ABSTRACT
Currently, much attention has been focused on the interaction of small molecules with biological macromolecules. The search for selective enzyme inhibitors and receptor agonists or antagonists is one of the keys for target-oriented research in the pharmaceutical industry. Increasing understanding of the mechanism of drug interaction on a molecular level has led to the increasing awareness of the importance of chirality as the key to the efficacy of many drug products. It is now known that, in many cases, only one stereoisomer of a drug substance is required for efficacy and the other stereoisomer is either inactive or exhibits considerably reduced activity. Pharmaceutical companies are aware that, where appropriate, new drugs for the clinic should be homochiral to avoid the possibility of unnecessary side effects due to an undesirable stereoisomer. In many cases where the switch from racemate drug substance to enantiomerically pure compound is feasible, there is the opportunity to double the use of an industrial process. The physical characteristic of enantiomers versus racemates may confer processing or formulation advantages.
