N-Aroyl-3,5-bis(benzylidene)-4-piperidones: a novel class of antimycobacterial agents.

Das U; Das S; Bandy BStables JPDimmock JR

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N-Aroyl-3,5-bis(benzylidene)-4-piperidones: a novel class of antimycobacterial agents.

机译：N-Aroyl-3,5-bis(benzylidene)-4-piperidones: a novel class of antimycobacterial agents.

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摘要

A number of 3,5-bis(benzylidene)-4-piperidones 1 and some N-4-(2-aminoethoxy)phenylcarbonyl analogs 3-6 display excellent in vitro antimycobacterial properties. In particular, 1c and 6d are potent antimycobacterials which are well tolerated in mice and are identified as important lead molecules. The nature of both the benzylidene aryl rings and the terminal basic groups which affect the antimycobacterial potencies and the absence of neurotoxic side effects were identified. Several representative compounds stimulated respiration in mitochondria isolated from rat liver and this effect was not caused by the swelling of these organelles. Various guidelines for the creation of further related novel antimycobacterial agents are provided.

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《Bioorganic and medicinal chemistry》 |2008年第7期|3602-3607|共6页
作者
Das U; Das S; Bandy BStables JPDimmock JR;
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作者单位

College of Pharmacy and Nutrition, University of Saskatchewan, Saskatoon, Sask., Canada S7N 5C9.;

ost.saga-med.ac.jp;

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原文格式 PDF
正文语种英语
中图分类药学;生物化学;
关键词
Animals; Anti-Bacterial Agents; Mice; Molecular Structure; Mycobacterium tuberculosis; 动物; 小鼠; 分子结构; 分支杆菌; 结核; 哌啶酮类; 大鼠; 构效关系;

N-Aroyl-3,5-bis(benzylidene)-4-piperidones: a novel class of antimycobacterial agents.

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