Design, synthesis, characterization, docking studies of novel 4-phenyl acrylamide-1,3-thiazole derivatives as anti-inflammatory and anti-ulcer agents

Abstract

A great extent of nitrogen containing heterocyclic moiety comprising sulfur atom is recognized as a valuable combination of therapeutics in medicinal chemistry. In particular, thiazoles analogs play a very significant pharmacological role in many potent biological activities, hence drugs like tiazofurin, abafungin, meloxicam, fanetinole, sulphathiazole and thiamine are well known in market. The incorporation of the thiaazole ring can offer enhanced physical-chemical properties to show a wide scope of targets and diverse biological applications. In this view, the title compounds 7(a-j) were synthesized in good yield. The purified compounds were explained by spectroscopic procedures (FT-IR, 1H NMR, 13CNMR, and LC-MS), and lastly, Among the series of (7a-j), compound (7e) showed maximum selectivity for COX-2 with an IC50 of 8.68±0.31 μM, and the rest of the compounds lies at just below the (7e) which reveals that this compound is quite effective for COX-1 rather than COX-2. The activity found in compound (7e) is attributable to the presence of electron releasing methyl group that has the strongest contact with the active site of H+/K+ ATPase in this study.