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In vitro antibacterial activity of trospectomycin (U-63366F) a novel spectinomycin analog.

机译:曲霉素(U-63366F)(一种新的壮观霉素类似物)的体外抗菌活性。

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摘要

Trospectomycin (U-63366F) is a novel spectinomycin analog with broad-spectrum antibacterial activity. The in vitro activity of this analog was compared with that of spectinomycin and other reference antibiotics against 411 clinical isolates of aerobic and anaerobic bacteria. MICs were determined by agar or broth dilution methods. The stability of trospectomycin in the presence of an enzyme extract derived from spectinomycin-resistant Escherichia coli was determined. Trospectomycin was more active than spectinomycin (4- to 32-fold) against strains of numerous bacterial species, including staphylococci, streptococci, Haemophilus influenzae, Branhamella catarrhalis, Neisseria gonorrhoeae, Proteus species, Bacteroides species, Clostridium difficile, Clostridium species, and Chlamydia trachomatis. Trospectomycin demonstrated a moderate level of activity (comparable to that of spectinomycin) for most species of the family Enterobacteriaceae tested and was generally cross resistant with spectinomycin. Trospectomycin was susceptible to inactivation by crude enzyme preparations from spectinomycin-inactivating strains of E. coli. Trospectomycin inhibited a variety of clinically important organisms, including agents of sexually transmitted diseases and pelvic inflammatory disease. Clinical studies with this novel aminocyclitol antibiotic are in progress.
机译:Trospectomycin(U-63366F)是一种新型的壮观霉素类似物,具有广谱抗菌活性。将该类似物的体外活性与壮观霉素和其他参考抗生素对411种需氧和厌氧细菌临床分离株的活性进行了比较。 MIC通过琼脂或肉汤稀释法确定。测定了在抗大观霉素的大肠杆菌衍生的酶提取物存在下的trospectomycin的稳定性。对许多细菌菌株,包括对葡萄球菌,链球菌,流感嗜血杆菌,卡他氏杆菌,淋病奈瑟菌,变形杆菌,变形杆菌,艰难梭菌,梭状芽胞杆菌和衣原体,曲霉菌霉素比壮观霉素(4-32倍)的活性更高。 。 Trospectomycin对测试的肠杆菌科的大多数菌种均表现出中等水平的活性(与壮观霉素相当),并且通常与壮观霉素交叉耐药。 Trospectomycin容易被大观霉素灭活菌株的粗制酶制剂灭活。曲霉切除素可抑制多种临床上重要的生物,包括性传播疾病和盆腔炎的药物。这种新型氨基环醇抗生素的临床研究正在进行中。

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