406954-88-9Relevant articles and documents
Praziquantel derivatives with antischistosomal activity: Aromatic ring modification
Wang, Zhi-Xia,Chen, Jing-Lei,Qiao, Chunhua
, p. 216 - 225 (2013/08/23)
A series of aromatic ring-modified praziquantel derivatives were prepared and evaluated against juvenile and adult stage of Schistosoma japonicumin. Several analogs comparable in activity to the drug praziquantel have been identified based on in vitro and in vivo japonuicum schistosomes worm viability assay. Structure and activity relationship of these praziquantel aromatic ring-modified compounds was revealed. Specifically, a compound in which a bromine has been introduced in the aromatic ring of praziquantel demonstrated close antischistosomal activity to praziquantel in vivo.
Amino acid derived heterocycles: Lewis acid catalyzed and radical cyclizations from peptide acetals
Todd, Matthew H.,Ndubaku, Chudi,Bartlett, Paul A.
, p. 3985 - 3988 (2007/10/03)
Bicyclization of peptide acetals via nucleophilic attack of a phenyl group on an endocyclic acyliminium ion 4 was explored as a route to novel amino acid derived heterocycles and peptidomimetic scaffolds. In the presence of protic acid, bridged structures such as 6 are formed readily from phenylalanine derivatives, but the fused-ring analogues 5 could not be obtained in good yield. In contrast, radical cyclization of the bromophenyl dihydropyrazinone 7 provides an effective alternative for the synthesis of 5 (n = 0, 1, 2). Additional versatility in this process was demonstrated by efficient synthesis of a different fused ring system, represented by the antihelmintic praziquantel, 8.
