Nicas T I, Mullen D L, Flokowitsch J E, Preston D A, Snyder N J, Stratford R E, Cooper R D
Lilly Research Laboratories, Indianapolis, Indiana 46285, USA.
Antimicrob Agents Chemother. 1995 Nov;39(11):2585-7. doi: 10.1128/AAC.39.11.2585.
LY191145 is the prototype of a series of compounds with activities against vancomycin-resistant enterococci derived by modification of the glycopeptide antibiotic LY264826. LY191145 had MICs for vancomycin- and teicoplanin-resistant enterococci of < or = 4 micrograms/ml for 50% of isolates and < or = 16 micrograms/ml for 90% of isolates. Its MICs for vancomycin-resistant, teicoplanin-susceptible enterococci were 1 to 8 micrograms/ml. LY191145 retains the potent activities of its parent compound against staphylococci and streptococci. In vivo studies in a mouse infection model confirmed these activities. This compound indicates the potential of semisynthetic glycopeptides as agents against antibiotic-resistant gram-positive bacteria.
LY191145是一系列通过修饰糖肽抗生素LY264826而获得的对耐万古霉素肠球菌具有活性的化合物的原型。LY191145对50%的耐万古霉素和替考拉宁肠球菌分离株的最低抑菌浓度（MIC）≤4微克/毫升，对90%的分离株MIC≤16微克/毫升。其对耐万古霉素、对替考拉宁敏感的肠球菌的MIC为1至8微克/毫升。LY191145保留了其母体化合物对葡萄球菌和链球菌的强效活性。在小鼠感染模型中的体内研究证实了这些活性。该化合物表明半合成糖肽作为抗耐药革兰氏阳性菌药物的潜力。
