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Design, Synthesis and Antidiabetic Activity of Biphenylcarbonitrile‐Thiazolidinedione Conjugates as Potential α‐Amylase Inhibitors
Author(s) -
Rathod Chirag H.,
Nariya Pankajkumar B.,
Maliwal Deepika,
Pissurlenkar Raghuvir R. S.,
Kapuriya Naval P.,
Patel Anilkumar S.
Publication year - 2021
Publication title -
chemistryselect
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.437
H-Index - 34
ISSN - 2365-6549
DOI - 10.1002/slct.202004362
Subject(s) - acarbose , pharmacophore , thiazolidinedione , chemistry , conjugate , docking (animal) , pharmacology , amylase , enzyme , in silico , biochemistry , stereochemistry , diabetes mellitus , medicine , type 2 diabetes , endocrinology , mathematical analysis , mathematics , nursing , gene
The α‐amylase inhibition has been considered as an effective therapeutic approach against chronic Type 2 Diabetes mellitus (DM). In the present study, a series of biphenylcarbonitrile‐thiazolidinedione conjugates have been synthesized and evaluated for their antidiabetic activity via α‐amylase inhibition. It was found that most of the conjugates ( 14 a – j ) exhibited significant α‐amylase inhibition activity compared to the standard drug Acarbose. Off these, compound 14 b , 14 c and 14 d were most potent with IC 50 value 0.13 μM, 0.15 μM and 0.13 μM respectively. To ascertain ligand‐receptor interactions, the in silico molecular docking studies of these conjugates ( 14 a – j ) have been carried out into the Acarbose active site of barley (malt) α‐amylase enzyme. The results have shown fair corroboration between significant α‐amylase inhibition activity of 14 b , 14 c and 14 d and their docking scores compared to the standard drug Acarbose. This study demonstrated that biphenylcarbonitrile‐thiazolidinedione conjugate could be a plausible pharmacophore for targeting α‐amylase for the treatment of Type 2 Diabetes mellitus.