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Human African trypanosomiasis: pharmacological re‐engagement with a neglected disease
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 hasExpand
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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 notExpand
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New Treatment Option for Second-Stage African Sleeping Sickness: In Vitro and In Vivo Efficacy of Aza Analogs of DB289
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
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Accumulation and Intracellular Distribution of Antitrypanosomal Diamidine Compounds DB75 and DB820 in African Trypanosomes
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 potentExpand
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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]
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 andExpand
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Transport of Dicationic Drugs Pentamidine and Furamidine by Human Organic Cation Transporters
The antiparasitic activity of aromatic diamidine drugs, pentamidine and furamidine, depends on their entry into the pathogenic protozoa via membrane transporters. However, no such diamidineExpand
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Novel Arylimidamides for Treatment of Visceral Leishmaniasis
ABSTRACT Arylimidamides (AIAs) represent a new class of molecules that exhibit potent antileishmanial activity (50% inhibitory concentration [IC50], <1 μM) against both Leishmania donovani axenicExpand
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Antileishmanial Activities of Several Classes of Aromatic Dications
ABSTRACT Aromatic dicationic molecules possess impressive activity against a broad spectrum of microbial pathogens, including Pneumocystis carinii, Cryptosporidium parvum, and Candida albicans. InExpand
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Efficient and specific cardiac IK₁ inhibition by a new pentamidine analogue.
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 potentialExpand
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Mechanisms Underlying Differences in Systemic Exposure of Structurally Similar Active Metabolites: Comparison of Two Preclinical Hepatic Models
Selection of in vitro models that accurately characterize metabolite systemic and hepatobiliary exposure remains a challenge in drug development. In the present study, mechanisms underlyingExpand
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