287952-66-3Relevant articles and documents
Pyrazolo[1,5-a]pyridine-3-carboxamide hybrids: Design, synthesis and evaluation of anti-tubercular activity
Lu, Xiaoyun,Tang, Jian,Cui, Shengyang,Wan, Baojie,Franzblauc, Scott G.,Zhang, Tianyu,Zhang, Xiantao,Ding, Ke
, p. 41 - 48 (2017)
A series of pyrazolo[1,5-a]pyridine-3-carboxamide hybrids were designed and evaluated as novel anti-tubercular agents. The representative hybrid 7 exhibited promising in?vitro activity against susceptive strain H37Rv and a panel of drug-resistant Mtb strains with MIC values of 0.006?μg/mL and ranged from 0.003 to 0.014?μg/mL, respectively. More importantly, the hybrid 7 also showed very low cytotoxicity, and could significantly reduce the mycobacterial burden in a mouse model infected with autoluminescent H37Ra strain, which may serve as a lead compound for further development of new anti-tubercular agents.
Method for preparing highly pure Delamanid intermediate
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Paragraph 0014; 0017; 0020; 0023; 0026; 0029; 0032; 0035, (2017/07/19)
The invention provides a method for preparing a highly pure delamanid intermediate. The intermediate is 4-[4-(trifluoromethoxy)phenoxyl]piperidine. Hydrogen chloride is dissolved in ethyl acetate in a Boc group removal step, and the dissolvability difference between the above product and impurities in ethylene acetate is used to carry out purification, so a column chromatography purifying method using tedious operation is avoided, the final product with high yield and high purity is also obtained, the production cost is reduced, and the method is suitable for industrial large-scale production.
(6,7-DIHYDRO-2-NITRO-5H-IMIDAZOL[2,1-B][1,3]OXAZIN-6-YL) AMIDE COMPOUNDS, PREPARATION METHODS AND USES THEREOF
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Paragraph 0050-0052, (2013/04/10)
(6,7-Dihydro-2-nitro-5H-imidazo [2,1-b][1,3]oxazin-6-yl)amide compounds of formula (I), and their pharmaceutically acceptable salts, preparation methods and pharmaceutical compositions thereof are disclosed, wherein m and R are defined as in the descripti
