Medicinal Chemistry of Drugs with Active Metabolites Following Conjugation

Author(s): Huba Kalász, Georg Petroianu, Sándor Hosztafi, Ferenc Darvas, Tamás Csermely, Ernest Adeghate, Afshan Siddiq, Kornélia Tekes

Journal Name: Mini-Reviews in Medicinal Chemistry

Volume 13 , Issue 11 , 2013

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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.

Keywords: Prodrugs, metabolic conjugation, morphine-6-glucuronide, glucuronide conjugation, acetyl conjugation, sulphate conjugation, phosphate conjugation.

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Article Details

Year: 2013
Published on: 26 August, 2013
Page: [1550 - 1563]
Pages: 14
DOI: 10.2174/1389557511313110002
Price: $65

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