Literature DB >> 15149643

N-isoquinolin-5-yl-N'-aralkyl-urea and -amide antagonists of human vanilloid receptor 1.

Michele C Jetter1, Mark A Youngman, James J McNally, Sui-Po Zhang, Adrienne E Dubin, Nadia Nasser, Scott L Dax.   

Abstract

Starting from a low micromolar agonist lead identified by high-throughput screening, series of N-isoquinolin-5-yl-N'-aralkyl ureas and analogous amides were developed as potent antagonists of human vanilloid receptor 1 (VR1). The synthesis and structure-activity relationships (SAR) of the series are described.

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Year:  2004        PMID: 15149643     DOI: 10.1016/j.bmcl.2004.04.038

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


  2 in total

1.  How Far Could We Go with Open Data - A Case Study for TRPV1 Antagonists.

Authors:  Daria A Tsareva; Gerhard F Ecker
Journal:  Mol Inform       Date:  2013-06-18       Impact factor: 4.050

2.  Novel scaffolds for modulation of TRPV1 identified with pharmacophore modeling and virtual screening.

Authors:  Daria Goldmann; Peter Pakfeifer; Steffen Hering; Gerhard F Ecker
Journal:  Future Med Chem       Date:  2015       Impact factor: 4.767

  2 in total

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