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Issue 11, 2019
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Saturated bioisosteres of benzene: where to go next?

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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.

Graphical abstract: Saturated bioisosteres of benzene: where to go next?

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Article information


Submitted
11 Nov 2018
Accepted
10 Jan 2019
First published
10 Jan 2019

Org. Biomol. Chem., 2019,17, 2839-2849
Article type
Review Article

Saturated bioisosteres of benzene: where to go next?

P. K. Mykhailiuk, Org. Biomol. Chem., 2019, 17, 2839
DOI: 10.1039/C8OB02812E

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