Abstract

Garima Kapoor¹, Dharam Pal Pathak¹, Rubina Bhutani¹, Asif Husain², Sandeep Jain³, Ravi Kant¹ and Md. Azhar Iqbal²

DOI : http://dx.doi.org/10.13005/ojc/340505

A receptor peroxisome proliferator activated receptor-gamma was targeted by series of new fatty acid chemical entities (M1- M22) which was designed, synthesized and characterized by spectral analysis. Metabolites molecular properties were calculated using Lipinski’s rule of five using molinspiration online software. Docking studies were done on co-crystallized protein structure of PPAR γ, PDB-1FM9 showing M15, M17 and M8 to be best located in the active sites with scores -10.43, -10.21 and -10.00 respectively. The free binding energy estimation was done using model of Maestro 9.0 (Schrodinger) and lies between -80.15 to -61.26 kcal/mol which is significant as compared to that of standard (-48.58 Kcal/mol). Nine best docked derivatives were evaluated in-vivo for oral glucose tolerance and antihyperglycemic activity by streptozotocin induced diabetes model and M15 exhibited most promising antidiabetic activity more than the standard glibenclamide. The promising results encourage future investigation on fatty acids for development of active compounds.

Fatty acids; Hyperglycaemic; OGTT; Oleic Acid; PPAR; STZ

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