Synthesis and antischistosomal activity of a new 2-nicotinoyl dipeptide analogue of praziquantel.
As an approach to a structure-antischistosomal activity-relationship with possible pharmacological potentiation of the anthelmintic drug praziquantel, a new dipeptide analogue, namely, N alpha-nicotinoyl-L-aspartyl-beta-(1,2,3,6,7,11b-hexahydro-4H-pyrazino[2- 1a]isoquinoline-4-one)-L-phenylalanine methyl ester, was synthesized and antischistosomally investigated in mice infected with S. mansoni cercariae. Parallely, its simple 2-nicotinoyl analogue was synthesized and tested. Both compounds were less, but still, interestingly active (approximately 63 and approximately 66%, respectively) compared to praziquantel (approximately 90%).
Abo-Ghalia
M H
MH
National Research Centre, Dokki, Cairo, Egypt.
Soliman
A E
AE
D000818:Animals; D005260:Female; D008099:Liver / Q000469:parasitology; D051379:Mice; D011223:Praziquantel / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*; D012550:Schistosoma mansoni / Q000187:drug effects / Q000254:growth & development; D012555:Schistosomiasis mansoni / Q000188:drug therapy / Q000469:parasitology; D012556:Schistosomicides / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D012556:Schistosomicides; D011223:Praziquantel