Of all marketed drugs, ca. 25% are sold as racemates, i.e., as 1.1 mixtures. Although it has been known for a long time that enantiomers can have very different biological properties, it is only during the last ca. ten years that the biomedical community in general has begun to recognize the importance of chirality for drug action and disposition. Indeed, the pharmacology, therapeutic efficacy, toxicity, biotransformations, and pharmacokinetics of enantiomeric drugs can differ drastically. As a result of the rapidly growing interest of a variety of biomedical scientists in drug chirality, a need has arisen for a comprehensive and readily accessible information source on and guide to the literature of drug chirality. Currently such information is scattered throughout the biomedical and chemical literature. Indeed, the lock of a """"""""Compendium of Chiral Drugs"""""""" is causing significant confusion and is clearly a hindrance to the development of the field. The purpose of this application is to obtain funds for the preparation of the CCD. During the project period of 18 months, the principal investigator will identify and review the literature on the chemistry and biology of ga. 700 chiral drugs from the chirality standpoint. The relevant information collected will be organized into the CCD. Each entry for a chiral drug will provide information and literature references on the chemistry, stereochemical identity or composition, pharmacology and toxicity, and metabolism and pharmacokinetics of the drug from the chirality standpoint. This information will be collected using an integrated chemical-structure-drawing and word-processing software and a micro-computer. A reputable scientific/medical publisher has indicated its intention to publish the manuscript of the CCD.
|Gal, J (1992) Rootworm pheromones: the root of a stereochemical mixup. Chirality 4:68-70|