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

@article{Chan1994IdentificationOA,
  title={Identification of a new class of ETA selective endothelin antagonists by pharmacophore directed screening.},
  author={Ming Fai Chan and Ilya Okun and F L Stavros and E Hwang and Manfred E. Wolff and V. N. Balaji},
  journal={Biochemical and biophysical research communications},
  year={1994},
  volume={201 1},
  pages={228-34}
}
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… CONTINUE READING