Pavel K. Mykhailiuk
Org. Biomol. Chem., 2019,17, 2839-2849
DOI:
10.1039/C8OB02812E,
Review Article
The replacement of para-substituted benzenes with saturated bi- and polycyclic bioisosteres – bicyclo[1.1.1]pentane, bicyclo[2.2.2]octane and cubane, – often increases the potency, selectivity and metabolic stability of bioactive compounds. The currently remaining challenge for chemists, however, is to rationally design, synthesize and validate the saturated bioisosteres for ortho- and meta-substituted benzenes.
