Retico A

Antifungal agents. 1. Synthesis and antifungal activities of estrogen-like imidazole and triazole derivatives

Abstract The synthesis of some 2-aryl-1-(4-methoxyphenyl)-1-(1 H -imidazol-1-yl)ethane derivatives and related 1 H -1,2,4- and 1 H -1,3,4-triazoles is described. The molecular structure of new derivatives has been established by 1H NMR spectra and X-ray crystallographic analysis. When tested in solid agar cultures the azole derivatives showed from moderate to potent in vitro antifungal activity against Candida albicans and Candida spp.

Studies on anti-Candida agents with a pyrrole moiety. Synthesis and microbiological activity of some 3-aminomethyl-1,5-diaryl-2-methyl-pyrrole derivatives

Abstract The synthesis and anti- Candida activity of some 3-aminomethyl-1,5-diaryl-2-methyl-pyrrole derivatives are reported. Some derivatives show a rather strong anti- Candida activity. On the basis of experimental results, microbiological activity of 1,5-diarylpyrroles appears to be mainly related to aminic nitrogen lone pair availability of C3 substituent of the pyrrole nucleus. The C5 and N1 substituents play an important role in modulating biological activity. Some structure-activity relationships are proposed.

Antifungal agents. 5. Chloro and amino derivatives of 1,2-diaryl-1-(1H-imidazol-1-yl)ethane with potent antifungal activities

Abstract Various derivatives of 1,2-diaryl-1-(1H-imidazol-1-yl)ethane have been synthesized and tested against Candida albicans and Candida spp. In vitro essays showed chloro and amino derivatives to be as active as miconazole and bifonazole and more potent than ketoconazole. Structure-activity relationships of the new imidazole antifungal agents are discussed.