发明名称 |
N,N,N-TRIMETHYLDERIVATE AMPHOTERER POLYENANTIBIOTIKA UND VERFAHREN ZU DEREN HERSTELLUNG |
摘要 |
<p>Trimethyl derivs. of amphoteric antibiotics of formula (I) are new: (R is the aglycone of an amphoteric polyene antibiotic less the carboxyl gp.). Specified are N,N,N-trimethylamphotericin B (Ia) and N,N,N-trimethylnystatin. They are made by exhaustive methylation of the amino gp. in the parent antibiotic by reacting in an organic solvent with methyl halide, a methyl sulphate or sulphonate ester. (I) are antifungals, e.g. (Ia) shows fungistatic effect against various pathogenic species at 0.39-6.3 mu g/ml, and has LD50 (intravenous in mice) of 60-6-100 mg/kg i.e. 10-15 times less toxic than the parent antibiotic.</p> |
申请公布号 |
DE2706156(A1) |
申请公布日期 |
1978.08.17 |
申请号 |
DE19772706156 |
申请日期 |
1977.02.14 |
申请人 |
VSESOJUZNYJ NAUTSCHNO-ISSLEDOVATELSKIJ TECHNOLOGITSCHESKIJ INSTITUT ANTIBIOTIKOV I FERMENTOV MEDICINSKOGO NAZNATSCHENIJA |
发明人 |
ABRAMOVITSCH VAINSTEIN,VIKTOR;OSVALDOVITSCH KULBACH,VALTER;DAVIDOVITSCH ETINGOV,JEVGENIJ;NIKOLAJEVITSCH NAUMTSCHIK,GRIGORIJ;NIKOLAJEVITSCH EKSEMPLJAROV,OLEG;AVKSENTJEVITSCH MICHAJLEZ,GEORGIJ;JEFIMOVITSCH GRINBERG,GRIGORIJ;NIKOLAJEVNA JEGORENKOVA,ALLA |
分类号 |
C07H17/08;(IPC1-7):C07H17/08;A61K31/71 |
主分类号 |
C07H17/08 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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