Synthesis and trichomonacidal activity of perketals and hydroperoxides.
Some perketals were synthesized by the Dussault procedure using simple bromides and 2-methoxyprop-2-yl hydroperoxide. Treatment with acetic acid gave the corresponding hydroperoxides. Both perketals and hydroperoxides were tested in vitro as trichomonacidal agents. Most of them exhibited very good activities. The most powerful compound was 2-methoxyprop-2-yl hexadec-l-yl peroxide which exhibited an IC50 value of 0.51 microM being 10 times more effective than the reference compound Metronidazole.
Cointeaux
L
L
Laboratoire de Chimie Organique, Faculté de Pharmacie, Châtenay-Malabry, France.
Berrien
J F
JF
Camuzat-Dedenis
B
B
Peyrou
V
V
Provot
O
O
Bories
C
C
Loiseau
P M
PM
Mayrargue
J
J
D000818:Animals; D000994:Antitrichomonal Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001965:Bromides / Q000737:chemistry; D004305:Dose-Response Relationship, Drug; D020128:Inhibitory Concentration 50; D009682:Magnetic Resonance Spectroscopy; D008795:Metronidazole / Q000494:pharmacology; D010545:Peroxides / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014246:Trichomonas vaginalis / Q000187:drug effects
D000994:Antitrichomonal Agents; D001965:Bromides; D010545:Peroxides; D008795:Metronidazole