antineoplásicos/química , Antineoplásicos/farmacologia , Antineoplásicos/uso terapêutico , Química Farmacêutica , Humanos , Masculino , Neoplasias/tratamento farmacológico , Inibidores de Proteínas Quinases/farmacologia , Inibidores de Proteínas Quinases/uso terapêutico , Proteínas Proto-Oncogênicas c-pim-1/química
19.
Gels ; 8(3)2022 Mar 04.
Artigo em Inglês | MEDLINE | ID: mdl-35323272

RESUMO

Interfacial interaction amongst the antidepressant drug-imipramine hydrochloride (IMP) and pharmaceutical excipient (triton X-100 (TX-100-nonionic surfactant)) mixed system of five various ratios in dissimilar media (H2O/50 mmol·kg-1 NaCl/250 mmol·kg-1 urea) was investigated through the surface tension method. In addition, in the aqueous solution, the 1H-NMR, as well as FT-IR studies of the studied pure and mixed system were also explored and deliberated thoroughly. In NaCl media, properties of pure/mixed interfacial surfaces enhanced as compared with the aqueous system, and consequently the synergism/attractive interaction among constituents (IMP and TX-100) grew, whereas in urea (U) media a reverse effect was detected. Surface excess concentration (Γmax), composition of surfactant at mixed monolayer (X1σ), activity coefficient (f1σ (TX-100) and f2σ (IMP)), etc. were determined and discussed thoroughly. At mixed interfacial surfaces interaction, parameter (ßσ) reveals the attractive/synergism among the components. The Gibbs energy of adsorption (ΔGadso) value attained was negative throughout all employed media viewing the spontaneity of the adsorption process. The 1H NMR spectroscopy was also employed to examine the molecular interaction of IMP and TX-100 in an aqueous system. FT-IR method as well illustrated the interaction amongst the component. The findings of the current study proposed that TX-100 surfactant could act as an efficient drug delivery vehicle for an antidepressant drug. Gels can be used as drug dosage forms due to recent improvements in the design of surfactant systems. Release mechanism of drugs from surfactant/polymer gels is dependent upon the microstructures of the gels and the state of the drugs within the system.

20.
Med Chem ; 18(10): 1044-1059, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35240964

RESUMO

BACKGROUND: Pyrazole is a bioactive heterocyclic congener with numerous biological and pharmacological functionalities. Due to their multiple prospective applications, developing innovative and novel pyrazoles and analogs, revealing revolutionary methods for synthesizing this nucleus, investigating diverse potencies of that heterocycle, and exploring possible pyrazole applications are becoming increasingly relevant. OBJECTIVES: Pyrazole scaffolds have been proven successful as antimicrobial, anticancer, and antimalarial therapeutics against multiple targets like DNA gyrase, topoisomerase IV, Hsp90, and several kinase enzymes. For this variability in the biotic zone, their moiety has gained the attention of many scientists interested in researching chemical and pharmacological profiles. RESULTS: The review covers pyrazole scaffolds with a variety of biological functions and attempts to connect the structure-activity relationship. Multiple pyrazole analogs have been produced as lead compounds, and their activities have been evaluated. CONCLUSION: The combination of pyrazole with other pharmacophores in a molecule might lead to novel potent therapeutic medicines, which could aid in the development of potent lead compounds.


Assuntos
Anti-Infecciosos , Antimaláricos , Antineoplásicos , Antibacterianos , Pirazóis , Relação Estrutura-Atividade
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