Investigations on praziquantel (PZQ) started fifty years ago by a cooperation between Bayer AG and Merck KGaA. Until today PZQ is the drug of choice for schistosomiasis in human medicine and used in many combinations with antinematode drugs in veterinary medicine. The Sm.TRPMPZQ, a Ca2+ ‐permeable transient receptor potential (TRP) channel, has been discovered as primary target of PZQ during the last decade. Furthermore, there is a short overview of routes of large‐scale synthesis of racemic and pure (R)‐PZQ. Until now racemic PZQ is used in veterinary and human medicine. In 2012 the Pediatric Praziquantel Consortium started PZQ chemistry and process development of pure (R)‐PZQ for human application. It is hoped that (R)‐PZQ will become available for pediatric use soon. The knowledge of the binding pocket of PZQ in Sm.TRPMPZQ allows to design synthesis of PZQ‐derivatives of the next generation for a target‐site directed screening. A similar screening should also be started for Fasciola hepatica TRPMPZQ.
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ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Alcohols
Alcohols P 0110Easy Access to Derivatives of 2-(Hydroxymethyl)propane-1,2,3-triol (Isoerythritol) with up to Four Separately Addressable Functionalities. -Cyclic sulfite (II) is oxidized by ruthenium tetroxide to give (VIII) which is protected with acetic anhydride. The resulting acetate can be treated with various nucleophiles leading to the corresponding monosubstitution products and after hydrolysis and aqueous work-up monoacetylated triols are isolated. Nucleophilic ring opening results in formation of open-chain sulfates. -(FRIEDRICH, M.; SAVCHENKO, A. I.; WAECHTLER, A.; DE MEIJERE*, A.; Eur.
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