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1.
Med Chem ; 16(6): 826-840, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-31195949

RESUMO

BACKGROUND: Results of our previous studies on antiglycation activity, and the noncytotoxicity of 2-mercapto benzothiazoles, encouraged us to further widen our investigation towards the identification of leads against diabetes mellitus. METHODS: 33 derivatives of 2-mercapto benzothiazoles 1-33 were evaluated for in vitro α- glucosidase inhibitory activity. Mode of inhibition was deduced by kinetic studies. To predict the interactions of 2-mercapto benzothiazole derivatives 1-33 with the binding pocket of α-glucosidase enzyme, molecular docking studies were performed on the selected inhibitors. RESULTS: Compounds 2-4, 6-7, 9-26, 28 and 30 showed many folds potent α-glucosidase inhibitory activity in the range of IC50 = 31.21-208.63 µM, as compared to the standard drug acarbose (IC50 = 875.75 ± 2.08 µM). It was important to note that except derivative 28, all other derivatives were also found previously to have antiglycating potential in the range of IC50 = 187.12-707.21 µM. CONCLUSION: A number of compounds were identified as dual nature as antiglycating agent and α- glucosidase inhibitors. These compounds may serve as potential lead candidates for the management of diabetes mellitus.


Assuntos
Benzotiazóis/química , Inibidores de Glicosídeo Hidrolases/síntese química , Inibidores de Glicosídeo Hidrolases/farmacologia , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Cinética , Modelos Moleculares , Simulação de Acoplamento Molecular , Ligação Proteica , Conformação Proteica , Saccharomyces cerevisiae/enzimologia , Relação Estrutura-Atividade , alfa-Glucosidases/química , alfa-Glucosidases/metabolismo
2.
RSC Adv ; 8(4): 1803-1807, 2018 Jan 05.
Artigo em Inglês | MEDLINE | ID: mdl-35542602

RESUMO

The development of new non-platinum catalysts for alcohol electrooxidation is of utmost importance. In this work, a bimetallic Pd-Cu loaded porous carbon material was first synthesized from a Cu-based metal-organic framework (MOF). The Cu loaded porous carbon was pre-synthesized through calcinating the Cu-based MOF under a N2 atmosphere. After loading Pd onto the precursor and heating, Pd-Cu loaded porous carbon (Pd-Cu/C) was obtained for alcohol electrooxidation. Electrooxidation experiments revealed that this Pd-Cu bimetal loaded porous carbon assisted steady state electrolysis for alcohol oxidation in alkaline media. Moreover, different alcohols were electrooxidated using the present electrocatalyst for the purposes of discussing the oxidation mechanism. This electrooxidation study of Pd-Cu/C derived from a MOF demonstrates a good understanding of the electrooxidation of different alcohols, and provides useful guidance for developing new electrocatalyst materials for energy conversion and electronic devices.

3.
Bioorg Chem ; 70: 133-143, 2017 02.
Artigo em Inglês | MEDLINE | ID: mdl-28038777

RESUMO

In this study, twenty-five (25) substituted aryl thiazoles (SAT) 1-25 were synthesized, and their in vitro cytotoxicity was evaluated against four cancer cell lines, MCF-7 (ER+ve breast), MDA-MB-231 (ER-ve breast), HCT116 (colorectal) and HeLa (cervical). The activity was compared with the standard anticancer drug doxorubicin (IC50=1.56±0.05µM). Among them, compounds 1, 4-8, and 19 were found to be toxic to all four cancer cell lines (IC50 values 5.37±0.56-46.72±1.80µM). Compound 20 was selectively active against MCF7 breast cancer cells with IC50 of 40.21±4.15µM, whereas compound 19 was active against MCF7 and HeLa cells with IC50 of 46.72±1.8, and 19.86±0.11µM, respectively. These results suggest that substituted aryl thiazoles 1 and 4 deserve to be further investigated in vivo as anticancer leads.


Assuntos
Antineoplásicos/química , Antineoplásicos/farmacologia , Sobrevivência Celular/efeitos dos fármacos , Tiazóis/química , Tiazóis/farmacologia , Antineoplásicos/síntese química , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Técnicas de Química Combinatória/métodos , Desenho de Fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Células HCT116 , Células HeLa , Humanos , Células MCF-7 , Neoplasias/tratamento farmacológico , Relação Estrutura-Atividade , Tiazóis/síntese química
4.
Bioorg Chem ; 62: 106-16, 2015 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-26318401

RESUMO

A series of thirty (30) thiazole analogs were prepared, characterized by (1)H NMR, (13)C NMR and EI-MS and evaluated for Acetylcholinesterase and butyrylcholinesterase inhibitory potential. All analogs exhibited varied butyrylcholinesterase inhibitory activity with IC50 value ranging between 1.59±0.01 and 389.25±1.75µM when compared with the standard eserine (IC50, 0.85±0.0001µM). Analogs 15, 7, 12, 9, 14, 1, 30 with IC50 values 1.59±0.01, 1.77±0.01, 6.21±0.01, 7.56±0.01, 8.46±0.01, 14.81±0.32 and 16.54±0.21µM respectively showed excellent inhibitory potential. Seven analogs 15, 20, 19, 24, 28, 30 and 25 exhibited good acetylcholinesterase inhibitory potential with IC50 values 21.3±0.50, 35.3±0.64, 36.6±0.70, 44.81±0.81, 46.36±0.84, 48.2±0.06 and 48.72±0.91µM respectively. All other analogs also exhibited well to moderate enzyme inhibition. The binding mode of these compounds was confirmed through molecular docking.


Assuntos
Doença de Alzheimer , Inibidores da Colinesterase/farmacologia , Tiazóis/farmacologia , Butirilcolinesterase , Domínio Catalítico , Simulação de Acoplamento Molecular
5.
Med Chem ; 10(8): 824-35, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-24693932

RESUMO

This manuscript describes the protein anti-glycation activity of thirty-three (33) benzothiazoles, out of which twenty-seven were the newly synthesized benzothiazoles. Compound 1 (IC50= 187 ± 2.6 µM) was found to be the most active, while compounds 2 (IC50= 219 ± 3.6 µM), 3 (IC50= 224 ± 1.9 µM), 4 (IC50= 223 ± 3.3 µM), 5 (IC50= 238 ± 2.2 µM), 7 (IC50= 266 ± 5.4 µM), 17 (IC50= 226 ± 1.6 µM) and 18 (IC50= 274 ± 2.4 µM) were significantly active, when compared with the standard rutin (IC50= 294 ± 1.5 µM). This study identified potential inhibitors of methylglyoxal mediated glycation of proteins, which is the pathophysiology of late diabetic complications.


Assuntos
Benzotiazóis/síntese química , Produtos Finais de Glicação Avançada/antagonistas & inibidores , Aldeído Pirúvico/química , Células 3T3 , Animais , Benzotiazóis/química , Benzotiazóis/farmacologia , Bovinos , Sobrevivência Celular/efeitos dos fármacos , Galinhas , Produtos Finais de Glicação Avançada/química , Glicosilação/efeitos dos fármacos , Camundongos , Muramidase/antagonistas & inibidores , Muramidase/química , Rutina/farmacologia , Soroalbumina Bovina/antagonistas & inibidores , Soroalbumina Bovina/química , Relação Estrutura-Atividade
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