INVESTIGADORES
DERITA marcos gabriel
artículos
Título:
Synthesis and antifungal activity of diverse C-2 pyridinyl and pyridinylvinyl substituted quinolines
Autor/es:
KOUZNETSOV, V.; MELÉNDEZ-GÓMEZ, C.; DERITA, M.; SVETAZ, L.; DEL OLMO, E.; ZACCHINO, S.
Revista:
BIOORGANIC & MEDICINAL CHEMISTRY.
Editorial:
PERGAMON-ELSEVIER SCIENCE LTD
Referencias:
Lugar: Amsterdam; Año: 2012 vol. 20 p. 6506 - 6512
ISSN:
0968-0896
Resumen:
A b s t r a c t: Diverse 2-pyridinyl quinolines 6?12 and 2-pyridinilvinyl quinolines 13?17 were prepared using a straightforward synthesis based on the BiCl3-catalyzed multicomponent imino Diels?Alder (imino DA) reaction or a novel tandem imino DA/catalytic tetrahydroquinoline ring oxidation/Perkin condensation sequential process. All members of the series showed activities against dermatophytes and some of them possessed a broad spectrum of action. 2-(Pyridin-4-yl)quinoline 9 and 2-(2-pyridin-4-yl)vinyl)quinoline 16 showed the best MIC80 and MIC50 against the clinically important fungi Candida albicans and non-albicans Candida species. In turn, 6-ethyl-2-(pyridin-2-yl)quinoline 6 showed the best properties against standardized as well as clinical strains of Cryptococcus neoformans.
