Design,synthesis and antibacterial activities of thiouracil derivatives containing acyl thiourea as SecA inhibitors |
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| Authors: | Penglei Cui Xiaoliu Li Mengyuan Zhu Binghe Wang Jing Liu Hua Chen |
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| Institution: | 1. Key Laboratory of Chemical Biology of Hebei Province, College of Chemistry and Environmental Science, Hebei University, Baoding 071002, China;2. College of Science, Agricultural University of Hebei, Baoding 071001, China;3. Department of Chemistry and Center for Diagnostics and Therapeutics, Georgia State University, Atlanta, GA 30302-4098, USA;4. College of Veterinary Medicine, Agricultural University of Hebei, Baoding 071001, China |
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| Abstract: | A series of novel thiouracil derivatives containing an acyl thiourea moiety (7a–7x) have been synthesized by structural modification of a lead SecA inhibitor, 2. All the compounds have been evaluated for their antibacterial activities against Bacillus amyloliquefaciens, Staphylococcus aureus, and Bacillus subtilis. Compounds 7c, 7m, 7u, 7v exhibited promising activities against above bacteria. Such four compounds were further tested for their inhibitory activity against SecA ATPase, and the results showed that compounds 7c and 7u had higher inhibitory activities than that of compound 2. Molecular docking work suggests that compound 7u might bind at a pocket close to the ATPase ATP-binding domain. |
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| Keywords: | SecA inhibitors Antibacterial activity Molecular simulation Thiouracil Acyl thiourea |
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