Synthesis and in vitro Trichomonacidal activities of some new dialkylperoxides and 1,2,4-trioxanes.
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 microM 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.
Camuzat-Dedenis
B
B
Laboratoire de Chimie Organique, ESA 8076 BioCIS, Faculté de Pharmacie, F-92296 cedex, Châtenay-Malabry, France.
Provot
O
O
Cointeaux
L
L
Peyrou
V
V
Berrien
J F
JF
Bories
C
C
Loiseau
P M
PM
Mayrargue
J
J
Perroux
V
V
D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D005609:Free Radicals / Q000737:chemistry; D020128:Inhibitory Concentration 50; D016877:Oxidants / Q000737:chemistry; D010545:Peroxides / Q000138:chemical synthesis*; D014246:Trichomonas vaginalis / Q000187:drug effects*
D000981:Antiprotozoal Agents; D005609:Free Radicals; D016877:Oxidants; D010545:Peroxides