958941-29-2Relevant academic research and scientific papers
4′-Methyl-4,5′-bithiazole-based correctors of defective ΔF508-CFTR cellular processing
Yoo, Choong Leol,Yu, Gui Jun,Yang, Baoxue,Robins, Lori I.,Verkman,Kurth, Mark J.
, p. 2610 - 2614 (2008/12/21)
The synthesis and ΔF508-CFTR corrector activity of a 148-member methylbithiazole-based library are reported. Synthetic routes were devised and optimized to generate methylbithiazole analogs in four steps. Corrector potency and efficacy were assayed using epithelial cells expressing human ΔF508-CFTR. These structure-activity data establish that the bithiazole substructure plays a critical function; eight novel methylbithiazole correctors were identified with low micromolar potencies.
