Design,Synthesis, Docking Study of Pyrazolohydrazinopyrimidin-4-one Derivatives and Their Application as Antimicrobials |
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| Authors: | Ruba A Alolayan Nadia Ali Ahmed Elkanzi Hajer Hrichi Rania B Bakr |
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| Institution: | 1. Chemistry Department, College of Science, Jouf University, P.O. Box 2014, Sakaka, Saudi Arabia;2. Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Beni-Suef University, Beni-Suef, 62514 Egypt |
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| Abstract: | New series of pyrazoles 4a – c and pyrazolopyrimidines 5a – f had been constructed. The newly synthesized compounds were assessed for their antimicrobial activity towards E. coli and P. aeruginosa (gram –ve bacteria), B. subtilis and S. aureus (gram +ve bacteria) and A. flavus and C. albicans (representative of fungi). The pyrazolylpyrimidine-2,4-dione derivative 5b is the most active candidate against B. subtilis (MIC=60 μg/mL) and P. aeruginosa (MIC=45 μg/mL). Regarding antifungal potential, compound 5f was the most effective against A. flavus (MIC=33 μg/mL). Similarly, compound 5c displayed strong antifungal activity towards C. Albicans (MIC=36 μg/mL) in reference to amphotericin B (MIC=60 μg/mL). Finally, the novel compounds had been docked inside dihydropteroate synthase (DHPS) to suggest the binding mode of these compounds. |
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| Keywords: | antimicrobial pyrazole derivatives pyrimidines molecular docking synthesis |
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