Discovery of novel antimicrobial agents effective against infections caused by drugresistant pathogens is an important objective. In order to find a new parenteral carbapenem antibiotic, which has potent antibacterial activity especially against methicillin-resistant staphylococci, vancomycin-resistant enterococci and penicillin-resistant Streptococcus pneumoniae, a series of 1β-methylcarbapenems with thiazol-2-ylthio groups at the C-2 position have been synthesized. Structure-activity relationships were investigated which led to SM-197436 (27), SM-232721 (44) and SM-232724 (41), being selected for further evaluation.
发现新型抗微
生物制剂,特别是针对耐药病原体引起的感染,是一项重要的目标。为了找到一种新的静脉注射碳青霉烯类抗生素,该抗生素具有强大的抗菌活性,尤其对耐
甲氧西林葡萄球菌、耐
万古霉素肠球菌和耐
青霉素肺炎链球菌有效,我们合成了一系列在C-2位点带有
噻唑-2-
硫基的1β-甲基碳青霉烯类化合物。通过研究结构-活性关系,我们选定了SM-197436(27)、SM-232721(44)和SM-232724(41)进行进一步评估。