当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Synthesis and antimycobacterial activity of new quinoxaline-2-carboxamide 1,4-di-N-oxide derivatives.

Synthesis and antimycobacterial activity of new quinoxaline-2-carboxamide 1,4-di-N-oxide derivatives.

Abstract：

:As a continuation of our research and with the aim of obtaining new anti-tuberculosis agents which can improve the current chemotherapeutic anti-tuberculosis treatments, forty-three new quinoxaline-2-carboxamide 1,4-di-N-oxide derivatives were synthesized and evaluated for in vitro anti-tuberculosis activity against Mycobacterium tuberculosis strain H(37)Rv. Active compounds were also screened to assess toxicity to a VERO cell line. Results indicate that compounds with a methyl moiety substituted in position 3 and unsubstituted benzyl substituted on the carboxamide group provide an efficient approach for further development of anti-tuberculosis agents.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Moreno E,Ancizu S,Pérez-Silanes S,Torres E,Aldana I,Monge A

doi

10.1016/j.ejmech.2010.06.036

subject

Has Abstract

pub_date

2010-10-01 00:00:00

pages

4418-26

issue

10

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(10)00480-0

journal_volume

45

pub_type

杂志文章

相关文献

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY文献大全
  • Synthesis, biological evaluation, and molecular docking study of 3-(3'-heteroatom substituted-2'-hydroxy-1'-propyloxy) xanthone analogues as novel topoisomerase IIα catalytic inhibitor.

    abstract：:Epoxide ring-opened xanthone derivatives were synthesized and tested for their topoisomerase inhibitory activity and cytotoxicity. Most of the compounds showed topo IIα specific inhibitory activity. To clarify the mechanism of action of these compounds, the most potent compound (compound 14) of the synthesized analogu...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2011.01.011

    authors： Jun KY,Lee EY,Jung MJ,Lee OH,Lee ES,Park Choo HY,Na Y,Kwon Y

    更新日期：2011-06-01 00:00:00

  • Structure-based approach to nanomolar, water soluble matrix metalloproteinases inhibitors (MMPIs).

    abstract：:N-arylsulfonyl-based MMPs inhibitors (MMPIs) are among the most prominent inhibitors possessing nanomolar affinity. However, their poor bioavailability remains critical for the drug development of this family of molecules. The structural analysis of the complex of NNGH (the most representative member of the family) wi...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2010.09.057

    authors： Attolino E,Calderone V,Dragoni E,Fragai M,Richichi B,Luchinat C,Nativi C

    更新日期：2010-12-01 00:00:00

  • Synthesis, characterization and antiamoebic activity of new indole-3-carboxaldehyde thiosemicarbazones and their Pd(II) complexes.

    abstract：:In continuation of our research on thiosemicarbazones and their metal complexes as antiamoebic agents, a new series of indole-3-carboxaldehyde thiosemicarbazones (TSC) 1-7 were prepared by condensing indole-3-carboxaldehyde with cycloalkylaminothiocarbonyl hydrazines. Their palladium(II) complexes of the [Pd(TSC)Cl2] ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2007.02.012

    authors： Husain K,Abid M,Azam A

    更新日期：2007-10-01 00:00:00

  • Design, synthesis and antiproliferative activities of biarylolefins based on polyhydroxylated and carbohydrate scaffolds.

    abstract：:A series of diversely substituted biarylolefins based on carbohydrate and dihydroxyethylene scaffolds were synthesized and evaluated for antiproliferative activity against a panel of human tumor cell lines. Among the thirty-five yet unknown biarylolefins prepared, six displayed potent antiproliferative activities with...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2011.05.021

    authors： Novoa A,Pellegrini-Moïse N,Bourg S,Thoret S,Dubois J,Aubert G,Cresteil T,Chapleur Y

    更新日期：2011-09-01 00:00:00

  • Synthetic cinnamylphenol derivatives as cancer chemopreventive agents.

    abstract：:Several substituted cinnamylphenol (1,3-diphenylpropene) derivatives were synthesized and tested for their inhibitory activities against in vitro Epstein-Barr virus early antigen activation induced by 12-O-tetradecanoylphorbol-13-acetate in Raji cells. The prenylated cinnamylphenols were found to show remarkably poten...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2006.12.024

    authors： Ito C,Itoigawa M,Kanematsu T,Imamura Y,Tokuda H,Nishino H,Furukawa H

    更新日期：2007-07-01 00:00:00

  • Synthesis and evaluation of 1-hydroxy/methoxy-4-methyl-2-phenyl-1H-imidazole-5-carboxylic acid derivatives as non-purine xanthine oxidase inhibitors.

    abstract：:Xanthine oxidase is a key enzyme that catalyses hypoxanthine and xanthine to uric acid, whose overproduction leads to the gout-causing hyperuricemia. In this study, a series of 1-hydroxy/methoxy-4-methyl-2-phenyl-1H-imidazole-5-carboxylic acid derivatives (4a-4k and 6a-6k) was synthesized and evaluated for their inhib...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.08.056

    authors： Chen S,Zhang T,Wang J,Wang F,Niu H,Wu C,Wang S

    更新日期：2015-10-20 00:00:00

  • Pyridazine as a privileged structure: An updated review on anticancer activity of pyridazine containing bioactive molecules.

    abstract：:Identification of potent anticancer agents with high selectivity and low toxicity remains on the way to human health. Pyridazine featuring advantageous physicochemical properties and antitumor potential usually is regarded as a central core in numerous anticancer derivatives. There are several approved pyridazine-base...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2020.112946

    authors： He ZX,Gong YP,Zhang X,Ma LY,Zhao W

    更新日期：2021-01-01 00:00:00

  • Known drug space as a metric in exploring the boundaries of drug-like chemical space.

    abstract：:In this work, marketed drug compounds (or known drug space) were used as a metric to test the principles of eliminating parent structures of the nitrenium ion (aryl-amine/nitro compounds) as well as sulphur and halogen containing molecules from screening compound collections. Molecules containing such moieties and/or ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2009.08.014

    authors： Mirza A,Desai R,Reynisson J

    更新日期：2009-12-01 00:00:00

  • Synthesis of cinnamic amide derivatives and their anti-melanogenic effect in α-MSH-stimulated B16F10 melanoma cells.

    abstract：:Of the three enzymes that regulate the biosynthesis of melanin, tyrosinase and its related proteins TYRP-1 and TYRP-2, tyrosinase is the most important because of its ability to limit the rate of melanin production in melanocytes. For treating skin pigmentation disorders caused by an excess of melanin, the inhibition ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.10.025

    authors： Ullah S,Kang D,Lee S,Ikram M,Park C,Park Y,Yoon S,Chun P,Moon HR

    更新日期：2019-01-01 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

  • Antiproliferative potency of novel benzofuran-2-carboxamides on tumour cell lines: cell death mechanisms and determination of crystal structure.

    abstract：:In this manuscript the synthesis and biological activity of novel heterocyclic derivatives of benzofuran-2-carboxamides 3a-j and 6a-f is presented. Biological evaluation in vitro revealed that only few compounds exerted concentration-depended antiproliferative effects on tumour cell lines at micromolar concentrations....

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2012.11.009

    authors： Hranjec M,Sović I,Ratkaj I,Pavlović G,Ilić N,Valjalo L,Pavelić K,Kraljević Pavelić S,Karminski-Zamola G

    更新日期：2013-01-01 00:00:00

  • Dual inhibition of the α-glucosidase and butyrylcholinesterase studied by molecular field topology analysis.

    abstract：:A striking dual inhibition of enzymes α-glucosidase and butyrylcholinesterase by small drug-like molecules, including 1,4-disubstituted-1,2,3-triazoles, chalcones, and benzothiazepines, was rationalized with the help of Molecular Field Topology Analysis, a 3D QSAR technique similar to CoMFA. A common pharmacophore sup...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.04.018

    authors： Jabeen F,Oliferenko PV,Oliferenko AA,Pillai GG,Ansari FL,Hall CD,Katritzky AR

    更新日期：2014-06-10 00:00:00

  • Synthesis and biological evaluation of dialkylsubstituted maleic anhydrides as novel inhibitors of Cdc25 dual specificity phosphatases.

    abstract：:An efficient synthesis of dialkylsubstituted maleic anhydrides 1a-j is described. The inhibitory potential of these original anhydride derivatives was tested toward the three human isoforms A, B and C of dual specific phosphatases Cdc25. A micromolar range inhibition of Cdc25s was observed with the maleic anhydrides b...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2006.09.014

    authors： Brault L,Denancé M,Banaszak E,El Maadidi S,Battaglia E,Bagrel D,Samadi M

    更新日期：2007-02-01 00:00:00

  • Inhibitors of phosphopantetheine adenylyltransferase.

    abstract：:Phosphopantetheine adenylyltransferase (PPAT) is an essential enzyme in Coenzyme A biosynthesis. Because bacterial PPAT and mammalian PPAT are dissimilar, this enzyme is an attractive antibacterial target. Based on the structure of the substrate, 4-phosphopantetheine, a dipeptide library was designed, synthesised and ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/s0223-5234(03)00047-3

    authors： Zhao L,Allanson NM,Thomson SP,Maclean JK,Barker JJ,Primrose WU,Tyler PD,Lewendon A

    更新日期：2003-04-01 00:00:00

  • Synthesis of oleanolic acid dimers linked at C-28 and evaluation of anti-tumor activity.

    abstract：:Five dimeric oleanolic acids linked at C-28 by 1,6-hexanediamine, or built around the carbon chains of varying lengths between two carboxyl groups were synthesized, to investigate the effect of internal spacer length and species upon the stereochemical features and anti-tumor activity of the resultant bis-oleanolic ac...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.10.066

    authors： Cheng KG,Su CH,Yang LD,Liu J,Chen ZF

    更新日期：2015-01-07 00:00:00

  • 3,5-Diaryl-1H-pyrazolo[3,4-b]pyridines as potent tubulin polymerization inhibitors: Rational design, synthesis and biological evaluation.

    abstract：:A series of novel 3,5-diaryl-1H-pyrazolo[3,4-b]pyridines as tubulin polymerization inhibitors targeting the colchicine site were designed via ring tethering strategy, which was supported by conformational analysis. The general, chemically unstable and rotational linker, carbanyl group, was locked by 1H-pyrazolo[3,4-b]...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.12.053

    authors： Zhai M,Liu S,Gao M,Wang L,Sun J,Du J,Guan Q,Bao K,Zuo D,Wu Y,Zhang W

    更新日期：2019-04-15 00:00:00

  • Novel 4-aryl-pyrido[1,2-c]pyrimidines with dual SSRI and 5-HT(1A) activity. Part 5.

    abstract：:A series of novel 4-aryl-pyrido[1,2-c]pyrimidine derivatives containing a 1-(2-quinoline)piperazine moiety was synthesized. The chemical structure of new compounds was confirmed by FT-IR, (1)H NMR, (13)C NMR and HRMS spectra as well as elemental analysis. Affinity of the novel pyrido[1,2-c]pyrimidine derivatives for 5...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.05.003

    authors： Gomółka A,Ciesielska A,Wróbel MZ,Chodkowski A,Kleps J,Dawidowski M,Siwek A,Wolak M,Stachowicz K,Sławińska A,Nowak G,Satała G,Bojarski AJ,Belka M,Ulenberg S,Bączek T,Skowronek P,Turło J,Herold F

    更新日期：2015-06-15 00:00:00

  • Discovery of lysosome-targeted covalent anticancer agents based on isosteviol skeleton.

    abstract：:Covalent drugs play corresponding bioactivities by forming covalent bonds with the target, which possess many significant pharmacological advantages including high potency, ligand efficiency, and long-lasting effects. However, development of covalent inhibitors is a challenge due to their presumed indiscriminate react...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.112896

    authors： Liu J,Li L,Li X,Wang X,Zhao X,Qiao Y,Xu Y,Sun Y,Qian L,Liu Z,Ji A,Lou H

    更新日期：2021-01-01 00:00:00

  • Modification of the anabaseine pyridine nucleus allows achieving binding and functional selectivity for the α3β4 nicotinic acetylcholine receptor subtype.

    abstract：:We report the design, synthesis and pharmacological screening of a group of analogues of anabaseine 2, a naturally occurring unselective nicotinic agonist. The novel nAChR ligands 5-15 were planned following a molecular modeling analysis which suggested the replacement of the pyridine ring of 2 with a 3-substituted be...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.11.045

    authors： Matera C,Quadri M,Sciaccaluga M,Pomè DY,Fasoli F,De Amici M,Fucile S,Gotti C,Dallanoce C,Grazioso G

    更新日期：2016-01-27 00:00:00

  • N6-cycloalkyl-2-phenyl-3-deaza-8-azaadenines: a new class of A1 adenosine receptor ligands. A comparison with the corresponding adenines and 8-azaadenines.

    abstract：:Several 9-benzyl-N6-cycloalkyl-2-phenyladenines, 9-benzyl-N6-cycloalkyl-2-phenyl-8-azaadenines and 4-cycloalkylamino-1-benzyl-6-phenyl-1H-1,2,3-triazolo[4,5-c]pyridines were prepared and assayed as A1 adenosine receptor ligands. The 1H-1,2,3-triazolo[4,5-c]pyridines were obtained starting from N,N-diethyl-1-benzyl-4-c...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2003.09.003

    authors： Biagi G,Giorgi I,Livi O,Nardi A,Pacchini F,Scartoni V,Lucacchini A

    更新日期：2003-11-01 00:00:00

  • Design, synthesis and biological evaluation of small-azo-dyes as potent Vesicular Glutamate Transporters inhibitors.

    abstract：:Vesicular Glutamate Transporters (VGLUTs) allow the loading of presynapic glutamate vesicles and thus play a critical role in glutamatergic synaptic transmission. VGLUTs have proved to be involved in several major neuropathologies and directly correlated to clinical dementia in Alzheimer and Parkinson's disease. Accor...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.03.056

    authors： Favre-Besse FC,Poirel O,Bersot T,Kim-Grellier E,Daumas S,El Mestikawy S,Acher FC,Pietrancosta N

    更新日期：2014-05-06 00:00:00

  • 2-cinnamamido, 2-(3-phenylpropiolamido), and 2-(3-phenylpropanamido)benzamides: synthesis, antiproliferative activity, and mechanism of action.

    abstract：:Several new benzamides 4a-q were synthesized by stirring in pyridine the acid chlorides 3a-q with the appropriate anthranilamide derivatives 2a-g. Some of the synthesized compounds were evaluated for their in vitro antiproliferative activity against a panel of 5 human cell lines (K562 human chronic myelogenous leukemi...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.04.068

    authors： Raffa D,Maggio B,Raimondi MV,Cusimano MG,Amico G,Carollo A,Conaldi PG,Bai R,Hamel E,Daidone G

    更新日期：2013-07-01 00:00:00

  • Ultra-short lipopeptides against gram-positive bacteria while alleviating antimicrobial resistance.

    abstract：:Facing the continuously urgent demands for novel antimicrobial agents since the growing emergence of bacterial resistance, a series of new ultra-short lipopeptides, composed of tryptophan and arginine and fatty acids, were de novo designed and synthesized in this study. Most of the new lipopeptides exhibited preferabl...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.113138

    authors： Zhong C,Zhang F,Zhu N,Zhu Y,Yao J,Gou S,Xie J,Ni J

    更新日期：2020-12-29 00:00:00

  • Benzoxazoles and oxazolopyridines in medicinal chemistry studies.

    abstract：:The benzoxazole heterocycle is often found in ligands targeting a plethora of receptors and enzymes. By analysis of published X-ray structures, this review aims at highlighting key interactions which the benzoxazole may engage in with its host protein. Furthermore, bioavailability, metabolism and the use of benzoxazol...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2014.11.064

    authors： Demmer CS,Bunch L

    更新日期：2015-06-05 00:00:00

  • Synthesis of novel thiazole-based 8,9-dihydro-7H-pyrimido[4,5-b][1,4]diazepines as potential antitumor and antifungal agents.

    abstract：:A new series of novel thiazole-based 8,9-dihydro-7H-pyrimido[4,5-b][1,4]diazepines 6a-g and 7a-g were obtained with high regioselectivity from the reaction of triamino- or tetraaminopyrimidines 4 and 5 with α,β-unsaturated carbonyl compounds 3a-g based on 2,4-dichlorothiazol-5-carbaldehyde 1. Twelve of the synthesized...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.01.053

    authors： Ramírez J,Svetaz L,Quiroga J,Abonia R,Raimondi M,Zacchino S,Insuasty B

    更新日期：2015-03-06 00:00:00

  • New chromene scaffolds for adenosine A(2A) receptors: synthesis, pharmacology and structure-activity relationships.

    abstract：:In silico screening of a collection of 1584 academic compounds identified a small molecule hit for the human adenosine A(2A) receptor (pK(i) = 6.2) containing a novel chromene scaffold (3a). To explore the structure-activity relationships of this new chemical series for adenosine receptors, a focused library of 43 2H-...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2012.05.009

    authors： Areias F,Costa M,Castro M,Brea J,Gregori-Puigjané E,Proença MF,Mestres J,Loza MI

    更新日期：2012-08-01 00:00:00

  • The chemical diversity and structure-based evolution of non-peptide CXCR4 antagonists with diverse therapeutic potential.

    abstract：:The CXC chemokine receptor 4 (CXCR4) is a highly reserved G-protein coupled 7-transmembrane (TM) chemokine receptor which consists of 352 amino acids. CXCR4 has only one endogenous chemokine ligand of CXCL12, besides several other natural nonchemokine ligands such as extracellular ubiquitin and noncognate ligand of MI...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2018.02.043

    authors： Peng D,Cao B,Zhou YJ,Long YQ

    更新日期：2018-04-10 00:00:00

  • Synthesis of Abyssinone II and related compounds as potential chemopreventive agents.

    abstract：:A facile and efficient approach to the synthesis of prenylated flavonoids as potential chemopreventive agents has been described. This features the synthesis of prenyl halide, prenylation of p-hydroxybenzaldehyde, formation of prenylated polyhydroxychalcone and cyclization of prenylated polyhydroxychalcone to flavanon...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2005.09.008

    authors： Moriarty RM,Grubjesic S,Surve BC,Chandersekera SN,Prakash O,Naithani R

    更新日期：2006-02-01 00:00:00

  • Novel N-benzylpiperidine carboxamide derivatives as potential cholinesterase inhibitors for the treatment of Alzheimer's disease.

    abstract：:A series of fifteen acetylcholinesterase inhibitors were designed and synthesised based upon the previously identified lead compound 5,6-dimethoxy-1-oxo-2,3-dihydro-1H-inden-2-yl 1-benzylpiperidine-4-carboxylate (5) which showed good inhibitory activity (IC50 0.03 ± 0.07 μM) against acetylcholinesterase. A series of c...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2019.06.088

    authors： van Greunen DG,Johan van der Westhuizen C,Cordier W,Nell M,Stander A,Steenkamp V,Panayides JL,Riley DL

    更新日期：2019-10-01 00:00:00

  • Development and biological evaluation of[18F]FMN3PA & [18F]FMN3PU for leucine-rich repeat kinase 2 (LRRK2) in vivo PET imaging.

    abstract：PURPOSE:Among all genetic mutations of LRRK2, the G2019S mutation is the most commonly associated with the late-onset of Parkinson's disease (PD). Hence, one potential therapeutic approach is to block the hyperactivity of mutated LRRK2 induced by kinase inhibition. To date, only a few LRRK2 kinase inhibitors have been ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.113005

    authors： Malik N,Kornelsen R,McCormick S,Colpo N,Merkens H,Bendre S,Benard F,Sossi V,Schirrmacher R,Schaffer P

    更新日期：2021-02-05 00:00:00