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Drug Racemization and Its Significance in Pharmaceutical Research

  • M. Reist
  • B. Testa
  • P.-A. Carrupt
Chapter
Part of the Handbook of Experimental Pharmacology book series (HEP, volume 153)

Abstract

The presence of one or more elements of chirality (i.e., centers, axes or planes of chirality, and generally helicity) (Cahn et al. 1966; Testa 1979) in drug molecules generates specific properties which may be advantageous in some cases, but inevitably require special consideration and studies. Examples of advantages include the possibility of increased selectivity and the fact that chirality per se is an invaluable probe in molecular pharmacology and biochemistry (Testa 1989,1990; Testa and Trager 1990). In contrast, problems generated by stereoisomerism include the need for stereospecific synthetic and analytical methods, the influence of the degree of resolution on activity (Barlow et al. 1972), and the increased complexity of metabolic, pharmacological, and clinical studies (AriËns 1986; Testa et al. 1993a).

Keywords

Pharmaceutical Research Configurational Stability Chiral Compound Chiral HPLC Chiral Drug 
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© Springer-Verlag Berlin Heidelberg 2003

Authors and Affiliations

  • M. Reist
  • B. Testa
  • P.-A. Carrupt

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