Synthesis and characterization of orally active nonpeptide vasopressin V2 receptor antagonists.

T Ohkawa, T Zenkoh, M Tomita, N Hosogai…

Index: Ohkawa, Takehiko; Zenkoh, Tatsuya; Tomita, Masayuki; Hosogai, Naomi; Hemmi, Keiji; Tanaka, Hirokazu; Setoi, Hiroyuki Chemical and Pharmaceutical Bulletin, 1999 , vol. 47, # 4 p. 501 - 510

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Citation Number: 11

Abstract

The present study was undertaken to evaluate whether a novel series of 2, 6-diaza-5- oxobicyclo [5.4. 0] undeca-1 (7), 8, 10-triene derivatives exhibited antagonistic activity for vasopressin V 1 and V 2 receptors. Most of these compounds were synthesized and showed a high affinity potential for V 2 receptor and low to moderate affinity potential for V 1 receptor. The most potent and V 2-selective compound, N-[4-[2, 6-diaza-6-[2-(4-methylpiper-azinyl)- ...