Studies on some derivatives of oxamniquine.
On the basis of the remarkable biological similarities between hycanthone and oxamniquine and as a sequel to our finding that some esters of hycanthone are active against hycanthone-resistant schistosomes, we prepared oxamniquine acetate, oxamniquine N-methylcarbamate, and four substituted phenylsulfonohydrazones of oxamniquine aldehyde. These compounds were tested for their effect on survival of and on [3H]uridine incorporation into hycanthone-sensitive and -resistant Schistosoma mansoni. All of these derivatives were effective to a greater or lesser degree in killing worms and in inhibiting [3H]uridine incorporation in the sensitive strain, but none was effective in the resistant strain.
el-Hamouly
W
W
Cogswell Laboratories, Chemistry Department, Rensselaer Polytechnic Institute, Troy, New York 12180-3590.
Pica-Mattoccia
L
L
Cioli
D
D
Schwartz
H M
HM
Archer
S
S
D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D009600:Nitroquinolines / Q000494:pharmacology*; D010073:Oxamniquine / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000494:pharmacology*; D012550:Schistosoma mansoni / Q000187:drug effects / Q000378:metabolism; D012556:Schistosomicides / Q000138:chemical synthesis*; D013329:Structure-Activity Relationship; D014316:Tritium; D014529:Uridine / Q000378:metabolism
D009600:Nitroquinolines; D012556:Schistosomicides; D010073:Oxamniquine; D014316:Tritium; D014529:Uridine