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Azole Antifungal Agents Related to Naftifine and Butenafine
Author(s) -
Castellano Sabrina,
La Colla Paolo,
Musiu Chiara,
Stefancich Giorgio
Publication year - 2000
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/1521-4184(20006)333:6<162::aid-ardp162>3.0.co;2-s
Subject(s) - allylamine , chemistry , azole , antifungal , alkylation , benzylamine , potency , stereochemistry , in vitro , combinatorial chemistry , pharmacology , biochemistry , organic chemistry , microbiology and biotechnology , medicine , biology , polyelectrolyte , catalysis , polymer
The methyl group of naftifine ( 1 ) and butenafine ( 2 ) was replaced by an azolic nucleus to obtain the new compounds 3—8 which exhibit the characteristics of both allylamine (or benzylamine) and azole antifungals. The title compounds were evaluated in vitro against several pathogenic fungi responsible for human disease. Among these, compounds 5 , 6 , and 8 were found to inhibit the growth of dermatophytes with a potency comparable to that of naftifine. The synthetic sequence includes the preparation of aminoazole Schiff bases, reduction, and alkylation of the corresponding secondary amines.