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.

Ashutosh Singh

Life Sciences

(SoNS) School of Natural Sciences

Subhabrata Sen

Chemistry

Hati S.

Madurkar S.M.

Bathula C.

Thulluri C.

Agarwal R.

Siddiqui F.A.

Dangi P.

Adepally U.

Singh S.

<p>Shiv Nadar University is a comprehensive, multidisciplinary, research-focused, and student-centric University offering a full range of academic programs at the undergraduate, postgraduate and doctoral level. With state-of-the-art infrastructure, the University comprises of academic wings, sophisticated labs, international standard sports facilities, amphitheaters, auditorium, conference rooms and smart classrooms. The University&rsquo;s goal is to become internationally recognized for the quality of its research and creative endeavors and their applicability to improving quality of life, generating new insights and expanding the boundaries of human knowledge creativity. Committed to excellence in teaching, research and service, the University aims to serve the higher education needs of India and the world beyond.</p>

Shiv Nadar University

European Journal of Medicinal Chemistry

Diabetes a non-communicable disease occurs either due to the lack of insulin or the inability of the human body to recognize it. The recent data indicated an increase in the trend of people diagnosed with type 2 diabetes mainly due to unhealthy life style. Here in we report a new class of oxindole derivatives 6a-k via scaffold hopping of known α-glucosidase inhibitors 1–4. When molecular docking was performed against a homology model of α-glucosidase the resulting compound 6d revealed binding interactions comparable to 1–4. The compounds were accessed through a unique condensation-ring opening protocol of pyridofuranone building blocks. Overall the compounds exhibited decent binding to the yeast α-glucosidase, where the most potent compound 6h, inhibited the enzyme with IC 50 of 0.6 µM. This was nearly threefold improvement from the original known compounds 1–4, selected to design the newer analogs. The reaction kinetics of 6h indicated competitive inhibition. © 2018 Elsevier Ltd

Bioorganic and Medicinal Chemistry

Design, synthesis and in vitro study of densely functionalized oxindoles as potent α-glucosidase inhibitors

Bioorganic & Medicinal Chemistry

Oxadiazoles and thiadiazoles: Novel α-glucosidase inhibitors

WITHDRAWN: 2-Arylquinazolin-4(3H)-ones: A new class of α-glucosidase inhibitors

Bioorganic Chemistry

3-Hydroxypyrrolidine and (3,4)-dihydroxypyrrolidine derivatives: Inhibition of rat intestinal α-glucosidase

Planta Medica

α-Glucosidase Inhibitory Activities of Isoflavanones, Isoflavones, and Pterocarpans from Mucuna pruriens

Chemical and Pharmaceutical Bulletin

Synthesis and Biological Evaluation of 3-Styrylchromone Derivatives as Free Radical Scavengers and α-Glucosidase Inhibitors

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