| Title : Identification of a novel boronic acid as a potent, selective, and orally active hormone sensitive lipase inhibitor - Ogiyama_2016_Bioorg.Med.Chem_24_3801 |
| Author(s) : Ogiyama T , Yamaguchi M , Kurikawa N , Honzumi S , Yamamoto Y , Sugiyama D , Inoue S |
| Ref : Bioorganic & Medicinal Chemistry , 24 :3801 , 2016 |
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Abstract :
Hormone sensitive lipase (HSL) is an attractive therapeutic target of dyslipidemia. We designed and synthesized several compounds as reversible HSL inhibitors with a focus on hydrophobic interactions, which was thought to be effective upon the HSL inhibitory activity. In these efforts, we identified boronated compound 12 showing a potent HSL inhibitory activity with an IC50 value of 7nM and a high selectivity against cholinesterases. Furthermore, compound 12 is the first boron containing HSL inhibitor that has shown an antilipolytic effect in rats after oral administration at 3mg/kg. |
| PubMedSearch : Ogiyama_2016_Bioorg.Med.Chem_24_3801 |
| PubMedID: 27338659 |
Ogiyama T, Yamaguchi M, Kurikawa N, Honzumi S, Yamamoto Y, Sugiyama D, Inoue S (2016)
Identification of a novel boronic acid as a potent, selective, and orally active hormone sensitive lipase inhibitor
Bioorganic & Medicinal Chemistry
24 :3801
Ogiyama T, Yamaguchi M, Kurikawa N, Honzumi S, Yamamoto Y, Sugiyama D, Inoue S (2016)
Bioorganic & Medicinal Chemistry
24 :3801