Premium
Synthesis and biological activity of (3,5‐disubstituted‐1 H ‐1,2,4‐triazol‐1‐yl)benzophenone derivatives
Author(s) -
Hirai Kentaro,
Sugimoto Hirohiko,
Ishiba Teruyuki,
Fujishita Toshio,
Tsukinoki Yuji,
Hirose Katsumi
Publication year - 1982
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.5570190621
Subject(s) - benzophenone , chemistry , tetrazole , acylation , triazole , d 1 , stereochemistry , combinatorial chemistry , organic chemistry , biochemistry , receptor , catalysis
The synthesis of (5‐acylaminomethyl‐3‐carbamoyl‐1 H ‐1,2,4‐triazol‐1‐yl)benzophenone derivatives 4a‐i, 14a‐d, 15a‐d, 16a‐c , is described. Acylation of the key intermediate, 1‐benzoylphenylazo‐1‐aminoacetamide 7, followed by cyclization in the presence of acid afforded 1 H ‐1,2,4‐triazole derivatives. These compounds were evaluated for their central nervous system (CNS) activity. Some of these compounds exhibited high activities in anti‐pentylene tetrazole and rotarod test in mice when orally administered.