Published in Bioorg Med Chem Lett on June 16, 2003
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In vitro and in vivo investigation of the efficacy of arylimidamide DB1831 and its mesylated salt form--DB1965--against Trypanosoma cruzi infection. PLoS One (2012) 0.99
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Novel linear triaryl guanidines, N-substituted guanidines and potential prodrugs as antiprotozoal agents. Eur J Med Chem (2008) 0.89
Evaluation of arylimidamides DB1955 and DB1960 as candidates against visceral leishmaniasis and Chagas' disease: in vivo efficacy, acute toxicity, pharmacokinetics, and toxicology studies. Antimicrob Agents Chemother (2012) 0.88
Di-cationic arylimidamides act against Neospora caninum tachyzoites by interference in membrane structure and nucleolar integrity and are active against challenge infection in mice. Int J Parasitol Drugs Drug Resist (2012) 0.87
The trypanocidal activity of amidine compounds does not correlate with their binding affinity to Trypanosoma cruzi kinetoplast DNA. Antimicrob Agents Chemother (2011) 0.86
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Structure-dependent binding of arylimidamides to the DNA minor groove. Chembiochem (2013) 0.81
Studies on the antileishmanial mechanism of action of the arylimidamide DB766: azole interactions and role of CYP5122A1. Antimicrob Agents Chemother (2014) 0.79
Activities of dicationic compounds against Trichomonas vaginalis. Antimicrob Agents Chemother (2004) 0.78
Experimental Chemotherapy for Chagas Disease: A Morphological, Biochemical, and Proteomic Overview of Potential Trypanosoma cruzi Targets of Amidines Derivatives and Naphthoquinones. Mol Biol Int (2011) 0.78
Discovery of novel polyamine analogs with anti-protozoal activity by computer guided drug repositioning. J Comput Aided Mol Des (2016) 0.76
Synthesis and pharmacological evaluation of mono-arylimidamides as antileishmanial agents. Bioorg Med Chem Lett (2016) 0.75
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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
Synthesis and antiprotozoal activity of aza-analogues of furamidine. J Med Chem (2003) 1.49
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
Discovery of a novel, monocationic, small-molecule inhibitor of scrapie prion accumulation in cultured sheep microglia and Rov cells. PLoS One (2012) 1.45
Novel arylimidamides for treatment of visceral leishmaniasis. Antimicrob Agents Chemother (2010) 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
Natural products from plants as drug candidates and lead compounds against leishmaniasis and trypanosomiasis. Curr Med Chem (2006) 1.25
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
Cytotoxic 5-aryl-1-(4-nitrophenyl)-3-oxo-1,4-pentadienes mounted on alicyclic scaffolds. Eur J Med Chem (2006) 1.21
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
Highly effective oral amphotericin B formulation against murine visceral leishmaniasis. J Infect Dis (2009) 1.13
Out-of-shape DNA minor groove binders: induced fit interactions of heterocyclic dications with the DNA minor groove. Biochemistry (2005) 1.12
Comparative thermodynamics for monomer and dimer sequence-dependent binding of a heterocyclic dication in the DNA minor groove. J Mol Biol (2002) 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
Quantitative analysis of small molecule-nucleic acid interactions with a biosensor surface and surface plasmon resonance detection. Methods Mol Biol (2010) 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
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
DNA binding affinity of bisguanidine and bis(2-aminoimidazoline) derivatives with in vivo antitrypanosomal activity. J Med Chem (2006) 1.08
Unusual dehydroxylation of antimicrobial amidoxime prodrugs by cytochrome b5 and NADH cytochrome b5 reductase. Drug Metab Dispos (2005) 1.08
1-Aryl-4-nitro-1H-imidazoles, a new promising series for the treatment of human African trypanosomiasis. Eur J Med Chem (2011) 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
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
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