volume 30, issue 43, Pno-no 2010
DOI: 10.1002/chin.199943156
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Venkatesan Aranapakam, J. Donald Albright, George T. Grosu, Peter S. Chan, Joseph Coupet, Trina Saunders, Xun Ru, H. Mazandarani

Abstract: Active Arginine Vasopressin Receptor Antagonists.-In continuation of developing vasopressin antagonists, the tricyclic pyrrolobenzodiazepine moiety in VPA-985 is replaced by the thienobenzazepine derivatives (IV) and (X). These ring systems are prepared by novel routes, the structure-activity relationship is described. Thienobenzazepines (XII) possess potent V 1a and V 2 receptor binding activity. Compound (XIIc) is a potent, orally active and highly selective V 2 antagonist. -(ARANAPAKAM, VENKATESAN; ALBRIGH…

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