148345-05-5Relevant articles and documents
Synthesis, bioevaluation and structural study of substituted phthalazin-1(2H)-ones acting as antifungal agents
Derita, Marcos,Del Olmo, Esther,Barboza, Bianca,Garcia-Cadenas, Ana Esther,Lopez-Perez, Jose Luis,Andujar, Sebastian,Enriz, Daniel,Zacchino, Susana,Feliciano, Arturo San
, p. 3479 - 3501 (2013/05/09)
Twenty-five polysubstituted phthalazinone derivatives were synthesized and tested for their antifungal activity against a panel of pathogenic and clinically important yeasts and filamentous fungi. Among them, the compound 4-(4-chlorobenzyl)-2- methylphthalazin-1(2H)-one (5) exhibited a remarkable antifungal activity against standardised strains of dermatophytes and Cryptococcus neoformans, as well as against some clinical isolates. A physicochemical study performed on compound 5 revealed its conformational and electronic characteristics, providing us with useful data for the future design of novel related antifungal analogues.
Copper-catalyzed preparation of γ-alkylidenebutenolides and isocoumarins under mild palladium-free conditions
Inack-Ngi, Samuel,Rahmani, Raphael,Commeiras, Laurent,Chouraqui, Gaelle,Thibonnet, Jerome,Duchene, Alain,Abarbri, Mohamed,Parrain, Jean-Luc
supporting information; experimental part, p. 779 - 788 (2009/11/30)
A general and efficient copper(I)-catalyzed cross-coupling and heterocyclization reaction of terminal alkynes and β-iodo-α,β- unsaturated acid derivatives has been developed under very mild conditions. This method provides easy access from good to excellent yields of a variety of 5-ylidenebutenolides and 3-substituted isocoumarins with excellent regio- and stereoselectivity. This procedure does not require the use of any expensive supplementary additives, and is palladium-free.
Vasorelaxant activity of phthalazinones and related compounds
Olmo, Esther del,Barboza, Bianca,Ybarra, Ma Ines,Lopez-Perez, Jose Luis,Carron, Rosalia,Sevilla, Ma Angeles,Boselli, Cinthia,Feliciano, Arturo San
, p. 2786 - 2790 (2007/10/03)
Several series of dihydrostilbenamide, imidazo[2,1-a]isoindole, pyrimido[2,1-a]isoindole and phthalazinone derivatives were obtained and their vasorelaxant activity was measured on isolated rat aorta rings pre-contracted with phenylephrine (10-5 M). Some phthalazinones attained, practically, the total relaxation of the organ at micromolar concentrations. For the most potent compound 9h (EC50 = 0.43 μM) the affinities for α1A, α1B and α1D adrenergic sub-receptors were determined.