2014
DOI: 10.1016/j.bmcl.2014.07.039
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Development of chiral praziquantel analogues as potential drug candidates with activity to juvenile Schistosoma japonicum

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Cited by 20 publications
(20 citation statements)
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“…Overall, all chiral PZQ derivatives display modest activity in vivo compared to that of PZQ1. Intriguingly, the size of the ring with a carbonyl group in these derivatives had an appreciable impact on R isomers, increasing their activity, but had almost no effect on S isomers (55). Using organometallic moieties such as ferrocenyl (already present in anticancer, antibacterial, and antimalarial drugs [56][57][58]) Fc-PZQ derivatives (types A and B, Fig.…”
Section: And S-trans-and S-cis-4-oh-pzq While Pzq2 Is Metabolized Tomentioning
confidence: 99%
“…Overall, all chiral PZQ derivatives display modest activity in vivo compared to that of PZQ1. Intriguingly, the size of the ring with a carbonyl group in these derivatives had an appreciable impact on R isomers, increasing their activity, but had almost no effect on S isomers (55). Using organometallic moieties such as ferrocenyl (already present in anticancer, antibacterial, and antimalarial drugs [56][57][58]) Fc-PZQ derivatives (types A and B, Fig.…”
Section: And S-trans-and S-cis-4-oh-pzq While Pzq2 Is Metabolized Tomentioning
confidence: 99%
“…( R )-PZQ and ( S )-PZQ were obtained with an improved method based on the reported procedure, 17 with the enantiomeric excess value >99% by high-performance liquid chromatography.…”
Section: Methodsmentioning
confidence: 99%
“…Furthermore, the presence of zone 4 evidences the recycling of the desorbent, which means less fresh desorbent should be consumed, is what increases the efficiency of the process. This is an interesting scenario, which allows further studies involving racemization and synthesis of PZQ analogs to fight against resistant and immature parasites . The actual SMB unit used in the present paper is going to help the development of control strategies, like NMPC, to provide in a semipreparative scale enantiomers with different optical purities, maximum productivity, and minimum desorbent consumption.…”
Section: Introductionmentioning
confidence: 99%
“…Trying to overcome this issue, researches are still in progress to generate a pioneering medicine to fight against many parasitic diseases mainly using racemates (eg, capsules) [4][5][6][7] or L-and D-PZQ in different proportions (eg, orally dispersible tablets with one fourth the size of commercial ones). 8 Better understanding of mechanism of action of pure PZQ enantiomers against Schistosoma bodies, [9][10][11][12][13] new molecular formulas to fight against adult 10,11,[14][15][16] and juvenile 13,17,18 worms should be also important issues to be studied using pure L-PZQ. Nowadays, racemate (rac-PZQ) is used in most of these studies.…”
Section: Introductionmentioning
confidence: 99%