Literature DB >> 24316668

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

Shinya Sogame1, Yoshihito Suenaga1, Masakazu Atobe2, Masashi Kawanishi1, Eiichi Tanaka1, Shiro Miyoshi1.   

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.

Entities:  

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

Mesh:

Substances:

Year:  2013        PMID: 24316668     DOI: 10.1016/j.ejmech.2013.10.075

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  2 in total

1.  Synthesis and biological profile of substituted benzimidazoles.

Authors:  Neelam Vashist; Surinder Singh Sambi; Balasubramanian Narasimhan; Sanjiv Kumar; Siong Meng Lim; Syed Adnan Ali Shah; Kalavathy Ramasamy; Vasudevan Mani
Journal:  Chem Cent J       Date:  2018-12-01       Impact factor: 4.215

2.  Synthesis, DFT studies, molecular docking, antimicrobial screening and UV fluorescence studies on ct-DNA for novel Schiff bases of 2-(1-aminobenzyl) benzimidazole.

Authors:  Sugandha Singhal; Pankaj Khanna; Leena Khanna
Journal:  Heliyon       Date:  2019-10-11
  2 in total

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