Evaluation of activity parameters of potential inhibitors of aldose reductase - a contribution to therapy of chronic diabetic complications.Supervisor: Ing. Pavel Májek, PhD.
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|Project description:||Inhibitors of the aldose reductase enzyme (ALR2) are drugs capable to prevent a tissue injure caused by diabetes, prevalently by type II, which is insulin-resistant and it is being spread epidemiologically. 3D structure of the ALR2 enzyme was already estimated from various biological sources and in complexes with different adducts. In this project we wish utilize connectivity with existing international and Slovak projects solved at IEPh SAS which are targeted to the projection of new ALR2 inhibitors missing in clinical praxis. We will use the experimental results on the inhibition activity for the pyridoindole-like (PyInd) substances which have been already synthesized and tested at Institute. First off, we will determine the best theoretical way of estimation of activity by means of the methods of computational chemistry. Then we will create a database of potential PyInd ALR2 inhibitors which shall fulfill the foregoing theoretical criteria as well as other conditions made for pharmacologically active substances. The most attractive derivatives will be proposed for synthesis and use in the connecting projects.|
|Kind of project:||VEGA ()|
|Department:||Department of Analytical Chemistry (IAC FCFT)|
|Project status:||Successfully completed|
|Project start date :||01. 01. 2007|
|Project close date:||31. 12. 2009|
|Number of workers in the project:||1|
|Number of official workers in the project:||0|