Drug design chirality

Given the importance of fluorination in drug design, chiral A/-fluoro reagents were also sought after and developed. The first such reagents to be developed were the V-fluorocamphorsultams (a sultam is a cyclic sulfonamide) ... 

It should be pointed out that one is focused on properties of molecules in the absence of the receptor in contrast to the detailed focus on the complex in drug design studies. Many approaches to similarity fail to even consider chirality, a common discriminator of receptors. For a recent overview of the current status of virtual screening in lead discovery, see the review by Oprea and Matter [82]. 

In 1993 Witte et al. [28] and in 1994 Rauws and Groen [29] reviewed the status of the regulation of chiral medicinal products on the pharmaceutical industries in the United States, Japan, and some European countries where designated authorities are responsible for the control and approval of newly developed drugs (both chiral and nonchiral). In the United States, new drug applications are submitted to the Food and Drug Administration (FDA), which requires appro-... 

Most of the molecules we find in nature are chiral—a complicated molecule is much more likely not to have a plane of symmetry than to have one. Nearly all of these chiral molecules in living systems are found not as racemic mixtures, but as single enantiomers. This fact has profound implications, for example, in the chemistry of drug design, and we will come back to it later. 

I. Lantos, V. Novack, in Chirality in Drug Design and Synthesis, C. Brown (ed.), Academic Press, New York, 1990, pp. 167-180. 

The C4-chiral thiazolidine-2-thiones and oxazolidine-2-thiones developed by us proved to be efficient for chiral induction. They should be applicable to practical syntheses of drugs. Novel chiral designs using these functional and chiral heterocycles seem likely in the future, especially when used in combination with organometallic reagents and/or molecular symmetry. Creative investigations employing such chiral heterocycles and related compounds will be extensively pursued. 

Hyneck, M. Dent, J. Hook, J. Chirality pharmacological action and drug development. In Chirality in Drug Design and Synthesis, Brown, C., Ed. Academic Press San Diego, 1990 1-28. 

Brown, C. Chirality in Drug Design and Synthesis Academic Press San Diego, 1990 243. 

M. Hamende, E. Cavoy, Book ofAbstracts of the Symposium on Chirality Impact on Drug Design and Development, Braine-LAlleud (Belgium), November 26,... 

---