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[Synthesis and antifungal activity of novel triazole antifungal agents].
- Source :
-
Yao xue xue bao = Acta pharmaceutica Sinica [Yao Xue Xue Bao] 2004 Dec; Vol. 39 (12), pp. 984-9. - Publication Year :
- 2004
-
Abstract
- Aim: A series of triazole antifungal agents were synthesized to search for novel triazole antifungal agents with more potent activity, less toxicity and broader spectrum.<br />Methods: Twenty-one 1-(1H-1, 2, 4-triazolyl)-2-(2, 4-diflurophenyl)-3-(4-substituted-1-piperazinyl)-2-propanols were synthesized, on the basis of the three dimensional structure of P450 cytochrome 14alpha-sterol demethylase (CYP51) and their antifungal activities were also evaluated.<br />Results: Results of preliminary biological tests showed that most of title compounds exhibited activity against the eight common pathogenic fungi to some extent and the activities against deep fungi were higher than that against shallow fungi. In general, phenyl and pyridinyl analogues showed higher antifungal activity than that of the phenylacyl analogues.<br />Conclusion: Several title compounds showed higher antifungal activities than fluconazole and terbinafine. Compound VIII-1, 4, 5 and IX-3 showed the best antifungal activity with broad antifungal spectrum and were chosen for further study.
- Subjects :
- Antifungal Agents chemistry
Antifungal Agents pharmacology
Aspergillus fumigatus drug effects
Cryptococcus neoformans drug effects
Fluconazole pharmacology
Microbial Sensitivity Tests
Molecular Structure
Naphthalenes pharmacology
Structure-Activity Relationship
Terbinafine
Triazoles chemistry
Triazoles pharmacology
Antifungal Agents chemical synthesis
Candida albicans drug effects
Triazoles chemical synthesis
Subjects
Details
- Language :
- Chinese
- ISSN :
- 0513-4870
- Volume :
- 39
- Issue :
- 12
- Database :
- MEDLINE
- Journal :
- Yao xue xue bao = Acta pharmaceutica Sinica
- Publication Type :
- Academic Journal
- Accession number :
- 15813026