Design, synthesis and biological evaluation of small molecules as potent glucosidase inhibitors

被引：16

作者：

Hati, Santanu ^{[1
]}

Madurkar, Sanjay M. ^{[2
]}

Bathula, Chandramohan ^{[1
]}

Thulluri, Chiranjeevi ^{[3
]}

Agarwal, Rahul ^{[4
]}

Siddiqui, Faiza Amber ^{[5
]}

Dangi, Poonam ^{[4
]}

Adepally, Uma ^{[3
]}

Singh, Ashutosh ^{[4
]}

Singh, Shailja ^{[4
]}

Sen, Subhabrata ^{[1
]}

机构：

[1] Shiv Nadar Univ, Sch Nat Sci, Dept Chem, Gautam Buddha Nagar 201314, UP, India

[2] Mahatma Gandhi Univ, Dept Chem, Ri Bhoi, Meghalaya, India

[3] Jawaharlal Nehru Tech Univ, Inst Sci, Hyderabad, Telangana, India

[4] Shiv Nadar Univ, Sch Nat Sci, Dept Life Sci, Gautam Buddha Nagar 201314, UO, India

[5] Int Ctr Genet Engn & Biotechnol, New Delhi, India

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2015年 / 100卷

关键词：

Antiplasmodial; Alpha-glucosidase; Epoxidation; Virtual screening; Dihydroxylation; DERIVATIVES; MALARIA;

D O I：

10.1016/j.ejmech.2015.04.059

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Herein we have reported design, synthesis and in vitro biological evaluation of a library of bicyclic lactams that led to the discovery of compounds 6 and 7 as a novel class of a-glucosidase inhibitors. They inhibited alpha-glucosidase (yeast origin) in a mixed type of inhibition with an IC50 of similar to 150 nM. Molecular docking studies further substantiated screening results. Interestingly phenotypic screening of this library against the human malaria parasite revealed 7 as a potent antiplasmodial agent. (C) 2015 Elsevier Masson SAS. All rights reserved.

引用

页码：188 / 196

页数：9

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