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1.
Artigo em Inglês | MEDLINE | ID: mdl-34886417

RESUMO

Program outcome assessment is a complex process that demands careful planning and resources in order to accurately assess higher-order thinking skills. A well-defined assessment approach provides detailed insights into program weaknesses and leads to continuous improvement. Whereas a poor assessment approach does not reflect the underlying weaknesses and may result in a useless effort. Furthermore, each accreditation body may have a different recommended outcome measurement approach. As a result, academic institutions may make adhoc choices just to satisfy accreditation requirements rather than designing a sustainable measurement approach. On the other hand, the magnitude of huge tasks for satisfying multiple accreditation bodies results in fatigue and mental stress for academic staff. ABET is a well-known international program accreditation body, and NCAAA is a local accreditation body for academic programs in the Kingdom of Saudi Arabia. In this paper, we have documented that how a sustainable outcome measurement mechanism can be designed to satisfy both ABET and NCAAA requirements. The core contribution of this paper is relevant specifically for academic programs in the Kingdom striving to meet both ABET and NCAAA requirements and is also relevant for all education programs to design an appropriate program assessment approach to ensure a sustainable process to foster better learning among students.


Assuntos
Acreditação , Universidades , Computadores , Humanos , Sistemas de Informação , Avaliação de Programas e Projetos de Saúde
2.
BMC Chem ; 13(1): 102, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31410413

RESUMO

We have synthesized new series of bisindole analogs (1-27), characterized by 1HNMR and HR-EI-MS and evaluated for their anti-leishmanial potential. All compounds showed outstanding inhibitory potential with IC50 values ranging from 0.7 ± 0.01 to 13.30 ± 0.50 µM respectively when compared with standard pentamidine with IC50 value of 7.20 ± 0.20 µM. All analogs showed greater potential than standard except 10, 19 and 23 when compared with standard. Structure activity relationship has been also established for all compounds. Molecular docking studies were carried out to understand the binding interaction of active molecules.

3.
Bioorg Med Chem ; 27(14): 3145-3155, 2019 07 15.
Artigo em Inglês | MEDLINE | ID: mdl-31196753

RESUMO

A new series of oxadiazole with thiadiazole moiety (6-27) were synthesized, characterized by different spectroscopic techniques and evaluated for ß-glucuronidase inhibitory potential. Sixteen analogs such as 6, 7, 8, 9, 10, 12, 13, 14, 17, 18, 20, 23, 24, 25, 26 and 27 showed IC50 values in the range of 0.96 ±â€¯0.01 to 46.46 ±â€¯1.10 µM, and hence were found to have excellent inhibitory potential in comparison to standard d-saccharic acid 1,4-lactone (IC50 = 48.4 ±â€¯1.25 µM). Two analogs such as 16 and 19 showed moderate inhibitory potential while analogs 11, 15, 21 and 22 were found inactive. Our study identifies new series of potent ß-glucuronidase inhibitors for further investigation. Structure activity relationships were established for all compounds which showed that the activity is varied due to different substituents on benzene ring. The interaction of the compounds with enzyme active site were confirmed with the help of docking studies, which reveals that the electron withdrawing group and hydroxy group make the molecules more favorable for enzyme inhibition.


Assuntos
Glicoproteínas/uso terapêutico , Simulação de Acoplamento Molecular/métodos , Oxidiazóis/síntese química , Glicoproteínas/farmacologia , Oxidiazóis/química
4.
Molecules ; 24(8)2019 Apr 18.
Artigo em Inglês | MEDLINE | ID: mdl-31003424

RESUMO

Chromen-4-one substituted oxadiazole analogs 1-19 have been synthesized, characterized and evaluated for ß-glucuronidase inhibition. All analogs exhibited a variable degree of ß-glucuronidase inhibitory activity with IC50 values ranging in between 0.8 ± 0.1-42.3 ± 0.8 µM when compared with the standard d-saccharic acid 1,4 lactone (IC50 = 48.1 ± 1.2 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
Benzopiranos/síntese química , Benzopiranos/farmacologia , Glicoproteínas/síntese química , Glicoproteínas/farmacologia , Oxidiazóis/síntese química , Oxidiazóis/farmacologia , Benzopiranos/química , Glucuronidase/química , Glucuronidase/metabolismo , Glicoproteínas/química , Concentração Inibidora 50 , Ligantes , Simulação de Acoplamento Molecular , Oxidiazóis/química
5.
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
6.
Bioorg Chem ; 85: 109-116, 2019 04.
Artigo em Inglês | MEDLINE | ID: mdl-30605884

RESUMO

New series of quinoline-based thiadiazole analogs (1-20) were synthesized, characterized by EI-MS, 1H NMR and 13C NMR. All synthesized compounds were subjected to their antileishmanial potential. Sixteen analogs 1-10, 12, 13, 16, 17, 18 and 19 with IC50 values in the range of 0.04 ±â€¯0.01 to 5.60 ±â€¯0.21 µM showed tremendously potent inhibition as compared to the standard pentamidine with IC50 value 7.02 ±â€¯0.09 µM. Analogs 11, 14, 15 and 20 with IC50 8.20 ±â€¯0.35, 9.20 ±â€¯0.40, 7.20 ±â€¯0.20 and 9.60 ±â€¯0.40 µM respectively showed good inhibition when compared with the standard. Structure-activity relationships have been also established for all compounds. Molecular docking studies were performed to determine the binding interaction of the compounds with the active site target.


Assuntos
Quinolinas/farmacologia , Tiadiazóis/farmacologia , Tripanossomicidas/farmacologia , Domínio Catalítico , Leishmania donovani/química , Leishmania major/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Simulação de Acoplamento Molecular , Estrutura Molecular , Oxirredutases/química , Oxirredutases/metabolismo , Ligação Proteica , Quinolinas/síntese química , Quinolinas/metabolismo , Relação Estrutura-Atividade , Tiadiazóis/síntese química , Tiadiazóis/metabolismo , Tripanossomicidas/síntese química , Tripanossomicidas/metabolismo
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