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

  • Bioorg Med Chem Lett. 2012 Dec 15;22(24):7326-9. doi: 10.1016/j.bmcl.2012.10.084.
Yoshito Terao  1 ,  Hideo Suzuki ,  Masato Yoshikawa ,  Hiroaki Yashiro ,  Shiro Takekawa ,  Yasushi Fujitani ,  Kengo Okada ,  Yoshihisa Inoue ,  Yoshio Yamamoto ,  Hideyuki Nakagawa ,  Shuhei Yao ,  Tomohiro Kawamoto ,  Osamu Uchikawa
Affiliations
  • 1. Pharmaceutical Research Division, Takeda Pharmaceutical Company Limited, 26-1, Muraoka-Higashi 2-Chome, Fujisawa, Kanagawa 251-8555, Japan. [email protected]
PMID: 23147077 DOI: 10.1016/j.bmcl.2012.10.084
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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