User profiles for Michael. P. Kozar

Michael P. Kozar

National Institutes of Health, Division of Microbiology and Infectious Diseases, Office of
Verified email at nih.gov
Cited by 793

[HTML][HTML] CYP450 phenotyping and accurate mass identification of metabolites of the 8-aminoquinoline, anti-malarial drug primaquine

…, C Vuong, RJ Sciotti, GA Reichard, MP Kozar… - Malaria journal, 2012 - Springer
Background The 8-aminoquinoline (8AQ) drug primaquine (PQ) is currently the only
approved drug effective against the persistent liver stage of the hypnozoite forming strains …

Antimalarial activity of novel 5-aryl-8-aminoquinoline derivatives

H Shiraki, MP Kozar, V Melendez… - Journal of medicinal …, 2011 - ACS Publications
In an attempt to separate the antimalarial activity of tafenoquine (3) from its hemolytic side
effects in glucose-6-phosphate dehydrogenase (G6PD) deficiency patients, a series of 5-aryl-8…

[HTML][HTML] Formulation and particle size reduction improve bioavailability of poorly water-soluble compounds with antimalarial activity

…, L Xie, V Melendez, M Hickman, MP Kozar - Malaria Research and …, 2013 - hindawi.com
Decoquinate (DQ) is highly effective at killing malaria parasites in vitro; however, it is extremely
insoluble in water. In this study, solid dispersion method was used for DQ formulation …

Nanoparticle formulations of decoquinate increase antimalarial efficacy against liver stage Plasmodium infections in mice

…, N Roncal, V Melendez, M Hickman, MP Kozar - … , Biology and Medicine, 2014 - Elsevier
Decoquinate has potent activity against both Plasmodium hepatic development and red cell
replication when tested in vitro. Decoquinate, however, is practically insoluble in water. To …

Synthesis and antimalarial activity of 2-guanidino-4-oxoimidazoline derivatives

X Liu, X Wang, Q Li, MP Kozar… - Journal of medicinal …, 2011 - ACS Publications
A series of 2-guanidino-4-oxoimidazoline (deoxo-IZ) derivatives was prepared and showed
potent antimalarial activities in rodent and Rhesus models. Compound 8e, the most potent …

In vitro biotransformation, in vivo efficacy and pharmacokinetics of antimalarial chalcones

CE Gutteridge, DS Thota, SM Curtis, MP Kozar, Q Li… - Pharmacology, 2011 - karger.com
4′-n-Butoxy-2,4-dimethoxy-chalcone (MBC) has been described as protecting mice from
an otherwise lethal infection with Plasmodium yoelii when dosed orally at 50 mg/kg/dose, …

Ketotifen is an antimalarial prodrug of norketotifen with blood schizonticidal and liver-stage efficacy

…, E Harris, M Hickman, MP Kozar, P Lee… - European journal of …, 2012 - Springer
Ketotifen is known to exhibit antimalarial activity in mouse and monkey malaria models.
However, the low plasma levels and short half life of the drug do not adequately explain its in …

Failure to detect muramic acid in normal rat tissues but detection in cerebrospinal fluids from patients with Pneumococcal meningitis

MP Kozar, MT Krahmer, A Fox, BM Gray - Infection and immunity, 2000 - Am Soc Microbiol
Muramic acid serves as a marker for the presence of bacterial cell wall debris in mammalian
tissues. There have been a number of controversial and sometimes conflicting results on …

Malaria causal prophylactic activity of imidazolidinedione derivatives

…, DE Kyle, WK Milhous, MP Kozar… - Journal of medicinal …, 2007 - ACS Publications
A series of acid-stable carboxamide derivatives of 2-guanidinoimidazolidinedione (5a−c and
6a−c) were prepared as potential malaria prophylactic and radical cure agents. The new …

In vitro metabolism of phenoxypropoxybiguanide analogues in human liver microsomes to potent antimalarial dihydrotriazines

TW Shearer, MP Kozar, MT O'Neil… - Journal of medicinal …, 2005 - ACS Publications
Phenoxypropoxybiguanides, such as 1 (PS-15), are prodrugs analogous to the relationship
of proguanil and its active metabolite cycloguanil. Unlike cycloguanil, however, 1a (…