Rifamycin derivs., such as I [R is hydrogen or acetyl R1 and R2 are independently selected from the group consisting of hydrogen, ( C1-4) alkyl, benzyloxy, mono- and di-(C1-3) alkylamino-(C1-4)alkyl, (C1-3)alkoxy, (C1-4) alkyl, hydroxy-Me, hydroxy-(C2-4)-alkyl, and nitro or R1R2 taken together with two consecutive carbon atoms of the pyridine nucleus form a benzene ring optionally substituted by one or two Me or Et groups and R3 is hydroxyalkyl (C1-4)], were prepd. for use in antibacterial pharmaceutical compns. The prepd. rifamycin derivs. were claimed for use in the prevention, treatment or amelioration of bacterial overgrowth in a patient suffering from a bowel related disorder, such as irritable bowel syndrome, travelers' diarrhea, small intestinal bacterial overgrowth, Crohn's disease, chronic pancreatitis, pancreatic insufficiency, hepatic encephalopathy, diverticulitis, enteritis or colitis. These rifamycin derivs. may be used optionally in combination with one or more addnl. antibiotics, such as rifamycin, or rifaximin. Thus, rifamycin deriv. I [R = COMe, R1 = 4-Me, R2 = H, R3 = CH2OH] was prepd. via a cyclocondensation reaction of the corresponding cyclic acetal II with 2-amino-4-methylpyridine. The cyclic acetal II was prepd. by a fermn. process mediated by Nocardia mediterranea. The prepd. rifamycin derivs. were evaluated in vitro for antibacterial activity against a panel of pathogenic bacterium, such as E. coli (ATCC 25922), P. aeruginosa (ATCC 27853) and E. faecalis (ATCC 259212). Pharmaceutical formulations for the delivery of these rifamycin derivs. were presented.
Rifamycin derivatives
RIGHI, PAOLO;ROSINI, GOFFREDO;
2013
Abstract
Rifamycin derivs., such as I [R is hydrogen or acetyl R1 and R2 are independently selected from the group consisting of hydrogen, ( C1-4) alkyl, benzyloxy, mono- and di-(C1-3) alkylamino-(C1-4)alkyl, (C1-3)alkoxy, (C1-4) alkyl, hydroxy-Me, hydroxy-(C2-4)-alkyl, and nitro or R1R2 taken together with two consecutive carbon atoms of the pyridine nucleus form a benzene ring optionally substituted by one or two Me or Et groups and R3 is hydroxyalkyl (C1-4)], were prepd. for use in antibacterial pharmaceutical compns. The prepd. rifamycin derivs. were claimed for use in the prevention, treatment or amelioration of bacterial overgrowth in a patient suffering from a bowel related disorder, such as irritable bowel syndrome, travelers' diarrhea, small intestinal bacterial overgrowth, Crohn's disease, chronic pancreatitis, pancreatic insufficiency, hepatic encephalopathy, diverticulitis, enteritis or colitis. These rifamycin derivs. may be used optionally in combination with one or more addnl. antibiotics, such as rifamycin, or rifaximin. Thus, rifamycin deriv. I [R = COMe, R1 = 4-Me, R2 = H, R3 = CH2OH] was prepd. via a cyclocondensation reaction of the corresponding cyclic acetal II with 2-amino-4-methylpyridine. The cyclic acetal II was prepd. by a fermn. process mediated by Nocardia mediterranea. The prepd. rifamycin derivs. were evaluated in vitro for antibacterial activity against a panel of pathogenic bacterium, such as E. coli (ATCC 25922), P. aeruginosa (ATCC 27853) and E. faecalis (ATCC 259212). Pharmaceutical formulations for the delivery of these rifamycin derivs. were presented.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
