The synthesis and vasopressin (AVP) antagonist activity of a novel series of N-aroyl-2, 4, 5, 6-tetrahydropyrazolo [3, 4-d] thieno [3, 2-b] azepines

…, PS Chan, J Coupet, X Ru, H Mazandarani

文献索引：Albright, J. Donald; Santos, Efren G. Delos; Dusza, John P.; Chan, Peter S.; Coupet, Joseph; Ru, Xun; Mazandarani Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 8 p. 695 - 698

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被引用次数: 30

摘要

Synthesis and SAR of N-[4-[(4, 5-dihydropyrazolo [3, 4-d] thieno [3, 2-b] azepin-6 (2H)-yl) carbonyl] phenyl] benzamides as arginine vasopressin (AVP) receptor antagonists are discussed. Potent orally active AVP receptor antagonists are produced when the benzamide moiety contains a phenyl group at the 2-position. Similar analogues of 4, 6, 7, 8-tetrahydro- 5H-thieno [3, 2-b] azepine and VPA-985 are reported.