Synthesis and in vitro Trichomonacidal activities of some new dialkylperoxides and 1,2,4-trioxanes
Autor: | B, Camuzat-Dedenis, O, Provot, L, Cointeaux, V, Peyrou, J F, Berrien, C, Bories, P M, Loiseau, J, Mayrargue, V, Perroux |
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Přispěvatelé: | Laboratoire de Chimie Thérapeutique (UPRES-A CNRS 8076 BIOCIS), Université Paris-Sud - Paris 11 (UP11) |
Jazyk: | angličtina |
Rok vydání: | 2001 |
Předmět: |
Free Radicals
Radical Antiprotozoal Agents chemistry.chemical_element [CHIM.THER]Chemical Sciences/Medicinal Chemistry 010402 general chemistry medicine.disease_cause 01 natural sciences Chemical synthesis Peroxide Oxygen chemistry.chemical_compound Inhibitory Concentration 50 Drug Discovery medicine Trichomonas vaginalis Molecule Organic chemistry Animals ComputingMilieux_MISCELLANEOUS Pharmacology 010405 organic chemistry Chemistry [CHIM.ORGA]Chemical Sciences/Organic chemistry Organic Chemistry General Medicine Oxidants Combinatorial chemistry In vitro 3. Good health 0104 chemical sciences Peroxides Active compound |
Zdroj: | European Journal of Medicinal Chemistry European Journal of Medicinal Chemistry, Elsevier, 2001, 36 (10), pp.837-842. ⟨10.1016/S0223-5234(01)01278-8⟩ |
ISSN: | 0223-5234 1768-3254 |
DOI: | 10.1016/S0223-5234(01)01278-8⟩ |
Popis: | Two series of three trioxanes and 18 disubstituted peroxides were synthesised and evaluated for their in vitro trichomonacidal activity against Trichomonas vaginalis . The most active compound, 2-methylprop-2-yl 2-methoxyeth-1-yl peroxide exhibited an IC 50 value of 1.0±0.2 μM whereas other dialkyl peroxides had various IC 50 values which could not be correlated to their molecule structure. The best compound was about five times more active than metronidazole. The amount of generated oxygen or free radicals cannot explain completely the activity suggesting another way of action for these compounds on T. vaginalis . |
Databáze: | OpenAIRE |
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