Details

Autor(en) / Beteiligte

• Dasgupta, Falguni
• Gangadhar, N.
• Bruhaspathy, M.
• Verma, Ashwani K.
• Sarin, Simi
• Mukherjee, Ashish K.

Titel

Peptoids as endothelin receptor antagonists

Ist Teil von

• Bioorganic & medicinal chemistry letters, 2001-02, Vol.11 (4), p.555-557

Ort / Verlag

Oxford: Elsevier Ltd

Erscheinungsjahr

2001

Link zum Volltext

Quelle

Elsevier Journal Backfiles on ScienceDirect (DFG Nationallizenzen)

Beschreibungen/Notizen

• 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 IC 50s in the low micromolar concentrations. Based on the structure–activity correlation of known short chain amino acids and the butenolides, a series of new peptoids as endothelin receptor antagonists has been synthesized. Screening of these novel compounds resulted in the discovery of ET antagonists with IC 50s in the low micromolar concentrations.