Projects / Programmes
Synthesis, identification, and properties of potential pharmaceuticals
| 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 |
pharmaceuticals, cephalosporin, fluoroquinolones, aldose reductase, antimigrenics, benzoŠaĆpyrene diol epoxides (BPDE), triazenes, fluorescent probes, NMR
Researchers (7)
Organisations (2)
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.
