91753-13-8Relevant academic research and scientific papers
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.
Identification and characterization of m4 selective muscarinic antagonists
Augelli-Szafran, Corinne E.,Jaen, Juan C.,Moreland, David W.,Nelson, Carrie B.,Penvose-Yi, Jan R.,Schwarz, Roy D.
, p. 1991 - 1996 (2007/10/03)
Our interest in the area of m4 muscarinic antagonists has led us to study a series of benzoxazine isoquinolines. One of the most potent and selective compounds of this series is example 1 with an IC50 value of 90.7nM at m4 receptors, and 72-fold (m1), 38-fold (m2), 10-fold (m3), and 82- fold (m5) more selective compared to the other receptors. The synthesis and receptor binding affinity of analogs of 1 are reported.
MOLECULAR CONFORMATION AND ELECTRONIC STRUCTURE OF AZOMETHINES. VIII. DIPOLE MOMENTS OF 3,4-DIHYDROISOQUINOLINES
Pitea, Demetrio,Beltrame, Pier Luigi,Ferrazza, Alberto,Todeschini, Roberto,Favini, Giorgio
, p. 35 - 40 (2007/10/02)
The dipole moments of some methyl derivatives of 3,4-dihydroisoquinoline have been measured in benzene at 25 deg C and the experimental directions determined.The correlation with the theoretical dipole moments of the corresponding benzaldimines supports the view that the 3,4-dihydroisoquinolines can be used as models for the Z conformation of N-benzylidenemethylamines.Moreover, the differences between the dipole moment of 3,4-dihydroisoquinolines and that of the corresponding benzaldimines can be ascribed to conjugation across the -CH2-CH2- bridge.Experimental and calculated values of the methyl replacement vectors are in good agreement.
