Pharmaceutisch Weekblad

, Volume 13, Issue 4, pp 161–166 | Cite as

The role of medicinal chemistry in drug research

  • W. Soudijn


Classical medicinal chemistry, that is molecular modifications of existing bioactive compounds, leading to me-too drugs with value added and often to me-too drugs which will never reach the market or to drugs in another pharmacological field than that originally intended, will be with us for a long time to come. The ultimate goal, however, is of course rational or at least semi-rational drug design. In some instances this goal seems to have already been reached as in the case of angiotensin-converting enzyme inhibitors and H2 antagonists. In the (near) future results from the steady progress in molecular biology in combination with computer-assisted drug modelling — possibly coupled with artificial intelligence techniques — will help the medicinal chemist in his efforts to attain this goal.


Chemistry, pharmaceutical Computers Drug development Molecular biology Research 


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  1. 1.
    Sanger GJ, King FD. From metoclopramide to selective gut motility stimulants and 5-HT3 receptor antagonists. Drug Design Deliv 1988;3:273–95.Google Scholar
  2. 2.
    Itil TM. Computer EEG profiles of antidepressants. New York: Industrial Pharmacology Futura Publishing Company, 1975:319–51.Google Scholar
  3. 3.
    Krapcho J, Spitzmiller ER, Turk CF. Substituted 2,3-dihydro-1,5-benzthiazepin-4-(5H)-ones and 3,4-dihydro-2-phenyl-(2H)-1,6-benzothiazocin-5-(6H)-ones. J Med Chem 1963;6:544–6.CrossRefGoogle Scholar
  4. 4.
    Kugita H, Inoue H, Ikezaki M, Konda M, Takeo S. Synthesis of 1,5-benzothiazepine derivatives. Chem Pharm Bull 1971;19:595–602.Google Scholar
  5. 5.
    Stähle H. Clonidine. Chronicles of drug discovery. New York: John Wiley & Sons, 1982:87–111.Google Scholar
  6. 6.
    Wilhelm M, De Stevens G. Antihypertensive agents. In: Jucker E, ed. Progress in drug research. Vol. 20. Basel: Birkhäuser Verlag, 1976:197–259.Google Scholar
  7. 7.
    Salvetti A, Leonetti G, Bernini GP, et al. Antihypertensive and renal effects of tertatolol, a new betablocking agent, in hypertensive patients. Am J Nephrol 1986;6(Suppl 2):45–9.PubMedGoogle Scholar
  8. 8.
    Beaufils M, Lantz B, Paillard F, Richet G. Effects of tertatolol in hypertensive patients with chronic renal failure. Am J Nephrol 1986;6(Suppl 2):50–4.PubMedGoogle Scholar
  9. 9.
    Ganellin CR. Cimetidine. In: Bindra JS, Lednicer D, eds. Chronicles of drug discovery. Vol. 1. New York: John Wiley & Sons, 1982:1–38.Google Scholar
  10. 10.
    Cushman DW, Ondetti MA, Cheung HS, Sabo EF, Antonaccio MJ, Rubin B. Angiotensin-converting enzyme inhibitors. Enzyme inhibitors as drugs. London: MacMillan Press, 1980:231–47.Google Scholar
  11. 11.
    Soudijn W. Angiotensin converting enzyme inhibitors. Pharm Weekbl [Sci] 1982;4:154–8.Google Scholar
  12. 12.
    Dolata DP, Leach AR, Prout K. WIZARD: AI in conformational analysis. J Comput Aided Mol Des 1987;1:73–85.CrossRefPubMedGoogle Scholar
  13. 13.
    Sokoloff P, Giros B, Martres MP, Bouthenet ML, Schwartz JC. Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics. Nature 1990;347:146–50.CrossRefPubMedGoogle Scholar

Copyright information

© Royal Dutch Association for Advancement of Pharmacy 1991

Authors and Affiliations

  • W. Soudijn
    • 1
  1. 1.Centre for Bio-Pharmaceutical Sciences, Division of Medicinal ChemistryLeiden UniversityRA LeidenThe Netherlands

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