ABSTRACT

A lead compound is active because it can interact with some or all of the binding regions present in a binding site. The functional groups involved in binding interactions may not be in the ideal positions for effective binding, so various tactics could be used to alter their relative positions such that both groups bind more strongly. If the binding groups are at either end of an alkyl chain then the chain could be extended or contracted to vary the separation and to improve the overlap of the binding groups with their relevant binding regions. If the lead compound contains an aromatic ring, it is possible to carry out reactions on the lead compound such that substituents are attached to different positions of the aromatic ring. The basicity of aromatic or heteroaromatic amines can be modified in a more predictable fashion by varying the substituents on the aromatic/heteroaromatic ring.