Synthesis, Biological Evaluation And Mechanistic Studies Of Totarol Amino Alcohol Derivatives As Potential Antimalarial Agents.
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Date
2012Author
Tacon, C. M
Guantai, Eric
Smith, P. J
Chibale, K
Type
ArticleLanguage
enMetadata
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Herein we report on the semisynthesis and biological evaluation of b-amino alcohol derivatives of the natural product totarol and other simple aromatic systems. All beta-amino alcohol derivatives of totarol exhibited higher antiplasmodial activity than totarol [IC50: 11.69 microM (K1, chloroquine and multi-drug resistant strain), and 11.78 microM (D10, chloroquine sensitive strain)]—12e was the most active [IC50: 0.63 microM (K1), and 0.61 microM (D10)]. The phenyl and naphthyl b-amino alcohol derivatives were much less active than their corresponding totarol equivalents. The majority of the b-amino alcohol derivatives of totarol were more active against K1 than the D10 strains of Plasmodium falciparum, a trend similar to the inverse relationship observed with the established aryl-amino alcohol antimalarial mefloquine. Selected compounds were shown to affect erythrocyte morphology, inhibit erythrocyte invasion and trigger CQ accumulation.
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Http://profiles.uonbi.ac.ke/eguantai/publications/synthesis-biological-evaluation-and-mechanistic-studies-totarol-amino-alcoholhttp://erepository.uonbi.ac.ke:8080/xmlui/handle/123456789/29251
http://www.ncbi.nlm.nih.gov/pubmed/22196513
Citation
Synthesis, Biological Evaluation And Mechanistic Studies Of Totarol Amino Alcohol Derivatives As Potential Antimalarial Agents., Tacon, C., M. Dr. Guantai Eric, Smith P. J., And Chibale K. , Bioorg. Med. Chem., Volume 20, P.893–902, (2012)Publisher
University of Nairobi Department of Biochemistry
Collections
- Faculty of Health Sciences (FHS) [10377]