- Design, synthesis and antitubercular activity of 4-alkoxy-triazoloquinolones able to inhibit the M. tuberculosis DNA gyrase
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A number of new F-triazolequinolones (FTQs) and alkoxy-triazolequinolones (ATQs) were designed, synthesized and evaluated for their activity against Mycobacterium tuberculosis H37Rv. Five out of 21 compounds exhibited interesting minimum inhibitory concen
- Carta, Antonio,Bua, Alessandra,Corona, Paola,Piras, Sandra,Briguglio, Irene,Molicotti, Paola,Zanetti, Stefania,Laurini, Erik,Aulic, Suzana,Fermeglia, Maurizio,Pricl, Sabrina
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- Preparation method of 2 - fluorine -6 - nitroaniline
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The invention discloses a preparation method of 2 -fluoro -6 - nitroaniline, and the specific steps of the preparation method are as follows: (1) taking M-fluoronitrobenzene as a starting raw material, reacting with hexachloroethane under the catalysis condition of tert-butyl alcohol lithium III, and reacting with hexachloroethane. (2) Compound III amine is hydrolyzed to give compound I. That is, the 2 - fluorine -6 - nitroaniline. To the invention, a large amount of easily toxic and easily-produced reagents are avoided in the full synthetic route process taking the meta-fluoronitrobenzene as a starting raw material, and the raw materials are low in price.
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Paragraph 0019-0020; 0022-0026; 0028-0030; 0032
(2021/09/08)
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- Synthesis and Evaluation of Novel 7- and 8-Aminophenoxazinones for the Detection of β-Alanine Aminopeptidase Activity and the Reliable Identification of Pseudomonas aeruginosa in Clinical Samples
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A series of novel 8-aminophenoxazin-3-one and 7-aminophenoxazin-3-one chromogens and their corresponding β-alanine derivatives were synthesized and evaluated for their ability to detect β-alanyl aminopeptidase activity in bacteria known to hydrolyze β-ala
- Bedernjak, Alexandre F.,Zaytsev, Andrey V.,Babolat, Michèle,Cellier, Marie,James, Arthur L.,Orenga, Sylvain,Perry, John D.,Groundwater, Paul W.,Anderson, Rosaleen J.
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supporting information
p. 4476 - 4487
(2016/06/13)
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- Fluorinated Fe(III) salophene complexes: Optimization of tumor cell specific activity and utilization of fluorine labeling for in vitro analysis
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Fluorine-substituted iron(III) salophene complexes (salophene = N,N'-bis(salicylidene)-1,2-phenylenediamine) were synthesized and evaluated for biological activity. All complexes showed growth inhibitory effects with IC50 values ranging from 0.
- Würtenberger, Irene,Follia, Valeria,Lerch, Fanni,Cwikla, Christiane,Fahrner, Nathalie,Kalchschmidt, Christina,Fl?gel, Brigitte,Kircher, Brigitte,Gust, Ronald
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supporting information
p. 588 - 597
(2015/01/30)
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- New fluorogenic benzothiadiazole and benzoselenadiazole reagents to yield environment-sensitive fluorophores via a reaction with amines
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We introduce 7-fluoro-4-N,N-dimethylaminosulfonyl-2,1,3-benzothiadiazole and 7-fluoro-4-N,N-dimethylaminosulfonyl-2,1,3-benzoselenadiazole as new fluorogenic reagents for amines. These reagents are nonfluorescent themselves and can easily react with nonfl
- Kawamoto, Kyoko,Uchiyama, Seiichi
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supporting information
p. 1451 - 1452
(2013/01/16)
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- A convenient copper-catalyzed direct animation of nitroarenes with 9-alkylhydroxylamines
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O-Alkylhydroxylamines, particularly O-methylhydroxylamine, aminate nitroarenes in the presence of a strong base and a copper catalyst to give aminonitroarenes in good yields, ortho- or para-Animation with respect to the nitro group takes place, and in some cases the ortho-aminated product is preferentially obtained. With 3-substituted nitrobenzenes where the substituent has a lone pair of electrons, preferential amination occurs at the 2-position to give the sterically most congested 3c-f, 14 and 22g.
- Seko, Shinzo,Miyake, Kunihito,Kavvamura, Norio
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p. 1437 - 1444
(2007/10/03)
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- HETEROCYCLIC SYSTEMS CONTAINING BRIDGEHEAD NITROGEN ATOM: PART LXVI. STUDIES OF ORIENTATION OF CYCLIZATION IN THE SYNTHESIS OF 8-FLUOROTHIAZOLOBENZIMIDAZOL-3(2H)-ONE
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2-Fluoro-6-nitroaniline, obtained by nitration of 2-fluoroacetanilide, on reduction with Raney nickel and hydrazine hydrate followed by treatment of the resulting diamine with carbon disulphide in situ gives 4-fluorobenzimidazolyl-2-thione.This thione on condensation with chloroacetic acid gives 4-fluorobenzimidazol-2-thiolacetic acid which on cyclization with a mixture of acetic anhydride and pyridine furnished 8-fluorothiazolobenzimidazol-3(2H)-one as revealed by 1H-NMR spectroscopy.The condensation of 4-fluorobenzimidazolyl-2-thione with 1,2-dibromoethane yields 2,3-dihydro-8-fluorothiazolobenzimidazole and sym-bis-(4-fluorobenzimidazol-2-ylmercapto)ethane.
- Dahiya, Rajinder,Pujari, H. K.
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p. 245 - 256
(2007/10/02)
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