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[2]-Ladderanes as isosteres for meta-substituted aromatic rings and rigidified cyclohexanes.


ABSTRACT: Aromatic ring isosteres and rigidified saturated hydrocarbons are important motifs to enable drug discovery. Herein we disclose [2]-ladderanes as a class of meta-substituted aromatic ring isosteres and rigidified cyclohexanes. A straightforward synthesis of the building blocks is presented along with representative derivatization. Preliminary studies reveal that the [2]-ladderanes offer similar metabolic and physicochemical properties thus establishing this class of molecules as interesting motifs.

SUBMITTER: Epplin RC 

PROVIDER: S-EPMC9561113 | biostudies-literature | 2022 Oct

REPOSITORIES: biostudies-literature