4′-Methyl-4, 5′-bithiazole-based correctors of defective ΔF508-CFTR cellular processing

CL Yoo, GJ Yu, B Yang, LI Robins, AS Verkman…

Index: Yoo, Choong Leol; Yu, Gui Jun; Yang, Baoxue; Robins, Lori I.; Verkman; Kurth, Mark J. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 8 p. 2610 - 2614

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Citation Number: 35

Abstract

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 ...