Synthesis and in Vitro and in Vivo Structure-Activity Relationships of Novel Antifungal Triazoles for Dermatology was written by Meerpoel, Lieven;Backx, Leo J. J.;Van der Veken, Louis J. E.;Heeres, Jan;Corens, David;De Groot, Alex;Odds, Frank C.;Van Gerven, Frans;Woestenborghs, Filip A. A.;Van Breda, Andre;Oris, Michel;Van Dorsselaer, Pascal;Willemsens, Gustaaf H. M.;Vermuyten, Karen J. P.;Marichal, Patrick J. M. G.;Vanden Bossche, Hugo F.;Ausma, Jannie;Borgers, Marcel. And the article was included in Journal of Medicinal Chemistry in 2005.Recommanded Product: 4-(4-(4-Methoxyphenyl)piperazin-1-yl)aniline This article mentions the following:
In search for new compounds with potential for clin. use as antifungal agents in dermatol., a series of 12 azole compounds, e.g. I, were synthesized stereospecifically and investigated specifically for their activity against dermatophyte fungal infections in animal models. This panel of azoles was studied in vitro and compared with itraconazole and terbinafine for their antifungal activity using a panel of 24 Candida spp. and 182 dermatophyte isolates. Three azoles (I, II, and III) showed in vitro antifungal potency equivalent to itraconazole, but superior to terbinafine, against a panel of 24 Candida spp. With comparable or lower activity than that of itraconazole and terbinafine against 182 dermatophyte isolates and only rare activity against other pathogenic fungi. However, in vivo I and III, both given orally, demonstrated antifungal activity at least three times greater than itraconazole and were superior compared to terbinafine in M. canis infected guinea pigs. In a mouse model infected by T. mentagrophytes, again III, but not I, showed 5-fold superior activity over itraconazole and terbinafine. Compound II was effective in both models but less effective than itraconazole in these models. On the basis of these promising results, III is currently being clin. investigated for its potential as a novel antifungal agent against dermatophytosis. In the experiment, the researchers used many compounds, for example, 4-(4-(4-Methoxyphenyl)piperazin-1-yl)aniline (cas: 74852-62-3Recommanded Product: 4-(4-(4-Methoxyphenyl)piperazin-1-yl)aniline).
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Piperazines – an overview | ScienceDirect Topics