Synthesis and pharmacological evaluation of 5-(4-biphenyl)-3-methyl-4-phenyl-1, 2, 4-triazole derivatives as a novel class of selective antagonists for the Human …

A Kakefuda, T Suzuki, T Tobe, J Tsukada…

Index: Kakefuda, Akio; Suzuki, Takeshi; Tobe, Takahiko; Tsukada, Junko; Tahara, Atsuo; Sakamoto, Shuichi; Tsukamoto, Shin-ichi Journal of Medicinal Chemistry, 2002 , vol. 45, # 12 p. 2589 - 2598

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Citation Number: 25

Abstract

A series of 5-(4-biphenyl)-3-methyl-4-phenyl-1, 2, 4-triazole derivatives were prepared and evaluated as selective antagonists for the human vasopressin V1A receptor. The compounds were examined for their affinity to the cloned human V1A receptor (hV1A) and selectivity vs the cloned human V2 receptor (hV2). By utilizing the structure-activity relationship on 4, 4-difluoro-5-methylidene-2, 3, 4, 5-tetrahydrobenzazepine derivatives ...