当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Heterocyclic analogs of benzanilide derivatives as potassium channel activators. IX.

Heterocyclic analogs of benzanilide derivatives as potassium channel activators. IX.

Abstract：

:On the basis of our previous works, addressed to synthesise new activators of BK potassium channels, and of many suggestions from the international literature, a simple pharmacophoric model, consisting of two suitably substituted phenyl rings bound to various kinds of linkers, was hypothesised. In particular, the effectiveness of the amidic linker was demonstrated, since several benzanilide derivatives showed interesting BK-opener properties. As a development of these benzanilides, in this work we introduced heterocyclic substituents, replacing the aryl ring on the acid side or on the basic one of the amide linker of the above pharmacophore. The pharmacological results indicated some relevant remarks about the structural requirements, needed for a satisfactory BK-opener activity. In particular, the presence of a phenolic function, with a possible H-bond donor role, has been confirmed. Furthermore, the presence of nitrogen heterocycles on the acid side of the amide linker seems to be a negative requirement, while furan and thiophene were well tolerated. On the contrary, the introduction of insaturated heterocyclic rings (pyridine and thiazole) on the basic side of the amide linker, led to satisfactory biological activity, while the presence of aliphatic heterocycles lowered the pharmacological effect.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Calderone V,Fiamingo FL,Giorgi I,Leonardi M,Livi O,Martelli A,Martinotti E

doi

10.1016/j.ejmech.2006.03.009

subject

Has Abstract

pub_date

2006-06-01 00:00:00

pages

761-7

issue

6

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(06)00100-0

journal_volume

41

pub_type

杂志文章

相关文献

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY文献大全
  • 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

  • A series of 1, 2-coupled indane dimers with mast cell stabilisation and smooth muscle relaxation properties.

    abstract：:Asthma is characterised by bronchoconstriction and inflammation, with infiltration and activation of inflammatory cells such as eosinophils and mast cells, and subsequent release of inflammatory mediators. Much of the therapy directed at the treatment of asthma is either to provide symptomatic relief through bronchodi...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2009.09.005

    authors： Sheridan H,Walsh JJ,Jordan M,Cogan C,Frankish N

    更新日期：2009-12-01 00:00:00

  • Recent advances in HER2 positive breast cancer epigenetics: Susceptibility and therapeutic strategies.

    abstract：:HER2 amplification/overexpression accounts for aggressive clinical features of HER2 positive breast cancer. Epigenetic changes including DNA methylation, histone modifications and ncRNAs/miRNAs are associated with regulation of DNA chromatin and specifically, gene transcription. Hence, these produce eminent effects up...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2017.07.075

    authors： Singla H,Ludhiadch A,Kaur RP,Chander H,Kumar V,Munshi A

    更新日期：2017-12-15 00:00:00

  • Identification of a novel 5-amino-3-(5-cyclopropylisoxazol-3-yl)-1-isopropyl-1H-pyrazole-4-carboxamide as a specific RET kinase inhibitor.

    abstract：:Activating mutations of REarrange during Transfection (RET) kinase frequently occur in human thyroid and lung cancers. An enormous effort has been devoted to discover potent and selective inhibitors of RET. Selective and potent inhibitors against constitutively active RET mutants are rare to date as identification of ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.10.050

    authors： Yoon H,Shin I,Nam Y,Kim ND,Lee KB,Sim T

    更新日期：2017-01-05 00:00:00

  • Synthesis of 1,3,4-oxadiazole derivatives with anticonvulsant activity and their binding to the GABAA receptor.

    abstract：:In this study, a series of 1,3,4-oxadiazole derivatives (5a-s, 10a-s, and 16a-d) were designed and synthesized using maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) models, to test the anticonvulsant activity of the target compounds in vivo. The neurotoxicity (NT) of the target compounds was mea...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.112672

    authors： Wang S,Liu H,Wang X,Lei K,Li G,Li J,Liu R,Quan Z

    更新日期：2020-11-15 00:00:00

  • Discovery of a true bivalent dopamine D2 receptor agonist.

    abstract：:Employing two different alkyne-modified dopamine agonists to construct bivalent compounds via click chemistry resulted in the identification of a bivalent ligand (11c) for dopamine D2 receptor homodimer, which, compared to its parent monomeric alkyne, showed a 16-fold higher binding affinity for the dopamine D2 recept...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.113151

    authors： Qian M,Ricarte A,Wouters E,Dalton JAR,Risseeuw MDP,Giraldo J,Van Calenbergh S

    更新日期：2021-01-04 00:00:00

  • Structure-activity relationship studies of acridones as potential antipsoriatic agents. 2. Synthesis and antiproliferative activity of 10-substituted hydroxy-10H-acridin-9-ones against human keratinocyte growth.

    abstract：:A series of 10-substituted hydroxy-10H-acridin-9-ones were synthesized and studied as potential antipsoriatic agents. The antiproliferative activity of the novel derivatives, which can be considered as aza-analogues of the antipsoriatic drug anthralin, was determined using the human keratinocyte cell line HaCaT. Struc...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2010.08.059

    authors： Putic A,Stecher L,Prinz H,Müller K

    更新日期：2010-11-01 00:00:00

  • Synthesis and anticancer activity of 6-heteroarylcoumarins.

    abstract：:A series of novel 7-hydroxy-8-methyl-coumarins with indole, pyrimidine, pyrazole, pyran, tetrazolo[1,5-a]pyrimidine, pyrimido[1,2-a]benzimidazol, 2-oxo-1,2-dihydropyridine and dihydropyrazolo[3,4-b]pyridine moieties at C6 position of heterocyclic core have been synthesized. Anticancer activity screening on NCI60 cell ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.10.021

    authors： Galayev O,Garazd Y,Garazd M,Lesyk R

    更新日期：2015-11-13 00:00:00

  • An improved synthesis of 5,6-dimethylxanthenone-4-acetic acid (DMXAA).

    abstract：:5,6-Dimethylxanthenone-4-acetic acid (DMXAA) is a novel anticancer agent with a number of unique activities, and is in clinical trial. The current synthesis of DMXAA involves six steps, beginning with a heterogeneous reaction to form an isonitrosoacetanilide, and gives an overall yield of 11% from 2,3-dimethylaniline....

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/s0223-5234(02)01406-x

    authors： Atwell GJ,Yang S,Denny WA

    更新日期：2002-10-01 00:00:00

  • X-ray crystal structures of Enterococcus faecalis thymidylate synthase with folate binding site inhibitors.

    abstract：:Infections caused by Enterococcus faecalis (Ef) represent nowadays a relevant health problem. We selected Thymidylate synthase (TS) from this organism as a potential specific target for antibacterial therapy. We have previously demonstrated that species-specific inhibition of the protein can be achieved despite the re...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.07.066

    authors： Catalano A,Luciani R,Carocci A,Cortesi D,Pozzi C,Borsari C,Ferrari S,Mangani S

    更新日期：2016-11-10 00:00:00

  • Design and synthesis of sulfonamide derivatives of pyrrolidine and piperidine as anti-diabetic agents.

    abstract：:Type 2 diabetes (T2D) is a lifestyle disease affecting millions of people worldwide. Various therapies are available for the management of T2D and dipeptidyl peptidase-IV (DPP-IV) inhibition has emerged as a promising therapy for the treatment of type 2 diabetes (T2D). Here we report design, synthesis and in vitro eff...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.11.041

    authors： Sharma R,Soman SS

    更新日期：2015-01-27 00:00:00

  • Synthesis and preliminary antibacterial evaluation of Linezolid-like 1,2,4-oxadiazole derivatives.

    abstract：:In the present study the synthesis of new Linezolid-like molecules has been achieved by substitution of the oxazolidinone central heterocyclic moiety with a 1,2,4-oxadiazole ring. Two series of 1,2,4-oxadiazoles, bearing different side-chains and containing a varying number of fluorine atoms, were synthesized and prel...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2012.02.002

    authors： Palumbo Piccionello A,Musumeci R,Cocuzza C,Fortuna CG,Guarcello A,Pierro P,Pace A

    更新日期：2012-04-01 00:00:00

  • QSAR study of 4-phenylpiperidine derivatives as mu opioid agonists by neural network method.

    abstract：:A nonlinear QSAR study was conducted on a series of 4-phenylpiperidine derivatives (4PPs) acting as mu opioid agonists by three-layer back-propagation neural network (NN) method. At first a variety of molecular descriptors were calculated and then selected with two-stage least squares combining partial least squares (...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2005.10.017

    authors： Wang XH,Tang Y,Xie Q,Qiu ZB

    更新日期：2006-02-01 00:00:00

  • Photoactivation provides a mechanistic explanation for pan-assay interference behaviour of 2-aminopyrroles in lipoxygenase inhibition.

    abstract：:Human 15-lipoxygenase-1 (h-15-LOX-1) is a promising drug target in inflammation and cancer. In this study substitution-oriented screening (SOS) has been used to identify compounds with a 2-aminopyrrole scaffold as inhibitors for h-15-LOX-1. The observed structure activity relationships (SAR) proved to be relatively fl...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2017.07.047

    authors： Guo H,Eleftheriadis N,Rohr-Udilova N,Dömling A,Dekker FJ

    更新日期：2017-10-20 00:00:00

  • New transition metal ion complexes with benzimidazole-5-carboxylic acid hydrazides with antitumor activity.

    abstract：:Metal complexes of 2-methyl-1H-benzimidazole-5-carboxylic acid hydrazide (4a; L(1)) and its Schiff base 2-methyl-N-(propan-2-ylidene)-1H-benzimidazole-5-carbohydrazide (5a; L(2)) with transition metal ions e.g., copper, silver, nickel, iron and manganese were prepared. The complexes formed were 1:1 or 1:2 M:L complexe...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2008.07.013

    authors： Galal SA,Hegab KH,Kassab AS,Rodriguez ML,Kerwin SM,el-Khamry AM,el-Diwani HI

    更新日期：2009-04-01 00:00:00

  • (5aR)-5a-C-Pentyl-4-epi-isofagomine: A powerful inhibitor of lysosomal β-galactosidase and a remarkable chaperone for mutations associated with GM1-gangliosidosis and Morquio disease type B.

    abstract：:This report is about the identification, synthesis and initial biological characterization of derivatives of 4-epi-isofagomine as pharmacological chaperones (PC) for human lysosomal β-galactosidase. The two epimers of 4-epi-isofagomine carrying a pentyl group at C-5a, namely (5aR)- and (5aS)-5a-C-pentyl-4-epi-isofagom...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.09.095

    authors： Front S,Biela-Banaś A,Burda P,Ballhausen D,Higaki K,Caciotti A,Morrone A,Charollais-Thoenig J,Gallienne E,Demotz S,Martin OR

    更新日期：2017-01-27 00:00:00

  • Synthesis and biological activities of dithiocarbamates containing 2(5H)-furanone-piperazine.

    abstract：:A series of new dithiocarbamates containing a 2(5H)-furanone-piperazine group was synthesized. These compounds show good in vitro cytoxic activity. Among them, compound 6c exhibits the best inhibitory activity against HeLa cell lines with an IC50 of 0.06 ± 0.01 μM for 72 h, and it has good inhibitory activity against ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.05.056

    authors： Wei MX,Zhang J,Ma FL,Li M,Yu JY,Luo W,Li XQ

    更新日期：2018-07-15 00:00:00

  • Synthesis and evaluation of in vitro anti-microbial and anti-tubercular activity of 2-styryl benzimidazoles.

    abstract：:A new series of novel 5-(nitro/bromo)-styryl-2-benzimidazoles (1-12) has been synthesized by simple, mild and efficient synthetic protocol by attempted condensation of 5-(nitro/bromo)-o-phenylenediamine with trans-cinnamic acids in ethylene glycol. Screening for in vitro anti-tubercular activity against Mycobacterium ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2009.05.021

    authors： Shingalapur RV,Hosamani KM,Keri RS

    更新日期：2009-10-01 00:00:00

  • Synthesis, biological activity and structure-activity relationships of new benzoic acid-based protein tyrosine phosphatase inhibitors endowed with insulinomimetic effects in mouse C2C12 skeletal muscle cells.

    abstract：:Insulin resistance is a complex altered metabolic condition characterized by impaired insulin signaling and implicated in the pathogenesis of serious human diseases, such as diabetes, obesity, neurodegenerative pathologies. In pursuing our aim to identify new agents able to improve cellular insulin sensitivity, we hav...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.11.001

    authors： Ottanà R,Maccari R,Mortier J,Caselli A,Amuso S,Camici G,Rotondo A,Wolber G,Paoli P

    更新日期：2014-01-01 00:00:00

  • Bismuth heterocycles based on a diphenyl sulfone scaffold: synthesis and substituent effect on the antifungal activity against Saccharomyces cerevisiae.

    abstract：:A series of heterocyclic organobismuth(III) compounds 2 [ClBi(5-R-C6H(3)-2-SO2C6H(4)-1'-): R=Me, Ph, MeO, Cl, H, t-Bu, CF3, F, Me2N] was synthesized in order to study the relative importance of structure and specific substitutions in relation to their lipophilicity and antifungal activity against the yeast Saccharomyc...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2010.11.031

    authors： Murafuji T,Fujiwara Y,Yoshimatsu D,Miyakawa I,Migita K,Mikata Y

    更新日期：2011-02-01 00:00:00

  • Synthesis, brain antihypoxic activity and cell neuroprotection of 1-substituted-3,7-dimethylxanthines.

    abstract：:Five newly synthesised original compounds were investigated for acute toxicity, influence on hexobarbital sleeping time, effect on the locomotor activity, and brain antihypoxic activity. Two of the compounds were tested in a model of glutamate induced neurotoxicity in the brain cell culture using a cell viability test...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/s0223-5234(00)01172-7

    authors： Zlatkov A,Peikov P,Rodriguez-Alvarez J,Danchev N,Nikolova I,Mitkov J

    更新日期：2000-10-01 00:00:00

  • Synthesis and antimicrobial activity of some novel dicationic sulphonophanes.

    abstract：:The synthesis of some novel imidazole-based dicationic sulfonophanes incorporating various spacer units is described. All the sulphonophanes exhibit good antibacterial and antifungal activity against five bacterial strains Bacillus subtilis, Staphylococcus aureus, Vibrio cholera, Escherichia coli, Proteus vulgaris and...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2011.03.063

    authors： Rajakumar P,Satheeshkumar C,Mohanraj G,Mathivanan N

    更新日期：2011-07-01 00:00:00

  • Synthesis, biological evaluation and structure-activity relationship of new GABA uptake inhibitors, derivatives of 4-aminobutanamides.

    abstract：:Six series of 2-substituted 4-aminobutanamide derivatives were synthesized and evaluated for their ability to inhibit GABA transport proteins mGAT1-4 stably expressed in HEK-293 cell lines. The pIC50 values determined were in the range 4.23-5.23. Two compounds (15b and 15c) were selected for further in vitro studies. ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.06.024

    authors： Kowalczyk P,Sałat K,Höfner GC,Mucha M,Rapacz A,Podkowa A,Filipek B,Wanner KT,Kulig K

    更新日期：2014-08-18 00:00:00

  • Design, synthesis and biological evaluation of a novel class of potent TGR5 agonists based on a 4-phenyl pyridine scaffold.

    abstract：:TGR5, a GPCR, is involved in energy and glucose homeostasis, and as such, is a target for the treatment of diabetes, obesity and other metabolic syndromes. A new class of TGR5 agonists based on a 4-phenyl pyridine scaffold was designed, synthesized and evaluated in vitro and in vivo. Extensive structure-activity relat...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.07.050

    authors： Zhu J,Ning M,Guo C,Zhang L,Pan G,Leng Y,Shen J

    更新日期：2013-11-01 00:00:00

  • Synthesis and biological evaluation of Schizandrin derivatives as potential anti-cancer agents.

    abstract：:A new series of Schizandrin (1) derivatives were synthesized utilizing the C-9 position of the Schizandrin core and evaluated for their cytotoxic activities against HeLa (cervical cancer), A549 (lung cancer), MCF-7 (breast cancer) and DU-145 (prostate cancer) cell lines. Among the synthesized series, 4e, 4f, 4g and 5 ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.02.066

    authors： Amujuri D,Siva B,Poornima B,Sirisha K,Sarma AVS,Lakshma Nayak V,Tiwari AK,Purushotham U,Suresh Babu K

    更新日期：2018-04-10 00:00:00

  • Synthesis and biological evaluation of novel pyranochalcone derivatives as a new class of microtubule stabilizing agents.

    abstract：:Twenty-five novel pyranochalcone derivatives were synthesized and evaluated for their in vitro and in vivo antiproliferative activities. Among them, compound 10i exhibited superior potent activity against 21 tumor cell lines including multidrug resistant phenotype with the IC50 values ranged from 0.09 to 1.30 μM. In a...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.01.007

    authors： Cao D,Han X,Wang G,Yang Z,Peng F,Ma L,Zhang R,Ye H,Tang M,Wu W,Lei K,Wen J,Chen J,Qiu J,Liang X,Ran Y,Sang Y,Xiang M,Peng A,Chen L

    更新日期：2013-04-01 00:00:00

  • Prodrugs of butyric acid. Novel derivatives possessing increased aqueous solubility and potential for treating cancer and blood diseases.

    abstract：:The synthesis and biological activities of acidic, basic and neutral types of butyric acid (BA) prodrugs possessing increased aqueous solubility are described. The compounds are butyroyloxyalkyl derivatives of carboxylic acids, which possess functionalities suitable for aqueous solubilization. The anticancer activity ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/s0223-5234(00)01199-5

    authors： Nudelman A,Gnizi E,Katz Y,Azulai R,Cohen-Ohana M,Zhuk R,Sampson SR,Langzam L,Fibach E,Prus E,Pugach V,Rephaeli A

    更新日期：2001-01-01 00:00:00

  • New Atglistatin closely related analogues: Synthesis and structure-activity relationship towards adipose triglyceride lipase inhibition.

    abstract：:Adipose Triglyceride Lipase (ATGL) performs the first and rate-limiting step in lipolysis by hydrolyzing triacylglycerols stored in lipid droplets to diacylglycerols. By mediating lipolysis in adipose and non-adipose tissues, ATGL is a major regulator of overall energy metabolism and plasma lipid levels. Since chronic...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.04.021

    authors： Roy PP,D'Souza K,Cuperlovic-Culf M,Kienesberger PC,Touaibia M

    更新日期：2016-08-08 00:00:00

  • New pseudodimeric aurones as palm pocket inhibitors of Hepatitis C virus RNA-dependent RNA polymerase.

    abstract：:The NS5B RNA-dependent RNA polymerase (RdRp) is a key enzyme for Hepatitis C Virus (HCV) replication. In addition to the catalytic site, this enzyme is characterized by the presence of at least four allosteric pockets making it an interesting target for development of inhibitors as potential anti-HCV drugs. Based on a...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.03.005

    authors： Meguellati A,Ahmed-Belkacem A,Nurisso A,Yi W,Brillet R,Berqouch N,Chavoutier L,Fortuné A,Pawlotsky JM,Boumendjel A,Peuchmaur M

    更新日期：2016-06-10 00:00:00

  • Design and studies of multiple mechanism of anti-Candida activity of a new potent Trp-rich peptide dendrimers.

    abstract：PURPOSE:Eight peptide dendrimers were designed as structural mimics of natural cationic amphiphilic peptides with antifungal activity and evaluated for their anti-Candida potential against the wild type strains and mutants. METHODS:Dendrimer 14 containing four Trp residues and dodecyl tail and a slightly smaller dendr...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.10.013

    authors： Zielińska P,Staniszewska M,Bondaryk M,Koronkiewicz M,Urbańczyk-Lipkowska Z

    更新日期：2015-11-13 00:00:00