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Synthesis and antiprotozoal activity of dicationic 2,6-diphenylpyrazines and aza-analogues

Hu, Laixing and Patel, Alpa and Bondada, Lavanya and Yang, Sihyung and Wang, Michael Zhuo and Munde, Manoj and Wilson, W. David and Wenzler, Tanja and Brun, Reto and Boykin, David W.. (2013) Synthesis and antiprotozoal activity of dicationic 2,6-diphenylpyrazines and aza-analogues. Bioorganic & medicinal chemistry, 21 (21). pp. 6732-6741.

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Official URL: http://edoc.unibas.ch/dok/A6194551

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Abstract

Dicationic 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. (4.8-37nM) and P. f. (10-52nM). 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.
Faculties and Departments:09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH)
09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) > Department of Medical Parasitology and Infection Biology > Parasite Chemotherapy (Mäser)
UniBasel Contributors:Wenzler, Tanja and Brun, Reto
Item Type:Article, refereed
Article Subtype:Research Article
Bibsysno:Link to catalogue
Publisher:Pergamon
ISSN:0968-0896
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:13 Sep 2018 14:44
Deposited On:06 Dec 2013 09:35

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