Synthesis and antifungal activity of diverse C-2 pyridinyl and pyridinylvinyl substituted quinolines
作者:Vladimir V. Kouznetsov、Carlos M. Meléndez Gómez、Marcos G. Derita、Laura Svetaz、Esther del Olmo、Susana A. Zacchino
DOI:10.1016/j.bmc.2012.08.036
日期:2012.11
Diverse 2-pyridinyl quinolines 6–12 and 2-pyridinilvinyl quinolines 13–17 were prepared using a straightforward synthesis based on the BiCl3-catalyzed multicomponent imino Diels–Alder (imino DA) reaction or a novel tandem imino DA/catalytic tetrahydroquinoline ring oxidation/Perkin condensation sequential process. All members of the series showed activities against dermatophytes and some of them possessed
多样2-吡啶基喹啉6 - 12和2-喹啉pyridinilvinyl 13 - 17使用基于BiCl一个简单的合成方法制备3 -催化的多组分亚氨基狄尔斯-阿尔德(亚氨基DA)反应或新的串联亚氨基DA /催化四氢喹啉环的氧化/珀金冷凝顺序过程。该系列的所有成员均表现出对抗皮肤癣菌的活性,其中一些具有广泛的作用范围。2-(吡啶-4-基)喹啉9和2-(2-吡啶-4-基)乙烯基)喹啉16对临床上重要的真菌白色念珠菌表现出最好的MIC 80和MIC 50和非白色念珠菌。反过来,6-乙基-2-(吡啶-2-基)喹啉6对新型隐球菌和临床菌株表现出最好的性能。