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A Novel Antifungal Agent with Broad Spectrum: 1‐(4‐Biphenylyl)‐3‐(1 H ‐imidazol‐1‐yl)‐1‐propanone
Author(s) -
Roman Gheorghe,
Mareş Mihai,
Năstasă Valentin
Publication year - 2013
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/ardp.201200287
Subject(s) - imidazole , chemistry , broad spectrum , antifungal , aryl , alkylation , medicinal chemistry , ketone , stereochemistry , combinatorial chemistry , organic chemistry , alkyl , catalysis , biology , microbiology and biotechnology
A series of (1‐substituted aryl)‐3‐(1 H ‐imidazol‐1‐yl)‐1‐propanones was synthesized through the N ‐alkylation of imidazole with 3‐dimethylamino‐1‐(substituted aryl)‐1‐propanone hydrochlorides (ketonic Mannich bases). A second series of N 1 ‐substituted imidazoles was obtained by the reduction of the carbonyl function of the imidazole–ketones in the previous series by means of NaBH 4 . All of the compounds were evaluated for antifungal activity against 16 strains of Candida , and 3‐(1 H ‐imidazol‐1‐yl)‐1‐(4‐biphenylyl)‐1‐propanone emerged as a broad‐spectrum antifungal agent. Several 3‐(1 H ‐imidazol‐1‐yl)‐1‐(2′‐(substituted benzyl)oxyphenyl)‐1‐propanones were also active towards Candida kefyr .