Novel thiazole derivatives: a patent review (2008 – 2012; Part 1)

Abstract

This review of patented products presents the thiazole ring as the nucleus of the derivatives considered from a medicinal chemistry perspective. The applications are based firstly on the specific enzyme target with very low development in the disease treatment. Most of the described compounds are shown to have beneficial therapeutic effects but at the same time these compounds, selective for 'multi-signaling pathway' targets, may also increase the side-effect potential.

Thiazole derivatives as inhibitors of cyclooxygenases in vitro and in vivo

“…We have described these molecules as specific anticyclooxygenase activities with no cytotoxic effects on cultured cells. Additional investigation is required to characterize their side effects, if any, in vivo (Leoni et al, 2014). In conclusion, our results further confirm a selective role of thiazoles as COX inhibitors.…”

Podophyllotoxin derivatives: a patent review (2012 – 2014)

“…Due to their versatile biological profiles these scaffolds have attracted great interest in the development of chemical libraries, which serve as one of the key sources for the identification of drug candidates. This is evident from the number of patents that have been granted in the past few years discussing the biological activities of heterocycles [42,43]. In view of this Mei et al have patented DEPPT-based furan derivatives as antitumor agents [44].…”

Thiazoles in Peptides and Peptidomimetics

“…Thiazole (C 3 H 3 NS) is a five-membered heterocyclic aromatic compound found in many natural products [1][2][3][4] including vitamin B1, and has been widely incorporated into synthetic molecules including pharmaceuticals, [5] catalysts [6] and dyes [7].…”