The Relation Between Chemical Structure and Biological Activity

Abstract

Abstract The number of new compounds being synthesised every year increases in an exponential way. Consequently investigations of the relation between chemical structure and biological activity similarly increases. Studies of this kind provide information about which moieties in the molecule are essential to obtain potent and specific drugs. Furthermore they may give a clue to the mechanism of the action of drugs. Two major aspects of structure-activity studies raise questions. Firstly, how do alterations in the chemical structure alter the geometry of the molecule and its physical properties? Secondly, what does the fact of biological activity imply? Do different drugs produce the same kind of effect; do they have an identical mechanism of action? In this review the value of studies on structure-activity, as well as some of the pitfalls and limitations of interpretation will be discussed. Work done on the pharmacology of the nervous system will be used to illustrate this discussion.