2. Academic Validation
  3. Identification of a new class of ETA selective endothelin antagonists by pharmacophore directed screening

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

Affiliation

  • 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.

Figures
Products
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z