Jones R N, Thornsberry C, Barry A L, Packer R R, Baker C N, Badal R E
Antimicrob Agents Chemother. 1980 Nov;18(5):773-9. doi: 10.1128/AAC.18.5.773.
O-Demethylfortimicin A (compound A49759) was tested against 445 bacteria, and the results were compared with those obtained with fortimicin A, amikacin, gentamicin, netilmicin, sisomicin, and tobramycin. A49759 was found to be active and bactericidal against the Enterobacteriaceae, nonfermentative gram-negative bacilli, and Staphylococcus aureus. A49759 was two- to fourfold more active than fortimicin A against most species tested, but generally fourfold less active than amikacin against this population of Pseudomonas aeruginosa (85% inhibited at less than or equal to 16 microgram of amikacin per ml and 85% inhibited at less than or equal to 64 microgram of A49759 per ml). Only amikacin and A49759 were resistant to most aminoglucoside-inactivating enzymes and also had significant antipseudomonal activity. Amikacin was inactivated by aminoglycoside 6'-acetyltransferase, and A49759 was inactivated by aminoglycoside 3-acetyltransferase. The minimal inhibitory concentrations of all tested aminoglycosides were increased by augmenting the inoculum size.
对O - 去甲基福提霉素A（化合物A49759）针对445种细菌进行了测试，并将结果与使用福提霉素A、阿米卡星、庆大霉素、奈替米星、西索米星和妥布霉素所获得的结果进行了比较。发现A49759对肠杆菌科细菌、非发酵革兰氏阴性杆菌和金黄色葡萄球菌具有活性且具有杀菌作用。对于大多数测试菌种，A49759的活性比福提霉素A高两到四倍，但通常对铜绿假单胞菌群体的活性比阿米卡星低四倍（每毫升小于或等于16微克阿米卡星时85%被抑制，每毫升小于或等于64微克A49759时85%被抑制）。只有阿米卡星和A49759对大多数氨基糖苷类失活酶具有抗性，并且也具有显著的抗假单胞菌活性。阿米卡星被氨基糖苷6'-乙酰转移酶灭活，A49759被氨基糖苷3-乙酰转移酶灭活。通过增加接种量，所有测试氨基糖苷类的最低抑菌浓度均升高。
