75822-32-1Relevant academic research and scientific papers
Strategic synthesis and in vitro antimicrobial evaluation of novel difluoromethylated 1-(1, 3-diphenyl-1H-pyrazol-4-yl)-3, 3-difluoro-1, 3-dihydro-indol-2-ones
Chundawat, Tejpal Singh,Kumari, Poonam,Sharma, Nutan,Bhagat, Sunita
, p. 2335 - 2348 (2016)
A strategic synthesis of 1-(1,3-diphenyl-1H-pyrazol-4-yl)-3,3-difluoro-1,3-dihydro-indol-2-ones has been achieved by the reaction of indole-2,3-dione (isatin) and substituted bromoacetyl benzene followed by cyclization reaction and evaluated for in vitro antibacterial and antifungal activities. Direct fluorination using diethylaminosulfur trifluoride as a nucleophilic fluorinating reagent was carried out in the present paper. Undoubtedly this methodology gives a facile and straightforward pathway to construct 1-(1,3-diphenyl-1H-pyrazol-4-yl)-3,3-difluoro-1,3-dihydro-indol-2-ones in good yields. The structure of new fluorinated 1-(1,3-diphenyl-1H-pyrazol-4-yl)-3,3-difluoro-1,3-dihydro-indol-2-ones was characterized based on 1H, 13C, and 19F nuclear magnetic resonance spectroscopy and mass spectrometry data. Structure of target compound was confirmed by Nuclear Overhauser Effect Spectroscopy spectra. Some of the synthesized compounds showed good antimicrobial activities against bacteria and fungi.
EIS INHIBITORS
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Paragraph 0019; 0125, (2018/06/30)
Compounds and compositions are disclosed, which are useful as inhibitors of acetyltransferase Eis, a mediator of kanamycin resistance in Mycobacterium tuberculosis.
Discovery and Optimization of Two Eis Inhibitor Families as Kanamycin Adjuvants against Drug-Resistant M. tuberculosis
Garzan, Atefeh,Willby, Melisa J.,Green, Keith D.,Tsodikov, Oleg V.,Posey, James E.,Garneau-Tsodikova, Sylvie
supporting information, p. 1219 - 1221 (2016/12/18)
Drug-resistant tuberculosis (TB) is a global threat and innovative approaches such as using adjuvants of anti-TB therapeutics are required to combat it. High-throughput screening yielded two lead scaffolds of inhibitors of Mycobacterium tuberculosis (Mtb)
Design, synthesis, computational and biological evaluation of new anxiolytics
Geronikaki, Athina,Babaev, Eugeni,Dearden, John,Dehaen, Wim,Filimonov, Dmitrii,Galaeva, Irina,Krajneva, Valentina,Lagunin, Alexey,MacAev, Fliur,Molodavkin, Guenadiy,Poroikov, Vladimir,Pogrebnoi, Serghei,Saloutin, Victor,Stepanchikova, Alla,Stingaci, Eugenia,Tkach, Natalia,Vlad, Liudmila,Voronina, Tatiana
, p. 6559 - 6568 (2007/10/03)
New anxiolytics have been discovered by prediction of biological activity with computer programs pass and derek for a heterogeneous set of 5494 highly chemically diverse heterocyclic compounds (thiazoles, pyrazoles, isatins, a-fused imidazoles and others)
