Abstract:
: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.
journal_name
Bioorg Med Chemjournal_title
Bioorganic & medicinal chemistryauthors
Das U,Das S,Bandy B,Stables JP,Dimmock JRdoi
10.1016/j.bmc.2008.02.009subject
Has Abstractpub_date
2008-04-01 00:00:00pages
3602-7issue
7eissn
0968-0896issn
1464-3391pii
S0968-0896(08)00115-6journal_volume
16pub_type
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