Thursday , 13 May 2021

Synthesis, characterization and in vitro biological evaluation of some new 3-substituted 3-(4-aryloxyaryl)-propanoic acids as GPR40 agonists

Chandra Sekhar Gudla*1, Madhavan .G.R1, Nagarajan Arumugam2
1Connexios Life Sciences Private Limited, 108/27, 29th main, 23rd cross, BTM Layout – II stage, Bangalore –560076, India
2Department of Pharmaceutical Chemistry, PSG College of Pharmacy, Peelamedu, Coimbatore-641004, Tamilnadu, India

In this letter, the series of 3-(4-aryloxyaryl) propanoic acid compounds design, synthesis, structure–activity relationship (SAR) and the ability to modulate the activity of GPR40 is described. The Systematic replacement of aryl, Heteroaryl groups, various substitutions and optimization of chain length led to identification of potent GPR40 agonists. In order to identify candidates suitable for in vivo validation of the target, pharmacokinetic properties were determined for few compounds and further profiling of these compounds are presented. The compound 16 may prove useful for the treatment of Type 2 diabetes.
Keywords: GPR40, SAR, In-vitro, pharmacokinetics

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