Praziquantel enantiomer

Xiao, S.H., Chollet, J., Booth, M., Weiss, N.A. and Tanner, M. (1 999) Therapeutic effect of praziquantel enantiomers in mice infected with Schistosoma mansoni. Transactions of the Royal Society of Tropical Medicine and Hygiene 93, 324-325. 

Solubility of racemic praziquantel was determined in MeOH and 2-PrOH in the temperature range between 0 °C and 40 °C. A ternary phase diagram of praziquantel enantiomers and the MeOH system was also determined (06CH259). The solubility phase and binary melting-point phase diagrams were determined. Experimental and predicted aqueous solubility of praziquantel was reported (07CPB669,08SQE191). Dissolution of praziquantel... 

It was determined by single crystal X-ray crystallography that (—(-praziquantel enantiomer has (R) absolute configuration (09PLN1). 

Lim, B.G. Ching, C.B. Preliminary design of a simulated counter-current chromatographic system for the separation of praziquantel enantiomers. J. Chromatogr. A, 1996, 734, 247-258. 

More then a dozen representatives of the above ring systems were introduced into the human therapy. Actisomide (2) and trequinsin (3) are used as antiarrhytmic and antihypertensive agents, respectively. Sunepitron (4), a a 2-adrenoceptor antagonist, is under clinical trials for the treatment of anxiety and depression. Representatives of the third generation of antibacterial quinolone-3-carboxylic acids the blockbluster ofloxacin (5), its levorotatory enantiomer, levofloxacin (6), and rufloxacin (7) have gained wide acceptance for the treatment of bacterial infections of the respiratory and urinary tracts, skin, and soft tissues, as well as sexually transmitted diseases, and pazufloxacin (8) is under development. Praziquantel (9) is widely applied for the treatment of schistosomes- and cestode-caused infection in both veterinary and human therapies (Scheme 4). 

In reference 22, only qualitative responses were examined in the 12-experiment PB design, i.e., the selectivity factor and the resolution of the propranolol, praziquantel, and warfarin enantiomers. In Table 8, the resolution results of the three chiral substances are given. 

Staudt, U., Schmahl, G., Blaschke, G. and Mehlhorn, H. (1992) Light and scanning electron microscopy studies on the effects of the enantiomers of praziquantel and its main metabolite on Schistosoma mansoni in vitro. Parasitology Research 78, 392-397. 

Praziquantel (PZQ) is an isoquinoline derivative with most of the biological activity found in the levo enantiomer. The compound has no activity against nematodes, but it is highly effective against cestodes and trematodes. 

Lim and Ching [20] published about the separation of enantiomers of Praziquantel in an 8-column SMB plant. They designed the SMB process on the basis of elution chromatograms by their own method. 

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