- RIFAMYCIN DERIVATIVES EFFECTIVE AGAINST DRUG-RESISTANT MICROBES
-
Rifamycin derivatives having antimicrobial activities, including activities against drug-resistant microorganisms are claimed in this invention. The inventive rifamycin derivatives are uniquely designed in that they have a rifamycin moiety covalently linked to a linker group through the C-3 carbon of the rifamycin moiety and the linker is, in turn covalently linked to a therapeutic moiety or antibacterial agent/pharmacophore. The therapeutic moiety can be a quinolone, an oxazolidinone, a macrolide, an aminoglycoside, a tetracycline core or a structure/pharmacophore associated with an antibacterial agent.
- -
-
Page/Page column 38
(2010/02/13)
-
- Process for producing 1-substituted aryl-1,4-dihydro-4-oxonaphthyridine derivatives, and processes for producing the intermediates
-
This invention relates to a process for industrially producing a 1-substituted aryl-1,4-dihydro-4-oxonaphthyridine derivative and a salt thereof which are useful as an antibacterial agent, and also to intermediates therefor and processes for producing the
- -
-
-
- Synthesis and Structure-Activity Relationships of New Arylfluoronaphthyridine Antibacterial Agents
-
Novel arylfluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid have been prepared and their antibacterial activity evaluated.These derivatives are characterized by having a fluorine atom at 6-position, substituted amino groups at the 7-position, and substituted phenyl groups at the 1-position.The in vitro antibacterial potency is greatest when the 1-substituent is either p-fluorophenyl or o,p-difluorophenyl and the 7-substituent is a 3-amino-1-pyrrolidinyl group. 1-(2,4-Difluorophenyl)-6-fluoro-7-(3-amino-1-pyrrolidinyl)-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid (38) was found to possess excellent in vitro potency and in vivo efficacy.
- Chu, Daniel T. W.,Fernandes, Prabhavathi B.,Claiborne, Akiyo K.,Gracey, Eugene H.,Pernet, Andre G.
-
p. 2364 - 2369
(2007/10/02)
-