Abstract
About one-half of the 2050 pharmaceutical substances reported in the U.S. Pharmacopoeial Dictionary of Drug Names [1] are chiral compounds from both natural or synthetic origin. Chirality gives rise to the problem of stereoisomerism [2]: for instance, a widely used drug such as propranolol, the second most prescribed drug in the USA [3], exists as a pair of enantiomers. The main consequence of chirality for substances with biological activity is that the effects of the (+) enantiomer may be completely different from the effects of the ( ) enantiomer, as demonstrated by several examples in the field of pharmacology [4]. This difference may be, in certain instances, particularly relevant because one of the antipodes can be toxic to the host, whilst the other shows its expected pharmaceutical properties. The tragic case of thalidomide [4] is perhaps the most striking example of the influence of chirality on the biological activity of organic molecules. The dimension of the problem has to be stressed: in the USA, 12 of the 20 most prescribed drugs and 104 of the top 200 contain one asymmetric centre [3]. For these reasons chiral pharmaceutical substances require a complete stereochemical characterization (i.e. determination of absolute configuration and enantiomeric purity) before marketing the product.
Published Version
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