Praziquantel derivatives I: Modification of the aromatic ring.
Several analogues of the potent anthelmintic praziquantel were prepared with variation in the aromatic ring. The biological activity of these analogues was evaluated and compared against known analogues. Amination of the ring was tolerated while other variations were not. These results have important implications for drug development for schistosomiasis.
Ronketti
Fiona
F
School of Biological and Chemical Sciences, Queen Mary, University of London, E1 4NS, UK.
Ramana
A Venkata
AV
Chao-Ming
Xia
X
Pica-Mattoccia
Livia
L
Cioli
Donato
D
Todd
Matthew H
MH
D000818:Animals; D000871:Anthelmintics / Q000737:chemistry* / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical; D009682:Magnetic Resonance Spectroscopy; D011223:Praziquantel / Q000031:analogs & derivatives* / Q000494:pharmacology; D012550:Schistosoma mansoni / Q000187:drug effects
D000871:Anthelmintics; D011223:Praziquantel