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Eur J Med Chem. 2014 Jan;71:250-8. doi: 10.1016/j.ejmech.2013.10.075. Epub 2013 Nov 15.

Discovery of a benzimidazole series of ADAMTS-5 (aggrecanase-2) inhibitors by scaffold hopping.

Author information

  • 1Pharmaceutical Research Center, Asahi Kasei Pharma Corporation, 632-1 Mifuku, Izunokuni-shi, Shizuoka 410-2321, Japan.
  • 2Pharmaceutical Research Center, Asahi Kasei Pharma Corporation, 632-1 Mifuku, Izunokuni-shi, Shizuoka 410-2321, Japan. Electronic address: atobe.mb@om.asahi-kasei.co.jp.

Abstract

We describe a medicinal chemistry approach to generate a series of benzimidazoles bearing thiazolidin-4-one using scaffold hopping from thiazole 1, our previously described thiazole. Our goal was to discover a potent and permeable small-molecule ADAMTS-5 inhibitor. The results suggest that small compound 22 shows promise as a potent small-molecule ADAMTS-5 inhibitor with good permeability.

Copyright © 2013 Elsevier Masson SAS. All rights reserved.

KEYWORDS:

ADAMTS-5; Benzimidazole; Inhibitor; Osteoarthritis; Thiazolidin-4-one

PMID:
24316668
[PubMed - in process]
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