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首页> 外文期刊>The Journal of Antibiotics: An International Journal >Structure-activity relationships of stemphones, potentiators of imipenem activity against methicillin-resistant Staphylococcus aureus.
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Structure-activity relationships of stemphones, potentiators of imipenem activity against methicillin-resistant Staphylococcus aureus.

机译：茎索，亚胺培南活性增强剂对耐甲氧西林金黄色葡萄球菌的构效关系。

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From a further purification study, four new stemphones D to G were isolated along with previously reported stemphones B and C from the culture broth of Aspergillus sp. FKI-2136. Twenty-one derivatives were semisynthetically prepared from stemphones C, E and G. Potentiation of imipenem activity against methicillin-resistant Staphylococcus aureus (MRSA) by all the stemphones including natural and semisynthetic ones was compared to study the structure-activity relationships. Derivatives with a free hydroxy or an O-acyl residue having a C2 to C5 carbon length at C-4 held the potentiating activity, but those with a longer acyl residue lost the activity. The presence of an oxo or a free hydroxy residue at C-10 is important for the potentiating activity because introduction of an alkyl or acyl residue at this position resulted in a loss of activity. Among them, stemphone E exhibited the most potent potentiation of imipenem activity against MRSA and the lowest cytotoxic activity against Jurkat cells.
机译：从进一步的纯化研究中，从曲霉属菌种的培养液中分离出四个新的干式耳机D至G，以及先前报道的干式耳机B和C。 FKI-2136。从茎音C，E和G合成了二十一种衍生物。比较了包括天然和半合成茎在内的所有茎音对亚甲培南对耐甲氧西林金黄色葡萄球菌（MRSA）的活性，以研究其构效关系。具有在C-4处的C 2至C 5碳长度的游离羟基或O-酰基残基的衍生物保持增强活性，但是具有较长酰基残基的那些衍生物失去活性。 C-10上的羰基或游离羟基残基的存在对于增强活性很重要，因为在此位置引入烷基或酰基残基会导致活性降低。其中，干手机E表现出亚胺培南对MRSA的活性最强，对Jurkat细胞的细胞毒活性最低。

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