In Vitro and in Vivo activities of sulfur-containing linear bisphosphonates against apicomplexan parasites

We tested a series of sulfur-containing linear bisphosphonates against Toxoplasma gondii, the etiologic agent of toxoplasmosis. The most potent compound (compound 22; 1-[(n-decylsulfonyl)ethyl]-1,1-bisphosphonic acid) is a sulfonecontaining compound, which had a 50% effective concentration (EC50) of...

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Detalles Bibliográficos
Autores principales: Szajnman, S.H., Galaka, T., Li, Z.-H., Li, C., Howell, N.M., Chao, M.N., Striepen, B., Muralidharan, V., Moreno, S.N.J., Rodriguez, J.B.
Formato: JOUR
Materias:
Bisphosphonates
Cryptosporidium parvum
Farnesyl diphosphate synthase
Isoprenoids
Plasmodium falciparum
Toxoplasma gondii
(2,2 diphosphonoethyl)(methyl)(hexyl)sulfonium tetrafluoroborate
(2,2 diphosphonoethyl)(methyl)(pentyl)sulfonium tetrafluoroborate
1 [(n decylsulfonyl)ethyl] 1,1 biphosphonic acid
1 [(n heptylsulfonyl)ethyl] 1,1 biphosphonic acid
1 [(n hexylsulfonyl)ethyl] 1,1 biphosphonic acid
1 [(n nonylsulfonyl)ethyl] 1,1 biphosphonic acid
1 [(n octylsulfonyl)ethyl] 1,1 biphosphonic acid
atorvastatin
bisphosphonic acid derivative
geranyltransferase
hydroxymethylglutaryl coenzyme A reductase inhibitor
pamidronic acid
risedronic acid
sulfone
sulfur
unclassified drug
zoledronic acid
antiprotozoal agent
enzyme inhibitor
animal cell
animal experiment
animal model
Apicomplexa
Article
controlled study
cryptosporidiosis
EC50
enzyme activity
experimental model
IC50
in vitro study
in vivo study
malaria
mouse
nonhuman
priority journal
selectivity index
tachyzoite
tissue culture
toxicity
Toxoplasma
toxoplasmosis
animal
antagonists and inhibitors
chemistry
dose response
drug effects
enzymology
growth, development and aging
human
inbred mouse strain
preclinical study
procedures
synthesis
Animals
Antiprotozoal Agents
Chemistry Techniques, Synthetic
Diphosphonates
Dose-Response Relationship, Drug
Drug Evaluation, Preclinical
Enzyme Inhibitors
Geranyltranstransferase
Humans
Mice, Inbred Strains
Sulfur
Toxoplasmosis
Acceso en línea:http://hdl.handle.net/20.500.12110/paper_00664804_v61_n2_p_Szajnman
Aporte de:
Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA) de Universidad de Buenos Aires

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