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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