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- Publications
- Influence
Human African trypanosomiasis: pharmacological re‐engagement with a neglected disease
- M. Barrett, D. Boykin, R. Brun, R. Tidwell
- Biology, Medicine
- British journal of pharmacology
- 1 December 2007
This review discusses the challenges of chemotherapy for human African trypanosomiasis (HAT). The few drugs registered for use against the disease are unsatisfactory for a number of reasons. HAT has… Expand
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
- M. Hammerschlag, C. Dykstra, +9 authors D. Vandewiele
- Medicine
- Antimicrobial Agents and Chemotherapy
- 1 January 2007
Limit the abstract to 250 words or fewer and concisely summarize the basic content of the paper without presenting extensive experimental details. Avoid abbreviations and references, and do not… Expand
New Treatment Option for Second-Stage African Sleeping Sickness: In Vitro and In Vivo Efficacy of Aza Analogs of DB289
- T. Wenzler, D. Boykin, M. Ismail, J. Hall, R. Tidwell, R. Brun
- Biology, Medicine
- Antimicrobial Agents and Chemotherapy
- 20 July 2009
ABSTRACT African sleeping sickness is a fatal parasitic disease, and all drugs currently in use for treatment have strong liabilities. It is essential to find new, effective, and less toxic drugs,… Expand
Accumulation and Intracellular Distribution of Antitrypanosomal Diamidine Compounds DB75 and DB820 in African Trypanosomes
- Amanda M Mathis, J. Holman, +4 authors J. Hall
- Biology, Medicine
- Antimicrobial Agents and Chemotherapy
- 1 June 2006
ABSTRACT The aromatic diamidine pentamidine has long been used to treat early-stage human African trypanosomiasis (HAT). Two analogs of pentamidine, DB75 and DB820, have been shown to be more potent… Expand
CYP4F Enzymes Are the Major Enzymes in Human Liver Microsomes That Catalyze the O-Demethylation of the Antiparasitic Prodrug DB289 [2,5-Bis(4-amidinophenyl)furan-bis-O-methylamidoxime]
- M. Z. Wang, Janelle Y Saulter, +13 authors J. Hall
- Chemistry, Medicine
- Drug Metabolism and Disposition
- 1 December 2006
DB289 [2,5-bis(4-amidinophenyl)furan-bis-O-methylamidoxime] is biotransformed to the potent antiparasitic diamidine DB75 [2,5-bis(4-amidinophenyl) furan] by sequential oxidative O-demethylation and… Expand
Transport of Dicationic Drugs Pentamidine and Furamidine by Human Organic Cation Transporters
- X. Ming, W. Ju, H. Wu, R. Tidwell, J. Hall, D. Thakker
- Biology, Medicine
- Drug Metabolism and Disposition
- 1 February 2009
The antiparasitic activity of aromatic diamidine drugs, pentamidine and furamidine, depends on their entry into the pathogenic protozoa via membrane transporters. However, no such diamidine… Expand
Novel Arylimidamides for Treatment of Visceral Leishmaniasis
- M. Z. Wang, Xiaohua Zhu, +15 authors K. Werbovetz
- Biology, Medicine
- Antimicrobial Agents and Chemotherapy
- 5 April 2010
ABSTRACT Arylimidamides (AIAs) represent a new class of molecules that exhibit potent antileishmanial activity (50% inhibitory concentration [IC50], <1 μM) against both Leishmania donovani axenic… Expand
Antileishmanial Activities of Several Classes of Aromatic Dications
- J. Brendle, Abram Outlaw, +4 authors K. Werbovetz
- Chemistry, Medicine
- Antimicrobial Agents and Chemotherapy
- 1 March 2002
ABSTRACT Aromatic dicationic molecules possess impressive activity against a broad spectrum of microbial pathogens, including Pneumocystis carinii, Cryptosporidium parvum, and Candida albicans. In… Expand
Efficient and specific cardiac IK₁ inhibition by a new pentamidine analogue.
- H. Takanari, L. Nalos, +10 authors M. V. D. van der Heyden
- Chemistry, Medicine
- Cardiovascular research
- 1 July 2013
AIMS
In excitable cells, KIR2.x ion-channel-carried inward rectifier current (IK₁) is thought to set the negative and stable resting membrane potential, and contributes to action potential… Expand
Mechanisms Underlying Differences in Systemic Exposure of Structurally Similar Active Metabolites: Comparison of Two Preclinical Hepatic Models
- Grace Zhixia Yan, K. Brouwer, +4 authors M. Paine
- Chemistry, Medicine
- Journal of Pharmacology and Experimental…
- 1 May 2011
Selection of in vitro models that accurately characterize metabolite systemic and hepatobiliary exposure remains a challenge in drug development. In the present study, mechanisms underlying… Expand