苯甲酰基哌嗪型青霉烯类新化合物的合成及抗菌活性研究

Synthesis and antibacterial activity of a series of penems with 2-phenacyl piperazine

目的设计并合成青霉烯类苯甲酰基哌嗪型新化合物并测定其抗菌活性。方法根据已报道的相关活性化合物的构效关系研究,设计出一系列2-取代苯甲酰基哌嗪甲基取代的新青霉烯类化合物,以2-羟甲基青霉烯双环母核为起始原料,经两次取代、两次脱保护基关环4步反应合成了目标化合物。采用二倍稀释法测定了其中8个化合物对耐甲氧西林金黄色葡萄球菌(MRSA)、耐甲氧西林表皮葡萄球菌(MRSE)、甲氧西林敏感金黄色葡萄球菌(MSSA)和甲氧西林敏感表皮葡萄球菌(MSSE)4组革兰阳性菌的抑菌活性。结果与结论合成了11个新青霉烯类化合物,其结构经MS1、H-NMR谱确证。抑菌实验结果表明,所测试的8个新化合物对MRSA、MRSE、MSSA、MSSE均有较好抗菌活性。

Aim To investigate the antibacterial activity of a series of penems with 2-phenacyl piperazine. Methods The target compounds were designed and synthesized from 2-hydroxymethyl penem. Antibacterial activity of compounds were determined against some Gram-positive microorganisms by MIC test. Results and conclusion Eleven target compounds were synthesized and their structures were confirmed by 1^H- NMR, MS. Eight determined compounds displayed good activity against MRSA, MRSE, MSSA, and MSSE.