title: Synthesis of a new series of angiotensin II receptor antagonists and antibacterial agents.
abstract: 2-(Arylmethylenehydrazono)-4,4-diphenyl-1H-imidazol-5(4H)-one 3 underwent regioselective cyclization upon treatment with bromine in acetic acid containing sodium acetate to give the respective 3-substituted-6,6-diphenyl-6,7-dihydro-imidazo[2,1-c][1,2,4]triazole-5-one 4 in overall good yields and not the isomeric structure 5. In addition, compound 4 was synthesized by alternative method via reaction of compound 1 with different acids in acetic acid. The synthesized hydrazone derivatives were screened for their angiotensin II receptor antagonists activity and the results showed promising activity. Also, imidazo[2,1-c][1,2,4]triazole-5-ones 4 were screened for the antibacterial activity and the result revealed that two derivatives have excellent activity.
authors.affiliation: Department of Chemistry, Faculty of Science, Cairo University, Giza, Egypt.
authors.forename: Thoraya A
authors.initials: TA
authors.lastname: Farghaly
authors.forename: Sobhi M
authors.initials: SM
authors.lastname: Gomha
authors.forename: Mohamed M
authors.initials: MM
authors.lastname: Abdalla
mesh_terms: D057911:Angiotensin Receptor Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship
chemical_list: D057911:Angiotensin Receptor Antagonists; D000900:Anti-Bacterial Agents