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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >A facile synthesis, antibacterial, and antitubercular studies of some piperidin-4-one and tetrahydropyridine derivatives.
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A facile synthesis, antibacterial, and antitubercular studies of some piperidin-4-one and tetrahydropyridine derivatives.

机译：对一些哌啶-4-酮和四氢吡啶衍生物的简便合成，抗菌和抗结核研究。

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摘要

The raise in clinical significance of multidrug-resistant bacterial pathogens has directed us to synthesize 2,6-diarylpiperidin-4-one and Delta(3)-tetrahydropyridin-4-ol based benzimidazole and O-arylsulfonyl derivatives. X-ray crystal structure of tetrahydropyridinol (23) confirmed a change in conformation and orientation of substituents upon amide formation. Antibacterial activities evaluated against a wide number of bacterial pathogens (both sensitive and multidrug-resistant) revealed that 19, 27 against Staphylococcus aureus, 27 against Enterococcus faecalis, and 19, 21, 23, and 27 against Enterococcus faecium are significantly good at lowest MIC(90) (16 microg/mL). Inhibitory power noticed by 23 against Vancomycin-Linezolid-resistant E. faecalis and 27 against Vancomycin-resistant E. faecium are onefold better than the standard Linezolid and Trovafloxacin drugs, respectively. Moreover, antitubercular activity for the selected compounds against Mycobacterium tuberculosis H37Rv revealed that compounds 23, 24, and 27 expressed onefold improved potency compared to the standard Rifampicin drug.
机译：对多药耐药细菌病原体的临床意义的提高已指导我们合成基于2,2-二芳基哌啶-4-酮和Delta（3）-四氢吡啶-4-醇的苯并咪唑和O-芳基磺酰基衍生物。四氢吡啶醇（23）的X射线晶体结构证实了酰胺形成后取代基的构象和方向发生了变化。对多种细菌病原体（敏感和耐多药）的抗菌活性进行了评估，结果显示，MIC最低时，分别对金黄色葡萄球菌19、27，对粪肠球菌27，对粪肠球菌19、21、23和27的效果显着。 （90）（16微克/毫升）。 23种药物对万古霉素耐药的粪肠球菌的抑制力和27种药物对万古霉素耐药的粪便的抑制力分别是标准Linezolid和Trovafloxacin药物的一倍。此外，所选化合物对结核分枝杆菌H37Rv的抗结核活性表明，与标准利福平药物相比，化合物23、24和27的效力提高了一倍。

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