当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Synthesis, in vitro β-glucuronidase inhibitory potential and molecular docking studies of quinolines.

Synthesis, in vitro β-glucuronidase inhibitory potential and molecular docking studies of quinolines.

Abstract：

:In this study synthesis and β-glucuronidase inhibitory potential of 3/5/8 sulfonamide and 8-sulfonate derivatives of quinoline (1-40) are discussed. Studies reveal that all the synthetic compounds were found to have good inhibitory activity against β-glucuronidase. Nonetheless, compounds 1, 2, 5, 13, and 22-24 having IC50 values in the range of 1.60-8.40 μM showed superior activity than the standard saccharic acid 1,4-lactone (IC50 = 48.4 ± 1.25 μM). Moreover, molecular docking studies of selected compounds were also performed to see interactions between active compounds and binding sites. Structures of all the synthetic compounds were confirmed through 1H NMR, EI-MS and HREI-MS spectroscopic techniques.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Bano B,Arshia,Khan KM,Kanwal,Fatima B,Taha M,Ismail NH,Wadood A,Ghufran M,Perveen S

doi

10.1016/j.ejmech.2017.08.052

subject

Has Abstract

pub_date

2017-10-20 00:00:00

pages

849-864

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(17)30663-3

journal_volume

139

pub_type

杂志文章

相关文献

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY文献大全
  • 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

  • Synthesis and anticancer activity of lavendustin A derivatives containing arylethenylchromone substituents.

    abstract：:2-Styrylchromones, which are relatively scarce in nature, have been reported to possess potent cytotoxicities on KB cell line. Lavendustin A, a metabolite of Streptomyces griseolavendus, has been shown to inhibit a growth of A431 cell line. Accordingly, a series of compounds 3a-g having structural features of styrylch...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2006.04.008

    authors： Lee KY,Nam DH,Moon CS,Seo SH,Lee JY,Lee YS

    更新日期：2006-08-01 00:00:00

  • Design, synthesis and structure-activity relationships of 4-phenyl-1H-1,2,3-triazole phenylalanine derivatives as novel HIV-1 capsid inhibitors with promising antiviral activities.

    abstract：:HIV-1 CA is involved in different stages of the viral replication cycle, performing essential roles in both early (uncoating, reverse transcription, nuclear import, integration) and late events (assembly). Recent efforts have demonstrated HIV-1 CA protein as a prospective therapeutic target for the development of new ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.112085

    authors： Sun L,Huang T,Dick A,Meuser ME,Zalloum WA,Chen CH,Ding X,Gao P,Cocklin S,Lee KH,Zhan P,Liu X

    更新日期：2020-03-15 00:00:00

  • 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

  • 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

  • One-pot synthesis and biological evaluation of 2-pyrrolidinyl-4-amino-5-(3',4',5'-trimethoxybenzoyl)thiazole: a unique, highly active antimicrotubule agent.

    abstract：:A wide variety of small molecules with diverse molecular scaffolds inhibit microtubule formation. In this article we report a one-pot procedure for the preparation of a novel 2-(N-pyrrolidinyl)-4-amino-5-(3',4',5'-trimethoxybenzoyl)thiazole in which the size of the substituent at the C-2 position of the thiazole ring ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2011.10.013

    authors： Romagnoli R,Baraldi PG,Lopez Cara C,Kimatrai Salvador M,Bortolozzi R,Basso G,Viola G,Balzarini J,Brancale A,Fu XH,Li J,Zhang SZ,Hamel E

    更新日期：2011-12-01 00:00:00

  • Identification of multi-target inhibitors of leukotriene and prostaglandin E2 biosynthesis by structural tuning of the FLAP inhibitor BRP-7.

    abstract：:Leukotrienes (LTs) and prostaglandin (PG)E2 are enzymatically produced from arachidonic acid and represent highly bioactive lipid mediators with pro-inflammatory functions. Here, we report on novel multi-target inhibitors that potently and dually interfere with 5-lipoxygenase-activating protein (FLAP) and microsomal p...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.03.045

    authors： Gür ZT,Çalışkan B,Garscha U,Olgaç A,Schubert US,Gerstmeier J,Werz O,Banoglu E

    更新日期：2018-04-25 00:00:00

  • Synthesis and cytotoxicity assay of four ganglioside GM3 analogues.

    abstract：:A concise and efficient synthetic route for preparation of four ganglioside GM3 analogues was described. The key step is a highly regioselective and stereoselective α-sialylation from a suitably protected glycoside acceptor with a sialyl xanthate to provide the sialo-oligosaccharide in good yield. The cytotoxic proper...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.01.054

    authors： Qu H,Liu JM,Wdzieczak-Bakala J,Lu D,He X,Sun W,Sollogoub M,Zhang Y

    更新日期：2014-03-21 00:00:00

  • Novel oxime-bearing coumarin derivatives act as potent Nrf2/ARE activators in vitro and in mouse model.

    abstract：:We have designed and synthesized certain novel oxime- and amide-bearing coumarin derivatives as nuclear factor erythroid 2 p45-related factor 2 (Nrf2) activators. The potency of these compounds was measured by antioxidant responsive element (ARE)-driven luciferase activity, level of Nrf2-related cytoprotective genes a...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.10.029

    authors： Chang KM,Chen HH,Wang TC,Chen IL,Chen YT,Yang SC,Chen YL,Chang HH,Huang CH,Chang JY,Shih C,Kuo CC,Tzeng CC

    更新日期：2015-12-01 00:00:00

  • Novel cajaninstilbene acid derivatives as antibacterial agents.

    abstract：:Discovery of novel antibacterial agents with new structural scaffolds that combat drug-resistant pathogens is an urgent task. Cajaninstilbene acid, which is isolated from pigeonpea leaves, has shown antibacterial activity. In this study, a series of cajaninstilbene acid derivatives were designed and synthesized. The a...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.06.008

    authors： Geng ZZ,Zhang JJ,Lin J,Huang MY,An LK,Zhang HB,Sun PH,Ye WC,Chen WM

    更新日期：2015-07-15 00:00:00

  • Design, synthesis, in vitro antiproliferative evaluation, and kinase inhibitory effects of a new series of imidazo[2,1-b]thiazole derivatives.

    abstract：:Design and synthesis of a new series of 5,6-diarylimidazo[2,1-b]thiazole derivatives possessing terminal aryl sulfonamide moiety are described. Their in vitro antiproliferative activities against a panel of 57 human cancer cell lines of nine different cancer types were tested at the NCI. Compounds 8a, 8b, 8n, 8q, 8t, ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.03.065

    authors： Abdel-Maksoud MS,Kim MR,El-Gamal MI,Gamal El-Din MM,Tae J,Choi HS,Lee KT,Yoo KH,Oh CH

    更新日期：2015-05-05 00:00:00

  • Arylnitroalkenes as scavengers of macrophage-generated oxidants.

    abstract：:Oxygen and nitrogen derived molecules mediated oxidation and nitration have been involved in several pathological conditions. Conversely, nitric oxide and hydrogen peroxide are important signalization intermediates, whose concentrations are tightly regulated by specialized enzyme repertoires and should remain undistur...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.12.029

    authors： Celano L,Carabio C,Frache R,Cataldo N,Cerecetto H,González M,Thomson L

    更新日期：2014-03-03 00:00:00

  • New imidazolidineiminothione derivatives: Synthesis, spectral characterization and evaluation of antitumor, antiviral, antibacterial and antifungal activities.

    abstract：:A series of new imidazolidineiminothione derivatives with various halogenated and alkylated aromatic substituents at N-(1) and at N-(3) was synthesized through the reaction of N-arylcyanothioformamides with arylisocyanate derivatives. Structure of imidazolidineiminothione derivatives were established based on spectros...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.06.051

    authors： Moussa Z,El-Sharief MAMS,Abbas SY

    更新日期：2016-10-21 00:00:00

  • 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 M...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2010.06.036

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

    更新日期：2010-10-01 00:00:00

  • Probing the aurone scaffold against Plasmodium falciparum: design, synthesis and antimalarial activity.

    abstract：:A library comprising 44 diversely substituted aurones derivatives was synthesized by straightforward aldol condensation reactions of benzofuranones and the appropriately substituted benzaldehydes. Microwave enhanced synthesis using palladium catalyzed protocols was introduced as a powerful strategy for extending the c...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.04.076

    authors： Carrasco MP,Newton AS,Gonçalves L,Góis A,Machado M,Gut J,Nogueira F,Hänscheid T,Guedes RC,dos Santos DJ,Rosenthal PJ,Moreira R

    更新日期：2014-06-10 00:00:00

  • Peptidomimetics containing a vinyl ketone warhead as falcipain-2 inhibitors.

    abstract：:The design, chemical synthesis, and enzymatic activity evaluation of a set of falcipain-2 inhibitors are reported. These compounds contain a proven peptidomimetic recognition motif based on a benzo[1,4]diazepin-2-one (1,4-BDZ) framework built on a dipeptide sequence, and a Michael acceptor terminal moiety capable of d...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2011.02.058

    authors： Ettari R,Zappalà M,Micale N,Grazioso G,Giofrè S,Schirmeister T,Grasso S

    更新日期：2011-06-01 00:00:00

  • Conformational studies of chiral D-Lys-PNA and achiral PNA system in binding with DNA or RNA through a molecular dynamics approach.

    abstract：:The growing interest in peptide nucleic acid (PNA) oligomers has led to the development of a very wide variety of PNA derivatives. Among others, the introduction of charged chiral groups on a PNA oligomer has proven effective in improving DNA binding ability, complexation direction and cellular uptake. In particular, ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.08.015

    authors： Autiero I,Saviano M,Langella E

    更新日期：2015-02-16 00:00:00

  • Synthesis and evaluation of some new benzimidazole derivatives as potential antimicrobial agents.

    abstract：:The efficient synthesis of novel azetidin-2-ones 6 has been established. Thus, condensation of 5-[(2-methyl-1H-benzimidazol-1-yl)methyl]-1,3,4-thiadiazol-2-amine 4 with various aromatic aldehydes afforded 5-[(2-methyl-1H-benzimidazol-1-yl)methyl]-N-[(substituted) phenylmethylidene]-1,3,4-thiadiazol-2-amine 5 which on ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2008.01.022

    authors： Ansari KF,Lal C

    更新日期：2009-05-01 00:00:00

  • Design and synthesis of new potent PTP1B inhibitors with the skeleton of 2-substituted imino-3-substituted-5-heteroarylidene-1,3-thiazolidine-4-one: Part I.

    abstract：:A new series of 2-substituted imino-3-substituted-5- heteroarylidene-1,3-thiazolidine-4-ones as the potent bidentate PTP1B inhibitors were designed and synthesized in this paper. All of the new compounds were characterized and identified by spectra analysis. The biological screening test against PTP1B showed that some...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.05.060

    authors： Meng G,Zheng M,Wang M,Tong J,Ge W,Zhang J,Zheng A,Li J,Gao L,Li J

    更新日期：2016-10-21 00:00:00

  • Synthesis and antiinflammatory activity of heterocyclic indole derivatives.

    abstract：:Chalcones of indole 1-5 and their corresponding products; pyrazolines 6-10 and azo compounds 11-15 were synthesised and evaluated for their antiinflammatory activity against carrageenan induced oedema in albino rats at a dose of 50 mg x kg(-1) oral. The structure of compounds was confirmed by IR, (1)H-NMR and mass spe...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2003.11.002

    authors： Rani P,Srivastava VK,Kumar A

    更新日期：2004-05-01 00:00:00

  • Biological potential of carbazole derivatives.

    abstract：:Carbazole skeleton is the key structural motif of many biologically active compounds including synthetic and natural products. Over the past several years, a large number of research highlighting the significance of carbazole derivatives has been reported in the literature. The present review focuses on the recent pro...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2015.02.059

    authors： Głuszyńska A

    更新日期：2015-04-13 00:00:00

  • High anticancer potency on tumor cells of dehydroabietylamine Schiff-base derivatives and a copper(II) complex.

    abstract：:Five bioactive dehydroabietylamine Schiff-base derivatives (L1-L5) had been synthesized from Dehydroabietylamine (L0), and the complex Cu(L1)2 had been obtained from the compound L1 and copper(II) acetate. Their activities against Hela (cervix), MCF-7 (breast), A549 (lung), HepG2 (liver) and HUVEC (umbilical vein, nor...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.01.041

    authors： Zhao F,Wang W,Lu W,Xu L,Yang S,Cai XM,Zhou M,Lei M,Ma M,Xu HJ,Cao F

    更新日期：2018-02-25 00:00:00

  • Synthesis, structure, toxicological and pharmacological investigations of 4-hydroxycoumarin derivatives.

    abstract：:Twenty 4-hydroxycoumarin derivatives were synthesized. Five of them are described for the first time. The X-ray crystal structure analysis of 3,3'-(2,3,4-trimethoxyphenylmethylene)bis-(4-hydroxy-2H-1-benzopyran-2-one) (7) and 3,3'-(3,5-dimethoxy-4-hydroxyphenylmethylene)bis-(4-hydroxy-2H-1-benzopyran-2-one) (9) confir...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2006.03.007

    authors： Manolov I,Maichle-Moessmer C,Danchev N

    更新日期：2006-07-01 00:00:00

  • Design, synthesis and evaluation of diarylpiperazine derivatives as potent anti-tubercular agents.

    abstract：:Molecular hybridization is an emerging approach to design novel ligands by combination of two or more pharmacophoric subunits of known bioactive compounds. In the present study, we have designed a novel series of diarylpiperazine analogues, synthesized, characterized using FTIR, (1)H NMR, Mass, Elemental analysis and ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.10.024

    authors： Penta A,Franzblau S,Wan B,Murugesan S

    更新日期：2015-11-13 00:00:00

  • Carboline- and phenothiazine-derivated heterocycles as potent SIGMA-1 protein ligands.

    abstract：:Sigma 1 receptors are associated with neurodegenerative and psychiatric disorders. These receptors, via their chaperoning functions that counteract endoplasmic reticulum stress and block neurodegeneration, may serve as a target for a new generation of antidepressants or neuroprotective agents. The involvement of these...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.10.053

    authors： Donnier-Maréchal M,Larchanché PE,Le Broc D,Furman C,Carato P,Melnyk P

    更新日期：2015-01-07 00:00:00

  • Synthesis and innate immunosuppressive effect of 1,2-cyclopentanediol derivatives.

    abstract：:Innate immunity is the front line of self-defense against infectious microorganisms. In mammals, innate immunity interacts with adaptive immunity and plays a key role in regulating the immune response. Therefore, innate immunity is a good pharmaceutical target for the development of immune regulators. After searching ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2011.01.049

    authors： Kikuchi H,Okazaki K,Sekiya M,Uryu Y,Ueda K,Katou Y,Kurata S,Oshima Y

    更新日期：2011-04-01 00:00:00

  • Discovery of SP-96, the first non-ATP-competitive Aurora Kinase B inhibitor, for reduced myelosuppression.

    abstract：:Aurora Kinase B is a serine-threonine kinase known to be overexpressed in several cancers, with no inhibitors approved for clinical use. Herein, we present the discovery and optimization of a series of novel quinazoline-based Aurora Kinase B inhibitors. The lead inhibitor SP-96 shows sub-nanomolar potency in Aurora B ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.112589

    authors： Lakkaniga NR,Zhang L,Belachew B,Gunaganti N,Frett B,Li HY

    更新日期：2020-10-01 00:00:00

  • Synthesis and in vitro anticancer activity evaluation of novel bioreversible phosphate inositol derivatives.

    abstract：:The chemistry and biology of phosphorylated inositols have become intense areas of research during the last two decades due to their involvement in various cellular signaling processes. However, the metabolic instability by phosphatases or kinases and poor penetration make it difficult to become a drug used in the cli...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.01.064

    authors： Chen W,Deng Z,Chen K,Dou D,Song F,Li L,Xi Z

    更新日期：2015-03-26 00:00:00

  • Aryl-1,3,5-triazine derivatives as histamine H4 receptor ligands.

    abstract：:A series of novel 2-amino-4-(4-methylpiperazin-1-yl)-1,3,5-triazine derivatives with different aryl substituents in the 6-position was designed, synthesized and evaluated for histamine H4 receptor (H4R) affinity in Sf9 cells expressing human H4R co-expressed with G-protein subunits. Triazine derivative 8 with a 6-(p-c...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.06.032

    authors： Łażewska D,Więcek M,Ner J,Kamińska K,Kottke T,Schwed JS,Zygmunt M,Karcz T,Olejarz A,Kuder K,Latacz G,Grosicki M,Sapa J,Karolak-Wojciechowska J,Stark H,Kieć-Kononowicz K

    更新日期：2014-08-18 00:00:00

  • Indole chalcones: Design, synthesis, in vitro and in silico evaluation against Mycobacterium tuberculosis.

    abstract：:Indole chalcones were designed and synthesized as a promising set of compounds against H37Rv strain of Mycobacterium tuberculosis. Within this library of compounds, (E)-1-(furan-3-yl)-3-(1H-indol-3-yl)prop-2-en-1-one (18), (E)-3-(1H-indol-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one (20) and (E)-2-((1H-indol-2-yl)methylene)...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.112358

    authors： Ramesh D,Joji A,Vijayakumar BG,Sethumadhavan A,Mani M,Kannan T

    更新日期：2020-07-15 00:00:00