Leitner F, Pursiano T A, Buck R E, Tsai Y H, Chisholm D R, Misiek M, Desiderio J V, Kessler R E
Antimicrob Agents Chemother. 1987 Feb;31(2):238-43. doi: 10.1128/AAC.31.2.238.
BMY 28100, a new oral cephalosporin with a (Z)-propenyl side chain at the 3 position and a p-hydroxyphenylglycyl substituent at the 7 position, was evaluated in comparison with cefaclor and cephalexin and, when appropriate, ampicillin and vancomycin. In vitro, BMY 28100 was more active than the reference cephalosporins against streptococci, Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, Haemophilus influenzae, Propionibacterium acnes, Clostridium perfringens, and Clostridium difficile. BMY 28100 was comparable to cefaclor and more active than cephalexin against Staphylococcus saprophyticus and ampicillin-susceptible strains of Branhamella catarrhalis; but against ampicillin-resistant strains of B. catarrhalis, BMY 28100 was comparable to cephalexin and more active than cefaclor. Against Neisseria gonorrhoeae, BMY 28100 was comparable to cephalexin, but less active than cefaclor. Members of the family Enterobacteriaceae overall were equally susceptible to BMY 28100 and cefaclor but were less susceptible to cephalexin. In human serum, BMY 28100 was 45% protein bound. After an oral dose to mice, 82% of the drug was recovered in urine. The oral therapeutic efficacy of BMY 28100 in systemically infected mice reflected its activity in vitro.
BMY 28100是一种新型口服头孢菌素，其3位带有(Z)-丙烯基侧链，7位带有对羟基苯甘氨酰取代基。将其与头孢克洛和头孢氨苄进行了比较评估，并在适当情况下与氨苄西林和万古霉素进行了比较。在体外，BMY 28100对链球菌、金黄色葡萄球菌、表皮葡萄球菌、单核细胞增生李斯特菌、流感嗜血杆菌、痤疮丙酸杆菌、产气荚膜梭菌和艰难梭菌的活性比对照头孢菌素更高。BMY 28100对腐生葡萄球菌和卡他布兰汉菌的氨苄西林敏感菌株的活性与头孢克洛相当，且比对头孢氨苄更具活性；但对卡他布兰汉菌的氨苄西林耐药菌株，BMY 28100与头孢氨苄相当，且比对头孢克洛更具活性。对淋病奈瑟菌，BMY 28100与头孢氨苄相当，但活性低于头孢克洛。肠杆菌科成员总体上对BMY 28100和头孢克洛的敏感性相同，但对头孢氨苄的敏感性较低。在人血清中，BMY 28100的蛋白结合率为45%。给小鼠口服给药后，82%的药物在尿液中回收。BMY 28100在全身感染小鼠中的口服治疗效果反映了其体外活性。
