5409-63-2Relevant articles and documents
A novel antifungal agent with broad spectrum: 1-(4-Biphenylyl)-3-(1H- imidazol-1-yl)-1-propanone
Roman, Gheorghe,Mare?, Mihai,Nǎstasǎ, Valentin
, p. 110 - 118 (2013/04/10)
A series of (1-substituted aryl)-3-(1H-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 N1-substituted imidazoles was obtained by the reduction of the carbonyl function of the imidazole-ketones in the previous series by means of NaBH4. All of the compounds were evaluated for antifungal activity against 16 strains of Candida, and 3-(1H-imidazol-1-yl)-1-(4-biphenylyl)-1- propanone emerged as a broad-spectrum antifungal agent. Several 3-(1H-imidazol-1-yl)-1-(2′-(substituted benzyl)oxyphenyl)-1-propanones were also active towards Candida kefyr. Copyright
Synthesis and Antifungal Activity of a Series of Novel 1,2-Disubstituted Propenones
Ogata, Masaru,Matsumoto, Hiroshi,Kida, Shiro,Shimizu, Sumio,Tawara, Katsuya,Kawamura, Yoshimi
, p. 1497 - 1502 (2007/10/02)
To find an antifungal agent other than those of the imidazole and triazole series, a new class of 1,2-disubstituted propenones I and II was prepared and tested for antifungal activity.Comparison of the structure-activity relationships showed that the conjugated structure of carbonyl and exomethylene groups in I and II plays an important role in potent antifungal acivity.However, it is noteworthy that compounds 53, 54, and 56, which have a hydroxymethyl or methoxymethyl group instead of an exo-methylene group in I, also showed potent activity.Although many compounds exhibited strong antifungal activity in vitro, none showed activity in vivo of oral efficacy against subacute systemic candidiasis in mice. '