叠氮化物-炔烃环加成反应合成4-氨基喹啉-二茂铁基查耳酮共轭物：合成与抗结核活性评价
Azide-alkyne cycloaddition en route to 4-aminoquinoline-ferrocenylchalcone conjugates: synthesis and anti-TB evaluation.
作者信息
Singh Amandeep, Viljoen Albertus, Kremer Laurent, Kumar Vipan
机构信息
Department of Chemistry, Guru Nanak Dev University, Amritsar-143005, India.
Institut de Recherche en Infectiologie (IRIM), CNRS, UMR 9004, Université de Montpellier, France.
出版信息
Future Med Chem. 2017 Oct;9(15):1701-1708. doi: 10.4155/fmc-2017-0098. Epub 2017 Sep 4.
AIM
Tuberculosis is responsible for 9.6 million infections and 1.5 million deaths in 2015. The development of multidrug-resistant and extensively drug-resistant strains has impeded the development of effective antitubercular therapy. Results/methodology: The present manuscript describes the synthesis of a series of 4-aminoquinoline-ferrocenylchalcone conjugates via Cu-promoted Huisgen's azide-alkyne cycloaddition reaction and evaluation of their antitubercular activities against mc6230 strain of Mycobacterium tuberculosis. The conjugate 11j proved to be the most potent of the synthesized conjugates with a minimum inhibitory concentration (MIC) value of 30 μM and proved to be noncytotoxic against HeLa cells.
CONCLUSION
The synthesized conjugates can act as starting point for the development of new antitubercular agents. Synthesis and antitubercular evaluation of 1H-1,2,3-triazole-tethered 4-aminoquinoline-ferrocenylchalcone conjugates. [Formula: see text].
目的
2015年，结核病导致960万例感染和150万人死亡。耐多药和广泛耐药菌株的出现阻碍了有效抗结核治疗的发展。结果/方法：本论文描述了通过铜促进的惠斯根叠氮化物-炔烃环加成反应合成一系列4-氨基喹啉-二茂铁基查尔酮共轭物，并评估它们对结核分枝杆菌mc6230菌株的抗结核活性。共轭物11j被证明是合成的共轭物中最有效的，最低抑菌浓度（MIC）值为30μM，并且对HeLa细胞无细胞毒性。
结论
合成的共轭物可作为开发新型抗结核药物的起点。1H-1,2,3-三唑连接的4-氨基喹啉-二茂铁基查尔酮共轭物的合成与抗结核评估。[化学式：见原文]
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