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[青霉素和去乙酰氧基头孢菌素的脒类似物对地衣芽孢杆菌749/c青霉素酶的稳定性]

[Stability of the amidine analogs of penicillin and deacetoxycephalosporin to the penicillinase of Bacillus licheniformis 749/c].

作者信息

Veĭnberg G A, Belevich E M

出版信息

Antibiotiki. 1977 May;22(5):411-3.

PMID:879725
Abstract

Fermentative hydrolysis of 3 derivatives of 6-beta-amidinopenicillanic acid and I derivative of 7-beta-amidinodeacetoxycephalosporanic acid by penicillinase produced by Bacillus licheniformis 749/c was studied. It was found that 6-beta-[(hexahydro-IH-azepin-I-yl) methyleneamino] penicillanic acid, 6-beta-(N1 N-dimethylformamidino-N1) penicillanic acid and 6-beta [(morpholin-I-yl) methylenemino] penicillanic acid were hydrolyzed by the enzyme 50, 70, and 160 times respectively slower than benzylpenicillin. 7-beta-[(Hexahydro-IH-azepin-I-yl)' methylenemino] deacetoxycephalosporanic acid proved to be at least 10 times more stable to the effect of penicillinase than methicillin. In addition unlike the amidine analogues of penicillin the above compound had an inhibitory effect on penicillinase produced by Bacillus licheniformis 749/c.

摘要

研究了地衣芽孢杆菌749/c产生的青霉素酶对6-β-脒基青霉烷酸的3种衍生物和7-β-脒基去乙酰氧基头孢烷酸的1种衍生物的发酵水解作用。结果发现,6-β-[(六氢-1H-氮杂环庚烷-1-基)亚甲基氨基]青霉烷酸、6-β-(N1,N-二甲基甲脒基-N1)青霉烷酸和6-β[(吗啉-1-基)亚甲基氨基]青霉烷酸被该酶水解的速度分别比苄青霉素慢50、70和160倍。7-β-[(六氢-1H-氮杂环庚烷-1-基)亚甲基氨基]去乙酰氧基头孢烷酸对青霉素酶作用的稳定性比甲氧西林至少高10倍。此外,与青霉素的脒类似物不同,上述化合物对地衣芽孢杆菌749/c产生的青霉素酶有抑制作用。

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