287952-66-3Relevant academic research and scientific papers
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.
Oxalic Diamides and tert-Butoxide: Two Types of Ligands Enabling Practical Access to Alkyl Aryl Ethers via Cu-Catalyzed Coupling Reaction
Chen, Zhixiang,Jiang, Yongwen,Zhang, Li,Guo, Yinlong,Ma, Dawei
supporting information, p. 3541 - 3549 (2019/02/26)
A robust and practical protocol for preparing alkyl aryl ethers has been developed, which relies on using two types of ligands to promote Cu-catalyzed alkoxylation of (hetero)aryl halides. The reaction scope is very general for a variety of coupling partners, particularly for challenging secondary alcohols and (hetero)aryl chlorides. In case of coupling with aryl chlorides and bromides, two oxalic diamides serve as the powerful ligands. The tert-butoxide is first demonstrated as a ligand for Cu-catalyzed coupling reaction, leading to alkoxylation of aryl iodides complete at room temperature. Additionally, a number of carbohydrate derivatives are applicable for this coupling reaction, affording the corresponding carbohydrate-aryl ethers in 29-98% yields.
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.
Pyrazolo[1, 5-a]pyridine compound and use thereof
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Paragraph 0475; 0476; 0477; 0478; 0480, (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.
(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
METHOD OF PRODUCING AMINOPHENOL COMPOUNDS
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Page/Page column 44-46, (2010/02/14)
The present invention provides an industrially advantageous method of producing aminophenol compounds represented by the formula (1) by a simple and easy procedure at a high yield and a high purity. The present invention provides a method of producing an aminophenol compound represented by the formula (1): (wherein each of R1 and R2, which may be the same or different, is a hydrogen atom, a substituted or unsubstituted lower alkyl group or the like; R1 and R2, taken together with the adjacent nitrogen atom, may form a 5- or 6-membered heterocycle with or without other intervening heteroatoms; the heterocycle may be substituted by 1 to 3 substituents selected from the group consisting of a hydroxyl group, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted aryloxy group and the like; and the hydroxyl group in the formula (1) is substituted on the 2- or 4-position to the amino group on the phenyl ring), which comprises allowing a cyclohexanedione compound represented by the formula (2) to react with an amine compound represented by the formula (3) (wherein R1 and R2 are as defined above), under a neutral or basic condition.
Sulfamato hydroxamic acid metalloprotease inhibitor
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, (2008/06/13)
A sulfamato hydroxamic acid compound that, inter alia, inhibits matrix metalloprotease (mmp) activity is disclosed as are a process for preparing the same, intermediate compounds useful in those syntheses, and a treatment process that comprises administering a contemplated sulfamato hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.
Synthesis and activity of selective MMP inhibitors with an aryl backbone
E. Barta, Thomas,P. Becker, Daniel,J. Bedell, Louis,A. De Crescenzo, Gary,J. McDonald, Joseph,E. Munie, Grace,Rao, Shashi,Shieh, Huey-Sheng,Stegeman, Roderick,M. Stevens, Anna,I. Villamil, Clara
, p. 2815 - 2817 (2007/10/03)
A series of novel, MMP-1 sparing arylhydroxamate sulfonamides with activity against MMP-2 and -13 is described. (C) 2000 Elsevier Science Ltd.
