AZD4017 is a potent, selective, and orally bioavailable11β-HSD1 inhibitor (11β-hydroxysteroid dehydrogenase type 1 inhibitor). Inhibition of 11β-HSD1 is an attractive mechanism for the treatment of obesity and other elements of the metabolic syndrome. AZD4017 is a nicotinic amide derived carboxylic acid class of inhibitors that has good potency, selectivity, and pharmacokinetic characteristics. AZD4017) is an effective inhibitor of 11β-HSD1 in human adipocytes and exhibits good druglike properties and as a consequence was selected for clinical development.
CAS 1024033-43-9 MFCD124033439
化学结构图
SMILES: CCCSc1nc(N2CCC[C@@H](CC(=O)O)C2)ccc1C(=O)NC1CCCCC1
化学属性
| Mol. Weight | 419.58 |
|---|---|
| Appearance | Solid powder |
| Solubility | Soluble in DMSO, not in water |
别名和识别编码
| Chemical Name | AZD4017 is a potent, selective, and orally bioavailable11β-HSD1 inhibitor (11β-hydroxysteroid dehydrogenase type 1 inhibitor). Inhibition of 11β-HSD1 is an attractive mechanism for the treatment of obesity and other elements of the metabolic syndrome. AZD4017 is a nicotinic amide derived carboxylic acid class of inhibitors that has good potency, selectivity, and pharmacokinetic characteristics. AZD4017) is an effective inhibitor of 11β-HSD1 in human adipocytes and exhibits good druglike properties and as a consequence was selected for clinical development. |
|---|---|
| Formula | C22H33N3O3S |
| Synonym | AZD4017; AZD-4017; AZD 4017. |
| IUPAC Name | 2-[(3S)-1-[5-(cyclohexylcarbamoyl)-6-propylsulfanylpyridin-2-yl]-3-piperidyl]acetic acid |
| InChIKey | NCDZABJPWMBMIQ-INIZCTEOSA-N |
| InChI | InChI=1S/C22H33N3O3S/c1-2-13-29-22-18(21(28)23-17-8-4-3-5-9-17)10-11-19(24-22)25-12-6-7-16(15-25)14-20(26)27/h10-11,16-17H,2-9,12-15H2,1H3,(H,23,28)(H,26,27)/t16-/m0/s1 |
| Canonical SMILES | O=C(O)C[C@H]1CN(C2=NC(SCCC)=C(C(NC3CCCCC3)=O)C=C2)CCC1 |
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- AZD4017 is a potent, selective, and orally bioavailable11β-HSD1 inhibitor (11β-hydroxysteroid dehydrogenase type 1 inhibitor). Inhibition of 11β-HSD1 is an attractive mechanism for the treatment of obesity and other elements of the metabolic syndrome. AZD4017 is a nicotinic amide derived carboxylic acid class of inhibitors that has good potency, selectivity, and pharmacokinetic characteristics. AZD4017) is an effective inhibitor of 11β-HSD1 in human adipocytes and exhibits good druglike properties and as a consequence was selected for clinical development.
