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Synthesis and Antiprotozoal Activity of Dicationic 2, 6-Diphenylpyrazines and Aza-Analogues
Hu, Laixing Patel, Alpa Bondada, Lavanya Yang, Sihyung Wang, Michael Zhuo Munde, Manoj Wilson, W. David Wenzler, Tanja Brun, Reto Boykin, David W.
Hu, Laixing
Patel, Alpa
Bondada, Lavanya
Yang, Sihyung
Wang, Michael Zhuo
Munde, Manoj
Wilson, W. David
Wenzler, Tanja
Brun, Reto
Boykin, David W.
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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 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.
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2013-08-13
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Elsevier
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Hu, 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.2013.08.006