【摘 要】
：
The incretin hormone glucagon-like peptide-1(GLP-1) plays the significant role in the regulation of postprandial glucose metabolism,[1] and the active form of GLP-1 is rapidly degraded by dipeptidyl p
【机 构】
：
Beijing Key Laboratory of Active Substances Discovery and Druggability Evaluation,Institute of Mater
【出 处】
：
第九届IUPAC化学生物学国际研讨会暨第八届世界华人药物化学研讨会
论文部分内容阅读
The incretin hormone glucagon-like peptide-1(GLP-1) plays the significant role in the regulation of postprandial glucose metabolism,[1] and the active form of GLP-1 is rapidly degraded by dipeptidyl peptidase-Ⅳ(DPP-4).[2][3]Therefore,inhibition of DPP-4 is a promising new treatment for type 2 diabetes.As off-target inhibitions of DPP-8 and/or DPP-9 have shown severe toxicities in the in vivo studies,[4] development of selective inhibitors of DPP-4 is a major challenge.We have previously identified some thiomorpholine-bearing compounds as potential DPP-4inhibitors.[5] Recently,a series of(S)-(γ-substituted prolyl)thiomorpholine were designed and synthesized.The results suggested that 8p was a potent and selective DPP-4 inhibitor that was valuable for further optimization.
其他文献
Nitrogen-incorporated polyhydroxylated carbocylic ring systems,commonly known as azasugars or iminosugars1,which are widesperade in plants and microorganisms,2 exhibit significant glycosidase and glyc
The syntheses and structures of four new uranyl complexes with [ONNO]type ligands are described.The reaction between uranyl nitrate hexahydrate and HMBUD,HMND,HMPBD ligands.uranyl complexes with the f
Spingosine-l-phosphate receptor 1(S1PR1) has attracted significant attention as a target for the treatment of autoimmune diseases and transplant rejection1.20 S1PR1 agonists have been docked into the
The inflammatory cytokines play a major role in osteoclastogenesis and lead to the bone resorption that is frequently associated with osteoporosis.Ipriflavone has been reported possessed anti-inflamma
A series of N-1 and N-2 aryl tetrahydroindazolone derivatives was synthesized and evaluated anticancer activity.The yield of N-1 products was more than those of corresponding N-2 by microwave core-cyc
Acetylcholinesterase inhibitors are the most frequently prescribed anti-Alzheimers drugs.A series of 6-acetyl-5H-thiazolo[3,2-a]pyrimidine derivatives as the novel acetylcholinesterase inhibitors were
Nuclear factor(erythroid-derived 2)-like 2(Nrf2) is a critical transcription factor regulating a cellular protective response that defends cells against toxic insults from a broad spectrum of chemical
In August 2008,racemic tetrabenazine ((±)-3-(2-methylpropyl)-9,10-dimethoxy-1,3,4,6,7,11 b-hexahydro-2H-benzo[a]quinolizin-2-one,(±)-TBZ) was approved for the treatment of chorea associated with Hunti
Inactivators of hypoxia-inducible factor(HIF-1) have been identified as possible treatments for cancer.Due to the importance of HIF-1 in tumor development and progression,a considerable amount of effo
(±)-7,8-dihydroxy-3-methyl-isochromanone-4((±)XJP) is a nature product contained in banana(Musa sapientum L.) peel.(-)-XJP and(+)-XJP was first obtained by chiral resolution,meanwhile circular dichroi