Abstract
Abstract The chapter addresses the design of nonprotein, nonpeptide drug analogs. Strategies and applications of classical and nonclassical bioisosteres, rigid and semirigid analogs; homologation of alkyl chains; changes in ring size and ring‐position isomers; substitution of aromatic for aliphatic rings; alteration of stereochemistry; design of fragments of lead molecules; and variation of interatomic distances are discussed. Numerous examples from the literature of each type of molecular modification are presented, together with summaries of pharmacological consequences of the modifications. Advantages and disadvantages of each category are cited.
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