1.
Bioorg Med Chem Lett
; 21(1): 276-9, 2011 Jan 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-21115249
RESUMEN
SAR studies and optimization of various modified Hygromycin A fluoroalkyl ethers, which led to the discovery of the highly potent 4'-(2-cyclopropyl-2-fluoroethyl ether) antibacterial CE-156811 (1) derived from truncation of the ribose ring and difluorination of the phenyl found in Hygromycin A, are discussed.
Asunto(s)
Antibacterianos/química , Cinamatos/química , Dioxoles/química , Higromicina B/análogos & derivados , Administración Oral , Animales , Antibacterianos/síntesis química , Antibacterianos/farmacocinética , Perros , Evaluación Preclínica de Medicamentos , Haplorrinos , Higromicina B/química , Ratones , Pruebas de Sensibilidad Microbiana , Ratas , Relación Estructura-Actividad
2.
Bioorg Med Chem Lett
; 20(22): 6730-4, 2010 Nov 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-20864341
RESUMEN
Novel hygromycin A derivatives bearing a variety of functionalized aminocyclitol moieties have been synthesized in an effort to increase the antibacterial activity and drug-like properties of this class of agents. A systematic study of the effect of alkylation and removal of the hydroxyls of the aminocyclitol directed us to a series of alkylated aminocyclitol derivatives with improved gram-positive activity.