Silvestri R, Pagnozzi E, Troccoli F, Stefancich G, Massa S, Apuzzo G, Perazzi M E, Artico M, Simonetti G
Dipartimento di Studi Farmaceutici, Università di Roma La Sapienza, Roma, Italy.
Farmaco. 1995 Apr;50(4):227-38.
Various aryl-(1H-imidazol-1-yl)-(isoquinolin-1-yl)methane derivatives have been synthesized and tested as antifungal agents. The new imidazoles have been obtained by the action of 1,1'-sulfinyldiimidazole on aryl-(isoquinolin-1-yl)carbinols, which have been prepared by standard procedures starting from isoquinoline. Among 44 test derivatives only a few have exhibited some antifungal activity, the most active compound (4e) being twofold less potent than miconazole, ketoconazole and bifonazole, used as standard drugs.
已合成了多种芳基 -（1H - 咪唑 - 1 - 基）-（异喹啉 - 1 - 基）甲烷衍生物，并作为抗真菌剂进行了测试。这些新型咪唑是通过1,1'-亚磺酰二咪唑对芳基 -（异喹啉 - 1 - 基）甲醇的作用得到的，芳基 -（异喹啉 - 1 - 基）甲醇是通过从异喹啉开始的标准程序制备的。在44种测试衍生物中，只有少数表现出一定的抗真菌活性，活性最高的化合物（4e）的效力比作为标准药物的咪康唑、酮康唑和联苯苄唑低两倍。
