Design and biological evaluation of imidazo [1, 2-a] pyridines as novel and potent ASK1 inhibitors

…, H Nakagawa, S Yao, T Kawamoto, O Uchikawa

Index: Terao, Yoshito; Suzuki, Hideo; Yoshikawa, Masato; Yashiro, Hiroaki; Takekawa, Shiro; Fujitani, Yasushi; Okada, Kengo; Inoue, Yoshihisa; Yamamoto, Yoshio; Nakagawa, Hideyuki; Yao, Shuhei; Kawamoto, Tomohiro; Uchikawa, Osamu Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 24 p. 7326 - 7329

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Citation Number: 18

Abstract

Imidazo [1, 2-a] pyridine derivatives were designed, synthesized, and evaluated as inhibitors of the apoptosis signal-regulating kinase 1 (ASK1). These were based on a benzothiazole derivative that was discovered from high-throughput screening of our compound library. As a result, we identified potent, selective, and orally bioavailable ASK1 inhibitors for wide range of therapeutic targets.