Antileishmanial Activity of a Series of N2,N4-Disubstituted Quinazoline-2,4-diamines
- Kurt S. Van Horn, Xiaohua Zhu, Roman Manetsch
- ChemistryJournal of Medicinal Chemistry
- 29 May 2014
A series of N2,N4-disubstituted quinazoline-2,4-diamines has been synthesized and tested against Leishmania donovani and L. amazonensis intracellular amastigotes. A structure–activity and…
Pharmacokinetic Comparison To Determine the Mechanisms Underlying the Differential Efficacies of Cationic Diamidines against First- and Second-Stage Human African Trypanosomiasis
- Sihyung Yang, T. Wenzler, Michael Zhuo Wang
- Biology, MedicineAntimicrobial Agents and Chemotherapy
- 5 May 2014
The results showed that DB829, an azadiamidine, had the highest systemic exposure and brain-to-plasma ratio, whereas pentamidine and DB75 had the lowest, and none of these diamidines was a P-gp substrate, and the binding of each to plasma proteins and brain differed greatly.
Pharmacokinetics, Trypanosoma brucei gambiense Efficacy, and Time of Drug Action of DB829, a Preclinical Candidate for Treatment of Second-Stage Human African Trypanosomiasis
- T. Wenzler, Sihyung Yang, O. Braissant, D. Boykin, R. Brun, Michael Zhuo Wang
- Biology, MedicineAntimicrobial Agents and Chemotherapy
- 19 August 2013
Isothermal microcalorimetry and in vivo time-to-kill studies revealed that DB829 is a slower-acting trypanocidal compound than pentamidine, which is a promising preclinical candidate for the treatment of first- and second-stage HAT caused by both Trypanosoma brucei subspecies.
Antileishmanial Efficacy and Pharmacokinetics of DB766-Azole Combinations
- April C. Joice, Sihyung Yang, K. Werbovetz
- Biology, MedicineAntimicrobial Agents and Chemotherapy
- 23 October 2017
The data indicate that the efficacy of DB766-posaconazole and DB7 66-ketoconazole combinations in vivo is influenced in part by the pharmacokinetics of the combination, and that the former combination deserves further consideration in developing new treatment strategies against visceral leishmaniasis.
Synthesis of novel amide and urea derivatives of thiazol-2-ethylamines and their activity against Trypanosoma brucei rhodesiense.
- D. A. Patrick, T. Wenzler, R. Tidwell
- Biology, ChemistryBioorganic & Medicinal Chemistry
- 1 June 2016
SAR refinement of antileishmanial N(2),N(4)-disubstituted quinazoline-2,4-diamines.
- Xiaohua Zhu, Kurt S. Van Horn, K. Werbovetz
- Chemistry, BiologyBioorganic & Medicinal Chemistry
- 15 August 2015
Evaluation of Arylimidamides DB1955 and DB1960 as Candidates against Visceral Leishmaniasis and Chagas' Disease: In Vivo Efficacy, Acute Toxicity, Pharmacokinetics, and Toxicology Studies
- Xiaohua Zhu, Qiang Liu, K. Werbovetz
- BiologyAntimicrobial Agents and Chemotherapy
- 16 April 2012
In a murine Trypanosoma cruzi infection model, DB1960 decreased the peak parasitemia levels that occurred at 8 days postinfection by 46% when given orally at 100 mg/kg/day × 5, while DB1955 had no effect on peak paras itemia levels when administered by the same dosing regimen.
Synthesis and pharmacological evaluation of mono-arylimidamides as antileishmanial agents
- Xiaohua Zhu, A. Farahat, K. Werbovetz
- ChemistryBioorganic & Medicinal Chemistry Letters
- 15 May 2016
The inward rectifier current inhibitor PA‐6 terminates atrial fibrillation and does not cause ventricular arrhythmias in goat and dog models
- Yuan Ji, R. Varkevisser, M. V. D. van der Heyden
- BiologyBritish Journal of Pharmacology
- 28 June 2017
The synthetic compound pentamidine analogue 6 (PA‐6) is a selective and potent IK1 inhibitor that is tested for anti‐AF efficacy and potential proarrhythmia, using established models in large animals.
Synthesis and antiprotozoal activity of dicationic 2,6-diphenylpyrazines and aza-analogues.
- Laixing Hu, Alpa Patel, D. Boykin
- Chemistry, BiologyBioorganic & Medicinal Chemistry
- 1 November 2013
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