Bioorganic & Medicinal Chemistry Letters 2012-12-15

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

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

Index: Bioorg. Med. Chem. Lett. 22(24) , 7326-9, (2012)

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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.Copyright © 2012 Elsevier Ltd. All rights reserved.