Medicinal Chemistry of Drugs with Active Metabolites Following Conjugation

Title:Medicinal Chemistry of Drugs with Active Metabolites Following Conjugation

Volume: 13 Issue: 11

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

Affiliation:

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

Abstract: 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.

Cite this article as:

Kalász Huba, Petroianu Georg, Hosztafi Sándor, Darvas Ferenc, Csermely Tamás, Adeghate Ernest, Siddiq Afshan and Tekes Kornélia, Medicinal Chemistry of Drugs with Active Metabolites Following Conjugation, Mini-Reviews in Medicinal Chemistry 2013; 13 (11) . https://dx.doi.org/10.2174/1389557511313110002