Artículo
Efficient synthesis under mild reaction conditions of novel 3-aryl-5-(4-chloro-2-morpholinothiazol-5-yl)-4,5-dihydro-1H-pyrazoles and their antifungal activity alone and in combination with commercial antifungal agents.
Ramirez, Juan; Rodriguez, Maria Victoria; Quiroga, Jairo; Abonia, Rodrigo; Sortino, Maximiliano Andrés
; Zacchino, Susana Alicia Stella; Insuasty, Braulio
Fecha de publicación:
04/2014
Editorial:
Wiley VCH Verlag
Revista:
Archiv Der Pharmazie
ISSN:
0365-6233
Idioma:
Inglés
Tipo de recurso:
Artículo publicado
Clasificación temática:
Resumen
The a,b-unsaturated carbonyl compounds 5a–f were prepared by reaction between 2-chloro-4- morpholinothiazol-5-carbaldehyde 3 and substituted acetophenones 4a–f. Treatment of compounds 5a–f with hydrazine hydrate employing mild reaction conditions led to the formation of 4,5-dihydro- 1H-pyrazoles 6a–f. Then the treatment with acetic anhydride or formic acid afforded the expected 4,5- dihydro-1H-pyrazoles 7a–f and 8a–f. The antifungal activity of each series of synthesized compounds was determined against the clinically important fungi Candida albicans and Cryptococcus neoformans. In addition, the most active compounds 7e and 7f were tested in combination with the commercial antifungal agents: fluconazole, itraconazole, and amphotericin B. Compound 7e showed a synergistic effect with fluconazole against C. albicans while 7f showed synergistic activities with all tested antifungal drugs against the same yeast
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Articulos(CCT - ROSARIO)
Articulos de CTRO.CIENTIFICO TECNOL.CONICET - ROSARIO
Articulos de CTRO.CIENTIFICO TECNOL.CONICET - ROSARIO
Citación
Ramirez, Juan; Rodriguez, Maria Victoria; Quiroga, Jairo; Abonia, Rodrigo; Sortino, Maximiliano Andrés; et al.; Efficient synthesis under mild reaction conditions of novel 3-aryl-5-(4-chloro-2-morpholinothiazol-5-yl)-4,5-dihydro-1H-pyrazoles and their antifungal activity alone and in combination with commercial antifungal agents.; Wiley VCH Verlag; Archiv Der Pharmazie; 347; 8; 4-2014; 566-575
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