Vigorita M G, Saporito G, Previtera T, Pizzimenti F C, Bisignano G
Farmaco Sci. 1986 Feb;41(2):168-74.
As part of our investigations on fluorine containing compounds of potential pharmacological interest, a series of N-substituted p-fluorobenzencarboxyamides, analogs of previously studied p-fluorobenzensolfonamides, was prepared. The in vitro antibacterial and antimycotic properties were also assayed. The replacement of the sulfonamide group with an isosteric carboxyamide one, was found to confer to trifluoromethylsubstituted compounds good activity against some strains of yeasts (Candida) and hyphomycetes (Tricophyton, Aspergillus, Microsporum, Epidermophyton). These compounds however are not very active against the gram-positive and gram-negative bacteria on which the corresponding sulfonanilides showed significant activity.
作为我们对具有潜在药理活性的含氟化合物研究的一部分,我们制备了一系列N-取代对氟苯甲酰胺,它们是之前研究过的对氟苯磺酰胺的类似物。同时也测定了它们的体外抗菌和抗真菌特性。结果发现,用等排体羧酰胺基团取代磺酰胺基团后,三氟甲基取代的化合物对某些酵母菌株(念珠菌属)和丝状真菌(毛癣菌属、曲霉属、小孢子菌属、表皮癣菌属)具有良好的活性。然而,这些化合物对相应的磺酰苯胺类化合物显示出显著活性的革兰氏阳性菌和革兰氏阴性菌的活性并不高。