Pharmacology & Pharmacy

Volume 11, Issue 1 (January 2020)

ISSN Print: 2157-9423   ISSN Online: 2157-9431

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“Atropisomeric” Drugs: Basic Concept and Example of Application to Drug Development

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DOI: 10.4236/pp.2020.111001    1,191 Downloads   3,120 Views  Citations


Many therapeutic drugs are racemates; i.e. they are chiral molecules consisting of “left”- and “right-handed” enantiomers (stereoisomers that are mirror images of each other, and are non-superimposable). In some cases, both enantiomers of the drug contribute to some extent (or equally) to the therapeutic effect; in other cases they contribute not at all. The same is true for the adverse effects of racemate drugs: the adverse effects of a racemate drug can be greater-than, less-than, or equal to one or the other enantiomer. An unusual situation arises when a drug consists of “atropisomers”, stereoisomers arising because of hindered rotation about a single chemical bond. We summarize the concept of atropisomerism, and give examples.

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Raffa, R. , Pergolizzi Jr., J. and Taylor Jr., R. (2020) “Atropisomeric” Drugs: Basic Concept and Example of Application to Drug Development. Pharmacology & Pharmacy, 11, 1-8. doi: 10.4236/pp.2020.111001.

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