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Published on: December 1, 2020
Identification of a new class of ETA selective endothelin antagonists by pharmacophore directed screening
M F Chan1, I Okun, F L Stavros
1Department of Medicinal Chemistry, ImmunoPharmaceutics, Inc., San Diego, CA 92127.
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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