| Title : Design, synthesis, and pharmacological evaluation of a novel series of hormone sensitive lipase inhibitor - Ogiyama_2017_Bioorg.Med.Chem_25_4817 |
| Author(s) : Ogiyama T , Yamaguchi M , Kurikawa N , Honzumi S , Terayama K , Nagaoka N , Yamamoto Y , Kimura T , Sugiyama D , Inoue SI |
| Ref : Bioorganic & Medicinal Chemistry , 25 :4817 , 2017 |
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Abstract :
HSL inhibition is a promising approach to the treatment of dyslipidemia. As a result of re-optimization of lead compound 2, we identified novel compound 25a exhibiting potent inhibitory activity against HSL enzyme and cell with high selectivity for cholinesterases (AChE and BuChE). Reflecting its potent in vitro activity, compound 25a exhibited antilipolytic effect in rats at 1mg/kg p.o., which indicated that this novel compound is the most potent orally active HSL inhibitor. Moreover, compound 25a did not show bioactivation liability. |
| PubMedSearch : Ogiyama_2017_Bioorg.Med.Chem_25_4817 |
| PubMedID: 28756012 |
| Gene_locus related to this paper: human-LIPE |
| Gene_locus | human-LIPE |
Ogiyama T, Yamaguchi M, Kurikawa N, Honzumi S, Terayama K, Nagaoka N, Yamamoto Y, Kimura T, Sugiyama D, Inoue SI (2017)
Design, synthesis, and pharmacological evaluation of a novel series of hormone sensitive lipase inhibitor
Bioorganic & Medicinal Chemistry
25 :4817
Ogiyama T, Yamaguchi M, Kurikawa N, Honzumi S, Terayama K, Nagaoka N, Yamamoto Y, Kimura T, Sugiyama D, Inoue SI (2017)
Bioorganic & Medicinal Chemistry
25 :4817