Identification of a new class of ETA selective endothelin antagonists by pharmacophore directed screening

  • Biochem Biophys Res Commun. 1994 May 30;201(1):228-34. doi: 10.1006/bbrc.1994.1693.
M F Chan  1 ,  I Okun ,  F L Stavros ,  E Hwang ,  M E Wolff ,  V N Balaji
Affiliations
  • 1. Department of Medicinal Chemistry, ImmunoPharmaceutics, Inc., San Diego, CA 92127.
PMID: 8198578 DOI: 10.1006/bbrc.1994.1693
Abstract

Novel endothelin antagonists were identified through a "pharmacophore directed screening" strategy. The sulfanilamide Antibacterial agent sulfisoxazole was found to be a good Endothelin Receptor Antagonist (IC50's of 0.60 microM and 22 microM for the ETA and ETB receptors, respectively). The structurally similar sulfamethoxazole was found to be a weaker antagonist (IC50 for ETA 16 microM and for ETB 230 microM). These compounds represent a new class of low molecular weight and ETA-selective non-peptide endothelin antagonists.

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