144059-86-9Relevant articles and documents
Synthesis, biological evaluation and molecular modeling studies of the PPARβ/δ antagonist CC618
Kaupang, ?smund,Paulsen, Steinar Martin,Steindal, Calin C.,Ravna, Aina W.,Sylte, Ingebrigt,Halvorsen, Trine G.,Thoresen, G. Hege,Hansen, Trond Vidar
, p. 229 - 236 (2015)
Herein, we describe the synthesis, biological evaluation and molecular docking of the selective PPARβ/δ antagonist (4-methyl-2-(4-(trifluoromethyl)phenyl)-N-(2-(5-(trifluoromethyl)-pyridin-2-ylsulfonyl)ethyl)thiazole-5-carboxamide)), CC618. Results from in vitro luciferase reporter gene assays against the three known human PPAR subtypes revealed that CC618 selectively antagonizes agonist-induced PPARβ/δ activity with an IC50 Combining double low line 10.0 μM. As observed by LC-MS/MS analysis of tryptic digests, the treatment of PPARβ/δ with CC618 leads to a covalent modification of Cys249, located centrally in the PPARβ/δ ligand binding pocket, corresponding to the conversion of its thiol moiety to a 5-trifluoromethyl-2-pyridylthioether. Finally, molecular docking is employed to shed light on the mode of action of the antagonist and its structural consequences for the PPARβ/δ ligand binding pocket.
Synthesis of Novel Thiazolyl Hydrazine Derivatives and Their Antifungal Activity
Chen, Yazhen,Su, Fen,Wang, Peiyi,Zhu, Jianjun
, (2021/09/13)
A series of novel thiazolyl hydrazine derivatives 3a-3o were synthesized and evaluated for their in vitro antifungal activity against six phytopathogenic strains, namely, Botryosphaeria dothidea (B. d.), Gibberella sanbinetti (G. s.), Fusarium oxysporum (F. o.), Thanatephorus cucumeris (T. c.), Sclerotinia sclerotiorum (S. s.), and Verticillium dahliae (V. d.), by the classical mycelial growth rate method. Biological assessment results showed that most of these target compounds showed good antifungal activity toward tested strains. Especially, compound 3l showed excellent antifungal activities against B. d. and G. s. with relatively lower EC50 values of 0.59 and 0.69 μg/mL, respectively, which were extremely superior to those of commercial fungicides fluopyram, boscalid, and hymexazol and were comparable to those of carbendazim. Given the excellent bioactivity of designed compounds, this kind of thiazolyl hydrazine framework can provide a suitable point for exploring highly efficient antifungal agents.
Identification, synthesis and photo-protection evaluation of arylthiazole derivatives as a novel series of sunscreens
Li, Guoliang,He, Yundong,Zhou, Wenbo,Wang, Peng,Zhang, Yong,Tong, Weiguang,Wu, Haigang,Liu, Mingyao,Ye, Xiyun,Chen, Yihua
, p. 453 - 464 (2014/03/21)
A novel series of arylthiazole derivatives have been designed, synthesized and evaluated in preventing keratinocytes cell (HaCaT) from UVB exposure induced cellar damage. The structure-activity relationship (SAR) was discussed. More importantly, compound 5a significantly protected the dorsal skin of BALB/c-nu mice against UVB-induced decrustation in vivo. The in vitro and in vivo data for these arylthiazole derivatives suggest further studies for their potential use as photo-protection agents as well as sunscreen candidates.