38512-77-5Relevant academic research and scientific papers
A convenient and efficient approach to polyfluorosalicylic acids and their tuberculostatic activity
Shchegol'Kov, Evgeny V.,Shchur, Irina V.,Burgart, Yanina V.,Saloutin, Victor I.,Solodnikov, Sergey Yu.,Krasnykh, Olga P.,Kravchenko, Marionella A.
, p. 2455 - 2458 (2016)
We have developed the practical method for polyfluorosalicylic acids synthesis via nucleophilic ortho-mono-substitution of fluorine atom with magnesium methoxide. We have managed to increase the yield of targeted polyfluorosalicylic acids from good to quantitative. We have studied the tuberculostatic activity of polyfluorosalicylic acids. It has been found that minimum inhibitory concentration (MIC) of compounds is from 0.7 to 6.5 μg/mL depending on the structure.
New fluoroaryl-containing β,β′-dioxoesters in the synthesis of fluorobenzopyran-2(4)-ones
Kisil',Burgart,Saloutin
, p. 1455 - 1462 (2007/10/03)
For the first time were obtained ethyl 2-(2-methoxy-3,4,5,6-tetrafluorobenzoyl)-3-oxobutanoate and ethyl 2-pentafluorobenzoyl-3-oxobutanoate and their copper chelates. The compounds were prepared by acylation of ethyl acetoacetate with 2-methoxy-3,4,5,6-t
The selective ortho-methoxylation of pentafluorobenzoic acid - A new way to tetrafluorosalicylic acid and its derivatives
Bazyl',Kisil',Burgart,Saloutin,Chupakhin
, p. 11 - 13 (2007/10/03)
A simple and efficient preparation of tetrafluorosalicylic acid has been developed which involves a selective substitution of fluorine in pentafluorobenzoic acid with methoxyl group by magnesium methoxide. The synthesis of 2,6-dimethoxy-3,4,5-trifluorobenzoic acid, 4,5,6-trifluororesorcinol and its dimethoxy ether is described.
Synthesis and biological activity of 5-amino- and 5-hydroxyquinolones, and the overwhelming influence of the remote N1-substituent in determining the structure-activity relationship
Domagala,Bridges,Culbertson,Gambino,Hagen,Karrick,Porter,Sanchez,Sesnie,Spense,Szotek,Wemple
, p. 1142 - 1154 (2007/10/02)
A series of 5-amino- and 5-hydroxyquinolone antibacterials substituted at C7 with a select group of common piperazinyl and 3-aminopyrrolidinyl side chains was prepared. These 5-substituted derivatives were compared to the analogous 5-hydrogen compounds for antiinfective activity by using DNA gyrase inhibition, minimum inhibitory concentrations against a variety of bacteria, and in vivo efficacy in the mouse infection model. The influence on the structure-activity relationships of varied substituents at C8 (H, F, Cl) and N1 (ethyl, cyclopropyl, difluorophenyl) was also studied. The results showed that several of the structure-activity conclusions regarding side-chain bulk at C7, the effect of halogen at C8, and the effect of the C5-amino group were greatly influenced by the choice of the N1-substituent. Several outstanding broad spectrum quinolones were identified in this work. In particular, the spectrum and potency of the 7-piperazinyl quinolones could be greatly enhanced by the judicious choice of C5-, C8-, and N1-substitutents.
4-oxo-1,4-dihydroquinoline-3-carboxylic acid derivative as antibacterial agents
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, (2008/06/13)
Novel naphthyridine-, quinoline- and benzoxazinecarboxylic acids as antibacterial agents are described as well as methods for their manufacture, formulation, and use in treating bacterial infections including the description of certain novel intermediates used in the manufacture of the antibacterial agents.
7-[[3-(aminomethyl)-3-alkyl]-1-pyrrolidinyl]-quinoline-carboxylic acids
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, (2008/06/13)
Novel, orally active antibacterial agents are described and characterized as 7-[[3-(aminomethyl)-3-alkyl]-1-pyrrolidinyl]-6-fluoro-1,4-dihydro-4-oxo-3-quinoline carboxylic acids or corresponding 1,8-naphthyridine derivatives as well as methods for their m
