杂化氯、二氯苯基噻唑基-s-三嗪的合成、构效关系及抗菌活性。
Synthesis, SAR and antibacterial activity of hybrid chloro, dichloro-phenylthiazolyl-s-triazines.
机构信息
Department of Pharmaceutical Sciences, Dibrugarh University, Dibrugarh 786004, India.
出版信息
Saudi Pharm J. 2012 Jan;20(1):35-43. doi: 10.1016/j.jsps.2011.05.003. Epub 2011 May 17.
Abstract
A series of hybrid novel chloro (1a-9a) and dichloro (10b-18b) phenylthiazolyl-s-triazine were synthesized and subsequently subjected to their antibacterial activity against three gram positive viz. Lactobacillus casei (NCIM-2651); Bacillus cereus (NCIM-2458); Staphylococcus aureus (NCIM-2120) and three gram negative viz Salmonella typhimurium (NCIM-2501); Escherichia coli (NCIM-2065); Klebsiella aerogenes (NCIM-2098). The SAR studies around the lead compound revealed that introduction of electron withdrawing groups and amino (-NH-) and mercapto (-S-) linker bridge seemed more promising towards antibacterial activity. Moreover, the virtual Molinspiration screenings are in compliance with Ghose's rule.
摘要
一系列混合新型氯（1a-9a）和二氯（10b-18b）苯基噻唑基-s-三嗪被合成，并随后对其针对三种革兰氏阳性菌（即乳杆菌属（NCIM-2651）；蜡状芽孢杆菌（NCIM-2458）；金黄色葡萄球菌（NCIM-2120））和三种革兰氏阴性菌（即鼠伤寒沙门氏菌（NCIM-2501）；大肠杆菌（NCIM-2065）；产气肠杆菌（NCIM-2098））的抗菌活性进行了测试。对先导化合物进行的 SAR 研究表明，引入吸电子基团和氨基（-NH-）和巯基（-S-）连接桥似乎更有希望提高抗菌活性。此外，虚拟 Molinspiration 筛选符合 Ghose 规则。
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