European Journal of Medicinal Chemistry 2015-07-15

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

Santanu Hati, Sanjay M Madurkar, Chandramohan Bathula, Chiranjeevi Thulluri, Rahul Agarwal, Faiza Amber Siddiqui, Poonam Dangi, Uma Adepally, Ashutosh Singh, Shailja Singh, Subhabrata Sen

Index: Eur. J. Med. Chem. 100 , 188-96, (2015)

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Abstract

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 α-glucosidase inhibitors. They inhibited α-glucosidase (yeast origin) in a mixed type of inhibition with an IC50 of ∼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. Copyright © 2015 Elsevier Masson SAS. All rights reserved.