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Synthesis and Antiprotozoal Activity of Dicationic 2, 6-Diphenylpyrazines and Aza-Analogues

dc.contributor.authorHu, Laixing
dc.contributor.authorPatel, Alpa
dc.contributor.authorBondada, Lavanya
dc.contributor.authorYang, Sihyung
dc.contributor.authorWang, Michael Zhuo
dc.contributor.authorMunde, Manoj
dc.contributor.authorWilson, W. David
dc.contributor.authorWenzler, Tanja
dc.contributor.authorBrun, Reto
dc.contributor.authorBoykin, David W.
dc.date.accessioned2017-05-04T19:54:32Z
dc.date.available2017-05-04T19:54:32Z
dc.date.issued2013-08-13
dc.identifier.citationHu, L., Patel, A., Bondada, L., Yang, S., Wang, M. Z., Munde, M., … Boykin, D. W. (2013). Synthesis and Antiprotozoal Activity of Dicationic 2, 6-Diphenylpyrazines and Aza-Analogues. Bioorganic & Medicinal Chemistry, 21(21), 10.1016/j.bmc.2013.08.006. http://doi.org/10.1016/j.bmc.2013.08.006en_US
dc.identifier.urihttp://hdl.handle.net/1808/23898
dc.description.abstractDicationic 2,6-diphenylpyrazines, aza-analogues and prodrugs were synthesized; evaluated for DNA affinity, activity against Trypanosoma brucei rhodesiense (T. b. r.) and Plasmodium falciparum (P. f.) in vitro, efficacy in T. b. r. STIB900 acute and T. b. brucei GVR35 CNS mouse models. Most diamidines gave poly(dA-dT)2 ΔTm values greater than pentamidine, IC50 values: T. b. r. (4.8 to 37 nM) and P. f. (10 to 52 nM). Most diamidines and prodrugs gave cures for STIB900 model (11, 19a and 24b 4/4 cures); 12 3/4 cures for GVR35 model. Metabolic stability half-life values for O-methylamidoxime prodrugs did not correlate with STIB900 results.en_US
dc.publisherElsevieren_US
dc.rightsThis article is made available under an Attribution-NonCommercial-NoDerivs 3.0 United States (CC BY-NC-ND 3.0 US) License.en_US
dc.rights.urihttps://creativecommons.org/licenses/by-nc-nd/3.0/us/en_US
dc.titleSynthesis and Antiprotozoal Activity of Dicationic 2, 6-Diphenylpyrazines and Aza-Analoguesen_US
dc.typeArticleen_US
kusw.kuauthorYang, Sihyung
kusw.kuauthorWang, Michael Zhuo
kusw.kudepartmentPharmaceutical Chemistryen_US
dc.identifier.doi10.1016/j.bmc.2013.08.006en_US
dc.identifier.orcidhttps://orcid.org/0000-0003-1751-4975
kusw.oaversionScholarly/refereed, author accepted manuscripten_US
kusw.oapolicyThis item meets KU Open Access policy criteria.en_US
dc.identifier.pmidPMC3846175en_US
dc.rights.accessrightsopenAccess


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This article is made available under an Attribution-NonCommercial-NoDerivs 3.0 United States (CC BY-NC-ND 3.0 US) License.
Except where otherwise noted, this item's license is described as: This article is made available under an Attribution-NonCommercial-NoDerivs 3.0 United States (CC BY-NC-ND 3.0 US) License.