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5-fluoro-2-methyl-N-[5-(5H-pyrrolo[2,1-c][1,4]benzodiazepine-10(11H)-yl carbonyl)-2-pyridinyl]benzamide (CL-385004) and analogs as orally active arginine vasopressin receptor antagonists

Bioorganic & Medicinal Chemistry LettersPublished 1 July 1999Open access
Venkatesan Aranapakam, J. Donald Albright, G Grosu, Efren G. Delos Santos, Peter S. Chan, Joseph Coupet
Citations20
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TL;DR

Synthesis and structure-activity relationships (SAR) of orally active arginine vasopressin (AVP) receptor antagonists are discussed.

Abstract

Synthesis and structure-activity relationships (SAR) of orally active arginine vasopressin (AVP) receptor antagonists are discussed. Potent and orally active AVP receptor antagonists are produced when ring A of VPA-985 (1) is replaced with a 3-pyridinyl unit (2b).

Keywords

MedicineBiochemistry, Genetics and Molecular Biology