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Projects / Programmes source: ARRS

Development of biologicaly active peptidomimetics

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Research activity

Code Science Field Subfield
1.09.00  Natural sciences and mathematics  Pharmacy   

Code Science Field
B740  Biomedical sciences  Pharmacological sciences, pharmacognosy, pharmacy, toxicology 
Keywords
peptidomimetics, drug design, blood coagulation, thrombin, inhibitor
Evaluation (rules)
source: COBISS
Citations Citations for bibliographic records in COBIB.SI that are linked to records in citation databases
source: WoS source: Scopus source: COBISS
Researchers (13)
no. Code Name and surname Research area Role Period No. of publications
1.  15490  PhD Pegi Ahlin Grabnar  Pharmacy  Researcher  2002 - 2003  191 
2.  16328  PhD Matej Breznik  Pharmacy  Researcher  2002  52 
3.  11102  PhD Rok Grahek  Chemistry  Researcher  2002 - 2003  86 
4.  12942  PhD Janez Kerč  Pharmacy  Researcher  2002 - 2003  240 
5.  15460  PhD Samo Kreft  Pharmacy  Researcher  2002 - 2003  767 
6.  09924  PhD Anton Lavrič  Pharmacy  Researcher  2002 - 2003  57 
7.  17437  Marjeta Mulej    Researcher  2002 - 2003  0 
8.  12634  PhD Mateja Salobir  Chemistry  Researcher  2002 - 2003  38 
9.  00830  PhD Anton Štalc  Biotechnology  Researcher  2002 - 2003  159 
10.  01878  PhD Uroš Urleb  Pharmacy  Principal Researcher  2002 - 2003  379 
11.  15956  MSc Darko Zadravec  Pharmacy  Researcher  2002 - 2003  13 
12.  17438  Damijana Zalar    Researcher  2002 - 2003  0 
13.  18633  PhD Anamarija Zega  Pharmacy  Researcher  2002 - 2003  178 
Organisations (2)
no. Code Research organisation City Registration number No. of publications
1.  0258  Lek Pharmaceutical Company d.d.  Ljubljana  1732811  9,974 
2.  0787  University of Ljubljana, Faculty of Pharmacy  Ljubljana  1626973  16,992 
Abstract
Biologically active inhibitors of thrombin will be developed. Thrombin is the key serine proteinase of the coagulation cascade and therefore a suitable target for the inhibition of blood coagulation. In the present project peptidomimetics will be designed and synthetised according to the medicinal chemistry principles. In order to obtain new lead compounds, plant and fungi extracts will be prepared as well and tested in vitro. Active fractions will be isolated and their structure determined by different scpectroscopic methods. The isolated compounds - lead compounds- will serve as a new starting-point for the development of (peptido)mimetics with antithrombotic activity. Basic properties of the newly synthsized compounds will be determind, using different physical and chemical methods. The potential therapeutic value of the new compounds will be estimated on the basis of various enzyme and coagulation tests; the inhibitory activity of the products on thrombin and trypsin will be determined spectrophotometrically, using an appropriate chromogenic substrat. For the most promising compounds the basic toxicity studies will be performed. The project also includes pre-formulation studies which should contribute to a more reliable evaluation of biological effects and to the optimization of the synthesis of new potential drugs.
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