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

咪唑并[1,2-a]吡啶作为新型强效 ASK1 抑制剂的设计和生物学评价

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作者:Yoshito Terao, Hideo Suzuki, Masato Yoshikawa, Hiroaki Yashiro, Shiro Takekawa, Yasushi Fujitani, Kengo Okada, Yoshihisa Inoue, Yoshio Yamamoto, Hideyuki Nakagawa, Shuhei Yao, Tomohiro Kawamoto, Osamu Uchikawa

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.

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