Synthesis of new 2-{2,3-dihydro-1, 4-benzodioxin-6-yl[(4-methylphenyl) sulfonyl]amino}-N-(un/substituted-phenyl)acetamides as α-glucosidase and acetylcholinesterase inhibitors and their in silico study
Braz. J. Pharm. Sci. (Online)
;
55: e17032, 2019. tab, graf
Artigo
em Inglês
| LILACS
| ID: biblio-1019533
ABSTRACT
The aim of the present research work was to investigate the enzyme inhibitory potential of some new sulfonamides having benzodioxane and acetamide moieties. The synthesis was started by the reaction of N-2,3-dihydrobenzo[1,4]-dioxin-6-amine (1) with 4-methylbenzenesulfonyl chloride (2) in the presence of 10% aqueous Na2CO3 to yield N-(2,3-dihydrobenzo[1,4]-dioxin-6-yl)-4-methylbenzenesulfonamide (3), which was then reacted with 2-bromo-N-(un/substituted-phenyl)acetamides (6a-l) in DMF and lithium hydride as a base to afford various 2-{2,3-dihydro-1,4-benzodioxin-6-yl[(4-methylphenyl)sulfonyl]amino}-N-(un/substituted-phenyl)acetamides (7a-l). All the synthesized compounds were characterized by their IR and 1H-NMR spectral data along with CHN analysis data. The enzyme inhibitory activities of these compounds were tested against a-glucosidase and acetylcholinesterase (AChE). Most of the compounds exhibited substantial inhibitory activity against yeast a-glucosidase and weak against AChE. The in silico molecular docking results were also consistent with in vitro enzyme inhibition data.
Texto completo:
DisponíveL
Índice:
LILACS (Américas)
Assunto principal:
Sulfonamidas
/
Inibidores da Colinesterase
/
Inibidores de Glicosídeo Hidrolases
Idioma:
Inglês
Revista:
Braz. J. Pharm. Sci. (Online)
Assunto da revista:
Farmacologia
/
Teraputica
/
Toxicologia
Ano de publicação:
2019
Tipo de documento:
Artigo
País de afiliação:
Malásia
/
Paquistão
Instituição/País de afiliação:
Abdul Wali Khan University/PK
/
Government College University/PK
/
The Islamia University of Bahawalpur/PK
/
Universiti Teknologi MARA/MY
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