AI Article Synopsis
- Researchers derived more effective benzoylpiperidine analogs from an existing piperazine-based SCD-1 inhibitor.
- The most optimized compound identified was 6-[4-(2-methylbenzoyl)piperidin-1-yl]pyridazine-3-carboxylic acid (24), which showed strong inhibition of SCD-1 in both human and mouse models.
- This compound also had good oral bioavailability and significantly reduced plasma triglycerides in Zucker fatty rats after daily administration for a week.
Article Abstract
Starting from a known piperazine-based SCD-1 inhibitor, we obtained more potent benzoylpiperidine analogs. Optimization of the structure of the benzoylpiperidine-based SCD-1 inhibitors resulted in the identification of 6-[4-(2-methylbenzoyl)piperidin-1-yl]pyridazine-3-carboxylic acid (2-hydroxy-2-pyridin-3-yl-ethyl)amide (24) which showed strong inhibitory activity against both human and murine SCD-1. In addition, this compound exhibited good oral bioavailability and demonstrated plasma triglyceride lowering effects in Zucker fatty rats in a dose-dependent manner after a 7-day oral administration (qd).
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| http://dx.doi.org/10.1016/j.bmcl.2009.10.101 | DOI Listing |
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