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Saturated bioisosteres of para-substituted benzenes

The residue of benzene comprises the structure of more than 500 FDA-approved drugs. In 2012, Stepan and coworkers showed that bicyclo[1.1.1]pentane skeleton could act as a saturated ‘nonclassical phenyl ring bioisostere’ in the design of a γ-secretase inhibitor. Since then, the core of bicyclo[1.1.1]pentane is often used in the design of analogues of natural compounds, peptide studies, medicinal chemistry, and supramolecular chemistry. Herein we have designed and synthesized a library of saturated mimics of the para-benzene ring for drug design.

Design and a full list of compounds you can find at our webpage in MedChem highlights section or by downloading the attached white paper.