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Synthesis and biological evaluation of [alpha-(1,5-disubstituted 1H-pyrazol-4-yl)benzyl]azoles, analogues of bifonazole.
- Source :
-
Farmaco (Societa chimica italiana : 1989) [Farmaco] 1999 Jun 30; Vol. 54 (6), pp. 416-22. - Publication Year :
- 1999
-
Abstract
- A series of pyrazole analogues of bifonazole, an antifungal drug used in clinical practice, 2a-h and 4a-h were synthesized and tested in vitro against Candida albicans, Cryptococcus neoformans and Aspergillus fumigatus, with no significant results. Imidazoles 2a-h were also tested in vivo for antiarrhythmic and antihypertensive activities; two of these compounds showed moderate activity against ventricular fibrillation caused by aconitine in rats. The above compounds were prepared by reaction of phenyl-[5 substituted 1-phenyl (or 1-methyl)-1H-pyrazol-4-yl]methanols with N,N'-carbonyldiimidazole (2a-h) or of the respective chloro derivatives with 1H-1,2,4-triazole (4a-h).
- Subjects :
- Animals
Anti-Arrhythmia Agents chemical synthesis
Anti-Arrhythmia Agents pharmacology
Anti-HIV Agents chemical synthesis
Anti-HIV Agents pharmacology
Antifungal Agents chemical synthesis
Antifungal Agents pharmacology
Antihypertensive Agents chemical synthesis
Antihypertensive Agents pharmacology
Antineoplastic Agents chemical synthesis
Antineoplastic Agents pharmacology
Drug Screening Assays, Antitumor
Fungi drug effects
HIV-1 drug effects
Hemodynamics drug effects
Imidazoles pharmacology
Magnetic Resonance Spectroscopy
Mice
Microbial Sensitivity Tests
Pyrazoles pharmacology
Rats
Salmonella drug effects
Spectrophotometry, Infrared
Imidazoles chemical synthesis
Pyrazoles chemical synthesis
Subjects
Details
- Language :
- English
- ISSN :
- 0014-827X
- Volume :
- 54
- Issue :
- 6
- Database :
- MEDLINE
- Journal :
- Farmaco (Societa chimica italiana : 1989)
- Publication Type :
- Academic Journal
- Accession number :
- 10443021
- Full Text :
- https://doi.org/10.1016/s0014-827x(99)00036-1