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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
biochemistry, genetics and molecular biology
Structure-activity relationship studies of orally active antimalarial 3,5-substituted 2-aminopyridines
Journal of Medicinal Chemistry, Volume 55, No. 24, Year 2012
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Description
In an effort to address potential cardiotoxicity liabilities identified with earlier frontrunner compounds, a number of new 3,5-diaryl-2-aminopyridine derivatives were synthesized. Several compounds exhibited potent antiplasmodial activity against both the multidrug resistant (K1) and sensitive (NF54) strains in the low nanomolar range. Some compounds displayed a significant reduction in potency in the hERG channel inhibition assay compared to previously reported frontrunner analogues. Several of these new analogues demonstrated promising in vivo efficacy in the Plasmodium berghei mouse model and will be further evaluated as potential clinical candidates. The SAR for in vitro antiplasmodial and hERG activity was delineated. © 2012 American Chemical Society.
Authors & Co-Authors
Gonzàlez Cabrera, Diego
South Africa, Cape Town
University of Cape Town
Douelle, Frederic
South Africa, Cape Town
University of Cape Town
Younis, Yassir
South Africa, Cape Town
University of Cape Town
Feng, Tzu Shean
South Africa, Cape Town
University of Cape Town
Le Manach, Claire
South Africa, Cape Town
University of Cape Town
Nchinda, Aloysius T.
South Africa, Cape Town
University of Cape Town
Street, Leslie J.
South Africa, Cape Town
University of Cape Town
Scheurer, Christian
Switzerland, Allschwil
Swiss Tropical and Public Health Institute Swiss Tph
Switzerland, Basel
Universitat Basel
Kamber, Jolanda
Switzerland, Allschwil
Swiss Tropical and Public Health Institute Swiss Tph
Switzerland, Basel
Universitat Basel
White, Karen L.
Australia, Melbourne
Monash University, Centre for Drug Candidate Optimisation
Montagnat, Oliver D.
Australia, Melbourne
Monash University, Centre for Drug Candidate Optimisation
Ryan, Eileen
Australia, Melbourne
Monash University, Centre for Drug Candidate Optimisation
Katneni, Kasiram
Australia, Melbourne
Monash University, Centre for Drug Candidate Optimisation
Zabiulla, K. Mohammed
India, Bengaluru
Syngene International Ltd
Joseph, Jayan T.
India, Bengaluru
Syngene International Ltd
Bashyam, Sridevi
India, Bengaluru
Syngene International Ltd
Waterson, David
Switzerland, Geneve
Icc
Witty, Michael J.
Switzerland, Geneve
Icc
Charman, Susan A.
Australia, Melbourne
Monash University, Centre for Drug Candidate Optimisation
Wittlin, Sergio
Switzerland, Allschwil
Swiss Tropical and Public Health Institute Swiss Tph
Switzerland, Basel
Universitat Basel
Chibale, Kelly
South Africa, Cape Town
University of Cape Town
Statistics
Citations: 40
Authors: 21
Affiliations: 6
Identifiers
Doi:
10.1021/jm301476b
ISSN:
00222623
e-ISSN:
15204804