Please use this identifier to cite or link to this item: http://www.arca.fiocruz.br/handle/icict/9894
Title: 1-Phenyl-1H- and 2-phenyl-2H-1,2,3-triazol derivatives: Design, synthesis and inhibitory effect on alpha-glycosidases
Authors: Gonzaga, Daniel
Senger, Mario Roberto
Da Silva, Fernando de Carvalho
Ferreira, Vitor Francisco
Silva, Floriano Paes
Affilliation: Universidade Federal Fluminense. Instituto de Química. Departamento de Química Orgânica. Niterói, RJ, Brasil.
Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Bioquímica de Proteínas e Peptídeos. RJ, Brasil
Universidade Federal Fluminense. Instituto de Química. Departamento de Química Orgânica. Niterói, RJ, Brasil.
Universidade Federal Fluminense. Instituto de Química. Departamento de Química Orgânica. Niterói, RJ, Brasil.
Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Bioquímica de Proteínas e Peptídeos. RJ, Brasil
Abstract: Due to aging and increasingly overweight in human population, the incidence of non-insulin dependent diabetes mellitus (NIDDM or Type 2 DM) is increasing considerably. Therefore, searching for new aglycosidase inhibitors (GIs) capable of slowing down carbohydrate assimilation by humans is an important strategy towards control of NIDDM. In this report, we disclose the search for new easily accessible synthetic triazoles as anti-diabetic compounds. Two series of non-glycosid triazoles were synthesized (series A and B) and screened against baker’s yeast a-glucosidase (MAL12) and porcine pancreatic a-amylase activity (PPA). Of the 60 compounds tested at 500 mM, were considered hits ( 60% inhibition) six triazoles against MAL12 and three against PPA, with the inhibition reaching up to 99.4% on MAL12 and 88.6% on PPA. The IC50 values were calculated for both enzymes and ranged from 54 to 482 mM for MAL12 and 145 to 282 mM for PPA. These results demonstrated the potential activity of simple and non-glycosidic triazoles as an important novel class of GIs for the development of drugs to treat Type 2 DM.
Keywords: Amylase
Diabetes
Drug design
Maltase
Triazole
Glycosidase inhibitors
Issue Date: 2014
Publisher: Elsevier
Citation: GONZAGA, Daniel; et al. 1-phenyl-1h- and 2-phenyl-2h-1,2,3-triazol derivatives: design, synthesis and inhibitory effect on alpha-glycosidases. European Journal of Medicinal Chemistry, v.74, p. 461-476,2014.
DOI: DOI:10.1016/j.ejmech.2013.12.039
ISSN: 02235234
Copyright: restricted access
Appears in Collections:IOC - Artigos de Periódicos

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