Antibacterial activities against Ralstonia solanacearum and Xanthomonas oryzae pv. oryzae of 6-chloro-4-(4-substituted piperazinyl)quinazoline derivatives |
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| Institution: | 1. School of Pharmacy, Lanzhou University, Lanzhou, 730000, People’s Republic of China;2. Lanzhou Institute of Husbandry and Pharmaceutical Sciences, Chinese Academy of Agricultural Sciences, Lanzhou, 730000, People’s Republic of China;1. State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Center for Research and Development of Fine Chemicals, Guizhou University, Guiyang, Guizhou 550025, China;2. School of Life Science, Bengbu Medical College, Anhui, Bengbu 233030, China;1. State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for R&D of Fine Chemicals, Guizhou University, Guiyang 550025, China;2. College of Pharmacy, East China University of Science & Technology, Shanghai 550025, China;1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy and Biotechnology, German University in Cairo, 11835 Cairo, Egypt;2. Helmholtz Institute for Pharmaceutical Research Saarland (HIPS), Helmholtz Centre for Infection Research, Saarland University Campus, 66123 Saarbrücken, Germany;3. German Centre for Infection Research (DZIF), partner site Hannover-Braunschweig, Germany;5. Department of Biology and Biochemistry, School of Life and Medical Sciences, University of Hertfordshire hosted by Global Academic Foundation, Cairo, Egypt;6. Drug Radiation Research Department, National Centre for Radiation Research and Technology, Egyptian Atomic Energy Authority, Ahmed El-Zomor St. 3, El-Zohoor Dist., 11765 Cairo, Egypt;7. Department of Microbiology and Immunology, Faculty of Pharmacy, Cairo University, 11562 Cairo, Egypt;8. Institute for Molecular Infection Biology, University of Würzburg, Josef-Schneider-Strasse 2/Bau D15, 97080 Würzburg, Germany;9. Pharmaceutical and Medicinal Chemistry, Saarland University, Campus C2.3, D-66123 Saarbrücken, Germany;10. Department of Pharmacy, Saarland University, 66123 Saarbrücken, Germany |
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| Abstract: | In this letter, a variety of simple 6-chloro-4-(4-substituted piperazinyl)quinazoline derivatives was prepared. Preliminary bioassays revealed that these compounds showed good antibacterial activities toward phytopathogens Ralstonia solanacearum and Xanthomonas oryzae pv. oryzae (Xoo). Among these derivatives, compounds 5a, 5d, 5e, 5f, 5p, 5q, 6b, and 6d exhibited potent inhibition effects against R. solanacearum with EC50 within 4.60–9.94 µg/mL, especially, compound 5g exerted the strongest activity with EC50 of 2.72 µg/mL; compound 6b possessed the best inhibitory activity toward Xoo with EC50 of 8.46 µg/mL. Subsequently, a good predictive three-dimensional quantitative structure–activity relationship (3D-QSAR) model was constructed via CoMFA to direct the future structural modification and optimization. Furthermore, the pathogens’ topological studies were performed to explore the possible antibacterial mechanism. Given their simple frameworks and facile synthesis, title compounds can serve as the potential antibacterial leads. |
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| Keywords: | Quinazoline Synthesis Antibacterial 3D-QSAR Morphological studies |
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