2. Academic Validation
  3. Discovery of a novel olefin derivative as a highly potent and selective acetyl-CoA carboxylase 2 inhibitor with in vivo efficacy

Discovery of a novel olefin derivative as a highly potent and selective acetyl-CoA carboxylase 2 inhibitor with in vivo efficacy

  • Bioorg Med Chem Lett. 2018 Aug 1;28(14):2498-2503. doi: 10.1016/j.bmcl.2018.05.055.
Yuji Nishiura 1,  Akira Matsumura 2,  Naotake Kobayashi 2,  Atsuyuki Shimazaki 3,  Shingo Sakamoto 4,  Naohisa Kitade 4,  Yutaka Tonomura 4,  Akira Ino 2,  Takayuki Okuno 2
Affiliations

Affiliations

  • 1 Medicinal Research Laboratory, Shionogi & Co., Ltd, 1-1, Futabacho 3-chome, Toyonaka, Osaka 561-0825, Japan. Electronic address: yuji.nishiura@shionogi.co.jp.
  • 2 Medicinal Research Laboratory, Shionogi & Co., Ltd, 1-1, Futabacho 3-chome, Toyonaka, Osaka 561-0825, Japan.
  • 3 Drug Discovery & Disease Research Developmental Research Laboratory, Shionogi & Co., Ltd, 1-1, Futabacho 3-chome, Toyonaka, Osaka 561-0825, Japan.
  • 4 Research Laboratory for Development, Shionogi & Co., Ltd, 1-1, Futabacho 3-chome, Toyonaka, Osaka 561-0825, Japan.
PMID: 29903660 DOI: 10.1016/j.bmcl.2018.05.055
Abstract

Novel Acetyl-CoA Carboxylase 2 (ACC2) selective inhibitors were identified by the conversion of the alkyne unit of A-908292 to the olefin linker. Modification of the center and left part of the lead compound 1b improved the ACC2 inhibitory activity and CYP450 inhibition profile, and afforded a highly selective ACC2 inhibitor 2e which showed in vivo efficacy in C57BL/6 mice.

Keywords

ACC2 inhibitor; Benzothiazole; Olefin; Type 2 diabetes.

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