951906-87-9Relevant academic research and scientific papers
Benzoquinone derivative, pharmaceutical composition, and applications thereof
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Paragraph 0249-0251; 0253; 0291-0292, (2019/11/29)
The invention discloses a benzoquinone derivative, a pharmaceutical composition, and applications thereof. According to the invention, the benzoquinone derivative (I), and the stereoisomer or the pharmaceutically acceptable salt thereof possess a structure disclosed in the invention. The benzoquinone derivative possesses excellent inhibition effect on STAT3 level both in vivo and in vitro, and further, the benzoquinone derivative is capable of inhibiting balling capacity of cancer cells.
TROPANE COMPOUNDS
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Page/Page column 370-371, (2009/05/30)
A compound according to Formula I or II: (I) or (II) wherein R1, R1b, R2, L1, and L2 and L2b are as defined in the specification, pharmaceutical compositions thereof, and methods of use thereof.
Synthesis and evaluation of cyclic secondary amine substituted phenyl and benzyl nitrofuranyl amides as novel antituberculosis agents
Tangallapally, Rajendra P.,Yendapally, Raghunandan,Lee, Robin E.,Lenaerts, Anne J. M.,Lee, Richard E.
, p. 8261 - 8269 (2007/10/03)
In an ongoing effort to develop new and potent antituberculosis agents, a second-generation series of nitrofuranyl amides was synthesized on the basis of the lead compound 5-nitrofuran-2-carboxylic acid 3,4-dimethoxybenzylamide. The primary design consideration was to improve the solubility and consequently the bioavailability of the series by the addition of hydrophilic rings to the benzyl and phenyl B ring core. The synthesis of 27 cyclic, secondary amine substituted phenyl and benzyl nitrofuranyl amides is described and their activity against Mycobacterium tuberculosis reported. The series showed a strong structure-activity relationship as the benzyl nitrofuranyl amides were significantly more active than similarly substituted phenyl nitrofuranyl amides. Para-substituted benzyl piperazines showed the most antituberculosis activity. Compounds in the series were subsequently selected for bioavailability and in vivo testing. This study led to the successful discovery of novel compounds with increased antituberculosis activity in vitro and a better understanding of the requisite pharmacological properties to advance this class.
