当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Synthesis of amphiphilic galactopyranosyl diamines and amino alcohols as antitubercular agents.

Synthesis of amphiphilic galactopyranosyl diamines and amino alcohols as antitubercular agents.

Abstract：

:Mono- and diacylated derivatives of galactopyranosyl amines were obtained from d-galactose, via aminated intermediates prepared by reaction of 6-deoxy-6-iodo-1,2:3,4-di-O-isopropylidene-alpha-d-galactopyranose with 1,3-propanediamine, 1,2-ethanediamine or ethanolamine. Monoacylated derivatives displayed antitubercular activity.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

de Almeida MV,Le Hyaric M,Amarante GW,Silva Lourenço MC,Lima Brandão ML

doi

10.1016/j.ejmech.2007.01.009

subject

Has Abstract

pub_date

2007-08-01 00:00:00

pages

1076-83

issue

8

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(07)00048-7

journal_volume

42

pub_type

杂志文章

相关文献

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY文献大全
  • 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

  • A new class of analgesic agents toward prostacyclin receptor inhibition: synthesis, biological studies and QSAR analysis of 1-hydroxyl-2-substituted phenyl-4,4,5,5-tetramethylimidazolines.

    abstract：:By studying the structural similarity of analgesic imidazolines and 2-phenylnitronyl nitroxides, 20 1-hydroxyl-2-substituted phenyl-4,4,5,5-tetramethylimidazolines (2a-t) were newly synthesized as selective antagonists of prostacyclin receptor (IP receptor). In the in vivo tail-flick assay, 2a-t (dose, 0.13 mmol/kg) r...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2007.07.007

    authors： Zhao M,Li Z,Peng L,Tang YR,Wang C,Zhang Z,Peng S

    更新日期：2008-05-01 00:00:00

  • 2-hydroxyisoquinoline-1,3(2H,4H)-diones as inhibitors of HIV-1 integrase and reverse transcriptase RNase H domain: influence of the alkylation of position 4.

    abstract：:We report herein the synthesis of a series of fifteen 2-hydroxyisoquinoline-1,3(2H,4H)-dione derivatives. Alkyl and arylalkyl groups were introduced on position 4 of the basis scaffold. All the compounds presented poor inhibitory properties against HIV-1 reverse transcriptase ribonuclease H (RNase H). Four compounds i...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2010.11.033

    authors： Billamboz M,Bailly F,Lion C,Calmels C,Andréola ML,Witvrouw M,Christ F,Debyser Z,De Luca L,Chimirri A,Cotelle P

    更新日期：2011-02-01 00:00:00

  • Synthesis and preliminary in vitro biological evaluation of 7α-testosterone-chlorambucil hybrid designed for the treatment of prostate cancer.

    abstract：:The synthesis of 7α-testosterone-chlorambucil hybrid is reported. This compound is made from testosterone in a 6 step reaction sequence and with 23% overall yield. An alternative convergent reaction sequence yielded the same hybrid through a Grubbs metathesis reaction between chlorambucil allyl ester and 7α-allyltesto...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.04.027

    authors： Bastien D,Hanna R,Leblanc V,Asselin É,Bérubé G

    更新日期：2013-06-01 00:00:00

  • Ruthenium(II) polypyridyl complex as inhibitor of acetylcholinesterase and Aβ aggregation.

    abstract：:Two ruthenium(II) polypyridyl complexes [Ru(phen)3](2+) (1) and [Ru(phen)2(bxbg)](2+) (2) (where phen = 1,10 phenanthroline, bxbg = bis(o-xylene)bipyridine glycoluril) have been evaluated for acetylcholinesterase (AChE) and Amyloid-β peptide (Aβ) aggregation inhibition. Complex 2 exhibits higher potency of AChE inhibi...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.01.052

    authors： Vyas NA,Bhat SS,Kumbhar AS,Sonawane UB,Jani V,Joshi RR,Ramteke SN,Kulkarni PP,Joshi B

    更新日期：2014-03-21 00:00:00

  • New thiazole-2(3H)-thiones containing 4-(3,4,5-trimethoxyphenyl) moiety as anticancer agents.

    abstract：:A new series of thiazole-2(3H)-thiones containing 4-(3,4,5-trimethoxyphenyl) moiety were synthesized as diaryl-heterocylic analogs of combretastatin A-4 with anticancer activity. The cytotoxicity evaluation of synthesized compounds against cancer cell lines (A549, MCF-7 and SKOV3) revealed that most of them had potent...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2019.111784

    authors： Ansari M,Shokrzadeh M,Karima S,Rajaei S,Fallah M,Ghassemi-Barghi N,Ghasemian M,Emami S

    更新日期：2020-01-01 00:00:00

  • Synthesis, structure-activity relationship and trypanocidal activity of pyrazole-imidazoline and new pyrazole-tetrahydropyrimidine hybrids as promising chemotherapeutic agents for Chagas disease.

    abstract：:Drug therapy for Chagas disease remains a major challenge as potential candidate drugs have failed clinical trials. Currently available drugs have limited efficacy and induce serious side effects. Thus, the discovery of new drugs is urgently needed in the fight against Chagas' disease. Here, we synthesized and evaluat...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2019.111610

    authors： Monteiro ME,Lechuga G,Lara LS,Souto BA,Viganó MG,Bourguignon SC,Calvet CM,Oliveira FOR Jr,Alves CR,Souza-Silva F,Santos MS,Pereira MCS

    更新日期：2019-11-15 00:00:00

  • QSAR analysis of 1,4-dihydro-4-oxo-1-(2-thiazolyl)-1,8-naphthyridines with anticancer activity.

    abstract：:In the present study a quantitative structure activity relationship (QSAR) analysis was applied to a series of 100 of 7- and 3-substituted 1,4-dihydro-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine derivatives. The Chem-X (version 2000) software was used to develop 3D QSAR models. The steric and electrostatic interactions be...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2007.01.029

    authors： Atanasova M,Ilieva S,Galabov B

    更新日期：2007-09-01 00:00:00

  • Discovery of novel indole derivatives as allosteric inhibitors of fructose-1,6-bisphosphatase.

    abstract：:A series of novel indole derivatives was designed and synthesized as inhibitors of fructose-1,6-bisphosphatase (FBPase). The most potent compound 14c was identified with an IC50 value of 0.10 μM by testing the inhibitory activity against recombinant human FBPase. The structure-activity relationships were investigated ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.11.049

    authors： Bie J,Liu S,Li Z,Mu Y,Xu B,Shen Z

    更新日期：2015-01-27 00:00:00

  • Design, synthesis and in vitro evaluation of heterobivalent peptidic radioligands targeting both GRP- and VPAC1-Receptors concomitantly overexpressed on various malignancies - Is the concept feasible?

    abstract：:Radiolabeled heterobivalent peptidic ligands (HBPLs), being able to address different receptors, are highly interesting tumor imaging agents as they can offer multiple advantages over monovalent peptide receptor ligands. However, few examples of radiolabeled HBPLs have been described so far. One promising approach is ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.05.047

    authors： Lindner S,Fiedler L,Wängler B,Bartenstein P,Schirrmacher R,Wängler C

    更新日期：2018-07-15 00:00:00

  • Novel NSAID 1-acyl-4-cycloalkyl/arylsemicarbazides and 1-acyl-5-benzyloxy/hydroxy carbamoylcarbazides as potential anticancer agents and antioxidants.

    abstract：:The novel 1-acyl-4-cycloalkyl/arylsemicarbazides (5a-y) and 1-acyl-5-benzyloxy/hydroxycarbamoylcarbazides (8a-f) derived from the nonsteroidal anti-inflammatory drugs ibuprofen, fenoprofen and reduced ketoprofen were prepared, fully chemically characterized and evaluated for their cytostatic, antiviral and antioxidant...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2012.02.046

    authors： Perković I,Butula I,Kralj M,Martin-Kleiner I,Balzarini J,Hadjipavlou-Litina D,Katsori AM,Zorc B

    更新日期：2012-05-01 00:00:00

  • The race to treat COVID-19: Potential therapeutic agents for the prevention and treatment of SARS-CoV-2.

    abstract：:The unforeseen emergence of coronavirus disease 2019 (COVID-19), a severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) at the Wuhan province of China in December 2019, subsequently its abrupt spread across the world has severely affected human life. In a short span of time, COVID-19 has sacked more than one m...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2021.113157

    authors： Shagufta,Ahmad I

    更新日期：2021-01-12 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

  • Benzenediol lactones: a class of fungal metabolites with diverse structural features and biological activities.

    abstract：:Benzenediol lactones are a structurally variable family of fungal polyketide metabolites possessing a macrolide core structure fused into a resorcinol aromatic ring. These compounds are widespread in fungi mainly in the genera such as Aigialus, Cochliobolus, Curvularia, Fusarium, Humicola, Lasiodiplodia, Penicillium a...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2014.11.067

    authors： Shen W,Mao H,Huang Q,Dong J

    更新日期：2015-06-05 00:00:00

  • Synthesis and antiproliferative activity of novel polynuclear heterocyclic compounds derived from 2,3-diaminophenazine.

    abstract：:2,3-Diaminophenazine 1 was used as a precursor for the preparation of some novel phenazine derivatives such as imidazo[4,5-b]phenazine-2-thione 2, its methylthio 3, ethyl 1-aryl-3H-[1,2,4]triazolo[2,3-a]imidazo[4,5-b]phenazines 8a-c, ethyl (2Z)-[3-aminophenazin-2-yl)amino](phenylhydrazono)ethanoate 9, pyrazino[2,3-b]p...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.12.007

    authors： Mahran AM,Ragab SSh,Hashem AI,Ali MM,Nada AA

    更新日期：2015-01-27 00:00:00

  • Design, synthesis and characterization of peptidomimetic conjugate of BODIPY targeting HER2 protein extracellular domain.

    abstract：:Among the EGFRs, HER2 is a major heterodimer partner and also has important implications in the formation of particular tumors. Interaction of HER2 protein with other EGFR proteins can be modulated by small molecule ligands and, hence, these protein-protein interactions play a key role in biochemical reactions related...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.04.038

    authors： Banappagari S,McCall A,Fontenot K,Vicente MG,Gujar A,Satyanarayanajois S

    更新日期：2013-07-01 00:00:00

  • N-Aryl-N'-(chroman-4-yl)ureas and thioureas display in vitro anticancer activity and selectivity on apoptosis-resistant glioblastoma cells: screening, synthesis of simplified derivatives, and structure-activity relationship analysis.

    abstract：:A series of chroman derivatives previously reported as potassium channel openers, as well as some newly synthesized simplified structures, were examined for their in vitro effects on the growth of three human high-grade glioma cell lines: U373, T98G, and Hs683. Significant in vitro growth inhibitory activity was obser...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2012.06.050

    authors： Goffin E,Lamoral-Theys D,Tajeddine N,de Tullio P,Mondin L,Lefranc F,Gailly P,Rogister B,Kiss R,Pirotte B

    更新日期：2012-08-01 00:00:00

  • Design, synthesis, cytotoxicity and mechanism of novel dihydroartemisinin-coumarin hybrids as potential anti-cancer agents.

    abstract：:To develop novel agents with anticancer activities, thirty-four new dihydroartemisinin-coumarin hybrids were designed and synthesized in this study. Those compounds were identified that had great anticancer activity against two cancer cell lines (MDA-MB-231 and HT-29). The structure-activity relationships of the deriv...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.04.005

    authors： Yu H,Hou Z,Tian Y,Mou Y,Guo C

    更新日期：2018-05-10 00:00:00

  • 3-Aryl-2-[1H-benzotriazol-1-yl]acrylonitriles: a novel class of potent tubulin inhibitors.

    abstract：:During a screening for compounds that could act against Mycobacterium tuberculosis, a series of new cellular antiproliferative agents was identified. The most cytotoxic molecules were evaluated against a panel of human cell lines derived from hematological and solid human tumors. In particular, (E)-2-(1H-benzo[d] [1,2...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2011.06.018

    authors： Carta A,Briguglio I,Piras S,Boatto G,La Colla P,Loddo R,Tolomeo M,Grimaudo S,Di Cristina A,Pipitone RM,Laurini E,Paneni MS,Posocco P,Fermeglia M,Pricl S

    更新日期：2011-09-01 00:00:00

  • 3-Pyrazolone analogues of the 3-isoxazolol metabotropic excitatory amino acid receptor agonist homo-AMPA. Synthesis and pharmacological testing.

    abstract：:We have previously shown that the higher homologue of (S)-glutamic acid [(S)-Glu], (S)-alpha-aminoadipic acid [(S)-alpha-AA] is selectively recognized by the mGlu(2) and mGlu(6) subtypes of the family of metabotropic glutamic acid (mGlu) receptors. Furthermore, a number of analogues of (S)-alpha-AA, in which the termi...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/s0223-5234(99)00122-1

    authors： Zimmermann D,Janin YL,Brehm L,Bräuner-Osborne H,Ebert B,Johansen TN,Madsen U,Krogsgaard-Larsen P

    更新日期：1999-11-01 00:00:00

  • Synthesis and biological activity of novel N6-substituted and 2,N6-disubstituted adenine ribo- and 3'-C-methyl-ribonucleosides as antitumor agents.

    abstract：:A series of N6-aminopurine-9-β-D-ribonucleosides and ribose-modified 3'-C-methyl analogues substituted at N6-position with a small group like hydroxy, methoxy or amino group or at C2(N6) position have been synthesized and tested against a panel of human leukemia and carcinoma cell lines. N6-Hydrazino-9-β-D-ribofuranos...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2011.01.055

    authors： Cappellacci L,Petrelli R,Franchetti P,Vita P,Kusumanchi P,Kumar M,Jayaram HN,Zhou B,Yen Y,Grifantini M

    更新日期：2011-05-01 00:00:00

  • Synthesis of new chalcone derivatives containing a rhodanine-3-acetic acid moiety with potential anti-bacterial activity.

    abstract：:With an intention to synergize the anti-bacterial activity of chalcones and rhodanine-3-acetic acid, several hybrid compounds possessing chalcone and rhodanine-3-acetic acid moieties were synthesized and tested for their anti-bacterial activity. Some compounds presented great anti-microbial activities against Gram-pos...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2010.09.031

    authors： Chen ZH,Zheng CJ,Sun LP,Piao HR

    更新日期：2010-12-01 00:00:00

  • Antidyslipidemic and antioxidative activities of 8-hydroxyquinoline derived novel keto-enamine Schiffs bases.

    abstract：:8-Hydroxyquinoline when subjected to Duff reaction resulted in the formation of unexpected 7-methylaminomethylene-8-oxo-7, 8-dihydroquinoline-5-carbaldehyde 2, which existed in the keto-enamine form, in which the aromaticity of the relevant ring was disrupted, which upon subsequent treatment with various primary amine...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2008.08.004

    authors： Sashidhara KV,Kumar A,Bhatia G,Khan MM,Khanna AK,Saxena JK

    更新日期：2009-04-01 00:00:00

  • Synthesis and cytotoxicity of 3-aryl acrylic amide derivatives of the simplified saframycin-ecteinascidin skeleton prepared from L-dopa.

    abstract：:Twenty four compounds with diversified 3-aryl acrylic amide side chains of the simplified saframycin-ecteinascidin pentacyclic skeleton were synthesized via a 14-step stereospecific route starting from L-dopa. The cytotoxicities of these compounds were tested against eight human tumor cell lines including HCT-8, BEL-7...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.01.033

    authors： Guo J,Dong W,Liu W,Yan Z,Wang N,Liu Z

    更新日期：2013-04-01 00:00:00

  • ROS-responsive and multifunctional anti-Alzheimer prodrugs: Tacrine-ibuprofen hybrids via a phenyl boronate linker.

    abstract：:Current drugs available in clinic for Alzheimer's disease (AD) treatment can only alleviate disease symptoms without clearly curing or delaying the process of AD. And some AD drugs failed in Phase III clinical trials are only focused on targeting amyloid-β (Aβ). Therefore, an alternative strategy in AD drug design is ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.112997

    authors： Liu Z,Zhang B,Xia S,Fang L,Gou S

    更新日期：2020-11-06 00:00:00

  • Newly designed organotin(IV) carboxylates with peptide linkage: Synthesis, structural elucidation, physicochemical characterizations and pharmacological investigations.

    abstract：:Fourteen new organotin(IV) carboxylate complexes with peptide linkage of (2-(4-methoxy-2-nitrophenylcarbamoyl)benzoic acid) were successfully synthesized and characterized by elemental analyses, FT-IR, NMR (1H, 13C and 119Sn) and single crystal X-ray techniques. FT-IR results of the sodium salt of 2-(4-methoxy-2-nitro...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2017.11.001

    authors： Sirajuddin M,McKee V,Tariq M,Ali S

    更新日期：2018-01-01 00:00:00

  • Synthesis, characterization and anticancer screening of some novel piperonyl-tetrazole derivatives.

    abstract：:A series of new 1,2-substituted tetrazole derivatives were synthesized and evaluated on MCF-7 (ER positive), MDA-MB-231 and ZR-75 (ER negative) breast cancer cell lines. Out of the fourteen compounds, three compounds 10, 12 and 14 showed higher inhibitory effects on MCF-7 cells. Whereas, compound 8 exhibited higher in...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.11.008

    authors： Arshad M,Bhat AR,Pokharel S,Kim JE,Lee EJ,Athar F,Choi I

    更新日期：2014-01-01 00:00:00

  • Synthesis and characterization of binary and ternary complexes of diclofenac with a methyl-beta-CD and monoethanolamine and in vitro transdermal evaluation.

    abstract：:Here, we describe the chemical characterization of the inclusion complex between diclofenac (DCF) and methyl-beta-cyclodextrin (M-beta-CD) in the presence or absence of monoethanolamine (MEA). Several techniques were used to analyze the complex both in solution and in the solid state. Solubility of DCF was increased b...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2010.05.068

    authors： Mora MJ,Longhi MR,Granero GE

    更新日期：2010-09-01 00:00:00

  • 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 effe...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2006.03.009

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

    更新日期：2006-06-01 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