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Synthesis, anti-tuberculosis activity and QSAR study of 2,4-diarylquinolines and analogous polycyclic derivatives
Arabian Journal of Chemistry ( IF 5.3 ) Pub Date : 2019-11-01 , DOI: 10.1016/j.arabjc.2018.10.003
Gisela C. Muscia , Juan P. Carnevale , Ayelen Luczywo , María Victoria Peláez , Ailen Rodríguez Ó Toole , Graciela Y. Buldain , Juan J. Casal , Silvia E. Asís

Abstract The multicomponent syntheses of 2,4-di-aryl-quinolines and analogous polycyclic derivatives as anti-tuberculosis agents were described. They were prepared via Beyer and Friedlander methods under microwave irradiation in short reaction times and good yields. Several homogeneous and heterogeneous acid catalysts were compared for preparing 2,4-di-arylquinolines and among them trifluoroacetic acid (TFA) reached the higher yields. Two derivatives exhibited activity against Mycobacterium tuberculosis H37Rv (Mtb), underwent additional testing and were considered lead compounds. The synthesis of a series of polycyclic analogous led to six new active compounds and a Quantitative Structure Activity Relationship study (QSAR) study was established.

中文翻译:

2,4-二芳基喹啉及类似多环衍生物的合成、抗结核活性及QSAR研究

摘要 描述了作为抗结核药物的 2,4-二-芳基-喹啉和类似多环衍生物的多组分合成。它们是通过 Beyer 和 Friedlander 方法在微波辐射下以短反应时间和良好收率制备的。比较了几种用于制备 2,4-二-芳基喹啉的均相和非均相酸催化剂,其中三氟乙酸 (TFA) 的产率较高。两种衍生物表现出抗结核分枝杆菌 H37Rv (Mtb) 的活性,经过额外测试,被认为是先导化合物。一系列多环类似物的合成产生了六种新的活性化合物,并建立了定量结构活性关系研究 (QSAR) 研究。
更新日期:2019-11-01
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