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

doi:10.2174/1389557511313110002

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

Department of Anatomy

Research output: Contribution to journal › Review article › peer-review

7 Citations (Scopus)

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.

Original language	English
Pages (from-to)	1550-1563
Number of pages	14
Journal	Mini-Reviews in Medicinal Chemistry
Volume	13
Issue number	11
DOIs	https://doi.org/10.2174/1389557511313110002
Publication status	Published - Jan 1 2013

Keywords

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

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.2174/1389557511313110002

Cite this

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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.",

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T1 - Medicinal chemistry of drugs with active metabolites following conjugation

AU - Kalász, Huba

AU - Petroianu, Georg

AU - Hosztafi, Sándor

AU - Darvas, Ferenc

AU - Csermely, Tamás

AU - Adeghate, Ernest

AU - Siddiq, Afshan

AU - Tekes, Kornélia

PY - 2013/1/1

Y1 - 2013/1/1

N2 - 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.

AB - 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.

KW - Acetyl conjugation

KW - Glucuronide conjugation

KW - Metabolic conjugation

KW - Morphine-6-glucuronide

KW - Phosphate conjugation

KW - Prodrugs

KW - Sulphate conjugation

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Medicinal chemistry of drugs with active metabolites following conjugation

Abstract

Keywords

ASJC Scopus subject areas

UN SDGs

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