Literature DB >> 21986586

Identification and SAR of selective inducible nitric oxide synthase (iNOS) dimerization inhibitors.

Timothy C Gahman1, Mark R Herbert, Henk Lang, Angie Thayer, Kent T Symons, Phan Manh Nguyen, Mark E Massari, Sara Dozier, Yan Zhang, Marciano Sablad, Tadimeti S Rao, Stewart A Noble, Andrew K Shiau, Christian A Hassig.   

Abstract

We have identified and synthesized a series of imidazole containing dimerization inhibitors of inducible nitric oxide synthase (iNOS). The necessity of key imidazole and piperonyl functionality was demonstrated and SAR studies led to the identification of compound 35, which showed a dose dependant inhibition in multiple pain models, including tactile allodynia induced by spinal nerve ligation (Chung model).
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID: 21986586     DOI: 10.1016/j.bmcl.2011.08.112

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  4 in total

Review 1.  Nitric oxide synthase enzymology in the 20 years after the Nobel Prize.

Authors:  Dennis J Stuehr; Mohammad Mahfuzul Haque
Journal:  Br J Pharmacol       Date:  2018-12-09       Impact factor: 8.739

2.  Mechanism of inducible nitric-oxide synthase dimerization inhibition by novel pyrimidine imidazoles.

Authors:  Latika Nagpal; Mohammad M Haque; Amit Saha; Nirmalya Mukherjee; Arnab Ghosh; Brindaban C Ranu; Dennis J Stuehr; Koustubh Panda
Journal:  J Biol Chem       Date:  2013-05-21       Impact factor: 5.157

3.  SUZUKI-MIYAURA COUPLING REACTIONS OF 3,5-DICHLORO-1,2,4-THIADIAZOLE.

Authors:  Abdelbasset A Farahat; David W Boykin
Journal:  Heterocycles       Date:  2012-08-21       Impact factor: 0.831

4.  Novel 2,4-disubstituted pyrimidines as potent, selective, and cell-permeable inhibitors of neuronal nitric oxide synthase.

Authors:  Paramita Mukherjee; Huiying Li; Irina Sevrioukova; Georges Chreifi; Pavel Martásek; Linda J Roman; Thomas L Poulos; Richard B Silverman
Journal:  J Med Chem       Date:  2014-12-29       Impact factor: 7.446

  4 in total

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