Nuovi 1,4-dimetil carbazoli:sintesi, reattività e valutazione biologicaDocumenti elettronici

Dipartimenti di Scienze Farmaceutiche, Dottorato di Ricerca in: "Ambiente, Salute e Processi Eco-Sostenibili, XXII Ciclo a.a. 2009-2010Università degli Studi della Calabri

Extraction of nutraceuticals from natural matrices

Doctor Of Philosophy: Environment, Health and Environmentally Sustainable Processes, Ciclo XXVII,a.a. 2014University of Calabri

Baker’s Yeast-Induced Asymmetric Reduction of alpha-Ketosulfides. Synthesis of optically active 1-(Benzothiazol-2-ylsulfanyl)-2-alkanols, 2-Alkanols, and Thiiranes

1-(Benzothiazol-2-ylsulfanyl)-2-alkanols 3 were prepared in very high enantiomeric excess by baker’s yeastinduced asymmetric reduction of 1-(benzothiazol-2-ylsulfanyl)-2-alkanones 1. Conversionof 3 into optically active simple 2-alkanols 4 and thiiranes 2 by reductive desulfurization and base treatment, respectively, is also described. The absolute configuration of the new compounds synthesized has been established by chemical correlation and specific rotation comparison

Candida Cylindracea lipase-mediated kinetic resolution of a-substituted a-aryloxyacetic acid methyl esters

Hydrolysis of several alpha-alkyl-alpha-aryloxyacetic acid methyl esters and of alpha-methyl-alpha-(n-propyl)-alpha-(p-chlorophenoxy)acetic acid methyl ester were performed in the presence of Candida cylindrarea lipase. The alpha-alkyl-alpha-aryloxyacetic acid methyl esters and alpha-methyl-alpha-(n-propyl)-alpha-(p-chlorophenoxy)acetic acid methyl ester were incubated in buffer phosphate (pH 7-8). The reaction mixture, containing the unreacted ester and corresponding acid, showed enantiomeric excesses (ee) up to 81%. The extent of conversion was quite low for the alpha-methyl-alpha-(n-propyl)-alpha-(p-chlorophenoxy) acid methyl ester, the corresponding acid was obtained with ee > 98%

Lipase-mediated kinetic resolution of rigid clofibrate analogues, with lipid-modifying activity

The lipase-catalysed kinetic resolution of methyl (+/-)-6-chloro-2.3-dihydro-4H-1-benzopyran-2-carboxylic acid. and (+/-)-6-chloro-2,3-dihydro-4H-1-benzopyran-3-carboxylic acid, rigid analogues of clofibrate. was effected with fair to moderate enantioselectivities (E = 1.0-4.8), enantiomeric excesses of up to 86%, and workable reaction rates. Enantiomerically pure (R)- and ( S)-5-chloro-2,3-dihydro-1-benzofuran-2-carboxylic acids were obtained by fractional crystallisation of the diastereomeric salts of the corresponding racemic acid with (+)- and (-)-amphetamine from ethanol; the absolute configuration of the products were established by chemical correlation

Acetamide derivatives with antioxidant activity and potential anti-inflammatory activity

This study reports the synthesis and antioxidant activity of some new acetamide derivatives. The compounds' structures were elucidated by NMR analysis and their melting points were measured. The in vitro antioxidant activity of these compounds was tested by evaluating the amount of scavenged ABTS radical and estimating ROS and NO production in tBOH- or LPS-stimulated J774.A1 macrophages. All compounds were tested for their effect on cell viability by an MTT assay and by a Brine Shrimp Test