Tumor Necrosis factor-a (TNF- a) is one of the most important mediators of inflammation. Drug discovery literature has several evidences wherein inhibitors of TNF- a were found to be efficacious for treating various inflammatory conditions. Therefore by taking romazarit which was a clinical candidate as a model and by using the template based approach we have designed and synthesized a series of 5-thiazolyl ketoxime derivatives and tested them for their anti-inflammatory and TNF- a release inhibitory potential. These compounds were found to be anti-inflammatory (in vivo), promising inhibitors of TNF-a release by WBC and also inhibitors of LPS induced TNF-a release by human peripheral blood mononuclear cells (hPBMC).  In this presentation the utility of novel 5-thiazolyl ketoxime as a useful epitope for designing potential inhibitors of TNF- a release and its utility as anti-inflammatory agents will be discussed.

Discovery of 5-thiazolyl ketoxime fragment as a pharmacophore for TNF-a release inhibition

241st National Meeting (2011)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.