1242339-45-2Relevant academic research and scientific papers
Efficient synthesis 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
Ramírez, Juan,Rodríguez, María Victoria,Quiroga, Jairo,Abonia, Rodrigo,Sortino, Maximiliano,Zacchino, Susana A.,Insuasty, Braulio
, p. 566 - 575 (2014/08/18)
The α,β-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.
Thiazole analogs of chalcones, capable of functionalization at the heterocyclic nucleus
Kotlyar,Pushkarev,Orlov,Chernenko,Desenko
, p. 334 - 341 (2011/04/22)
The synthesis of new amino and alkoxy derivatives of thiazole-5- carbaldehyde, on the basis of which a,β-unsaturated ketones of the thiazole series were synthesized, are described in this paper. The possibility of obtaining chalcones and variation of substitution reactions in the thiazole ring has been shown. 2010 Springer Science+Business Media, Inc.
