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PPAR gamma targeted molecular docking and synthesis of some new amide and urea substituted 1, 3, 4‐thiadiazole derivative as antidiabetic compound
Author(s) -
Vaishnav Yogesh,
Dewangan Dhansay,
Verma Shekhar,
Mishra Achal,
Thakur Alok Singh,
Kashyap Pranita,
Verma Santosh Kumar
Publication year - 2020
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.3941
Subject(s) - chemistry , amide , urea , benzamide , agonist , docking (animal) , stereochemistry , carboxamide , combinatorial chemistry , receptor , organic chemistry , biochemistry , medicine , nursing
The PPAR‐γ agonist enhances the insulin sensitivity and avoids the disorganized hyperglycemic by promoting the insulin guided cellular uptake of blood glucose. Therefore, in the present work PPAR‐γ has chosen as the target for the molecular docking study to design an effective agonist of the same. By this research work an effort has been made to prepare amide and urea series of 1, 3, 4‐thiadiazole derivatives as 4‐substituted‐N‐(5‐(4‐(1‐piperidino)1‐piperidinyl)‐1,3,4‐(2‐thiadiazolyl)benzamide (4a‐f) and 1‐(4‐substitutedphenyl)‐3‐(5‐(4‐(1‐piperidino)1‐piperidinyl)‐1,3,4‐(2‐thiadiazolyl)urea (6a‐f) . Both the docking score as well as the pharmacological animal study data has been suggested that the electron donating group containing compound 4f and 6f are most potent molecules for the antidiabetic activity close to the standard drug pioglitazone. It was further observed that the unsubstituted aromatic ring containing derivatives have also considerable effect (4a and 6a) than the electron withdrawing containing derivatives. After the comparison of biological data for amide and urea series, it was concluded that the urea (6a‐f) series is more effective than the amide series.