Journal of Medicinal Chemistry p. 1466 - 1473 (1982)
Update date:2022-07-30
Topics:
Hirai
Fujishita
Ishiba
Sugimoto
Matsutani
Tsukinoki
Hirose
A series of the title compounds was prepared via condensation of the 3-(aminomethyl)triazolylbenzophenone with N-protected amino acids, followed by deprotection, amination of the 3-[(chloroacetamido)methyl]triazolylbenzophenone, or reduction of the relevant azide derivative. Some of the title compounds were also derived directly from the quinazolines by acid-induced rearrangement, followed by deprotection. These new amino acid amide derivatives of the triazolylbenzophenones were evaluated for central nervous system (CNS) activity. Members of this class of compounds exhibited a high level of CNS activities. For example, 2',5-dichloro-2-[3-[(glycylamino)methyl]-5-methyl-4H-1,2,4-triazol-4-yl ]benzophenone was as active as triazolam, with an ED50 of 0.58 mg/kg (mice, po), against antifighting activity in the foot shock-induced fighting test. Other triazolylbenzophenone derivatives showed similar pharmacological activities.
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