title: Medicinal chemistry of drugs with active metabolites following 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.
authors.affiliation: Department of Pharmacology and Pharmacotherapy, Semmelweis University, Budapest, Hungary. drkalasz@gmail.com
authors.forename: Huba
authors.initials: H
authors.lastname: Kalász
authors.forename: Georg
authors.initials: G
authors.lastname: Petroianu
authors.forename: Sándor
authors.initials: S
authors.lastname: Hosztafi
authors.forename: Ferenc
authors.initials: F
authors.lastname: Darvas
authors.forename: Tamás
authors.initials: T
authors.lastname: Csermely
authors.forename: Ernest
authors.initials: E
authors.lastname: Adeghate
authors.forename: Afshan
authors.initials: A
authors.lastname: Siddiq
authors.forename: Kornélia
authors.initials: K
authors.lastname: Tekes
mesh_terms: D000085:Acetates / Q000737:chemistry; D002626:Chemistry, Pharmaceutical; D020719:Glucuronides / Q000737:chemistry; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D004364:Pharmaceutical Preparations / Q000737:chemistry / Q000378:metabolism*; D010710:Phosphates / Q000737:chemistry; D013431:Sulfates / Q000737:chemistry
chemical_list: D000085:Acetates; D020719:Glucuronides; D004364:Pharmaceutical Preparations; D010710:Phosphates; D013431:Sulfates