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

European journal of medicinal chemistry (2015-06-19)
Santanu Hati, Sanjay M Madurkar, Chandramohan Bathula, Chiranjeevi Thulluri, Rahul Agarwal, Faiza Amber Siddiqui, Poonam Dangi, Uma Adepally, Ashutosh Singh, Shailja Singh, Subhabrata Sen
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.

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