22258-56-6Relevant articles and documents
-
Smushkevich,Yu.I. et al.
, (1969)
-
Synthesis and evaluation of 5,6-disubstituted thiopyrimidine aryl aminothiazoles as inhibitors of the calcium-activated chloride channel TMEM16A/Ano1
Piechowicz, Katarzyna A.,Truong, Eric C.,Javed, Kashif M.,Chaney, Rachelle R.,Wu, Johnny Y.,Phuan, Puay W.,Verkman, Alan S.,Anderson, Marc O.
, p. 1362 - 1368 (2016/10/09)
Transmembrane protein 16A (TMEM16A), also called Ano1, is a Ca2+ activated Cl? channel expressed widely in mammalian epithelia, as well as in vascular smooth muscle and some tumors and electrically excitable cells. TMEM16A inhibitors have potential utility for treatment of disorders of epithelial fluid and mucus secretion, hypertension, some cancers and other diseases. 4-Aryl-2-amino thiazole T16Ainh-01 was previously identified by high-throughput screening. Here, a library of 47 compounds were prepared that explored the 5,6-disubstituted pyrimidine scaffold found in T16Ainh-01. TMEM16A inhibition activity was measured using fluorescence plate reader and short-circuit current assays. We found that very little structural variation of T16Ainh-01 was tolerated, with most compounds showing no activity at 10 μM. The most potent compound in the series, 9bo, which substitutes 4-methoxyphenyl in T16Ainh-01 with 2-thiophene, had IC50 ～1 μM for inhibition of TMEM16A chloride conductance.
Synthesis of some new formazanyl-thiazolyl-indoles and formazanyl-oxazolyl-indoles as inflammation inhibitors
Bansal,Srivastava,Kumar
, p. 357 - 362 (2007/10/03)
Various 3-(2-arylideneaminothiazol-4-yl)indoles 3a-e and 3-(2-arylideneaminooxazol-4-yl)indoles 3a'-e' on diazotisation with aniline afford 3-[2-(1'-phenyl-3'-substituted-aryl-formazan-4'-yl)thiazol-4-yl] indoles 4a-e and 3-[2-(1'-substituted-phenyl-3'-substituted aryl-formazan-4'-yl)oxazol-4-yl]indoles 4a'-e' respectively. All the compounds have shown interesting antiinflammatory activity in carrageenan induced oedema in rats at 50 mg/kg p.o. The most active compound in the series is 3-[2-(o-methoxybenzylidene)aminothiazol-4-yl]indole which has shown higher antiinflammatory activity and lower ulcerogenic property than phenylbutazone.
