- ANTIVIRAL AND ANTIMICROBIAL COMPOUNDS
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Disclosed are guanidine and biguanidine derivatives which have anti-viral and antibacterial activity. Also disclosed are pharmaceutical compositions containing such compounds as an active ingredient, and anti-viral and anti-bacterial methods utilizing such compounds. Methods of treating infections using the guanidine and biguanidine derivatives are also disclosed.
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Paragraph 0128; 0129
(2014/03/25)
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- Process for the preparation of nicotinic acids
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The present invention relates to an improved process for the preparation of nicotinic acids represented by the following structural formula (I): STR1 which are prepared by reacting a nicotinic amide compound having the formula: STR2 under acidic conditions with a nitrite salt. In the process of the invention have the groups R1, R2, and R3, in the compounds are independently selected from the group consisting of hydrogen, and halogen atoms and R4 is selected from the group consisting of hydrogen, lower alkyl and aryl. The process provides the nicotinic acid compounds in improved yields.
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- Process for the synthesis of 2,6-dichloro-5-fluoronicotinic acid and 2,6-dichloro-5-fluoronicotinoyl chloride
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An improved process for the preparation of 2,6-dichloro-5-fluoronicotinoyl chloride is described where a 2,6-dihydroxy-5-fluoronicotinic acid ester is converted in one step using phosphorus oxychloride and a lithium reagent to 2,6-dichloro-5-fluoronicotinoyl chloride and subsequent basic hydrolysis affords 2,6-dichloro-5-fluoronicotinic acid.
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- Process for the preparation of substituted pyridines
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A process for the preparation of the substituted pyridines 2,6-dihydroxy-3-cyano-5--fluoropyridine, 2,6-dihydroxy-3-acetyl-5-fluoropyridine, 2,6-dichloro-3-cyano-5-fluoropyridine, 2,6-dichloro-5-fluoronicotinamide and 2,6-dichloro--5-fluoronicotinic acid.
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- Naphthyridine antianaerobic compounds
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The naphthyridine compounds having the formula: wherein R1 is hydrogen or a carboxy protecting group have unexpected and superior antianaerobic activity.
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- 6,7-disubstituted 1-cycloproply-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acids
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New 6,7-disubstituted-1-cyclopropyl-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxy lic acids of the formula (I) STR1 in which X represents halogen or nitro and A represents STR2 wherein R1, R2, R3 and R4 are defined hereinbelow are disclosed as well as their usefulness as antibacterial agents.
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- Antibacterial 7-(3-amino-1-pyrrolidinyl)-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid derivatives
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The present invention relates to a 1,8-naphthyridine derivative of the formula STR1 wherein R1, R2 and R3 are the same or different and each hydrogen or lower alkyl having 1 to 5 carbon atoms; and esters thereof and salts thereof and processes for preparation thereof. These compounds show excellent antibacterial activity and are useful antibacterial agents.
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- Synthesis and Structure-Activity Relationships of New Arylfluoronaphthyridine Antibacterial Agents
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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.
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p. 2364 - 2369
(2007/10/02)
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