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Comparative studies on conventional and microwave-assisted synthesis of a series of 2,4-di and 2,3,4-trisubstituted benzimidazo[1,2-a] pyrimidines and their antimicrobial activities
Authors:Oztekin Algul  Asiye Meric  Serpil Polat  N. Didem Yuksek  Mehmet S. Serin
Affiliation:(1) Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Mersin University, 33169 Mersin, Turkey;(2) Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, 26470 Eskisehir, Turkey;(3) Department of Pharmaceutical Microbiology, Faculty of Pharmacy, Mersin University, 33169 Mersin, Turkey
Abstract:Comparative studies were performed on a series of 2,4-di and 2,3,4-trisubstituted benzimidazo[1,2-a]pyrimidines, which were synthesized with conventional and microwave heating methods. In microwave irradiation method, approximately, 95–97.5% of the reaction time was increased and 1–45% yield increase was obtained. All compounds were able to inhibit the growth of the screened microorganisms in vitro with MIC values between 3.9–250 μg mL−1. The highest activity was expressed by compound IIId (2,4-diphenyl-benzo[4,5]imidazo[1,2-a] pyrimidine), which has the MIC value of 3.9 μg mL−1 and 31.2 μg mL-1 for Penicillium natatum ATCC 24791 and E. faecalis ATCC 29212, respectively. MediaObjects/11532_2009_23_Fig1_HTML.jpg
Keywords:Benzimidazo[1,2-a]pyrimidines  Fused azole heterocycles  Microwave irradiation  Antimicrobial activity
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