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Administrator* 20.06.05


Pharmaceutical Chemistry and Technology, Karl-Franzens-University Graz Univ.-Prof. Dr. Winfried Wendelin

Building: Universitätsplatz 1, Room: 0.10
A-8010 Graz / Austria

Tel: +43-316-380-5374 (Office)
Tel: +43-316-380-5365 (Institute Secretary)
Fax: +43-316-380-9847

e-mail: Winfried.Wendelin@uni-graz.at





Technician:




Collaborator and Substitute:





Research:


Project 1:

Search for new leads: Basis Research in the field of partly hydrogenated hetero- und carbocycles:
Synthesis, resolution, enantio- und diastereoselective syntheses, elucidation of structure und stereochemistry by NMR, pharmacological and microbiological screening of the prepared compounds, investigation of the mechanism in case of highly active compounds.

Project 2:

Development of new Gyrase inhibitors with increased antibacterial activity:
Design including molecular-modelling-studies, synthesis, elucidation of structure und stereochemistry by NMR, molecular modelling studies with the prepared substances basing on quantitative NOE-experiments, testing of the antibacterial activity (cooperations), examination of the inhibition of bacterial DNA-Gyrase (cooperation).

Project 3:

Development of new inhibitors of the ergosterol biosynthesis, type "high energy intermediate analogues":
Design including molecular-modelling-studies, synthesis, elucidation of structure und stereochemistry by high resolution NMR, molecular modelling studies with the prepared substances basing on quantitative NOE-experiments, testing of the antifungal activity, examination of the inhibition of enzymes of the ergosterol biosynthesis (FWF-project).

Project 4:

Development of new heterocyclic anthelminthics (type fused azaheterocycles):
Synthesis, elucidation of structure und stereochemistry by NMR, testing of the anthelminthic activity (cooperation).

Project 5:

Development of new antiinflammatory drugs (type polyarylazoles and azines, and fused derivatives):
Design, synthesis, elucidation of structure and stereo-chemistry by NMR, testing of the analgesic, antiinflammatory and spasmolytic effects (cooperations).





Collaborations:

1. Existing cooperations:

2. Wanted new cooperations:

Cooperations with laboratories of universities, research institutes and pharmaceutical companies which are interested and potent in the screening and testing of new compounds for all types of pharmacological, antimicrobial, antiviral, antiparasitic, antitumor and biochemical effects and in the cooperative development of new drugs. Cooperations with biochemical and microbiological laboratories specialized in the testing of enzyme inhibitions (for example with isolated enzymes of the ergosterol biosynthesis, bacterial Gyrases, cyclooxygenases, lipoxygenases, etc.).

Note: According to preliminary tests a great number of the prepared heterocycles exert remarkable pharmacological and biological effects (among others hypotensive/bronchospasmolytic/antiphlogistic/diuretic/antimykotic/antiviral/antitrichomonal and anthelminthic effects). These compounds should be submitted to further tests and might be leads for the development of new drugs.





Publications:
  • W. Wendelin, E. Gößnitzer, D. Abou El Ella, Monatsh. Chem. 131, 353 (2000). Synthesis and Structure Elucidation of Pyrimidobenzimidazoles and Fused Derivatives II. Dodecahydrobenzimidazo[2,1-b]quinazolines and Decahydrobenzimidazo[2,1-b]benzo[h]quinazolines
  • K. Görlitzer, H. J. Baltrusch, E. Gößnitzer, W. Wendelin, Die Pharmazie 55, 35 (2000). Eine 1-Hydroxyindol-2-carbonsäure und eine 9-Hydroxy-ß-carbolin-4-carbonsäure aus dem Nifedipinanalogen Bis(cyanoethyl)ester
  • E. Gößnitzer, W. Wendelin, Monatsh. Chem. 132, 607 (2001). Synthese und Strukturaufklärung von Pyrimidobenzimidazolen und kondensierten Derivativen III. Decahydropyrimido[1,2-a] benzimidazol-2-ole und Octahydropyrimido[1,2-a]benzimidazole
  • E. Gößnitzer, W. Wendelin, Magn. Reson. Chem. 39, 471 (2001). Special Reactions of a,ß-unsaturated Ketones, II. Structure and stereochemistry of perhydro-5a,11a-epoxydibenz[b,f]oxepin-4a-ol, a bridged Diels-Alder dimer of 2-methylencyclohexanone
  • E. Gößnitzer, W. Wendelin, K. Schermanz, K. Frieberger, Monatsh. Chem. 132 (2001), in press Special Reactions of a,ß-Unsaturated Ketones, III. Formation and Structure Elucidation of Dimers of 2-Benzylideneketones: (5E)-5-Benzylidene-9ß-phenyl-trans-4a-1,2,3,4,4a,5,6,7,8,9a-decahydroxanthen- 4aa -ol and 3ß,5ß-Bis-(4-methoxyphenyl)- 2a,4a, 6a -trimethyl-4a -propionylcyclohexanone