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Synthesis of substituted pyrazolines as inhibitors of Staphylococcus aureus

机译:取代吡唑啉类化合物作为金黄色葡萄球菌的抑制剂

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摘要

One of the greatest global health concerns since the development of antibiotics has been the ability of bacteria to become resistant to the drugs known to treat infection. Staphylococcus aureus, is one of the most common bacteria involved in infection in the United States and some strains of S. aureus have found ways to become resistant to many drugs. Methicillin-resistant S. aureus, also known as MRSA, is hard to treat once an individual becomes infected due to its antibiotic resistance. A different approach to treating bacterial infections is needed to limit the possibility of resistance occurring.A compound that has shown promise is ML141, which is a pyrazoline derivative that was discovered to inhibit CDC42. ML141 has a high specificity for CDC42, which is necessary to prevent the compound from binding to other similar sites which would cause unwanted interactions that would produce undesired side effects. Inhibition of CDC42 results in the inhibition of internalization of S. aureus. Goals of this research include developing compounds that have the same high selectivity for CDC42 while increasing the solubility and stability.
机译:自从抗生素开发以来,全球最大的健康问题之一就是细菌对已知治疗感染的药物产生耐药性的能力。金黄色葡萄球菌是美国感染中最常见的细菌之一,某些金黄色葡萄球菌菌株已找到对多种药物产生抗药性的方法。耐甲氧西林的金黄色葡萄球菌,也称为MRSA,一旦由于其抗生素抗性而被感染就很难治疗。需要一种不同的方法来治疗细菌感染以限制产生耐药性的可能性。ML141是一种有前途的化合物,它是一种吡唑啉衍生物,被发现可以抑制CDC42。 ML141对CDC42具有很高的特异性,这对于防止该化合物与其他类似位点结合会是必不可少的,因为其他类似位点会引起不必要的相互作用,从而产生不良副作用。 CDC42的抑制导致金黄色葡萄球菌内在化的抑制。这项研究的目标包括开发对CDC42具有相同的高选择性同时增加溶解度和稳定性的化合物。

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    Drinnon Teage Kailyn;

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  • 年度 2015
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