Medicinal chemistry of drugs with active metabolites following conjugation

Huba Kalász, Georg Petroianu, Sándor Hosztafi, Ferenc Darvas, Tamás Csermely, Ernest Adeghate, Afshan Siddiq, Kornélia Tekes

Research output: Contribution to journalReview articlepeer-review

7 Citations (Scopus)


Authorities of Drug Administration in the United States of America approved about 5000 drugs for use in the therapy or management of several diseases. About two hundred of these drugs have active metabolites and the knowledge of their medicinal chemistry is important both in medical practice and pharmaceutical research. This review gives a detailed description of the medicinal chemistry of drugs with active metabolites generated after conjugation. This review focused on glucuronide-, acetyl-, sulphate- and phosphate-conjugation of drugs, converting the drug into an active metabolite. This conversion essentially changed the lipophilicity of the drug.

Original languageEnglish
Pages (from-to)1550-1563
Number of pages14
JournalMini-Reviews in Medicinal Chemistry
Issue number11
Publication statusPublished - Jan 1 2013


  • Acetyl conjugation
  • Glucuronide conjugation
  • Metabolic conjugation
  • Morphine-6-glucuronide
  • Phosphate conjugation
  • Prodrugs
  • Sulphate conjugation

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology
  • Drug Discovery
  • Cancer Research


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