In search of new α-glucosidase inhibitors: Imidazolylpyrazole derivatives.
Bioorg Chem
; 71: 102-109, 2017 04.
Article
em En
| MEDLINE
| ID: mdl-28160945
ABSTRACT
Under three different reaction conditions (conventional heating, microwave irradiations and amino acid catalysis), a series of imidazolylpyrazoles (2a-2k) were synthesized in good to excellent yields from a mixture of three precursors aryl(hetaryl)pyrazole-4-carbaldehydes (1a-1k), benzil and ammonium acetate. α-Glucosidase inhibition assay revealed a new class of highly potent agents wherein each compound displayed significant inhibitory potentials (in terms of percentage inhibition and relative IC50 values) as compared to that of the reference drug (Acarbose). Moreover, molecular modelling of most potent compounds 2h, 2j and 2k also helped in understanding the structure and activity relationship.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Pirazóis
/
Saccharomyces cerevisiae
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Alfa-Glucosidases
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Inibidores de Glicosídeo Hidrolases
Limite:
Humans
Idioma:
En
Revista:
Bioorg Chem
Ano de publicação:
2017
Tipo de documento:
Article
País de afiliação:
Paquistão