Bioorganic & Medicinal Chemistry Letters 2002-01-21

N-Methylbenzanilide derivatives as a novel class of selective V(1A) receptor antagonists.

Akio Kakefuda, Junko Tsukada, Toshiyuki Kusayama, Atsuo Tahara, Shin-ichi Tsukamoto

Index: Bioorg. Med. Chem. Lett. 12(2) , 229-32, (2002)

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Abstract

During our efforts to develop a novel class of selective V(1A) receptor antagonists, the N-methylbenzanilide structure was applied to a 4,4-difluoro-1-benzazepine derivative, 4, which is a selective V(1A) receptor antagonist. Further structural modifications gave 16a with high V(1A) affinity and V(2)/V(1A) selectivity (K(i)=5.71 nM, V(2)/V(1A)=140) and potent V(1A) receptor antagonist activity (ID(50)=0.0080 mg/kg iv).