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Projects / Programmes source: ARIS

Synthesis, identification, and properties of potential pharmaceuticals

Research activity

Code Science Field Subfield
1.09.00  Natural sciences and mathematics  Pharmacy   

Code Science Field
P390  Natural sciences and mathematics  Organic chemistry 
P320  Natural sciences and mathematics  Nucleic acids, protein synthesis 
Keywords
pharmaceuticals, cephalosporin, fluoroquinolones, aldose reductase, antimigrenics, benzoŠaĆpyrene diol epoxides (BPDE), triazenes, fluorescent probes, NMR
Evaluation (rules)
source: COBISS
Researchers (7)
no. Code Name and surname Research area Role Period No. of publicationsNo. of publications
1.  00184  PhD Franc Kozjek  Pharmacy  Researcher  1997 - 1999  487 
2.  05044  PhD Andrej Petrič  Chemistry  Head  1997 - 1999  217 
3.  02310  PhD Slovenko Polanc  Chemistry  Researcher  1999  550 
4.  09066  PhD Stanislav Primožič  Pharmacy  Researcher  1997 - 1999  302 
5.  06061  PhD Boris Šket  Chemistry  Researcher  1997 - 1999  349 
6.  10249  PhD Marjan Valenčič  Chemical engineering  Researcher  1998 - 1999  21 
7.  06940  PhD Barbara Zajc  Chemistry  Researcher  1997 - 1999  49 
Organisations (2)
no. Code Research organisation City Registration number No. of publicationsNo. of publications
1.  0103  University of Ljubljana, Faculty of Chemistry and Chemical Technology  Ljubljana  1626990  23,454 
2.  0787  University of Ljubljana, Faculty of Pharmacy  Ljubljana  1626973  17,415 
Abstract
The aim of the proposed project is to develop synthetic routes to new potential pharmaceuticals and probes for in vitro and in vivo investigation of biological processes. We will investigate new possibilities of removal of tert-butyl protection from the carboxylate group in b-lactames under mild conditions, using inexpensive reagents. The results will be applied in the production of cephalosporin antibiotics. The pharmacokinetic properties of fluoroquinolone antibiotics and the relation of their content in plasma and saliva will be investigated. Using quantum mechanic descriptors determination of contributions of different interactions to the binding of compounds to aldose reductase will be attempted. We intend to develop new synthetic pathways to indol-containing anti migrene agents. Modified oligonucleotides, containing guanine, modified at the exocyclic amine functional group by benzoŠaĆpyrene, will be prepared. These will serve as substrates for investigation of mutagenic effects of common polutant, benzoŠaĆpyrene diol epoxide. As potential antitumor agents we intend to prepare different triazene derivatives, in particular such derivatives which are inaccessible through classical synthetic routes. Based on the structure of 2-(1,1-dicyanopropenyl-2)-6-dimethylamino-naphtalene (DDNP), new fluorescent probes for in vitro and in vivo investigation of dopaminergic D2 system will be prepared and characterized. The structure of DNP will be modified at the amine functional group to enable for the attachment of a specific ligand. Using classical and modern NMR techniques structures of compounds in solutions will be studied.
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