2. Academic Validation
  3. Discovery and structure-activity relationships of sulfonamide ETA-selective antagonists

Discovery and structure-activity relationships of sulfonamide ETA-selective antagonists

  • J Med Chem. 1995 Apr 14;38(8):1344-54. doi: 10.1021/jm00008a013.
P D Stein 1,  D M Floyd,  S Bisaha,  J Dickey,  R N Girotra,  J Z Gougoutas,  M Kozlowski,  V G Lee,  E C Liu,  M F Malley
Affiliations

Affiliation

  • 1 Department of Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, New Jersey 08543-4000, USA.
PMID: 7731020 DOI: 10.1021/jm00008a013
Abstract

Random screening of compounds in an ETA receptor binding assay led to the discovery of a class of benzenesulfonamide ligands. Optimization led to the development of 5-amino-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulfonamides which were functional antagonists. Structural features which were important to activity included a 1,5-substitution pattern on the naphthalene ring; a sulfonamide NH with a pK value < 7; an amine, preferably with alkyl substituents, at the 5-position; and methyl groups on both the 3- and 4-positions of the isoxazole.

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