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Saturated bioisosteres of benzene: where to go next?

Org. Biomol. Chem. 2019, 17 (11), 2839-2849

DOI: 10.1039/c8ob02812e

Mykhailiuk P.

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.

Saturated bioisosteres of benzene: where to go next?

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