About: Development of novel acetylcholinesterase inhibitors as treatment of Myasthenia Gravis     Goto   Sponge   NotDistinct   Permalink

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  • The treatment of autoimmune disease Myasthenia gravis (MG) is based on a combination of various drugs. The acetylcholinesterase (AChE) inhibitors are used at the first stage of MG (e.g. pyridostigmine bromide) as a symptomatic treatment. These drugs are effective both in peripheral and central nervous system (cross blood-brain barrier - BBB). Their administration causes a huge amount of undesirable effects and it is necessary to reduce their dosage. The preparation, in vitro testing and structure-activity relationship (SAR) of novel AChE inhibitors will be done in our project. Novel compounds will be designed as the bispyridinium molecules with various functional groups and linkers. The bisquaternary structure should guarantee the minimal penetration through BBB and their peripheral effectiveness. SAR will be considered via experimental results (in vitro - IC50) and quantitatively via computer programs (QSAR). The peripheral AChE inhibitors suitable for application in vivo on animals and for further testing as relevant candidates for MG treatment should become the project results. (en)
  • 1) Příprava periferních inhibitorů acetylcholinesterasy (symetrické i nesymetrické sloučeniny) 2) In vitro hodnocení (IC50) připravených sloučenin 3) Hodnocení vztahů mezi strukturou a aktivitou připravených látek 4) Doporučení perspektivních periferních inhibitorů AChE k testování in vivo. (cs)
Title
  • Vývoj nových inhibitorů acetylcholinesterasy jako léčiv Myasthenia gravis (cs)
  • Development of novel acetylcholinesterase inhibitors as treatment of Myasthenia Gravis (en)
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  • Myasthenia gravis; acetylcholinesterasa; inhibitor; syntéza; in vitro (en)
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