当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Recent progress of the development of dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus.

Recent progress of the development of dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus.

Abstract：

:Diabetes is a fast growing chronic metabolic disorder around the world. Dipeptidyl peptidase-4 (DPP-4) is a new promising target during type 2 diabetes glycemic control. Thus, a number of potent DPP-4 inhibitors were developed and play a rapidly evolving role in the management of type 2 diabetes in recent years. This article reviews the development of synthetic and natural DPP-4 inhibitors from 2012 to 2017 and provides their physico-chemical properties, biological activities against DPP-4 and selectivity over dipeptidyl peptidase-8/9. Moreover, the glucose-lowering mechanisms and the active site of DPP-4 are also discussed. We also discuss strategies and structure-activity relationships for identifying potent DPP-4 inhibitors, which will provide useful information for developing potent DPP-4 drugs as type 2 diabtes treatments.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Li N,Wang LJ,Jiang B,Li XQ,Guo CL,Guo SJ,Shi DY

doi

10.1016/j.ejmech.2018.03.041

subject

Has Abstract

pub_date

2018-05-10 00:00:00

pages

145-157

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(18)30284-8

journal_volume

151

pub_type

杂志文章,评审

相关文献

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY文献大全
  • 2,4-Disubstituted quinazolines as amyloid-β aggregation inhibitors with dual cholinesterase inhibition and antioxidant properties: Development and structure-activity relationship (SAR) studies.

    abstract：:A library of fifty-seven 2,4-disubstituted quinazoline derivatives were designed, synthesized and evaluated as a novel class of multi-targeting agents to treat Alzheimer's disease (AD). The biological assay results demonstrate the ability of several quinazoline derivatives to inhibit both acetyl and butyrylcholinester...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.12.005

    authors： Mohamed T,Rao PPN

    更新日期：2017-01-27 00:00:00

  • Anthranilic acid based CCK1 receptor antagonists: preliminary investigation on their second "touch point".

    abstract：:In this phase of structure-affinity relationship study of VL-0395, a new anthranilic acid based CCK1 selective antagonist, we propose a series of unnatural aminoacidic derivatives. The result of this work is the identification of a new CCK ligand, which possesses an affinity (IC50 = 35 nm) one order of magnitude great...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2005.01.002

    authors： Varnavas A,Lassiani L,Valenta V,Mennuni L,Makovec F,Hadjipavlou-Litina D

    更新日期：2005-06-01 00:00:00

  • Concise synthesis of carbazole-1,4-quinones and evaluation of their antiproliferative activity against HCT-116 and HL-60 cells.

    abstract：:We report a convenient synthesis of carbazole-1,4-quinone alkaloid koeniginequinones A and B using a tandem ring-closing metathesis with the dehydrogenation reaction sequence under an O2 atmosphere as an important step. Using this method, carbazole-1,4-quinones substituted at the 5-, 6-, 7-, and/or 8-positions have be...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.05.065

    authors： Nishiyama T,Hatae N,Yoshimura T,Takaki S,Abe T,Ishikura M,Hibino S,Choshi T

    更新日期：2016-10-04 00:00:00

  • Design, synthesis and screening of 1, 2, 4-triazinone derivatives as potential antitumor agents with apoptosis inducing activity on MCF-7 breast cancer cell line.

    abstract：:Some triazinone derivatives are designed and synthesized as potential antitumor agents. Triazinone derivatives 4c, 5e and 7c show potent anticancer activity over MCF-7 breast cancer cells higher than podophyllotoxin (podo) by approximate 6-fold. DNA flow cytometry analysis for the compounds 3c, 4c, 5e, 6c and 7c show ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.07.003

    authors： Zaki I,Abdelhameid MK,El-Deen IM,Abdel Wahab AHA,Ashmawy AM,Mohamed KO

    更新日期：2018-08-05 00:00:00

  • Benzofuran derivatives as anticancer inhibitors of mTOR signaling.

    abstract：:A series of 32 derivatives and isosteres of the mTOR inhibitor 2 were synthesized and compared for their cytotoxicity in radioresistant SQ20B cancer cell line. Several of these compounds, in particular 30b, were significantly more cytotoxic than 2. Importantly, 30b was shown to block both mTORC1 and Akt signaling, sug...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.05.014

    authors： Salomé C,Ribeiro N,Chavagnan T,Thuaud F,Serova M,de Gramont A,Faivre S,Raymond E,Désaubry L

    更新日期：2014-06-23 00:00:00

  • Synthesis and antibacterial activity evaluation of novel biaryloxazolidinone analogues containing a hydrazone moiety as promising antibacterial agents.

    abstract：:A series of linezolid analogues containing a hydrazone moiety were designed, synthesized and evaluated for their antibacterial activity. Most compounds exhibited more potent antibacterial activity against S.aureus, MRSA, MSSA, LREF and VRE pathogens as compared with linezolid and radezolid. Compounds 9a, 9c, 9f, 9g, 1...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.09.004

    authors： Wu Y,Ding X,Ding L,Zhang Y,Cui L,Sun L,Li W,Wang D,Zhao Y

    更新日期：2018-10-05 00:00:00

  • Chalcones: Unearthing their therapeutic possibility as monoamine oxidase B inhibitors.

    abstract：:In the last years the continuous efforts in the development of novel and effective inhibitors of human monoamine oxidases (hMAOs) promoted the discovery of new agents able to effectively and selectively bound one of the two isoforms (hMAO-A and hMAO-B). However, the parent chalcone scaffold still covers an important r...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2020.112650

    authors： Guglielmi P,Mathew B,Secci D,Carradori S

    更新日期：2020-11-01 00:00:00

  • Polyamine-based analogs and conjugates as antikinetoplastid agents.

    abstract：:Naturally occurring polyamines: putrescine, spermidine and spermine are crucial for Kinetoplastid growth and persistence. These aliphatic polycations are either biosynthesized or internalized into Kinetoplastid by active transport. Impairing the polyamine metabolism using polyamine derivatives is an interesting path i...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2017.08.014

    authors： Jagu E,Pomel S,Pethe S,Loiseau PM,Labruère R

    更新日期：2017-10-20 00:00:00

  • Synthesis and in vitro antitumour activity evaluation of 1-aryl-1H,3H-thiazolo[4,3-b]quinazolines.

    abstract：:A series of 1H,3H-thiazolo[4,3-b]quinazolines (2a-i) were synthesized and evaluated for their in vitro antitumour activity against ca. 60 human tumour cell lines. They exhibited moderate (2c, 2d, 2f and 2g) to strong (2a, 2b, 2e, 2h and 2i) cell-growth inhibition at a concentration of 10(-4) M, but weak activity at lo...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/s0223-5234(00)01195-8

    authors： Grasso S,Micale N,Monforte AM,Monforte P,Polimeni S,Zappalà M

    更新日期：2000-12-01 00:00:00

  • Design, synthesis and biological evaluation of novel 2-methoxyestradiol analogs as dual selective estrogen receptor modulators (SERMs) and antiangiogenic agents.

    abstract：:2-methoxyestradiol is a novel agent showing both anti-angiogenic and vascular disrupting properties. In this study, a series of 11α-substituted 2-methoxyestradiol analogs have been designed and synthesized targeting dual ERα and microtubulin. Biological evaluation was performed on their anti-proliferative activities a...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2017.08.016

    authors： Lao K,Wang Y,Chen M,Zhang J,You Q,Xiang H

    更新日期：2017-10-20 00:00:00

  • Development of novel 4-aminopyridine derivatives as potential treatments for neurological injury and disease.

    abstract：:The amine position of the K+ channel blocker 4-aminopyridine was functionalized to form amide, carbamate and urea derivatives in an attempt to identify novel compounds which restore conduction in injured spinal cord. Eight derivatives were tested in vitro, using a double sucrose gap chamber, for the ability to restore...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2005.04.017

    authors： Smith DT,Shi R,Borgens RB,McBride JM,Jackson K,Byrn SR

    更新日期：2005-09-01 00:00:00

  • New styryl sulfones as anticancer agents.

    abstract：:New styryl sulfone compounds have been synthesized and evaluated for their anti-proliferative activity. Among the compounds synthesized, one compound (7k) has shown 51% tumor growth inhibition in mice implanted with HT-29 human carcinoma at 400 mg kg(-1) orally. ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/s0223-5234(03)00144-2

    authors： Vedula MS,Pulipaka AB,Venna C,Chintakunta VK,Jinnapally S,Kattuboina VA,Vallakati RK,Basetti V,Akella V,Rajgopal S,Reka AK,Teepireddy SK,Mamnoor PK,Rajagopalan R,Bulusu G,Khandelwal A,Upreti VV,Mamidi SR

    更新日期：2003-09-01 00:00:00

  • Development of novel theranostic agents for in vivo amyloid imaging and protective effects on human neuroblastoma cells.

    abstract：:Brain amyloid deposits have been identified as the main neuropathological hallmarks of Alzheimer's diseases (AD) and intensive efforts have been devoted to develop aggregation inhibitors preventing the formation of toxic oligomeric Aβ for therapeutic. In addition, evidence indicates that the formation and accumulation...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2019.111585

    authors： Li Y,Yan L,Cai J,Zhang W,Li L,Du Z,Dong C,Meunier B,Chen H

    更新日期：2019-11-01 00:00:00

  • Novel substituted quinoxaline 1,4-dioxides with in vitro antimycobacterial and anticandida activity.

    abstract：:Thirty-six 6(7)-substituted-3-methyl- or 3-halogenomethyl-2-phenylthio-phenylsulphonyl-chloro-quinoxaline 1,4-dioxides belonging to series 3-6 were synthesised and submitted to a preliminary in vitro evaluation for antimycobacterial, anticandida and antibacterial activities. Antitubercular screening showed a generally...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/s0223-5234(02)01346-6

    authors： Carta A,Paglietti G,Rahbar Nikookar ME,Sanna P,Sechi L,Zanetti S

    更新日期：2002-05-01 00:00:00

  • Health protective effects of carotenoids and their interactions with other biological antioxidants.

    abstract：:Carotenoids are natural pigments attracting attention of physicists, chemists and biologists due to their multiple functions in the nature. While carotenoids have unusually high extinction coefficients, they do not exhibit adequate emission. This fact has resulted in detailed studies of photophysical and photochemical...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2013.09.054

    authors： Jomova K,Valko M

    更新日期：2013-01-01 00:00:00

  • 2-Amino-thiophene derivatives present antileishmanial activity mediated by apoptosis and immunomodulation in vitro.

    abstract：:This study evaluated the effects of 2-amino-thiophene derivatives on the promastigote and amastigote forms of Leishmania (Leishmania) amazonensis and their possible mechanisms of action. Initially, we evaluated the antileishmanial activity of ten 2-amino-thiophene derivatives on promastigote and axenic amastigote form...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.10.011

    authors： Rodrigues KA,Dias CN,Néris PL,Rocha Jda C,Scotti MT,Scotti L,Mascarenhas SR,Veras RC,de Medeiros IA,Keesen Tde S,de Oliveira TB,de Lima Mdo C,Balliano TL,de Aquino TM,de Moura RO,Mendonça Junior FJ,de Oliveira MR

    更新日期：2015-12-01 00:00:00

  • New quinoxalinecarbonitrile 1,4-di-N-oxide derivatives as hypoxic-cytotoxic agents.

    abstract：:We report the synthesis and biological in vitro activities of 16 new 2-quinoxalinecarbonitrile 1,4-di-N-oxides. These compounds present new basic lateral chains (piperazines and anilines) in the 3 position as well as different substituents in the 6 and/or 7 positions of the quinoxaline ring. Among piperazine derivativ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/s0223-5234(00)00112-4

    authors： Ortega MA,Morancho MJ,Martínez-Crespo FJ,Sainz Y,Montoya ME,López de Ceráin A,Monge A

    更新日期：2000-01-01 00:00:00

  • Design, synthesis and biological evaluation of monobactams as antibacterial agents against gram-negative bacteria.

    abstract：:A series of monobactam derivatives were prepared and evaluated for their antibacterial activities against susceptible and resistant Gram-negative strains, taking Aztreonam and BAL30072 as the leads. Six conjugates (12a-f) bearing PIH-like siderophore moieties were created to enhance the bactericidal activities against...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.01.024

    authors： Fu HG,Hu XX,Li CR,Li YH,Wang YX,Jiang JD,Bi CW,Tang S,You XF,Song DQ

    更新日期：2016-03-03 00:00:00

  • Copper(II/I) complexes of 5-pyridin-2-yl-[1,3]dioxolo[4,5-g]isoquinoline: synthesis, crystal structure, antitumor activity and DNA interaction.

    abstract：:Three new copper(II) complexes of 5-pyridin-2-yl-[1,3]dioxolo[4,5-g]isoquinoline (PYP), i.e. [Cu₂(PYP)₂Cl₄] (1), [Cu₄(PYP)₄(ClO₄)₂(H₂O)₂](ClO₄)₂·2H₂O (2), and [Cu₂(PYP)2Cl4]n (3), were synthesized and fully characterized. In comparison to free PYP, complexes 1-3 exhibited enhanced cytotoxicity against tested human tum...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.10.031

    authors： Huang KB,Chen ZF,Liu YC,Wang M,Wei JH,Xie XL,Zhang JL,Hu K,Liang H

    更新日期：2013-01-01 00:00:00

  • 3D-QSAR analysis of human immunodeficiency virus entry-1 inhibitors by CoMFA and CoMSIA.

    abstract：:3D-QSAR studies namely CoMFA, CoMFA region focusing and CoMSIA have been carried out on a series (36 compounds) of HIV-1 entry inhibitors. An alignment rule for the compounds was defined using Distill in SYBYL 7.3. Models were validated using a data set obtained by dividing the data set into a training set and test se...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2010.07.062

    authors： Pirhadi S,Ghasemi JB

    更新日期：2010-11-01 00:00:00

  • Design, synthesis and biological evaluation of 1,3-diphenyl-1H-pyrazole derivatives containing benzimidazole skeleton as potential anticancer and apoptosis inducing agents.

    abstract：:A series of forty different pyrazole containing benzimidazole hybrids (6-45) have been designed, synthesized and evaluated for their potential anti-proliferative activity against three human tumor cell lines - lung (A549), breast (MCF-7), and cervical (HeLa). Some of the compounds, specifically 9, 17, and 28, showed p...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.07.031

    authors： Reddy TS,Kulhari H,Reddy VG,Bansal V,Kamal A,Shukla R

    更新日期：2015-08-28 00:00:00

  • Synthesis, beta-adrenoceptor pharmacology and toxicology of S-(-)-1-(4-(2-ethoxyethoxy)phenoxy)-2-hydroxy-3-(2-(3,4-dimethoxyphenyl)ethylamino)propane hydrochloride, a short acting beta(1)-specific antagonist.

    abstract：:The synthesis of S-(-)-1-(4-(2-ethoxyethoxy)phenoxy)-2-hydroxy-3-(2-(3,4-dimethoxyphenyl)ethylamino)propane hydrochloride (D140S.HCl 6), a novel short acting beta(1)-specific adrenoceptor antagonist, has been described. The antagonist potency for D140S.HCl 6 has been compared with esmolol, another short acting agent, ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/s0223-5234(02)01399-5

    authors： Jackman GP,Iakovidis D,Nero TL,Anavekar NS,Rezmann-Vitti LA,Louis SN,Mori M,Drummer OH,Louis WJ

    更新日期：2002-09-01 00:00:00

  • Targeting Aryl hydrocarbon receptor for next-generation immunotherapies: Selective modulators (SAhRMs) versus rapidly metabolized ligands (RMAhRLs).

    abstract：:Aryl Hydrocarbon Receptor (AhR) constitutes a major network hub of genomic and non-genomic signaling pathways, connecting host's immune cells to environmental factors. It shapes innate and adaptive immune processes to environmental stimuli with species-, cell- and tissue-type dependent specificity. Although an ever in...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2019.111842

    authors： Dolciami D,Ballarotto M,Gargaro M,López-Cara LC,Fallarino F,Macchiarulo A

    更新日期：2020-01-01 00:00:00

  • Synthesis, antiproliferative activity and inhibition of tubulin polymerization by anthracenone-based oxime derivatives.

    abstract：:A series of anthracenone-based oxime ethers and -esters were synthesized in order to evaluate their antiproliferative activity. Several investigated compounds displayed strong antiproliferative activity against K562 leukemia cells and proved to be strong inhibitors of tubulin polymerization. In this context, anthracen...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2010.04.019

    authors： Surkau G,Böhm KJ,Müller K,Prinz H

    更新日期：2010-08-01 00:00:00

  • Inhibition of vertebrate aldehyde oxidase as a therapeutic treatment for cancer, obesity, aging and amyotrophic lateral sclerosis.

    abstract：:The aldehyde oxidases (AOXs) are a small sub-family of cytosolic molybdo-flavoenzymes, which are structurally conserved proteins and broadly distributed from plants to animals. AOXs play multiple roles in both physiological and pathological processes and AOX inhibition is of increasing significance in the development ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2019.111948

    authors： Qiao Y,Maiti K,Sultana Z,Fu L,Smith R

    更新日期：2020-02-01 00:00:00

  • Design, synthesis and anticholinesterase activity of novel benzylidenechroman-4-ones bearing cyclic amine side chain.

    abstract：:A series of 3-(4-(aminoalkoxy)benzylidene)-chroman-4-ones 7a-r were designed and synthesized as analogs of homoisoflavonoids which are well known natural products with diverse pharmacological properties related to Alzheimer's disease. The in vitro anti-cholinesterase activity of designed compounds 7a-r against AChE an...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.04.055

    authors： Pourshojaei Y,Gouranourimi A,Hekmat S,Asadipour A,Rahmani-Nezhad S,Moradi A,Nadri H,Moghadam FH,Emami S,Foroumadi A,Shafiee A

    更新日期：2015-06-05 00:00:00

  • Discovery of novel HSP90 inhibitors that induced apoptosis and impaired autophagic flux in A549 lung cancer cells.

    abstract：:Heat shock protein 90 (HSP90) inhibition has aroused increasing enthusiasm in antitumor strategies in recent years. According to our previous studies, we synthesized a series of coumarin pyrazoline compounds HCP1-HCP6 that might be HSP90 inhibitors. Interactions between HCP1-HCP6 and HSP90 were examined and antitumor ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.01.024

    authors： Wei Q,Ning JY,Dai X,Gao YD,Su L,Zhao BX,Miao JY

    更新日期：2018-02-10 00:00:00

  • New azole antifungals with a fused triazinone scaffold.

    abstract：:We identified a new series of azole antifungal agents bearing a pyrrolotriazinone scaffold. These compounds exhibited a broad in vitro antifungal activity against pathogenic Candida spp. (fluconazole-susceptible and fluconazole-resistant) and were 10- to 100-fold more active than voriconazole against two Candida albic...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.112082

    authors： Montoir D,Guillon R,Gazzola S,Ourliac-Garnier I,Soklou KE,Tonnerre A,Picot C,Planchat A,Pagniez F,Le Pape P,Logé C

    更新日期：2020-03-01 00:00:00

  • Synthesis and biological evaluation of aminomethylphenol derivatives as inhibitors of the murine GABA transporters mGAT1-mGAT4.

    abstract：:A series of N-substituted aminomethylphenol derivatives was synthesized by reductive amination. To study the inhibitory potency of the target compounds at the murine GABA transporters (mGAT1-mGAT4), a [(3)H]GABA uptake test system in a 96-well format based on HEK cells stably expressing mGAT1-mGAT4 was established and...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2008.01.005

    authors： Kragler A,Höfner G,Wanner KT

    更新日期：2008-11-01 00:00:00

  • Synthesis and biological evaluation of novel coumarin-pyrazoline hybrids endowed with phenylsulfonyl moiety as antitumor agents.

    abstract：:Two groups of coumarin-pyrazoline hybrids were synthesized. The target compounds were obtained by cyclization of the coumarin chalcones with various substituted hydrazines to produce the corresponding pyrazolines through 1,4-addition on α,β-unsaturated carbonyl system. Selected compounds were investigated for their an...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2012.12.004

    authors： Amin KM,Eissa AA,Abou-Seri SM,Awadallah FM,Hassan GS

    更新日期：2013-02-01 00:00:00