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Design, synthesis and biological evaluation of small molecules as potent glucosidase inhibitors
Hati S., Madurkar S.M., Bathula C., Thulluri C., Agarwal R., Siddiqui F.A., Dangi P., Adepally U., , Singh S.Show More
Published in Elsevier Masson SAS
PMID: 26087029
Volume: 100
Pages: 188 - 196
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. © 2015 Elsevier Masson SAS.
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Published in Elsevier Masson SAS
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