Published in J Med Chem on October 23, 2003
Human African trypanosomiasis: pharmacological re-engagement with a neglected disease. Br J Pharmacol (2007) 2.96
Antiparasitic compounds that target DNA. Biochimie (2008) 2.00
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289. Antimicrob Agents Chemother (2009) 1.73
Accumulation and intracellular distribution of antitrypanosomal diamidine compounds DB75 and DB820 in African trypanosomes. Antimicrob Agents Chemother (2006) 1.57
Diphenyl furans and aza analogs: effects of structural modification on in vitro activity, DNA binding, and accumulation and distribution in trypanosomes. Antimicrob Agents Chemother (2007) 1.44
Arginine Methylation Initiates BMP-Induced Smad Signaling. Mol Cell (2013) 1.14
Novel amidines and analogues as promising agents against intracellular parasites: a systematic review. Parasitology (2013) 1.07
Pharmacology of DB844, an orally active aza analogue of pafuramidine, in a monkey model of second stage human African trypanosomiasis. PLoS Negl Trop Dis (2012) 1.04
Synthesis and antiprotozoal activity of cationic 1,4-diphenyl-1H-1,2,3-triazoles. J Med Chem (2010) 1.00
Role of Plasmodium falciparum digestive vacuole plasmepsins in the specificity and antimalarial mode of action of cysteine and aspartic protease inhibitors. Antimicrob Agents Chemother (2009) 0.98
Pharmacokinetics, Trypanosoma brucei gambiense efficacy, and time of drug action of DB829, a preclinical candidate for treatment of second-stage human African trypanosomiasis. Antimicrob Agents Chemother (2013) 0.93
In vitro and in vivo evaluation of 28DAP010, a novel diamidine for treatment of second-stage African sleeping sickness. Antimicrob Agents Chemother (2014) 0.90
Novel linear triaryl guanidines, N-substituted guanidines and potential prodrugs as antiprotozoal agents. Eur J Med Chem (2008) 0.89
Dicationic phenyl-2,2'-bichalcophenes and analogues as antiprotozoal agents. Bioorg Med Chem (2010) 0.89
Mechanisms underlying differences in systemic exposure of structurally similar active metabolites: comparison of two preclinical hepatic models. J Pharmacol Exp Ther (2011) 0.88
The trypanocidal activity of amidine compounds does not correlate with their binding affinity to Trypanosoma cruzi kinetoplast DNA. Antimicrob Agents Chemother (2011) 0.86
Safety, pharmacokinetic, and efficacy studies of oral DB868 in a first stage vervet monkey model of human African trypanosomiasis. PLoS Negl Trop Dis (2013) 0.85
Synthesis and antiprotozoal activity of 2,5-bis[amidinoaryl]thiazoles. Bioorg Med Chem (2010) 0.84
In vivo investigations of selected diamidine compounds against Trypanosoma evansi using a mouse model. Antimicrob Agents Chemother (2009) 0.84
Pharmacokinetic comparison to determine the mechanisms underlying the differential efficacies of cationic diamidines against first- and second-stage human African trypanosomiasis. Antimicrob Agents Chemother (2014) 0.83
Chemotherapy of second stage human African trypanosomiasis: comparison between the parenteral diamidine DB829 and its oral prodrug DB868 in vervet monkeys. PLoS Negl Trop Dis (2015) 0.82
Synthesis and activity of azaterphenyl diamidines against Trypanosoma brucei rhodesiense and Plasmodium falciparum. Bioorg Med Chem (2009) 0.81
Synthesis and antiprotozoal activity of dicationic 2,6-diphenylpyrazines and aza-analogues. Bioorg Med Chem (2013) 0.80
Neglected disease - african sleeping sickness: recent synthetic and modeling advances. Sci Pharm (2011) 0.80
Activities of dicationic compounds against Trichomonas vaginalis. Antimicrob Agents Chemother (2004) 0.78
Novel diamidines with activity against Babesia divergens in vitro and Babesia microti in vivo. Antimicrob Agents Chemother (2011) 0.78
Evaluation of the biological activity of novel monocationic fluoroaryl-2,2'-bichalcophenes and their analogues. Drug Des Devel Ther (2014) 0.78
CYP1A1 and CYP1B1-mediated biotransformation of the antitrypanosomal methamidoxime prodrug DB844 forms novel metabolites through intramolecular rearrangement. J Pharm Sci (2013) 0.77
Anticancer, antioxidant activities, and DNA affinity of novel monocationic bithiophenes and analogues. Drug Des Devel Ther (2014) 0.77
Bis-benzimidazole hits against Naegleria fowleri discovered with new high-throughput screens. Antimicrob Agents Chemother (2015) 0.76
Synthesis, antimicrobial, and antiproliferative activities of substituted phenylfuranylnicotinamidines. Drug Des Devel Ther (2016) 0.75
Spiroindolones, a potent compound class for the treatment of malaria. Science (2010) 5.94
Identification of an antimalarial synthetic trioxolane drug development candidate. Nature (2004) 4.57
Antimalarial drug discovery: efficacy models for compound screening. Nat Rev Drug Discov (2004) 3.90
Kinetoplastids: related protozoan pathogens, different diseases. J Clin Invest (2008) 3.59
Synthetic ozonide drug candidate OZ439 offers new hope for a single-dose cure of uncomplicated malaria. Proc Natl Acad Sci U S A (2011) 3.23
A selective TrkB agonist with potent neurotrophic activities by 7,8-dihydroxyflavone. Proc Natl Acad Sci U S A (2010) 2.57
Fexinidazole--a new oral nitroimidazole drug candidate entering clinical development for the treatment of sleeping sickness. PLoS Negl Trop Dis (2010) 2.08
Antiparasitic compounds that target DNA. Biochimie (2008) 2.00
Detection of arsenical drug resistance in Trypanosoma brucei with a simple fluorescence test. Lancet (2005) 1.94
Mechanisms of arsenical and diamidine uptake and resistance in Trypanosoma brucei. Eukaryot Cell (2003) 1.94
Telomestatin and diseleno sapphyrin bind selectively to two different forms of the human telomeric G-quadruplex structure. J Am Chem Soc (2005) 1.87
Spirotetrahydro beta-carbolines (spiroindolones): a new class of potent and orally efficacious compounds for the treatment of malaria. J Med Chem (2010) 1.84
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289. Antimicrob Agents Chemother (2009) 1.73
Dications that target the DNA minor groove: compound design and preparation, DNA interactions, cellular distribution and biological activity. Curr Med Chem Anticancer Agents (2005) 1.66
SCYX-7158, an orally-active benzoxaborole for the treatment of stage 2 human African trypanosomiasis. PLoS Negl Trop Dis (2011) 1.66
Eflornithine for the treatment of human African trypanosomiasis. Parasitol Res (2002) 1.61
Biosensor-surface plasmon resonance: quantitative analysis of small molecule-nucleic acid interactions. Methods (2007) 1.58
Accumulation and intracellular distribution of antitrypanosomal diamidine compounds DB75 and DB820 in African trypanosomes. Antimicrob Agents Chemother (2006) 1.57
Inhibitory activity of marine sponge-derived natural products against parasitic protozoa. Mar Drugs (2010) 1.52
Advancing drug innovation for neglected diseases-criteria for lead progression. PLoS Negl Trop Dis (2009) 1.48
Antitrypanosomal and antileishmanial activities of flavonoids and their analogues: in vitro, in vivo, structure-activity relationship, and quantitative structure-activity relationship studies. Antimicrob Agents Chemother (2006) 1.48
Activities of psilostachyin A and cynaropicrin against Trypanosoma cruzi in vitro and in vivo. Antimicrob Agents Chemother (2013) 1.47
Novel arylimidamides for treatment of visceral leishmaniasis. Antimicrob Agents Chemother (2010) 1.45
Discovery of a novel, monocationic, small-molecule inhibitor of scrapie prion accumulation in cultured sheep microglia and Rov cells. PLoS One (2012) 1.45
In vitro assessment of the pharmacodynamic properties and the partitioning of OZ277/RBx-11160 in cultures of Plasmodium falciparum. J Antimicrob Chemother (2006) 1.44
Inhibition of Plasmodium falciparum fatty acid biosynthesis: evaluation of FabG, FabZ, and FabI as drug targets for flavonoids. J Med Chem (2006) 1.44
DNA sequence dependent monomer-dimer binding modulation of asymmetric benzimidazole derivatives. J Am Chem Soc (2004) 1.44
Diphenyl furans and aza analogs: effects of structural modification on in vitro activity, DNA binding, and accumulation and distribution in trypanosomes. Antimicrob Agents Chemother (2007) 1.44
Diamidines for human African trypanosomiasis. Curr Opin Investig Drugs (2010) 1.42
Design and synthesis of an expanded porphyrin that has selectivity for the c-MYC G-quadruplex structure. J Am Chem Soc (2005) 1.40
Pharmacokinetics and clinical utility of sodium bromide (NaBr) as an estimator of extracellular fluid volume in horses. J Vet Intern Med (2003) 1.38
Synthesis of some new 2-substituted-phenyl-1H-benzimidazole-5-carbonitriles and their potent activity against Candida species. Bioorg Med Chem (2002) 1.37
Imidazolopiperazines: hit to lead optimization of new antimalarial agents. J Med Chem (2011) 1.36
Discovery of dual function acridones as a new antimalarial chemotype. Nature (2009) 1.36
Spiro and dispiro-1,2,4-trioxolanes as antimalarial peroxides: charting a workable structure-activity relationship using simple prototypes. J Med Chem (2005) 1.35
Peroxide bond-dependent antiplasmodial specificity of artemisinin and OZ277 (RBx11160). Antimicrob Agents Chemother (2007) 1.35
Ancistrotanzanine C and related 5,1'- and 7,3'-coupled naphthylisoquinoline alkaloids from Ancistrocladus tanzaniensis. J Nat Prod (2004) 1.33
Structure-specific recognition of quadruplex DNA by organic cations: influence of shape, substituents and charge. Biophys Chem (2006) 1.32
Surface sialic acids taken from the host allow trypanosome survival in tsetse fly vectors. J Exp Med (2004) 1.31
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]. Drug Metab Dispos (2006) 1.30
Characterization of a defensin from the sand fly Phlebotomus duboscqi induced by challenge with bacteria or the protozoan parasite Leishmania major. Infect Immun (2004) 1.29
Bottlenecks and the maintenance of minor genotypes during the life cycle of Trypanosoma brucei. PLoS Pathog (2010) 1.28
Antitrypanosomal activity of fexinidazole, a new oral nitroimidazole drug candidate for treatment of sleeping sickness. Antimicrob Agents Chemother (2011) 1.26
Antiparasitic agents: new drugs on the horizon. Curr Opin Pharmacol (2012) 1.25
Global metabolic responses of mice to Trypanosoma brucei brucei infection. Proc Natl Acad Sci U S A (2008) 1.24
Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. J Med Chem (2012) 1.22
Efficacy of DB289 in Thai patients with Plasmodium vivax or acute, uncomplicated Plasmodium falciparum infections. J Infect Dis (2005) 1.22
Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment. Antimicrob Agents Chemother (2010) 1.20
Thiophene-based diamidine forms a "super" at binding minor groove agent. J Am Chem Soc (2004) 1.18
Synthesis, DNA affinity, and antiprotozoal activity of linear dications: Terphenyl diamidines and analogues. J Med Chem (2006) 1.17
Structure-activity study of pentamidine analogues as antiprotozoal agents. J Med Chem (2009) 1.16
Selective recognition of G-qQuadruplex telomeric DNA by a bis(quinacridine) macrocycle. J Am Chem Soc (2003) 1.15
Intraspecific competition between co-infecting parasite strains enhances host survival in African trypanosomes. Ecology (2009) 1.15
Design and synthesis of a series of melamine-based nitroheterocycles with activity against Trypanosomatid parasites. J Med Chem (2005) 1.15
Genotypic and phenotypic characterization of Trypanosoma brucei gambiense isolates from Ibba, South Sudan, an area of high melarsoprol treatment failure rate. Acta Trop (2007) 1.15
Comparative thermodynamics for monomer and dimer sequence-dependent binding of a heterocyclic dication in the DNA minor groove. J Mol Biol (2002) 1.12
Out-of-shape DNA minor groove binders: induced fit interactions of heterocyclic dications with the DNA minor groove. Biochemistry (2005) 1.12
Synthesis and biological evaluation of pyrazolylnaphthoquinones as new potential antiprotozoal and cytotoxic agents. Chembiochem (2003) 1.12
Trisubstituted acridines as G-quadruplex telomere targeting agents. Effects of extensions of the 3,6- and 9-side chains on quadruplex binding, telomerase activity, and cell proliferation. J Med Chem (2006) 1.11
The activity of diguanidino and 'reversed' diamidino 2,5-diarylfurans versus Trypanosoma cruzi and Leishmania donovani. Bioorg Med Chem Lett (2003) 1.11
Distribution of furamidine analogues in tumor cells: targeting of the nucleus or mitochondria depending on the amidine substitution. Cancer Res (2002) 1.11
Quantitative analysis of small molecule-nucleic acid interactions with a biosensor surface and surface plasmon resonance detection. Methods Mol Biol (2010) 1.11
Natural products active against African trypanosomes: a step towards new drugs. Nat Prod Rep (2004) 1.10
A role for water molecules in DNA-ligand minor groove recognition. Acc Chem Res (2009) 1.10
Dicationic near-linear biphenyl benzimidazole derivatives as DNA-targeted antiprotozoal agents. Bioorg Med Chem (2005) 1.10
Malaria-infected mice are cured by oral administration of new artemisinin derivatives. J Med Chem (2008) 1.10
Unusual dehydroxylation of antimicrobial amidoxime prodrugs by cytochrome b5 and NADH cytochrome b5 reductase. Drug Metab Dispos (2005) 1.08
DNA binding affinity of bisguanidine and bis(2-aminoimidazoline) derivatives with in vivo antitrypanosomal activity. J Med Chem (2006) 1.08
Pharmacokinetics and metabolism of the prodrug DB289 (2,5-bis[4-(N-methoxyamidino)phenyl]furan monomaleate) in rat and monkey and its conversion to the antiprotozoal/antifungal drug DB75 (2,5-bis(4-guanylphenyl)furan dihydrochloride). Drug Metab Dispos (2007) 1.07
Marine natural products from the Turkish sponge Agelas oroides that inhibit the enoyl reductases from Plasmodium falciparum, Mycobacterium tuberculosis and Escherichia coli. Bioorg Med Chem (2007) 1.07
Identification of a 1,2,4,5-tetraoxane antimalarial drug-development candidate (RKA 182) with superior properties to the semisynthetic artemisinins. Angew Chem Int Ed Engl (2010) 1.07
1-Aryl-4-nitro-1H-imidazoles, a new promising series for the treatment of human African trypanosomiasis. Eur J Med Chem (2011) 1.07
New bis(2-aminoimidazoline) and bisguanidine DNA minor groove binders with potent in vivo antitrypanosomal and antiplasmodial activity. J Med Chem (2008) 1.06
Exploration of larger central ring linkers in furamidine analogues: synthesis and evaluation of their DNA binding, antiparasitic and fluorescence properties. Bioorg Med Chem (2011) 1.06