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Structure-activity relationship studies of orally active antimalarial 3,5-substituted 2-aminopyridines

González, Cabrera and Douelle, F. and Younis, Y. E. and Feng, T. S. and Lemanach, C. and Nchinda, A. T. and Street, L. J. and Scheurer, C. and Kamber, J. and White, K. L. and Montagnat, O. D. and Ryan, E. and Katneni, K. and Zabiulla, K. M. and Joseph, J. T. and Bashyam, S. and Waterson, D. and Witty, M. J. and Charman, S. A. and Wittlin, S. and Chibale, K.. (2012) Structure-activity relationship studies of orally active antimalarial 3,5-substituted 2-aminopyridines. Journal of medicinal chemistry, 55 (24). pp. 11022-11030.

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Official URL: http://edoc.unibas.ch/dok/A6094391

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Abstract

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 P. berghei mouse model and will be further evaluated as potential clinical candidates. The SAR for in vitro antiplasmodial and hERG activity was delineated
Faculties and Departments:09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) > Department of Medical Parasitology and Infection Biology (MPI) > Parasite Chemotherapy (Mäser)
UniBasel Contributors:Wittlin, Sergio
Item Type:Article, refereed
Article Subtype:Research Article
Bibsysno:Link to catalogue
Publisher:American Chemical Society
ISSN:0022-2623
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:20 Oct 2017 06:39
Deposited On:16 Aug 2013 07:30

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