- Total syntheses of paraconic acids and 1,10-seco-guaianolides via a barbier allylation/translactonization cascade of 3-(Bromomethyl)-2(5H)-furanone
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A palladium-catalyzed Barbier allylation/translactonization cascade reaction was established for the rapid construction of β,γdisubstituted α-exo-methylene-γ-butyrolactone, an important motif in sesquiterpenes. Dimethyl zinc played significant roles in bo
- Liu, Weilong,Yu, Zhimei,Winssinger, Nicolas
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supporting information
p. 969 - 973
(2021/03/03)
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- Enzymatic resolution of α-methyleneparaconic acids and evaluation of their biological activity
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Both enantiomers of three biologically relevant paraconic acids-MB-3, methylenolactocin, and C75-were obtained with enantioselectivities up to 99% by kinetic enzymatic resolutions. Good enantiomeric excesses were obtained for MB-3 and methylenolactocin, using α-chymotrypsin and aminoacylase as enantiocomplementary enzymes, while C75 was resolved with aminoacylase. They all were evaluated for their antiproliferative, antibacterial, and antifungal activities, showing weak effects and practically no difference between enantiomers in each case. At high concentrations (16-64μg/mL), (-)- C75 acted as an antimicrobial agent against Gram-positive bacteria.
- Chakrabarty, Kuheli,Defrenza, Ivana,Denora, Nunzio,Drioli, Sara,Forzato, Cristina,Franco, Massimo,Lentini, Giovanni,Nitti, Patrizia,Pitacco, Giuliana
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p. 239 - 246
(2015/03/18)
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- The first kinetic enzymatic resolution of methyl ester of C75
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Enantioselective hydrolysis of methyl ester of (±)-C75 was successfully accomplished by means of Acylase I from Aspergillus to afford (2,R,3S)-(+)-C75 with 96% e.e. The unreacted methyl ester was recovered with >99% e.e. This latter compound was either chemically or enzymatically hydrolyzed to furnish (2S,3,R)-(-)-C75 with >99% e.e.
- Chakrabarty, Kuheli,Forzato, Cristina,Nitti, Patrizia,Pitacco, Giuliana,Valentin, Ennio
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p. 245 - 248
(2011/06/28)
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- INHIBITION OF FATTY ACID SYNTHASE AS A MEANS TO REDUCE ADIPOCYTE MASS
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Weight loss was noted in nude mice treated with cerulenin, a non-competitive inhibitor of FAS. Sustained reduction of adipocyte mass in humans without toxicity would significantly impact disease prevention worldwide. Aside from psychological and self-este
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Page/Page column 10; 11
(2010/02/13)
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