On June 30, 2021, Abdel-Aziz, Salah A.; Taher, Ehab S.; Lan, Ping; Asaad, Gihan F.; Gomaa, Hesham A. M.; El-Koussi, Nawal A.; Youssif, Bahaa G. M. published an article.Safety of 4-Phenylthiazol-2-amine The title of the article was Design, synthesis, and biological evaluation of new pyrimidine-5-carbonitrile derivatives bearing 1,3-thiazole moiety as novel anti-inflammatory EGFR inhibitors with cardiac safety profile. And the article contained the following:
A new series of pyrimidine-5-carbonitrile derivatives carrying the 1,3-thiazole moiety has been designed and synthesized as novel anti-inflammatory EGFR inhibitors with cardiac and gastric safety profiles and have been assessed for their inhibitory activity against COX-1/COX-2. Compounds 8h, 8n, and 8p (I – III, resp.) were found to be potent and selective COX-2 inhibitors (IC50 = 1.03-1.71μM) relative to celecoxib (IC50 = 0.88μM). The most potent COX-2 inhibitors have been further investigated for their in-vivo anti-inflammatory effect. Compounds 8h, 8n, and 8p showed anti-inflammatory activity up to 90%, 94% and 86% of meloxicam after 4 h interval. 8h, 8n, and 8p showed higher gastric safety profiles than meloxicam. A substantial reduction in serum concentrations of PGE2, TNF-α, IL-6, iNO and MDA and a significant induction of TAC was also observed In vivo experiments on heart rate and blood pressure established the cardiovascular safety profile of 8h, 8n, and 8p. Anti-proliferative and wild-type EGFR inhibitory assays displayed similar results to selective COX-2 inhibition where compounds 8h, 8n, and 8p had a superior inhibition than other tested ones. Mol. docking study demonstrated that these compounds revealed similar orientation and binding interactions as selective COX-2 inhibitors with a higher liability to enter the side pocket selectively. Also, they interacted with EGFR tyrosine kinase main amino acids similar to erlotinib with a strong binding energy score. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Safety of 4-Phenylthiazol-2-amine
The Article related to pyrimidinecarbonitrile thiazole antiinflammatory egfr inhibitor cardiac safety, cox, egfr, il-6, lox, pge(2), pyrimidine, thiazole, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Safety of 4-Phenylthiazol-2-amine
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica