Background: We have developed a new series of 36 substituted thiazole derivatives
prepared via reaction of substituted benzothiazole-2-amine with substituted phenacyl
Objective: This study was aimed to develop and successfully evaluate anti-inflammatory activity
of substituted thiazole derivatives.
Method: A new series of 36 substituted thiazole derivatives was synthesized and derivatives
were characterized by analytical and spectrometric methods like IR, MS, and 1H NMR. The
molecular docking was performed for all the synthesized thiazole derivatives to assess their
binding affinities to COX-2 isozyme. The best compounds from docking study were subjected
for their anti-inflammatory activity by using rat hind paw edema method.
Results: Results from carrageenan-induced hind paw edema showed that compounds 3h,
5a, 5e, 9d, and 9h possess significant anti-inflammatory activity. The result from vascular
permeability indicating inhibition of vascular permeability with compounds 3h and 9h is
significant and results from cotton pellet granuloma formation models show greater degree
of inhibition with compounds 3h and 5a to contribute to their significant anti-inflammatory
Conclusion: This study provides successful development of novel thiazole derivatives.
Their binding affinities to COX-2 enzyme were also confirmed, indicating that developed
molecules are comparable to diclofenac and hence could be promising anti-inflammatory