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Published on: December 11, 2014
Saturated bioisosteres of benzene: where to go next?
1Enamine Ltd, Chervonotkatska 78, 02094 Kyiv, Ukraine. Pavel.Mykhailiuk@mail.enamine.net.
Abstract:
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.
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