Synthesis and biological activity of (3,5‐disubstituted‐1H‐1,2,4‐triazol‐1‐yl)benzophenone derivatives

The synthesis of (5‐acylaminomethyl‐3‐carbamoyl‐1H‐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 1H‐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.