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Peptoids as endothelin receptor antagonists
F Dasgupta1, N Gangadhar, M Bruhaspathy
1New Drug Discovery Research, Ranbaxy Laboratories Limited, New Delhi, India. fdcarbo@hotmail.com
Bioorganic & Medicinal Chemistry Letters
|March 7, 2001
Abstract:
A series of new peptoids as endothelin receptor antagonists has been synthesized. Screening them for their ability to bind with endothelin receptors (ET(A) and ET(B)) competitively in the presence of (125I) endothelin led to the discovery of compounds as possible leads with IC50s in the low micromolar concentrations.