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糖肉桂酰亚精胺,一类新型抗生素。五、LL-BM123γ异丙基衍生物的抗菌评估。

Glycocinnamoylspermidines, a new class of antibiotics. V. Antibacterial evaluation of the isopropyl derivative of LL-BM123gamma.

作者信息

Kuck N A, Redin G S

出版信息

J Antibiot (Tokyo). 1978 May;31(5):405-9. doi: 10.7164/antibiotics.31.405.

Abstract

Isopropyl LL-BM123gamma, a novel semisynthetic glycocinnamoylspermidine antibiotic, was active in vitro against both Gram-negative and Gram-positive bacteria with broad spectrum bactericidal activity against clinically important Gram-negative strains. In parallel tests, it was equal to or more potent than reference aminoglycoside antibiotics against Escherichia coli, Proteus, Enterobacter-Klebsiella, Serratia, Salmonella, and Acinetobacter strains. Against clinical isolates of Pseudomonas aeruginosa, isopropyl LL-BM123gamma compared favorably with gentamicin, verdamicin and amikacin but was less potent than tobramycin. Isopropyl LL-BM123gamma was active against many Gram-negative bacteria that were relatively resistant to aminoglycosides. It was rapidly absorbed following subcutaneous administration in mice and showed greater potency than gentamicin on both dosage and plasma concentration bases against several experimental infections.

摘要

异丙基LL - BM123γ是一种新型半合成糖肉桂酰亚精胺抗生素,在体外对革兰氏阴性菌和革兰氏阳性菌均有活性,对临床上重要的革兰氏阴性菌株具有广谱杀菌活性。在平行试验中,它对大肠杆菌、变形杆菌、肠杆菌 - 克雷伯菌、沙雷氏菌、沙门氏菌和不动杆菌菌株的活性与参考氨基糖苷类抗生素相当或更强。对于铜绿假单胞菌的临床分离株,异丙基LL - BM123γ与庆大霉素、弗氏霉素和阿米卡星相比有优势,但比妥布霉素效力稍弱。异丙基LL - BM123γ对许多对氨基糖苷类相对耐药的革兰氏阴性菌有活性。在小鼠皮下给药后它能迅速吸收,并且在剂量和血浆浓度方面,对几种实验性感染的效力都比庆大霉素更强。

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