Design of Analogues and Prodrugs

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Chapter: Medicinal Chemistry : Concepts of Drug Design

The term prodrug implies an appropriate derivative of a drug. The prodrugs are discovered by the screening of active metabolites after in vivo biotransformation that are formed from parent compounds.


DESIGN OF ANALOGUES AND PRODRUGS

Drug design involves the development of analogues and prodrugs by some chemical modiļ¬cations from the lead molecule or from a parent compound by modifying the carbon skeletal transformation or by the synthesis of compounds of the same nucleus with various substitutions. Analogues can also be synthesized by changing the position of substitution group. For example, synthesis of trans-diethylstilbosterol by the modiļ¬cation of oestradiol produced better oestrogenic activity than the latter one.

The term prodrug implies an appropriate derivative of a drug. The prodrugs are discovered by the screening of active metabolites after in vivo biotransformation that are formed from parent compounds. For example, phenylbutazone is transformed into oxyphenbutazone by hydroxylation reaction mediated by phase I (nonsynthetic) metabolic reaction.


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