Peptoids as endothelin receptor antagonists.
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.
New Drug Discovery Research, Ranbaxy Laboratories Limited, New Delhi, India. fdcarbo@hotmail.com
F
F
Dasgupta
N
N
Gangadhar
M
M
Bruhaspathy
A K
AK
Verma
S
S
Sarin
A K
AK
Mukherjee
D065128:Endothelin Receptor Antagonists; D010455:Peptides / Q000138:chemical synthesis* / Q000494:pharmacology; D034444:Peptoids; D044022:Receptor, Endothelin A; D044023:Receptor, Endothelin B; D013329:Structure-Activity Relationship
D065128:Endothelin Receptor Antagonists; D010455:Peptides; D034444:Peptoids; D044022:Receptor, Endothelin A; D044023:Receptor, Endothelin B