Asmaa F. Kassem, Fatimah Alshehrei, Eman M.H. Abbas and Thoraya A. Farghaly* Pages 418 - 429 ( 12 )
Background & Objective: Quinazolines and their fused systems are noteworthy in pharmaceutical chemistry due to their wide range of biological activities.Methods: A direct and efficient approach for the synthesis of new series of fused quinazolines with triazole, thiazole, benzimidazole and tetrazole has been preceded via the reaction of quinazoline thione derivative with halogenated compounds or cyclocondensation of arylidene of quinazoline derivative with heterocyclic amines. Also, dibenzo[b,e][1,4]thiazepine derivatives was synthesized through the reaction of 2,6-bis-(2-chloro-benzylidene)-cyclohexanone with o-aminothiophenol. Results: The structures of all new synthesized heterocyclic compounds were confirmed and discussed on the bases of spectral data. The utility of the preparation and design of the above mentioned compounds has been shown to be clear in the results of their antimicrobial activity which revealed that some derivatives have potent activity exceeding or similar to the activity of the reference drugs. Conclusion: The insertion of triazole or thiazole moieties to be fused with quinazoline ring helps to enhance its antimicrobial activity.
Azoloquinazolines, hydrazonoyl chlorides, benzothiazepine, thiazoles, triazoles, antimicrobial agents.
Chemistry of Natural and Microbial Products Department, Pharmaceutical and Drug Industries Research Division, National Research Center, 33 El Bohouth St. (Former El Tahrir St.) Dokki, Giza, P.O. Box 12622, Department of Biology, Jumom College, Umm Al-Qura University, P.O Box 7388, Makkah, 21955, Chemistry of Natural and Microbial Products Department, Pharmaceutical and Drug Industries Research Division, National Research Center, 33 El Bohouth St. (Former El Tahrir St.) Dokki, Giza, P.O. Box 12622, Department of Chemistry, Faculty of Science, Cairo University, Giza, 12613