Design, synthesis, calorimetry, and crystallographic analysis of 2-alkylaminoethyl-1,1-bisphosphonates as inhibitors of trypanosoma cruzi farnesyl diphosphate synthase

Linear 2-alkylaminoethyl-1,1-bisphosphonates are effective agents against proliferation of Trypanosoma cruzi, the etiologic agent of American trypanosomiasis (Chagas disease), exhibiting IC 50 values in the nanomolar range against the parasites. This activity is associated with inhibition at the low...

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Detalles Bibliográficos
Autores principales: Aripirala, S., Szajnman, S.H., Jakoncic, J., Rodriguez, J.B., Docampo, R., Gabelli, S.B., Amzel, L.M.
Formato: JOUR
Materias:
alkyl group
allyl compound
amine
antitrypanosomal agent
bisphosphonic acid derivative
geranyltransferase
geranyltransferase inhibitor
isoprenoid
methyl group
unclassified drug
article
binding affinity
Chagas disease
chemical bond
complex formation
conformation
crystal structure
drug design
drug protein binding
drug synthesis
enthalpy
entropy
enzyme active site
enzyme inhibition
hydrophobicity
IC 50
isothermal titration calorimetry
nonhuman
structure activity relation
thermodynamics
Trypanosoma cruzi
X ray crystallography
Calorimetry
Crystallography, X-Ray
Drug Design
Enzyme Inhibitors
Geranyltranstransferase
Magnesium
Models, Molecular
Phosphonic Acids
Protein Conformation
Thermodynamics
Acceso en línea:http://hdl.handle.net/20.500.12110/paper_00222623_v55_n14_p6445_Aripirala
Aporte de:
Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA) de Universidad de Buenos Aires

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