Literature DB >> 11755336

The design and synthesis of a novel series of indole derived selective ET(A) antagonists.

David J Rawson1, Kevin N Dack, Roger P Dickinson, Kim James.   

Abstract

Conformational constraint has been used as the key design element in the identification of a series of potent and selective ET(A) antagonists. The most potent antagonist, 32, (ET(A) IC(50)=0.55nM) is 722-fold selective over the ET(B) receptor, as measured by binding experiments.

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Year:  2002        PMID: 11755336     DOI: 10.1016/s0960-894x(01)00660-6

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


  1 in total

1.  Myoglobin-Catalyzed C-H Functionalization of Unprotected Indoles.

Authors:  David A Vargas; Antonio Tinoco; Vikas Tyagi; Rudi Fasan
Journal:  Angew Chem Int Ed Engl       Date:  2018-07-06       Impact factor: 15.336

  1 in total

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