Literature DB >> 17851073

Structure-activity relationship (SAR) investigations of substituted imidazole analogs as TRPV1 antagonists.

Vijay K Gore1, Vu V Ma, Rami Tamir, Narender R Gavva, James J S Treanor, Mark H Norman.   

Abstract

A novel series of 4,5-biarylimidazoles as TRPV1 antagonists were designed based on the previously reported 4,6-disubstituted benzimidazole series. The analogs were evaluated for their ability to block capsaicin- or acid-induced calcium influx in TRPV1-expressing CHO cells. These studies led to the identification of a highly potent and orally bioavailable TRPV1 antagonist, imidazole 33.

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Year:  2007        PMID: 17851073     DOI: 10.1016/j.bmcl.2007.08.044

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


  5 in total

1.  Dialkylbiaryl Phosphines in Pd-Catalyzed Amination: A User's Guide.

Authors:  David S Surry; Stephen L Buchwald
Journal:  Chem Sci       Date:  2011       Impact factor: 9.825

Review 2.  Biaryl phosphane ligands in palladium-catalyzed amination.

Authors:  David S Surry; Stephen L Buchwald
Journal:  Angew Chem Int Ed Engl       Date:  2008       Impact factor: 15.336

3.  Palladium-catalyzed amination of unprotected five-membered heterocyclic bromides.

Authors:  Mingjuan Su; Naoyuki Hoshiya; Stephen L Buchwald
Journal:  Org Lett       Date:  2014-01-13       Impact factor: 6.005

Review 4.  A structural view of ligand-dependent activation in thermoTRP channels.

Authors:  Ximena Steinberg; Carolyne Lespay-Rebolledo; Sebastian Brauchi
Journal:  Front Physiol       Date:  2014-05-05       Impact factor: 4.566

5.  Site-selective Suzuki-Miyaura coupling of heteroaryl halides - understanding the trends for pharmaceutically important classes.

Authors:  Joshua Almond-Thynne; David C Blakemore; David C Pryde; Alan C Spivey
Journal:  Chem Sci       Date:  2016-08-09       Impact factor: 9.825

  5 in total

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