Your browser doesn't support javascript.
loading
Show: 20 | 50 | 100
Results 1 - 1 de 1
Filter
Add more filters










Database
Language
Publication year range
1.
Bioorg Med Chem Lett ; 24(24): 5814-5817, 2014 Dec 15.
Article in English | MEDLINE | ID: mdl-25455496

ABSTRACT

This study describes the synthesis of compound (7), a highly hydrosoluble phosphonooxymethyl prodrug of compound alpha (4). Compound (7) improved the aqueous solubility of its precursor compound (4) by 50,000 times and it is stable at neutral pH. The prodrug showed faciolicidal activity when evaluated in vitro against excysted Fasciola hepatica metacercariae. The in vivo evaluation of (7) was carried out via oral, intramuscular and subcutaneous administration in sheep artificially infected with F. hepatica metacercariae. At an intramuscular dose of 4 mg/kg, the activity of (7) was similar to that of compound alpha (4) at an oral dose of 15 mg/kg.


Subject(s)
Antiprotozoal Agents/chemistry , Benzimidazoles/chemistry , Fascioliasis/drug therapy , Organophosphates/chemistry , Administration, Oral , Animals , Antiprotozoal Agents/pharmacology , Antiprotozoal Agents/therapeutic use , Benzimidazoles/pharmacology , Benzimidazoles/therapeutic use , Fasciola hepatica/drug effects , Fascioliasis/parasitology , Fascioliasis/veterinary , Injections, Intramuscular , Injections, Subcutaneous , Organophosphates/pharmacology , Organophosphates/therapeutic use , Prodrugs/chemistry , Prodrugs/pharmacology , Prodrugs/therapeutic use , Sheep , Solubility , Water/chemistry
SELECTION OF CITATIONS
SEARCH DETAIL
...