Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 61, Issue 19, Pages 8934-8943Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.8b01148
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In this article, we report our investigation of a phenomenon by which bridging morpholines across the ring with one-carbon tethers leads to a counterintuitive reduction in lipophilicity. This effect was also found to occur in piperazines and piperidines and lowered the measured log D-7.4 of the bridged molecules by as much as -0.8 relative to their unbridged counterparts. As lowering lipophilicity without introducing additional heteroatoms can be desirable, we believe this potentially provides a useful tactic to improve the drug-like properties of molecules containing morpholine-, piperazine-, and piperidine-like motifs.
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