Strategies towards Improving the Pharmacokinetic Profile of ε‐Substituted Lysinol‐Derived HIV Protease Inhibitors

Compounds that are all HAART: Subsequent to accessing the S2 subpocket of HIV protease from the novel lysinol series of HIV protease inhibitors, we now report a comprehensive structure–activity relationship study at this position. Balancing physical properties via truncation of the substituent binding in the S1′ subpocket enabled the discovery of inhibitors with improved pharmacokinetic properties, while maintaining the functional potency of these inhibitors. Detailed facts of importance to specialist readers are published as ”Supporting Information”. Such documents are peer-reviewed, but not copy-edited or typeset. They are made available as submitted by the authors. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.