Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Carlos García-Aparicio"'
Autor:
Jan Balzarini, Sonsoles Velázquez, Carlos García-Aparicio, Robert Snoeck, María-José Camarasa, Sonia de Castro, Graciela Andrei
Publikováno v:
Journal of Medicinal Chemistry. 52:1582-1591
We report the synthesis and antiviral activity of a new family of non-nucleoside antivirals, derived from the 4-keto-1,2-oxathiole-2,2-dioxide (beta-keto-gamma-sultone) heterocyclic system. Several 4- and 5-substituted-5H-1,2-oxathiole-2,2-dioxide de
Autor:
Ingrid De Meester, María-Cruz Bonache, Sonsoles Velázquez, Carlos García-Aparicio, Jan Balzarini, María-José Camarasa, Ana San-Félix
Publikováno v:
Journal of medicinal chemistry
Here we describe a novel type of enzyme-based prodrug approach in which a dipeptide moiety is linked to a nonpeptidic therapeutic drug through an amide bond which is specifically cleaved by the dipeptidyl-peptidase IV (DPP IV/CD26) enzyme activity pr
Autor:
Erik De Clercq, Sonia de Castro, Jan Balzarini, E. Lobaton, Carlos García-Aparicio, Sonsoles Velázquez, María-José Camarasa, Federico Gago, Kristel Van Laethem
Publikováno v:
Antiviral Research. 71:15-23
The very first TSAO derivative that lacks the 4''-amino group at the 3'-spiro moiety (compound 3) has been prepared and the effect of this modification on the activity/resistance profile has been evaluated. This molecule proved HIV-1 specific (NNRTI-
Autor:
Ma Angeles Bonache, Pilar López, Mercedes Martín-Martínez, Ma Teresa García-López, Rosario González-Muñiz, Carlos Cativiela, Miriam Alías, Guillermo Gerona-Navarro, Carlos García-Aparicio
Publikováno v:
Tetrahedron: Asymmetry. 14:2161-2169
The enantioselectivity of the base-promoted cyclization of N -alkyl- N -chloroacetyl amino acid derivatives to β-lactams is dependent on the substituents on the starting material. While t Bu esters are preferred over Me esters, and N -Bzl-, N -Pmb,
Diffusion of small molecules in a chitosan/water gel determined by proton localized NMR spectroscopy
Publikováno v:
Journal of colloid and interface science. 368(1)
Proton localized NMR spectroscopy (MRS) has been applied to study the diffusion of three small molecules, caffeine, theophylline and caprolactam, in chitosan gels with different concentration of water. This technique allows the non-destructive monito
Autor:
Sonsoles Velázquez, Alberto Diez-Torrubia, Ingrid De Meester, Carlos García-Aparicio, Silvia Cabrera, María-José Camarasa, Jan Balzarini
Publikováno v:
Journal of medicinal chemistry
Here we explore the applicability of the dipeptidyl peptidase IV (DPPIV/CD26) based prodrug approach to a variety of amine-containing drugs. Efficient procedures have been developed for the synthesis of dipeptide and tetrapeptide amide prodrugs inclu
Autor:
Rosario González-Muñiz, Aisling O'Byrne, Fran O'Reilly, Paula Pérez-Faginas, M. Teresa García-López, M. Jesús Pérez de Vega, Carlos García-Aparicio, Mercedes Martín-Martínez
Publikováno v:
Organic letters. 9(8)
[reaction: see text] The base-promoted cyclization of optically pure N-(p-methoxybenzyl)-N-(2-chloro)propionyl amino acid derivatives resulted in a diastereo- and enantioselective approach to valuable 1,3,4,4-tetrasubstituted beta-lactams. The stereo
Autor:
María-José Camarasa, Carlos García-Aparicio, Alberto Diez-Torrubia, Sonsoles Velázquez, Anne-Marie Lambeir, Jan Balzarini
Publikováno v:
Antiviral research
A novel prodrug approach has been evaluated using the anti-HIV-active TSAO molecule as the prototype drug to prove the kinetics with purified enzyme and the principles of conversion to the parent compound in sera and cell culture. When a variety of t
Autor:
Rosario González-Muñiz, Mercedes Martín-Martínez, Guillermo Gerona-Navarro, Carlos García-Aparicio, Fernando Albericio, Ma Angeles Bonache, Ma Teresa García-López, Miriam Royo
Publikováno v:
ChemInform. 35
Autor:
M. Teresa Peromingo, Jan Balzarini, Sonsoles Velázquez, Carlos García-Aparicio, María-José Camarasa, Alberto Diez-Torrubia
Publikováno v:
Antiviral Research. 78:A66