Antiparasitic compounds that target DNA

WD Wilson, FA Tanious, A Mathis, D Tevis, JE Hall… - Biochimie, 2008 - Elsevier
Designed, synthetic heterocyclic diamidines have excellent activity against eukaryotic
parasites that cause diseases such as sleeping sickness and leishmania and adversely affect …

Extended Aromatic Furan Amidino Derivatives as Anti-Pneumocystis carinii Agents

…, BC Bender, DR McCurdy, JE Hall… - Journal of medicinal …, 1998 - ACS Publications
The syntheses of nine new derivatives of 2,5-bis[4-(N-alkylamidino)phenyl]furans with
extended aromatic systems are reported. The interaction of these dicationic furans with poly(dA)*…

Dications that target the DNA minor groove: compound design and preparation, DNA interactions, cellular distribution and biological activity

…, FA Tanious, A Mathis, JE Hall… - … -Anti-Cancer Agents, 2005 - ingentaconnect.com
Fluorescence microscopy of trypanosomes from drug treated mice shows that biologically
active heterocyclic diamidines that target the DNA minor groove bind rapidly and specifically to …

Confronting the risks of terrorism: making the right decisions

BJ Garrick, JE Hall, M Kilger, JC McDonald… - Reliability Engineering & …, 2004 - Elsevier
This report offers a methodology for assessing, quantitatively, the risks of terrorism. The
purpose of the methodology is to support effective decision making to combat terrorism. The …

New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289

T Wenzler, DW Boykin, MA Ismail, JE Hall… - Antimicrobial agents …, 2009 - Am Soc Microbiol
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, ideally …

Accumulation and intracellular distribution of antitrypanosomal diamidine compounds DB75 and DB820 in African trypanosomes

…, DW Boykin, RR Tidwell, JE Hall - Antimicrobial agents …, 2006 - Am Soc Microbiol
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 …

Structure-activity relationships of analogs of pentamidine against Plasmodium falciparum and Leishmania mexicana amazonensis

CA Bell, JE Hall, DE Kyle, M Grogl… - Antimicrobial agents …, 1990 - Am Soc Microbiol
The antiprotozoal compound 1,5-di(4-amidinophenoxy)pentane (pentamidine) and 36 of its
analogs were screened for in vitro activity against Leishmania mexicana amazonensis clone …

Prodrugs for Amidines:  Synthesis and Anti-Pneumocystis carinii Activity of Carbamates of 2,5-Bis(4-amidinophenyl)furan

SM Rahmathullah, JE Hall, BC Bender… - journal of medicinal …, 1999 - ACS Publications
Syntheses of several carbamate analogues of 2,5-bis(4-amidinophenyl)furan (1) under mild
conditions and their evaluation as prodrugs against Pneumocystis carinii pneumonia (PCP) …

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) …

…, JY Saulter, E Usuki, YL Cheung, M Hall… - Drug metabolism and …, 2006 - ASPET
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-…

Analogs of 1, 5-bis (4-amidinophenoxy) pentane (pentamidine) in the treatment of experimental Pneumocystis carinii pneumonia

…, JD Geratz, KA Ohemeng, M Cory, JE Hall - Journal of Medicinal …, 1990 - ACS Publications
A series of 33 analogues of the anti-Pneumocystis carinii drug l, 5-bis (4-amidinophenoxy)
pentane (pentamidine) was synthesized for screening against a rat model of P. carinii …