- Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety
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A series of novel 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety were synthesized and evaluated for their biological activity. Our results reveal that compounds 9a-9c have considerable activity against both of MTB H37Rv ATCC 27294 (MICs: 3.81-7.13 μg/mL) and methicillin-sensitive Staphylococcus aureus strains (MICs: 0.008-0.5 μg/mL).
- Huang, Ju,Wang, Minghua,Wang, Bin,Wu, Zhaoyang,Liu, Mingliang,Feng, Lianshun,Zhang, Jun,Li, Xiaoning,Yang, Yang,Lu, Yu
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supporting information
p. 2262 - 2267
(2016/04/20)
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- 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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- 1,8-Naphthyridine-3-carboxamide derivatives with anticancer and anti-inflammatory activity
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A number of 1-propargyl-1,8-naphthyridine-3-carboxamide derivatives (15-35) have been synthesized and screened for their in vitro cytotoxicity and anti-inflammatory activity. Compounds 22, 31 and 34 have shown high cytotoxicity against a number of cancer cell lines, while compound 24 showed significant anti-inflammatory activity.
- Kumar, Vivek,Jaggi, Manu,Singh, Anu T.,Madaan, Alka,Sanna, Vinod,Singh, Pratibha,Sharma, Pramod K.,Irchhaiya, Raghuveer,Burman, Anand C.
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body text
p. 3356 - 3362
(2009/10/23)
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- Process for Preparing Beta-Ketoester Compounds
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The present invention relates to a process for preparing a beta-keto ester compound of formula (1), which is an intermediate for the synthesis of quinolone antibiotics. Particularly, the present invention is characterized by the reaction of an organo nitrile compound with a salt of mono-alkyl malonate in the presence of metal salt, and so the reaction is easy to control due to its endothermic nature, and is devoid of lachrymatory reagents with excellent reproducibility. Subsequent in situ hydrolysis in the presence of aqueous acid solution provided the compound of formula (1).
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Page/Page column 3
(2008/12/08)
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- A PROCESS FOR PREPARING BETA-KETOESTER COMPOUNDS
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The present invention relates to a process for preparing a beta-keto ester compound of formula (1) , which is an intermediate for the synthesis of quinolone antibiotics. Particularly, the present invention is characterized by the reaction of an organo nitrile compound with a salt of mono-alkyl malonate in the presence of metal salt, and so the reaction is easy to control due to its endothermic nature, and is devoid of lachrymatory reagents with excellent reproducibility. Subsequent in situ hydrolysis in the presence of aqueous acid solution provided the compound of formula (1).
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Page/Page column 7
(2010/11/27)
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- Discovery of the decarboxylative biaise reaction and its application to the efficient synthesis of ethyl 2,6-dichloro-5-fluoronicotinoylacetate
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An efficient synthesis of 2,6-dichloro-5-fluoronicotinoylacetate (1) has been accomplished in a single step using the unprecedented decarboxylative Biaise reaction of 3-cyano-2,6-dichloro-5-fluoropyridine (4) with potassium ethyl malonate in the presence of zinc chloride.
- Lee, Jae Hoon,Choi, Bo Seung,Chang, Jay Hyok,Kim, Sam Sik,Shin, Hyunik
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p. 1062 - 1064
(2012/12/30)
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- ANTIMICROBIAL QUINOLONES, THEIR COMPOSITIONS AND USES
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Compounds of the following formula (I) are effective antimicrobial agents.
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- A safe, economical method for the preparation of β-oxo esters
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A high yield, economical method for preparation of β-oxo esters has been developed involving the reaction of acid chlorides with potassium ethyl malonate using a magnesium chloride-triethylamine base system in either acetonitrile or ethyl acetate solvents. The method is suitable for the preparation of high purity β-oxo esters in the laboratory and also in large scale production.
- Clay,Collom,Karrick,Wemple
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p. 290 - 292
(2007/10/02)
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- Fluoronaphthyridines as Antibacterial Agents. 4. Synthesis and Structure-Activity Relationships of 5-Substituted-6-fluoro-7-(cycloalkylamino)-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic Acids
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A series of 5-substituted-6-fluoro-7-(cycloalkylamino)-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acids have been prepared and tested for their in vitro and in vivo antibacterial activities.The 5-methyl group gave better in vitro activity with the 1-cyclopropyl appendage, but poorer activity with the 1-tert-butyl moiety.With the 1-(2,4-difluorophenyl) substitution, the influence of the 7-cycloalkylamino group was determinant: a (3S)-3-aminopyrrolidine was shown to enhance greatly the in vitro and in vivo activity of the 5-methyl derivative.Compound 33 (BMY 43748) was selec ted as a promising candidate for an improved therapeutic agent.
- Bouzard, D.,Cesare, P. Di,Essiz, M.,Jacquet, J. P.,Ledoussal, B.,et al.
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p. 518 - 525
(2007/10/02)
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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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