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Eur J Med Chem. 2014 Mar 3;74:461-76. doi: 10.1016/j.ejmech.2013.12.039. Epub 2014 Jan 8.

1-Phenyl-1H- and 2-phenyl-2H-1,2,3-triazol derivatives: design, synthesis and inhibitory effect on alpha-glycosidases.

Author information

1
Universidade Federal Fluminense, Instituto de Química, Departamento de Química Orgânica, Campus do Valonguinho, 24210-141 Niterói, RJ, Brazil.
2
Fundação Oswaldo Cruz, Instituto Oswaldo Cruz, Laboratório de Bioquímica de Proteínas e Peptídeos, 21040-360 Rio de Janeiro, RJ, Brazil.
3
Universidade Federal Fluminense, Instituto de Química, Departamento de Química Orgânica, Campus do Valonguinho, 24210-141 Niterói, RJ, Brazil. Electronic address: cegvito@vm.uff.br.
4
Fundação Oswaldo Cruz, Instituto Oswaldo Cruz, Laboratório de Bioquímica de Proteínas e Peptídeos, 21040-360 Rio de Janeiro, RJ, Brazil. Electronic address: floriano@ioc.fiocruz.br.

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 α-glycosidase 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 α-glucosidase (MAL12) and porcine pancreatic α-amylase activity (PPA). Of the 60 compounds tested at 500 μM, 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 μM for MAL12 and 145 to 282 μM 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; Glycosidase inhibitors; Maltase; Triazole

PMID:
24487194
DOI:
10.1016/j.ejmech.2013.12.039
[Indexed for MEDLINE]
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