331835-06-4Relevant academic research and scientific papers
Regioselective sy nthesis and antimicrobial evaluation of new 1-aryloxyacetyl-, 1-thiophenoxyacetyl- and 1-phenylaminoacetylsubstituted 3-alkyl(aryl/heteroaryl)-5-trifluoromethyl-5-hydroxy-4,5-dihydro-1H-pyrazoles
Bonacorso, Helio G.,Pittaluga, Everton P.,Alves, Sydney H.,Schaffer, Larissa F.,Cavinatto, Susiane,Porte, Liliane M. F.,Paim, Gisele R.,Martins, Marcos A. P.,Zanatta, Nilo
, p. 62 - 75 (2012/07/31)
This paper describes an efficient approach for the regioselective synthesis of new series of twenty 1-aryloxy(thio)acetyl and 1-(phenylamino)acetyl- substituted 5-trifluoromethyl-5-hydroxy-4,5-dihydro-1H-pyrazoles (3) in 34-96% yields from the cyclocondensation reaction of 4-alkoxy-4-alkyl-(aryl/heteroaryl) -1,1,1-trifluoroalk-3-en-2-ones with different substituted acetohydrazides. Dehydration reactions of 3, carried out in the presence of thionyl chloride, furnished two examples of aromatic 5-trifluoromethyl-1H-pyrazole derivatives, in 78-82% yields. From antimicrobial tests the fungi C. albicans proved to be particularly susceptible to the action of 1-(phenylamino)acetyl-substituted 3-alkyl-2-pyrazoline derivatives; however the first results are still weak when compared to standard drugs. ARKAT-USA, Inc.
