Examinando por Autor "Enriz, Ricardo Daniel"

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    ÍtemAcceso Abierto
    Structural requirements for the antifungal activities of natural drimane sesquiterpenes and analogues, supported by conformational and electronic studies
    (MDPI, 2013-02-05) Derita, Marcos Gabriel; Montenegro, Iván; Garibotto, Francisco; Enriz, Ricardo Daniel; Cuellar Fritis, Mauricio; Zacchino, Susana; https://orcid.org/0000-0002-7112-5500
    Seventeen drimanes including polygodial (1), isopolygodial (2), drimenol (3) and confertifolin (4) obtained from natural sources and the semi-synthetic derivatives 5–17 obtained from 1–3, were evaluated in vitro for antifungal properties against a unique panel of fungi with standardized procedures by using two end-points, MIC100 and MIC50. A SAR analysis of the whole series, supported by conformational and electronic studies, allowed us to show that the Δ7,8 -double bond would be one of the key structural features related to the antifungal activity. The MEPs obtained for active compounds exhibit a clear negative minimum value (deep red zone) in the vicinity of the Δ7,8 -double bond, which is not present in the inactive ones. Apart of this negative zone, a positive region (deep blue) appears in 1, which is not observed either in its epimer 2 nor in the rest of the active compounds. The LogP of active compounds varies between 2.33 and 3.84, but differences in MICs are not correlated with concomitant variations in LogP values.
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    ÍtemAcceso Abierto
    Synthesis, Bioevaluation and Structural Study of Substituted Phthalazin-1(2H)-ones Acting as Antifungal Agents
    (MDPI Open Access Publishing, 2013-03) Derita, Marcos Gabriel; Del Olmo, Esther; Barboza, Bianca; García Cadenas, Ana E.; López Pérez, José L.; Andújar, Sebastián; Enriz, Ricardo Daniel; Zacchino, Susana; San Feliciano, Arturo
    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.