354525-36-3Relevant academic research and scientific papers
Discovery of (3-Benzyl-5-hydroxyphenyl)carbamates as new antitubercular agents with potent in vitro and in vivo efficacy
Cheng, Ya-Juan,Liu, Zhi-Yong,Liang, Hua-Ju,Fang, Cui-Ting,Zhang, Niu-Niu,Zhang, Tian-Yu,Yan, Ming
, (2019/06/07)
A series of 3-amino-5-benzylphenol derivatives were designed and synthesized. Among them, (3-benzyl-5-hydroxyphenyl)carbamates were found to exert good inhibitory activity against M. tuberculosis H37Ra, H37Rv and clinically isolated multidrug-resistant M. tuberculosis strains (MIC = 0.625-6.25 μg/mL). The privileged compounds 3i and 3l showed moderate cytotoxicity against cell line A549. Compound 3l also exhibited potent in vivo inhibitory activity on a mouse infection model via the oral administration. The results demonstrated 3-hydroxyphenylcarbamates as a class of new antitubercular agents with good potential.
Design, synthesis, and biological evaluation of m-amidophenol derivatives as a new class of antitubercular agents
Zhang, Niu-niu,Liu, Zhi-yong,Liang, Jie,Tang, Yun-xiang,Qian, Lu,Gao, Ya-min,Zhang, Tian-Yu,Zhang, Tian-yu,Yan, Ming
supporting information, p. 1293 - 1304 (2018/08/28)
A series of m-amidophenol derivatives (6a-6l, 7a-7q, 9a, 9b, 12a-12c, 14 and 15) were designed and synthesized. Their antitubercular activities were evaluated in vitro against M. tuberculosis strains H37Ra and H37Rv and clinically isolated multidrug-resistant M. tuberculosis strains. Ten compounds displayed minimal inhibitory concentrations (MICs) against M. tuberculosis H37Ra below 2.5 μg mL?1 and 6g was the most active compound (MIC = 0.625 μg mL?1). Compounds 6g and 7a also showed potent inhibitory activity against M. tuberculosis H37Rv (MIC = 0.39 μg mL?1) and several clinically isolated multidrug-resistant M. tuberculosis strains (MIC = 0.39-3.125 μg mL?1). The compounds did not show inhibitory activity against normal Gram-positive and Gram-negative bacteria. They exhibited low cytotoxicity against HepG2 and RAW264.7 cell lines. The results demonstrated m-amidophenol as an attractive scaffold for the development of new antitubercular agents.
M-di-substituted phenol compound as well as preparation method thereof and application of tubercle bacillus resistance
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Paragraph 0048; 0080, (2018/05/16)
The invention provides an m-di-substituted phenol compound with a general formula (I) as well as a preparation method and application thereof. The m-di-substituted phenol compound provided by the invention has a novel tubercle bacillus resistance drug parent nucleus structure and excellent tubercle bacillus resistance activity and especially has very strong inhibition activity on a drug-resistantvariant tubercle bacillus strain. The invention further provides the preparation method of the m-di-substituted phenol compound; the preparation method has the advantages that raw materials are cheapand easy to obtain, a high-toxicity and high-pollution reagent are not needed, reaction steps are simple and industrialized production can be realized; the m-di-substituted phenol compound has a goodmedicinal prospect.
PHENYL-UREA AND PHENYL-CARBAMATE DERIVATIVES AS INHIBITORS OF PROTEIN AGGREGATION
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Paragraph 0094, (2013/10/21)
The present invention relates to certain phenyl-urea and phenyl-carbamate derivatives, pharmaceutical compositions containing them, and methods of using them, including methods for preventing, reversing, slowing, or inhibiting protein aggregation, and methods of treating diseases that are associated with protein aggregation, including neurodegenerative diseases such as Parkinson's disease, Alzheimer's disease, Lewy body disease, and multiple system atrophy.
(3-HYDROXY-4-AMINO-BUTAN-2-YL) -3- (2-THIAZOL-2-YL-PYRROLIDINE-1-CARBONYL) BENZAMIDE DERIVATIVES AND RELATED COMPOUNDS AS BETA-SECRETASE INHIBITORS FOR TREATING
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Page/Page column 100, (2009/05/29)
The present invention provides novel beta-secretase inhibitors and methods for their use, including methods of treating of Alzheimer's disease. (Formula)
QUINAZOLINE DERIVATIVES
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Page/Page column 144, (2008/06/13)
The invention concerns quinazoline derivatives of Formula (I) or a pharmaceutically-acceptable salt, solvate or pro-drug thereof, wherein each of X1, p, R1, q, R2, R3, R4, R5, Ring A, r and R6 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders or in the treatment of disease states associated with angiogenesis and/or vascular permeability.
Synthesis and structure-activity relationships of 3-aminobenzophenones as antimitotic agents
Liou, Jing-Ping,Chang, Jang-Yang,Chang, Chun-Wei,Chang, Chi-Yen,Mahindroo, Neeraj,Kuo, Fu-Ming,Hsieh, Hsing-Pang
, p. 2897 - 2905 (2007/10/03)
A new series of 3-aminobenzophenone compounds as potent inhibitors of tubulin polymerization was discovered based on the mimic of the aminocombretastatin molecular skeleton. Lead compounds 5 and 11, with alkoxy groups at the C-4 position of B-ring, were p
