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1.
Org Lett ; 23(9): 3282-3286, 2021 05 07.
Artículo en Inglés | MEDLINE | ID: mdl-33904740

RESUMEN

Enantioselective syntheses of nonracemic secondary alcohols have been achieved in an aqueous micellar medium via copper-catalyzed (Cu(OAc)2·H2O/(R)-3,4,5-MeO-MeO-BIPHEP) reduction of aryl/heteroaryl ketones. This methodology serves as a green protocol to access enantio-enriched alcohols under mild conditions (0-22 °C) using a base metal catalyst, together with an inexpensive, innocuous, and convenient stoichiometric hydride source (PMHS). The secondary alcohol products are formed in good to excellent yields with ee values greater than 90%.

2.
Bioorg Med Chem Lett ; 20(18): 5572-6, 2010 Sep 15.
Artículo en Inglés | MEDLINE | ID: mdl-20724151

RESUMEN

A series of fluorine containing 4-(substituted-2-hydroxybenzoyl) pyrazoles and pyrazolyl benzo[d]oxazoles were synthesized and evaluated for their antibacterial activity against Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa and Bacillus subtilis and antifungal activity against Candida albicans. The antibacterial activities were expressed as the minimum inhibitory concentration (MIC50) in microg/ml. The compounds 1-(3,4-difluorophenyl)-4-(5-fluoro-2-hydroxybenzoyl)-1H-pyrazole (4b), oxime derivatives such as 1-(3,4-difluorophenyl)-1H-pyrazol-4-yl)(2-hydroxy-4-methylphenyl)methanone oxime (5b) and (5-chloro-2-hydroxyphenyl)(1-(3,4-difluorophenyl)-1H-pyrazol-4-yl)methanone oxime (5e) exhibited promising activities against tested bacterial strains. Except compound 1-(3,4-difluorophenyl)-4-(2-hydroxybenzoyl)-1H-pyrazole (4d), none of the other compounds showed promising antifungal activity.


Asunto(s)
Antiinfecciosos/farmacología , Bacterias/efectos de los fármacos , Candida albicans/efectos de los fármacos , Flúor/farmacología , Oxazoles/farmacología , Pirazoles/farmacología , Antibacterianos/síntesis química , Antibacterianos/química , Antibacterianos/farmacología , Antiinfecciosos/síntesis química , Antiinfecciosos/química , Antifúngicos/síntesis química , Antifúngicos/química , Antifúngicos/farmacología , Bacillus subtilis/efectos de los fármacos , Infecciones Bacterianas/tratamiento farmacológico , Candidiasis/tratamiento farmacológico , Escherichia coli/efectos de los fármacos , Flúor/química , Humanos , Pruebas de Sensibilidad Microbiana , Oxazoles/síntesis química , Oxazoles/química , Pseudomonas aeruginosa/efectos de los fármacos , Pirazoles/síntesis química , Pirazoles/química , Staphylococcus aureus/efectos de los fármacos , Relación Estructura-Actividad
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