Pharmaceutical Chemistry Journal ( IF 0.8 ) Pub Date : 2023-11-07 , DOI: 10.1007/s11094-023-02954-6 T. S. Vedekhina , M. Z. Dogonadze , T. I. Vinogradova , M. V. Chudinov , A. Yu. Lukin
The reaction of nicotinic and isonicotinic propargylamides with lipophilic aliphatic amines yielded a series of 3- or 4-(5-methyl-1H-imidazol-2-yl)pyridines containing a lipophilic substituent in the imidazole ring 1-position. The new compounds were characterized by physicochemical methods. The antituberculosis and antimicrobial activities against ESKAPE pathogens were studied. 3-[1-(1-n-Octadecyl)-5-methyl-1Himidazol-2-yl]pyridine (IIId) had antituberculosis activity (MIC 6.2 μg/mL) while 3-[1-(1-adamantylmethyl)-5-methyl-1H-imidazol-2-yl]pyridine (IIIa) exhibited activity against S. aureus (MIC 16 μg/mL).
中文翻译:
具有抗菌活性的亲脂性咪唑基吡啶
烟碱和异烟碱炔酰胺与亲脂性脂肪胺反应生成一系列在咪唑环1位含有亲脂取代基的3-或4-(5-甲基-1H-咪唑-2-基)吡啶。通过物理化学方法对新化合物进行了表征。研究了针对 ESKAPE 病原体的抗结核和抗菌活性。3-[1-(1-正十八烷基)-5-甲基-1 H咪唑-2-基]吡啶 (IIId) 具有抗结核活性 (MIC 6.2 μg/mL),而 3-[1-(1-金刚烷基甲基) -5-甲基-1 H-咪唑-2-基]吡啶 (IIIa) 对金黄色葡萄球菌具有活性(MIC 16 μg/mL)。