42086-75-9Relevant 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.
Anti-HIV activity of stilbene-related heterocyclic compounds
Bedoya, Luis M.,del Olmo, Esther,Sancho, Rocio,Barboza, Bianca,Beltran, Manuela,Garcia-Cadenas, Ana E.,Sanchez-Palomino, Sonsoles,Lopez-Perez, Jose L.,Munoz, Eduardo,Feliciano, Arturo San,Alcami, Jose
, p. 4075 - 4079 (2007/10/03)
Viral transcription has not been routinely targeted in the development of new antiviral drugs. This crucial step of the viral cycle depends on the concerted action of cellular and viral proteins such as NF-κB and Tat. In the present study, stilbene-related heterocyclic compounds including benzalphthalide, phthalazinone, imidazoindole and pyrimidoisoindole derivatives are tested for their anti-HIV activity. Original assays based on recombinant viruses were used to evaluate HIV replication inhibition and stably transfected cell lines were used to evaluate inhibition of Tat and NF-κB proteins. Some of the stilbene-related heterocyclic compounds analysed displayed anti-HIV activity through interference with NF-κB and Tat function. Moreover, compounds inhibiting both targets displayed a stronger activity on viral replication.
Anxiolytic effects of benzalphthalides
Zamilpa, Alejandro,Herrera-Ruiz, Maribel,Del Olmo, Esther,Lopez-Perez, Jose L.,Tortoriello, Jaime,San Feliciano, Arturo
, p. 3483 - 3486 (2007/10/03)
Anxiolytic effects induced by benzalphthalides on mice have been evaluated. The evaluation was based on the spent time and the number of entries of animals into the open arms in the elevated plus maze test. Single administration of benzalphthalides 1 and 11 induced significant increments in both parameters, thus revealing their potentiality as new leads for the development of non-benzodiazepinic and non-nitrogenated antianxiety agents.