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dc.contributor.authorComer, Eamonen_US
dc.contributor.authorBeaudoin, Jennifer A.en_US
dc.contributor.authorKato, Nobutakaen_US
dc.contributor.authorFitzgerald, Mark E.en_US
dc.contributor.authorHeidebrecht, Richard W.en_US
dc.contributor.authorLee, Maurice duPonten_US
dc.contributor.authorMasi, Danielaen_US
dc.contributor.authorMercier, Marionen_US
dc.contributor.authorMulrooney, Carolen_US
dc.contributor.authorMuncipinto, Giovannien_US
dc.contributor.authorRowley, Annen_US
dc.contributor.authorCrespo-Llado, Keilaen_US
dc.contributor.authorSerrano, Adelfa E.en_US
dc.contributor.authorLukens, Amanda K.en_US
dc.contributor.authorWiegand, Roger C.en_US
dc.contributor.authorWirth, Dyann F.en_US
dc.contributor.authorPalmer, Michelle A.en_US
dc.contributor.authorFoley, Michael A.en_US
dc.contributor.authorMunoz, Benitoen_US
dc.contributor.authorScherer, Christina A.en_US
dc.contributor.authorDuvall, Jeremy R.en_US
dc.contributor.authorSchreiber, Stuart L.en_US
dc.date.accessioned2015-10-01T14:55:13Z
dc.date.issued2014en_US
dc.identifier.citationComer, E., J. Beaudoin, N. Kato, M. E. Fitzgerald, R. Heidebrecht, M. d. Lee, D. Masi, et al. 2014. “Diversity-Oriented Synthesis-Facilitated Medicinal Chemistry: Toward the Development of Novel Antimalarial Agents.” Journal of Medicinal Chemistry 57 (20): 8496-8502. doi:10.1021/jm500994n. http://dx.doi.org/10.1021/jm500994n.en
dc.identifier.issn0022-2623en
dc.identifier.urihttp://nrs.harvard.edu/urn-3:HUL.InstRepos:22856842
dc.description.abstractHere, we describe medicinal chemistry that was accelerated by a diversity-oriented synthesis (DOS) pathway, and in vivo studies of our previously reported macrocyclic antimalarial agent that derived from the synthetic pathway. Structure–activity relationships that focused on both appendage and skeletal features yielded a nanomolar inhibitor of P. falciparum asexual blood-stage growth with improved solubility and microsomal stability and reduced hERG binding. The build/couple/pair (B/C/P) synthetic strategy, used in the preparation of the original screening library, facilitated medicinal chemistry optimization of the antimalarial lead.en
dc.language.isoen_USen
dc.publisherAmerican Chemical Societyen
dc.relation.isversionofdoi:10.1021/jm500994nen
dc.relation.hasversionhttp://www.ncbi.nlm.nih.gov/pmc/articles/PMC4207553/pdf/en
dash.licenseLAAen_US
dc.subjectArticleen
dc.titleDiversity-Oriented Synthesis-Facilitated Medicinal Chemistry: Toward the Development of Novel Antimalarial Agentsen
dc.typeJournal Articleen_US
dc.description.versionVersion of Recorden
dc.relation.journalJournal of Medicinal Chemistryen
dash.depositing.authorLukens, Amanda K.en_US
dc.date.available2015-10-01T14:55:13Z
dc.identifier.doi10.1021/jm500994n*
dash.authorsorderedfalse
dash.contributor.affiliatedLukens, Amanda
dash.contributor.affiliatedWirth, Dyann
dash.contributor.affiliatedSchreiber, Stuart


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