当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Attenuation of Mycobacterium species through direct and macrophage mediated pathway by unsymmetrical diaryl urea.

Attenuation of Mycobacterium species through direct and macrophage mediated pathway by unsymmetrical diaryl urea.

Abstract：

:Tuberculosis is a major threat for mankind and the emergence of resistance strain of Mycobacterium tuberculosis (Mtb) against first line antibiotics makes it lethal for human civilization. In this study, we have synthesized different diaryl urea derivatives targeting the inhibition of mycolic acid biosynthesis. Among the 39 synthesized molecules, compounds 46, 57, 58 and 86 showed MIC values ≤ 10 μg/ml against H37Rv and mc26030 strains. The best molecule with a methyl at ortho position of the first aromatic ring and prenyl group at the meta position of the second aromatic ring showed the MIC value of 5.2 μg/ml and 1 μg/ml against H37Rv and mc26030 respectively, with mammalian cytotoxicity of 163.4 μg/ml. The effective compounds showed selective inhibitory effect on mycolic acid (epoxy mycolate) biosynthesis in 14C-radiolabelled assay. At the same time these molecules also executed their potent immunomodulatory activity by up-regulation of IFN-γ and IL-12 and down-regulation of IL-10.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Velappan AB,Charan Raja MR,Datta D,Tsai YT,Halloum I,Wan B,Kremer L,Gramajo H,Franzblau SG,Kar Mahapatra S,Debnath J

doi

10.1016/j.ejmech.2016.09.083

subject

Has Abstract

pub_date

2017-01-05 00:00:00

pages

825-841

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(16)30817-0

journal_volume

125

pub_type

杂志文章

相关文献

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY文献大全
  • Monocarboxylate transporter 1 and 4 inhibitors as potential therapeutics for treating solid tumours: A review with structure-activity relationship insights.

    abstract：:Development of multidrug resistance (MDR) is one of the major causes leading to failure of cancer chemotherapy and radiotherapy. Monocarboxylate transporters (MCTs) MCT1 and MCT4, which are overexpressed in solid tumours, play a very important role in cancer cell survival and proliferation. These lactate transporters ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2020.112393

    authors： Puri S,Juvale K

    更新日期：2020-08-01 00:00:00

  • Synthesis of [11C]FEDAA1106 as a new PET imaging probe of peripheral benzodiazepine receptor expression.

    abstract：:Peripheral benzodiazepine receptor (PBR) is associated with neuroinflammation and tumor progression. [(11)C]DAA1106 and [(18)F]FEDAA1106 are two promising radioligands for positron emission tomography (PET) imaging of PBR. This study was designed to develop a new radiolabeled analog of [(11)C]DAA1106 and [(18)F]FEDAA1...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2008.08.001

    authors： Wang M,Gao M,Hutchins GD,Zheng QH

    更新日期：2009-06-01 00:00:00

  • The conversion of oridonin to spirolactone-type or enmein-type diterpenoid: synthesis and biological evaluation of ent-6,7-seco-oridonin derivatives as novel potential anticancer agents.

    abstract：:Starting from commercial available natural product oridonin (1), a practical synthesis of ent-6,7-seco-oridonin derivatives (2, 3, 5, and 9) was accomplished and their biological activities were evaluated. The conversion of spirolactone-type diterpenoid to enmein-type was first completed. The results demonstrated that...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2012.03.024

    authors： Wang L,Li D,Xu S,Cai H,Yao H,Zhang Y,Jiang J,Xu J

    更新日期：2012-06-01 00:00:00

  • Nature-based molecules combined with rivastigmine: A symbiotic approach for the synthesis of new agents against Alzheimer's disease.

    abstract：:Starting from nature as original source, new potential agents with pleiotropic activities have been synthesized and evaluated as neuroprotective agents. In this work, novel nature-based hybrids, combining antioxidant motifs with rivastigmine, have been designed and synthesized. The biological results revealed that the...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2017.10.006

    authors： Nesi G,Chen Q,Sestito S,Digiacomo M,Yang X,Wang S,Pi R,Rapposelli S

    更新日期：2017-12-01 00:00:00

  • Design, synthesis and in vivo evaluation of 3-arylcoumarin derivatives of rhenium(I) tricarbonyl complexes as potent antibacterial agents against methicillin-resistant Staphylococcus aureus (MRSA).

    abstract：:We have prepared a series of ten 3-arylcoumarin molecules, their respective fac-[Re(CO)3(bpy)L]+ and fac-[Re(CO)3(L⁀L)Br] complexes and tested all compounds for their antimicrobial efficacy. Whereas the 3-arylcoumarin ligands are virtually inactive against the human-associated pathogens with minimum inhibitory concent...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.112533

    authors： Sovari SN,Vojnovic S,Bogojevic SS,Crochet A,Pavic A,Nikodinovic-Runic J,Zobi F

    更新日期：2020-11-01 00:00:00

  • Design and one-pot synthesis of alpha-aminophosphonates and bis(alpha-aminophosphonates) by iron(III) chloride and cytotoxic activity.

    abstract：:In this study, we used a solution of FeCl(3) in THF to facilitate the Mannich-type reaction of aldehyde, amine and phosphite compounds to form corresponding alpha-aminophosphonates in a one-pot, three-component reaction. Selected alpha-aminophosphonates were entered into a biological assay test and were studied by doc...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2009.07.009

    authors： Rezaei Z,Firouzabadi H,Iranpoor N,Ghaderi A,Jafari MR,Jafari AA,Zare HR

    更新日期：2009-11-01 00:00:00

  • Vocational training for medicinal chemists: views from industry.

    abstract：:The Medicinal Chemistry Section of IUPAC sent a questionnaire regarding academic training for medicinal chemists to major research pharmaceutical companies in various countries in July 1992 and again in July 1993. A total of 102 replies were received from 65 companies, mainly from Germany, Italy, Japan, the UK and the...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/0223-5234(96)83968-7

    authors： Busse W,Ganellin C,Mitscher L

    更新日期：1996-01-01 00:00:00

  • Novel Biginelli dihydropyrimidines with potential anticancer activity: a parallel synthesis and CoMSIA study.

    abstract：:Novel Biginelli dihydropyrimidines of biological interest were prepared using p-toluene sulphonic acid as an efficient catalyst. All the thirty-two synthesised dihydropyrimidines were evaluated for their in vitro antioxidant activity using DPPH method. Only, compounds 28 and 29 exhibited reasonably good antioxidant ac...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2009.05.014

    authors： Prashantha Kumar BR,Sankar G,Nasir Baig RB,Chandrashekaran S

    更新日期：2009-10-01 00:00:00

  • The synthesis and biological evaluation of novel Danshensu-cysteine analog conjugates as cardiovascular-protective agents.

    abstract：:A series of novel amide and thioester conjugates between Danshensu and cysteine derivatives have been designed and synthesized based on the strategy of "medicinal chemical hybridization". Pharmacological evaluation indicated that the amide conjugates 3a/4a/17a and thioester conjugates 6a-d exhibited obvious protective...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2012.07.016

    authors： Jia Y,Dong X,Zhou P,Liu X,Pan L,Xin H,Zhu YZ,Wang Y

    更新日期：2012-09-01 00:00:00

  • Umbelliferone aminoalkyl derivatives, a new class of squalene-hopene cyclase inhibitors.

    abstract：:The synthesis is described of several aminoalkyl derivatives of coumarin, obtained in good yields under microwave or high-intensity ultrasound irradiation. These compounds proved uniformly active as inhibitors of squalene-hopene cyclase (SHC) from Alicyclobacillus acidocaldarius. Their design stemmed from our recent f...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2004.06.010

    authors： Cravotto G,Balliano G,Tagliapietra S,Palmisano G,Penoni A

    更新日期：2004-11-01 00:00:00

  • Development of 3-aryl-1-isoquinolinamines as potent antitumor agents based on CoMFA.

    abstract：:Various substituted 3-aryl-1-isoquinolinamines were designed and synthesized based on the previously constructed CoMFA model. Most of the synthesized compounds showed excellent potency in eight different human tumor cell lines as expected. In order to find the exact cytotoxic mechanism of these 3-aryl-1-isoquinolinami...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2010.08.042

    authors： Yang SH,Van HT,Le TN,Khadka DB,Cho SH,Lee KT,Lee ES,Lee YB,Ahn CH,Cho WJ

    更新日期：2010-11-01 00:00:00

  • A novel bis-furan scaffold for transthyretin stabilization and amyloid inhibition.

    abstract：:The design and synthesis of a novel bis-furan scaffold tailored for high efficiency at inhibiting transthyretin amyloid formation is reported. In vitro results show that the discovered compounds are more efficient inhibitors of amyloid formation than tafamidis, a drug currently used in the treatment of familial amyloi...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.02.074

    authors： Simões CJV,Almeida ZL,Costa D,Jesus CSH,Cardoso AL,Almeida MR,Saraiva MJ,Pinho E Melo TMVD,Brito RMM

    更新日期：2016-10-04 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

  • 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

  • Synthesis and SAR studies of mono O-prenylated coumarins as potent 15-lipoxygenase inhibitors.

    abstract：:All of the mono isopentenyloxy, -geranyloxy and -farnesyloxy derivatives of coumarin were synthesized and their inhibitory potency against soybean 15-lipoxygenase (SLO) and human 15-lipoxygenase-1 (HLO-1) were determined. Amongst the synthetic analogs, 5-farnesyloxycoumarin showed the most potent inhibitory activity a...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2012.09.006

    authors： Iranshahi M,Jabbari A,Orafaie A,Mehri R,Zeraatkar S,Ahmadi T,Alimardani M,Sadeghian H

    更新日期：2012-11-01 00:00:00

  • Evaluation of the local anaesthetic activity of 3-aminobenzo[d]isothiazole derivatives using the rat sciatic nerve model.

    abstract：:On the basis of computer prediction of biological activity by PASS and toxicity by DEREK, the most promising 32-alkylaminoacyl derivatives of 3-aminobenzo[d]isothiazole were selected for possible local anaesthetic action. This action was evaluated using an in vitro preparation of the isolated sciatic nerve of the rat ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2008.04.006

    authors： Geronikaki A,Vicini P,Dabarakis N,Lagunin A,Poroikov V,Dearden J,Modarresi H,Hewitt M,Theophilidis G

    更新日期：2009-02-01 00:00:00

  • Rational design, synthesis and QSAR study of vasorelaxant active 3-pyridinecarbonitriles incorporating 1H-benzimidazol-2-yl function.

    abstract：:A variety of 2-alkoxy-4-aryl-6-(1H-benzimidazol-2-yl)-3-pyridinecarbonitriles 4a-r were prepared via either regioselective reaction of 3-aryl-1-(1H-benzimidazol-2-yl)-2-propen-1-ones 3 with malononitrile or ylidenemalononitriles 6 with 2-acetyl-1H-benzimidazoles 1 in the presence of sodium alkoxide in the correspondin...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.01.042

    authors： Nofal ZM,Srour AM,El-Eraky WI,Saleh DO,Girgis AS

    更新日期：2013-05-01 00:00:00

  • Mannich bases in medicinal chemistry and drug design.

    abstract：:The biological activity of Mannich bases, a structurally heterogeneous class of chemical compounds that are generated from various substrates through the introduction of an aminomethyl function by means of the Mannich reaction, is surveyed, with emphasis on the relationship between structure and biological activity. T...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2014.10.076

    authors： Roman G

    更新日期：2015-01-07 00:00:00

  • Structure-activity study of quinazoline derivatives leading to the discovery of potent EGFR-T790M inhibitors.

    abstract：:We have developed a series of 6, 7-disubstituted-4-(arylamino) quinazoline derivatives that functioned as irreversible EGFR inhibitors, and these compounds exhibited excellent enzyme inhibition potency. As compared with afatinib, some of them showed significantly enhanced activities towards H1975 cells (EGFR-T790M). F...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.08.026

    authors： Zhang L,Yang Y,Zhou H,Zheng Q,Li Y,Zheng S,Zhao S,Chen D,Fan C

    更新日期：2015-09-18 00:00:00

  • Design and regioselective synthesis of trifluoromethylquinolone derivatives as potent antimicrobial agents.

    abstract：:Three series of new trifluoromethyl substituted quinolone derivatives were synthesized (4a-f, 6a-f and 8a-f) from corresponding substituted anilines by multi-step reactions. The regioselective alkylation with different alkyl halides were carried out by approaching two different routes to get the final products in good...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.07.021

    authors： Garudachari B,Isloor AM,Satyanarayana MN,Fun HK,Pavithra N,Kulal A

    更新日期：2013-10-01 00:00:00

  • Epoxide-containing side chains enhance antiproliferative activity of paullones.

    abstract：:The introduction of side chains bearing epoxide motifs into the molecular scaffold of kenpaullone and 9-trifluoromethylpaullone led to improved antiproliferative activity of the novel derivatives for human tumor cell lines. The syntheses were accomplished applying Stille coupling for the introduction of unsaturated si...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2005.02.004

    authors： Xie X,Lemcke T,Gussio R,Zaharevitz DW,Leost M,Meijer L,Kunick C

    更新日期：2005-07-01 00:00:00

  • Design, synthesis and antitubercular evaluation of benzothiazinones containing a piperidine moiety.

    abstract：:We herein report the design and synthesis of benzothiazinones containing a piperidine moiety as new antitubercular agents based on the structure feature of IMB-ZR-1 discovered in our lab. Some of them were found to have good in vitro activity (MIC < 1 μg/mL) against drug-susceptible Mycobacterium tuberculosis H37RV st...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.03.060

    authors： Lv K,Tao Z,Liu Q,Yang L,Wang B,Wu S,Wang A,Huang M,Liu M,Lu Y

    更新日期：2018-05-10 00:00:00

  • Synthesis and in vitro cytotoxic activity of pyrrolo[2,3-e]indole derivatives and a dihydro benzoindole analogue.

    abstract：:The synthesis of pyrrolo[2,3-e]indole derivatives with the structural characteristics of DNA bis- and mono-intercalators are described. A dihydro benzoindol analogue was also synthesised to elucidate the major structural requirements for cytotoxic activity. A biological evaluation of the test compounds was carried out...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/s0223-5234(01)01328-9

    authors： Chacón-García L,Martínez R

    更新日期：2002-03-01 00:00:00

  • Synthesis and initial tumor affinity testing of iodine-123 labelled EGFR-affine agents as potential imaging probes for hormone-refractory prostate cancer.

    abstract：UNLABELLED:The epidermal growth factor receptor (EGFR) is over-expressed in a variety of human cancers, including in hormone-refractory prostate carcinomas, in which the EGFR has been associated with advanced disease stage, resistance to standard treatment and poor prognosis. Therefore, the EGFR is considered to be a p...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2010.05.027

    authors： Fozing T,Scheuer C,Samnick S

    更新日期：2010-09-01 00:00:00

  • Present status of quinoxaline motifs: excellent pathfinders in therapeutic medicine.

    abstract：:Quinoxalines belong to a class of excellent heterocyclic scaffolds owing to their wide biological properties and diverse therapeutic applications in medicinal research. They are complementary in shapes and charges to numerous biomolecules they interact with, thereby resulting in increased binding affinity. The pharmac...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2014.08.034

    authors： Ajani OO

    更新日期：2014-10-06 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

  • Novel pentacyclic triterpenes exhibiting strong neuroprotective activity in SH-SY5Y cells in salsolinol- and glutamate-induced neurodegeneration models.

    abstract：:Novel triterpene derivatives were prepared and evaluated in salsolinol (SAL)- and glutamate (Glu)-induced models of neurodegeneration in neuron-like SH-SY5Y cells. Among the tested compounds, betulin triazole 4 bearing a tetraacetyl-β-d-glucose substituent showed a highly potent neuroprotective effect. Further studies...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2021.113168

    authors： Gonzalez G,Hodoň J,Kazakova A,D'Acunto CW,Kaňovský P,Urban M,Strnad M

    更新日期：2021-01-16 00:00:00

  • Combined inhibition of the EGFR/AKT pathways by a novel conjugate of quinazoline with isothiocyanate.

    abstract：:Epidermal growth factor receptor inhibitors (EGFR-TKIs) represent a class of compounds widely used in anticancer therapy. An increasing number of studies reports on combination therapies in which the block of the EGFR-TK activity is associated with inhibition of its downstream pathways, as PI3K-Akt. Sulforaphane targe...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.04.002

    authors： Tarozzi A,Marchetti C,Nicolini B,D'Amico M,Ticchi N,Pruccoli L,Tumiatti V,Simoni E,Lodola A,Mor M,Milelli A,Minarini A

    更新日期：2016-07-19 00:00:00

  • An insight into the biological activities of heterocyclic-fatty acid hybrid molecules.

    abstract：:Heterocyclic compounds are the interesting core structures for the development of new bioactive compounds. Fatty acids are derived from renewable raw materials and exhibit various biological activities. Several researchers are amalgamating these two bioactive components to yield bioactive hybrid molecules with some de...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2017.09.069

    authors： Venepally V,Reddy Jala RC

    更新日期：2017-12-01 00:00:00

  • Synthesis, characterization and DNA binding studies of new ruthenium(II)bisterpyridine complexes.

    abstract：:Two new ruthenium(II) complexes, [Ru(itpy)2](PF6)2, 1 and [Ru(bitpy)2](PF6)2 2, were synthesized and characterized by ESI-Mass, UV-Visible, 1H NMR, fluorescence spectroscopy and cyclic voltammetry. Complex 1 has been characterized crystallographically. Interaction of these complexes with CT-DNA has been studied using ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2009.10.008

    authors： Sathyaraj G,Weyhermüller T,Nair BU

    更新日期：2010-01-01 00:00:00