Robert Weis

Summary

Affiliation: University of Graz
Country: Austria

Publications

  1. ncbi request reprint New 4-aminobicyclo[2.2.2]octane derivatives and their activities against Plasmodium falciparum and Trypanosoma b. rhodesiense
    Werner Seebacher
    Institute of Pharmaceutical Chemistry and Pharmaceutical Technology, Karl Franzens University, Universitatsplatz 1, A 8010, Graz, Austria
    Eur J Pharm Sci 21:225-33. 2004
  2. doi request reprint Antimycobacterial and H1-antihistaminic activity of 2-substituted piperidine derivatives
    Robert Weis
    Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Universitatsplatz 1, A 8010 Graz, Austria
    Bioorg Med Chem 16:10326-31. 2008
  3. ncbi request reprint Antiplasmodial and antitrypanosomal activity of new esters and ethers of 4-dialkylaminobicyclo[2.2.2]octan-2-ols
    Robert Weis
    Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, Karl Franzens University, Universitatsplatz 1, A 8010 Graz, Austria
    Eur J Pharm Sci 28:361-8. 2006
  4. ncbi request reprint Antimycobacterial activity of diphenylpyraline derivatives
    Robert Weis
    Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, Karl Franzens University, Universitatsplatz 1, A 8010 Graz, Austria
    Eur J Med Chem 43:872-9. 2008
  5. doi request reprint Antiplasmodial and antitrypanosomal activity of bicyclic amides and esters of dialkylamino acids
    Johanna Faist
    Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Universitatsplatz 1, A 8010 Graz, Austria
    Bioorg Med Chem 17:3595-603. 2009
  6. doi request reprint Synthesis of bicyclic amines and their activities against Trypanosoma brucei rhodesiense and Plasmodium falciparum K1
    Robert Weis
    Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, Karl Franzens University, Universitatsplatz 1, A 8010, Graz, Austria
    Arch Pharm Res 31:688-97. 2008
  7. ncbi request reprint Bicyclo[2.2.2]octyl esters of dialkylamino acids as antiprotozoals
    Christian Schlapper
    Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, Karl Franzens University, Universitatsplatz 1, A 8010 Graz, Austria
    Bioorg Med Chem 15:5543-50. 2007
  8. doi request reprint Antiplasmodial and antitrypanosomal activities of aminobicyclo[2.2.2]octyl omega-aminoalkanoates
    Christian Schlapper
    Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, Karl Franzens University, Universitatsplatz 1, A 8010 Graz, Austria
    Eur J Med Chem 44:736-44. 2009
  9. ncbi request reprint Antiprotozoal activities of new bis-chlorophenyl derivatives of bicyclic octanes and aza-nonanes
    Heinrich Berger
    Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, Karl Franzens University, Universitatsplatz 1, A 8010 Graz, Austria
    Bioorg Med Chem Lett 16:5457-61. 2006
  10. doi request reprint Dialkylaminoalkyl derivatives of bicyclic compounds with antiplasmodial activity
    Johanna Faist
    Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Universitatsplatz 1, A 8010 Graz, Austria
    Bioorg Med Chem 18:6796-804. 2010

Collaborators

Detail Information

Publications23

  1. ncbi request reprint New 4-aminobicyclo[2.2.2]octane derivatives and their activities against Plasmodium falciparum and Trypanosoma b. rhodesiense
    Werner Seebacher
    Institute of Pharmaceutical Chemistry and Pharmaceutical Technology, Karl Franzens University, Universitatsplatz 1, A 8010, Graz, Austria
    Eur J Pharm Sci 21:225-33. 2004
    ..68microM) of the so far prepared 4-amino-6,7-diarylbicyclo[2.2.2]octane derivatives, but is distinctly less active than suramin (IC(50)=0.0075microM)...
  2. doi request reprint Antimycobacterial and H1-antihistaminic activity of 2-substituted piperidine derivatives
    Robert Weis
    Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Universitatsplatz 1, A 8010 Graz, Austria
    Bioorg Med Chem 16:10326-31. 2008
    ..A correlation between the two activities was not detected for those compounds...
  3. ncbi request reprint Antiplasmodial and antitrypanosomal activity of new esters and ethers of 4-dialkylaminobicyclo[2.2.2]octan-2-ols
    Robert Weis
    Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, Karl Franzens University, Universitatsplatz 1, A 8010 Graz, Austria
    Eur J Pharm Sci 28:361-8. 2006
    ..The 4-chlorobenzoate 9b exhibited good antiplasmodial activity and low cytotoxicity. The most active antiplasmodial agent was the benzhydryl ether 13c which was nearly as active as chloroquine against sensitive strains...
  4. ncbi request reprint Antimycobacterial activity of diphenylpyraline derivatives
    Robert Weis
    Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, Karl Franzens University, Universitatsplatz 1, A 8010 Graz, Austria
    Eur J Med Chem 43:872-9. 2008
    ..The antimycobacterial potency was in general increased by substitution in ring position 2. The most promising modifications were a 2-isopropyl derivative and a 1,2-diphenyl analogue...
  5. doi request reprint Antiplasmodial and antitrypanosomal activity of bicyclic amides and esters of dialkylamino acids
    Johanna Faist
    Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Universitatsplatz 1, A 8010 Graz, Austria
    Bioorg Med Chem 17:3595-603. 2009
    ..Structure-activity relationships were discussed. Particularly the ester compounds showed good antiplasmodial and antitrypanosomal activity and a single compound was tested in vivo against Plasmodium berghei...
  6. doi request reprint Synthesis of bicyclic amines and their activities against Trypanosoma brucei rhodesiense and Plasmodium falciparum K1
    Robert Weis
    Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, Karl Franzens University, Universitatsplatz 1, A 8010, Graz, Austria
    Arch Pharm Res 31:688-97. 2008
    ..2.2]nonanes. Some of the 4-aminobicyclo[2.2.2]oct-2-ylamines exhibit moderate in vivo activity in mice against Trypanosoma brucei brucei...
  7. ncbi request reprint Bicyclo[2.2.2]octyl esters of dialkylamino acids as antiprotozoals
    Christian Schlapper
    Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, Karl Franzens University, Universitatsplatz 1, A 8010 Graz, Austria
    Bioorg Med Chem 15:5543-50. 2007
    ..The antiprotozoal activities were remarkably increased by insertion of a second basic centre. The selectivity indices of the most active compounds are superior in the bicyclo-octane series...
  8. doi request reprint Antiplasmodial and antitrypanosomal activities of aminobicyclo[2.2.2]octyl omega-aminoalkanoates
    Christian Schlapper
    Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, Karl Franzens University, Universitatsplatz 1, A 8010 Graz, Austria
    Eur J Med Chem 44:736-44. 2009
    ..The most active antiplasmodial ester was as active as chloroquine. One of the new compounds exhibited the highest antitrypanosomal activity and selectivity of all bicyclo-octane derivatives prepared so far...
  9. ncbi request reprint Antiprotozoal activities of new bis-chlorophenyl derivatives of bicyclic octanes and aza-nonanes
    Heinrich Berger
    Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, Karl Franzens University, Universitatsplatz 1, A 8010 Graz, Austria
    Bioorg Med Chem Lett 16:5457-61. 2006
    ..Especially the bis-(chlorophenyl)-azabicyclo[3.2.2]nonanes exhibit promising antitrypanosomal activity and were tested in vivo against Trypanosoma brucei brucei featuring moderate activities...
  10. doi request reprint Dialkylaminoalkyl derivatives of bicyclic compounds with antiplasmodial activity
    Johanna Faist
    Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Universitatsplatz 1, A 8010 Graz, Austria
    Bioorg Med Chem 18:6796-804. 2010
    ..Some of the more potent compounds were tested in vivo against Plasmodium berghei showing weak to moderate activity. A single compound was able to increase the mean survival days of infected mice...
  11. ncbi request reprint Synthesis and evaluation of the antitrypanosomal and antiplasmodial activities of new 4-aminobicyclo[2.2.2]octane derivatives
    Werner Seebacher
    Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, Karl Franzens University, Universitatsplatz 1, A 8010 Graz, Austria
    Eur J Med Chem 40:888-96. 2005
    ..The methylthiosemicarbazones show moderate antiprotozoal activities whereas some of the esters of piperonylic acid, homopiperonylic acid and 2-naphtoic acid exhibit remarkable antitrypanosomal and antiplasmodial activity...
  12. doi request reprint Antiprotozoal activity of bicyclic diamines with a N-methylpiperazinyl group at the bridgehead atom
    Johanna Faist
    Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Stremayrgasse 16, A 8010 Graz, Austria
    Bioorg Med Chem 21:4988-96. 2013
    ..The results of the newly synthesized compounds were compared with the activities of already synthesized compounds and of drugs in use. Structure-activity relationships were discussed. ..
  13. ncbi request reprint Epimers of bicyclo[2.2.2]octan-2-ol derivatives with antiprotozoal activity
    Christian Schlapper
    Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, Karl Franzens University, Universitatsplatz 1, A 8010 Graz, Austria
    Eur J Med Chem 43:800-7. 2008
    ..The most active antitrypanosomal agents were the benzoate 8b and the 4-chlorobenzoate 9b of the 4-pyrrolidino series. The nicotinate 10a and the isonicotinate 11a showed the highest antiplasmodial activities...
  14. doi request reprint New N-methylpiperazinyl derivatives of bicyclic antiprotozoal compounds
    Johanna Faist
    Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, Karl Franzens University, Universitatsplatz 1, A 8010 Graz, Austria
    Eur J Med Chem 47:510-9. 2012
    ..023μM) and selectivity (S.I.=IC(50) (Cytotox.)/IC(50) (P. falciparum)=2188) than the antimalarial drug chloroquine (IC(50)=0.15μM, S.I.=1257)...
  15. doi request reprint Novel azabicyclo[3.2.2]nonane derivatives and their activities against Plasmodium falciparum K1 and Trypanosoma brucei rhodesiense
    Heinrich Berger
    Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, Karl Franzens University, Universitatsplatz 1, A 8010 Graz, Austria
    Bioorg Med Chem 16:6371-8. 2008
    ..Some of the new compounds are amongst the most active antitrypanosomal agents in this series, and the selectivity index of a single derivative is superior in the 2-azabicyclo-nonane series...
  16. doi request reprint Alkyl and dialkylaminoethyl derivatives of 5-amino-2-azabicyclo[3.2.2]nonanes and their antiplasmodial and antitrypanosomal activities
    Johanna Faist
    Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, Karl Franzens University, Universitatsplatz 1, A 8010 Graz, Austria
    Eur J Med Chem 45:179-85. 2010
    ..In comparison all of the new N-(2-dialkylaminoethyl) analogues possessed a much better selectivity and a single of these compounds showed even better antiplasmodial activity and selectivity than chloroquine...
  17. ncbi request reprint Antiprotozoal activities of new bicyclo[2.2.2]octan-2-imines and esters of bicyclo[2.2.2]octan-2-ols
    Werner Seebacher
    Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, Karl Franzens University, Universitatsplatz 1, A 8010 Graz, Austria
    Eur J Pharm Sci 24:281-9. 2005
    ..2.2]octan-2-yl benzoate exhibit attractive antimalarial activity (IC(50)=0.23-0.72 microM). Two bicyclooctanone oximes are even as active as chloroquine (IC(50)=0.08-0.15 microM, chloroquine: IC(50)=0.12 microM against sensitive strains)...
  18. ncbi request reprint Synthesis of 2-azabicyclo[3.2.2]nonanes from bicyclo[2.2.2]octan-2-ones and their activities against Trypanosoma brucei rhodesiense and Plasmodium falciparum K1
    Werner Seebacher
    Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, Karl Franzens University, A 8010 Graz, Austria
    J Pharm Pharm Sci 8:578-85. 2005
    ..2.2]octan-2-ones to investigate the influence of the replacement of the rigid bicyclo-octane structure by the more flexible bicyclo-nonane system on the antiplasmodial and antitrypanosomal activity...
  19. doi request reprint Antiprotozoal activity of bicycles featuring a dimethylamino group at their bridgehead
    Johanna Faist
    Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Schubertstraße 1, A 8010 Graz, Austria Electronic address
    Bioorg Med Chem 24:3781-9. 2016
    ..The results of the biological tests of the novel compounds were compared with the activities of already synthesized compounds and of drugs in use. Structure-activity relationships were discussed. ..
  20. doi request reprint New derivatives of 7-chloroquinolin-4-amine with antiprotozoal activity
    Johanna Faist
    Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Austria Electronic address
    Bioorg Med Chem . 2016
    ..However, in comparison to chloroquine, the activity of the new compounds was decreased much less in the resistant strain. Several possessed activity against both strains in low nanomolar concentration...
  21. doi request reprint Synthesis of 3-azabicyclo[3.2.2]nonanes and their antiprotozoal activities
    Werner Seebacher
    Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, Karl Franzens University, Schubertstrasse 1, Graz A 8010, Austria Electronic address
    Bioorg Med Chem Lett 25:1390-3. 2015
    ..For the first time, a distinct in vivo activity was observed against Plasmodium berghei in a mouse model. The active compound was further investigated. ..
  22. doi request reprint Synthesis of new 4-phenylpyrimidine-2(1H)-thiones and their potency to inhibit COX-1 and COX-2
    Werner Seebacher
    Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Universitatsplatz 1, 8010 Graz, Austria Electronic address
    Eur J Med Chem 101:552-9. 2015
    ..Structure-activity-relationships and physicochemical parameters are discussed. Pharmacophore screening and docking studies were carried out for the most active compound. ..
  23. ncbi request reprint Investigations on the formation of 4-aminobicyclo[2.2.2]-octanones
    Werner Seebacher
    Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, Karl Franzens University, Universitatsplatz 1, A 8010 Graz, Austria
    Molecules 10:521-33. 2005
    ..The reaction of ethyl styryl ketone with thiocyanates of secondary amines yielded cyclohexanone derivatives instead of the expected bicyclo- octanones. Their structures were established by means of a single crystal structure analysis...