Computed Properties of C11H22N2O2. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: 1-Boc-4-(Aminomethyl)piperidine, is researched, Molecular C11H22N2O2, CAS is 144222-22-0, about Design, synthesis, and biological evaluation of 1,2,5-oxadiazole-3-carboximidamide derivatives as novel indoleamine-2,3-dioxygenase 1 inhibitors. Author is Song, Xiaohan; Sun, Pu; Wang, Jiang; Guo, Wei; Wang, Yi; Meng, Ling-hua; Liu, Hong.
A novel series of 1,2,5-oxadiazole-3-carboximidamide derivatives I [R = (1-sulfamoylpyrrolidin-3-yl)methyl, (1-methanesulfonylpyrrolidin-3-yl)methyl, [1-(cyclopropanesulfonyl)piperidin-3-yl]methyl, etc] bearing cycle in the side chain were designed, synthesized, and biol. evaluated for their anti-tumor activity. Most of them exhibited potent activity against hIDO1 in enzymic assays and in HEK293T cells over-expressing hIDO1. Among them, compound I [R = [(3R)-1-sulfamoylpyrrolidin-3-yl]methyl, [(3R)-1-sulfamoylpiperidin-3-yl]methyl, [(3S)-1-sulfamoylpiperidin-3-yl]methyl] showed significant inhibitory activity against hIDO1 (IC50 = 108.7, 178.1 and 139.1 nM resp.) and in HEK293T cells expressing hIDO1 (cellular IC50 = 19.88, 68.59 and 57.76 nM resp.). Moreover, compound I [R = [(3R)-1-sulfamoylpiperidin-3-yl]methyl] displayed improved PK property with longer half-life (t1/2 = 3.81 h in CD-1 mice) and better oral bioavailability (F = 33.6%) compared with epacadostat. In addition, compound I [R = [(3R)-1-sulfamoylpiperidin-3-yl]methyl] showed similar potency to inhibit the growth of CT-26 syngeneic xenograft compared to epacadostat, making it justifiable for further investigation.
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Reference:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem