Department of Chemistry, Sardar Patel University, Vallabh Vidyanagar 388120, Gujarat, India.
Eur J Med Chem. 2013 Jul;65:348-59. doi: 10.1016/j.ejmech.2013.05.003. Epub 2013 May 14.
Twenty four biquinolone-isoniazid hybrids were designed based on molecular hybridization technique and synthesized via multicomponent cyclocondensation (MCC) approach. All the newly synthesized compounds were screened for their antimicrobial and antitubercular activities. The brine shrimp bioassay was carried out to study the cytotoxicity of the synthesized compounds. Hybrids 7f (MIC = 25 μg/mL); 7a, 7e and 7m (MIC = 50 μg/mL); 7g, 7h and 7k (MIC = 62.5 μg/mL) exhibited excellent antimicrobial activity as compared with standard drugs. Hybrids 7l and 7j displayed 99% inhibition against Mycobacterium tuberculosis bacteria with better LC50 values 35.39 and 34.59 μg/mL, respectively. These results indicate that the synthesized compounds can act as leads for the development of newer antimicrobial and antitubercular compounds.
基于分子杂交技术设计了 24 种双喹诺酮-异烟肼杂合体，并通过多组分环缩合（MCC）方法合成。对所有新合成的化合物进行了抗菌和抗结核活性筛选。进行了卤虫生物测定以研究合成化合物的细胞毒性。与标准药物相比，杂合体 7f（MIC = 25 μg/mL）；7a、7e 和 7m（MIC = 50 μg/mL）；7g、7h 和 7k（MIC = 62.5 μg/mL）表现出优异的抗菌活性。杂合体 7l 和 7j 对结核分枝杆菌的抑制率达到 99%，LC50 值分别为 35.39 和 34.59 μg/mL。这些结果表明，所合成的化合物可以作为开发新型抗菌和抗结核化合物的先导化合物。
