472964-25-3Relevant articles and documents
Pyrazolo[1, 5-a]pyridine compound and use thereof
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Paragraph 0454; 0455; 0456; 0457; 0458, (2016/10/08)
The invention discloses a pyrazolo[1, 5-a]pyridine compound with the structure characteristic shown in the formula (I) or its pharmaceutically acceptable salt, stereoisomer or prodrug molecule and a use thereof. The compound has good in-vitro anti-tubercle bacillus activity, has the minimal inhibitory concentration (MIC) less than 0.1 micrograms per milliliter and partial MIC of 0.01 micrograms per milliliter and has strong inhibition effects on a clinically sorted multi-drug-resistant tuberculosis (MDR-TB) strain. In an in-vivo experiment, at a dosage of 20mg/kg/d, the pyrazolo[1, 5-a]pyridine compound can effectively eliminate H37Ra infection in a mouse and is a novel anti-tuberculosis compound.
Substituted N -(biphenyl-4′-yl)methyl (R)-2-acetamido-3- methoxypropionamides: Potent anticonvulsants that affect frequency (Use) dependence and slow inactivation of sodium channels
Lee, Hyosung,Park, Ki Duk,Torregrosa, Robert,Yang, Xiao-Fang,Dustrude, Erik T.,Wang, Yuying,Wilson, Sarah M.,Barbosa, Cindy,Xiao, Yucheng,Cummins, Theodore R.,Khanna, Rajesh,Kohn, Harold
supporting information, p. 6165 - 6182 (2014/08/18)
We prepared 13 derivatives of N-(biphenyl-4′-yl)methyl (R)-2-acetamido-3-methoxypropionamide that differed in type and placement of a R-substituent in the terminal aryl unit. We demonstrated that the R-substituent impacted the compound's whole animal and cellular pharmacological activities. In rodents, select compounds exhibited excellent anticonvulsant activities and protective indices (PI = TD50/ED50) that compared favorably with clinical antiseizure drugs. Compounds with a polar, aprotic R-substituent potently promoted Na+ channel slow inactivation and displayed frequency (use) inhibition of Na+ currents at low micromolar concentrations. The possible advantage of affecting these two pathways to decrease neurological hyperexcitability is discussed.
PYRAZOLECARBOXAMIDE DERIVATIVE, INTERMEDIATE THEREFOR, AND PEST CONTROL AGENT CONTAINING THE SAME AS ACTIVE INGREDIENT
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Page 25, (2008/06/13)
The present invention provides novel compounds with fungicidal and bactericidal activity as well as insecticidal and miticidal activity, which are useful for controlling hazardous biological organisms and belong to pyrazolecarboxamides represented by the