Source:http://linkedlifedata.com/resource/pubmed/id/19679378
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
11
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pubmed:dateCreated |
2009-10-9
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pubmed:abstractText |
As part of an ongoing effort to develop highly potent anti-tuberculosis agents, fourteen pentacyclo-undecane (PCU) tetra-amine compounds were synthesized and screened for their in vitro anti-mycobacterial activity against two TB strains, H37Rv and XDR 194 [an extensively drug-resistant strain of tuberculosis]. Using the broth macrodilution method, nitrofuranylamide based compounds (6a and 6b) showed almost similar activities against the H37Rv strain of Mycobacterium tuberculosis when compared with the control drug, ethambutol. N-Geranyl piperazine PCU (8a) and trans-trans farnesyl piperazine PCU (8b) were 3.2 and 3.7 times more potent than commercially available ethambutol. Both isoprenyl PCU tetra-amine derivatives and N-decyl piperazine PCU (9a) were highly active against the XDR 194 strain of tuberculosis with MICs in the range of 0.63-3.02 microM. Cytotoxicities (IC(50)) of isoprenyl based compounds (8a, 8b) and compound 9a were tested on a mammalian cell line [MDBK (Madin Darby bovine kidney epithelium)] with values of 30, 24 and 25 microM respectively.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
1768-3254
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pubmed:author |
pubmed-author:GovenderKarnishreeK,
pubmed-author:GovenderPatrickP,
pubmed-author:GovenderThavendranT,
pubmed-author:KrugerHendrik GHG,
pubmed-author:MaguireGlenn E MGE,
pubmed-author:MuthusamyKarenK,
pubmed-author:OnajoleOluseye KOK,
pubmed-author:PillayManormoneyM,
pubmed-author:VongB GBG,
pubmed-author:van HeldenPaul DPD
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pubmed:issnType |
Electronic
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pubmed:volume |
44
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4297-305
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pubmed:meshHeading |
pubmed-meshheading:19679378-Alkanes,
pubmed-meshheading:19679378-Animals,
pubmed-meshheading:19679378-Antitubercular Agents,
pubmed-meshheading:19679378-Cattle,
pubmed-meshheading:19679378-Cell Line,
pubmed-meshheading:19679378-Cell Survival,
pubmed-meshheading:19679378-Inhibitory Concentration 50,
pubmed-meshheading:19679378-Microbial Sensitivity Tests,
pubmed-meshheading:19679378-Molecular Structure,
pubmed-meshheading:19679378-Mycobacterium tuberculosis,
pubmed-meshheading:19679378-Prenylation
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pubmed:year |
2009
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pubmed:articleTitle |
Pentacyclo-undecane derived cyclic tetra-amines: synthesis and evaluation as potent anti-tuberculosis agents.
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pubmed:affiliation |
School of Chemistry, University of KwaZulu-Natal, Durban, South Africa.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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