dc.contributor.author | Tacon, C. M | |
dc.contributor.author | Guantai, Eric | |
dc.contributor.author | Smith, P. J | |
dc.contributor.author | Chibale, K | |
dc.date.accessioned | 2013-06-06T12:17:50Z | |
dc.date.available | 2013-06-06T12:17:50Z | |
dc.date.issued | 2012 | |
dc.identifier.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) | en |
dc.identifier.uri | Http://profiles.uonbi.ac.ke/eguantai/publications/synthesis-biological-evaluation-and-mechanistic-studies-totarol-amino-alcohol | |
dc.identifier.uri | http://erepository.uonbi.ac.ke:8080/xmlui/handle/123456789/29251 | |
dc.identifier.uri | http://www.ncbi.nlm.nih.gov/pubmed/22196513 | |
dc.description.abstract | 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. | en |
dc.language.iso | en | en |
dc.publisher | University of Nairobi | en |
dc.title | Synthesis, Biological Evaluation And Mechanistic Studies Of Totarol Amino Alcohol Derivatives As Potential Antimalarial Agents. | en |
dc.type | Article | en |
local.publisher | Department of Biochemistry | en |