AI Article Synopsis
- - A metabolic weak point was found in a bicyclo[2.2.2]octyltriazole compound that led to efforts to enhance its pharmacokinetics (PK) and reduce oxidative breakdown.
- - The research involved a systematic study of different alkyl chain substitutions on the lead compound to optimize its effectiveness.
- - The result of these efforts was the identification of an effective ethyl sulfone inhibitor that showed better PK behavior and favorable physical characteristics in various species.
Article Abstract
Following the discovery of a metabolic 'soft-spot' on a bicyclo[2.2.2]octyltriazole lead, an extensive effort was undertaken to block the oxidative metabolism and improve PK of this potent HSD1 lead. In this communication, SAR survey focusing on various alkyl chain replacements will be detailed. This effort culminated in the discovery of a potent ethyl sulfone inhibitor with an improved PK profile across species and improved physical properties.
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| http://dx.doi.org/10.1016/j.bmcl.2011.01.018 | DOI Listing |
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