Mercaptopropionamide compounds and preparation method and medicinal application thereof

The invention belongs to the field of biomedicine, particularly relates to mercaptopropionamide compounds shown in a formula (I) and medicinal salts thereof, and a preparation method and medicinal application thereof, and in particular relates to application in preparation of drugs against gram-nega...

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Bibliographische Detailangaben
Hauptverfasser: SUN XUN, HU FUPIN, YU LITING, MENG ZHI, HAN JILAI
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention belongs to the field of biomedicine, particularly relates to mercaptopropionamide compounds shown in a formula (I) and medicinal salts thereof, and a preparation method and medicinal application thereof, and in particular relates to application in preparation of drugs against gram-negative drug-resistant bacteria. Some compounds are tested for NDM-1 enzyme activity, and are combinedwith meropenem to carry out in vitro antibacterial activity tests. Experimental results show that some compounds have better NDM-1 enzyme inhibitory activity and can obviously reduce the minimum inhibitory concentration (MIC value) of the meropenem. The compound and salts thereof can be used for preparing NDM-1 enzyme inhibitors, and can be combined with the meropenem to prepare a compound preparation for resisting the gram-negative drug-resistant bacteria. 本发明属于生物医药领域,具体涉及式(Ⅰ)所示的巯基丙酰胺类化合物及其药用盐及其制备方法和药用用途,特别是在制备抗革兰氏耐药阴性菌药物中的应用。本发明的部分化合物进行了NDM-1酶活性测试,并将其与美罗培南联用进行了体外抗菌活性的测试,实验结果表明,本发明的部分化合物具有较优的NDM-1酶抑制活性,并可显著降低美罗培南的最低抑