当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Preparation and antitubercular activities in vitro and in vivo of novel Schiff bases of isoniazid.

Preparation and antitubercular activities in vitro and in vivo of novel Schiff bases of isoniazid.

Abstract：

:Structural modification of the frontline antitubercular isonicotinic acid hydrazide (INH) provides lipophilic adaptations (3-46) of the drug in which the hydrazine moiety of the parent compound has been chemically blocked from the deactivating process of N(2)-acetylation by N-arylaminoacetyl transferases. As a class, these compounds show high levels of activity against Mycobacterium tuberculosis in vitro and in tuberculosis-infected macrophages. They provide strong protection in tuberculosis-infected mice and have low toxicity. With some representatives of this class achieving early peak plasma concentrations approximately three orders of magnitude above minimum inhibitory concentration, they may serve as tools for improving our understanding of INH-based treatment modalities, particularly for those patients chronically underdosed in conventional INH therapy.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Hearn MJ,Cynamon MH,Chen MF,Coppins R,Davis J,Joo-On Kang H,Noble A,Tu-Sekine B,Terrot MS,Trombino D,Thai M,Webster ER,Wilson R

doi

10.1016/j.ejmech.2009.05.009

subject

Has Abstract

pub_date

2009-10-01 00:00:00

pages

4169-78

issue

10

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(09)00302-X

journal_volume

44

pub_type

杂志文章

相关文献

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY文献大全
  • 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

  • Glycosylation enhances the anti-migratory activities of isomalyngamide A analogs.

    abstract：:Three, new, fully synthetic glycosylated isomalyngamide A analogs 4-6 were prepared and evaluated for their anti-migratory activities in human breast cancer cells. The results of the study show that two glycosylated derivatives 4 and 5, containing mannose and galactose appendages, suppress metastatic events (e.g., mig...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.03.044

    authors： More SV,Chang TT,Chiao YP,Jao SC,Lu CK,Li WS

    更新日期：2013-06-01 00:00:00

  • Synthesis and in vitro evaluation of novel substituted isatin-propylene-1H-1,2,3-triazole-4-methylene-moxifloxacin hybrids for their anti-mycobacterial activities.

    abstract：:Twelve novel substituted isatin-propylene-1H-1,2,3-triazole-4-methylene-moxifloxacin hybrids 5a-l were designed, synthesized and screened for their in vitro anti-mycobacterial activities against drug-sensitive and multidrug-resistant Mycobacterium tuberculosis as well as cytotoxicity in VERO cell line. All hybrids exh...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2017.11.090

    authors： Yan X,Lv Z,Wen J,Zhao S,Xu Z

    更新日期：2018-01-01 00:00:00

  • Fluorinated benzophenone derivatives: balanced multipotent agents for Alzheimer's disease.

    abstract：:In an effort to develop multipotent agents against β-secretase (BACE-1) and acetylcholinesterase (AChE), able to counteract intracellular ROS formation as well, the structure of the fluorinated benzophenone 3 served as starting point for the synthesis of a small library of 3-fluoro-4-hydroxy- analogues. Among the seri...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.03.042

    authors： Belluti F,De Simone A,Tarozzi A,Bartolini M,Djemil A,Bisi A,Gobbi S,Montanari S,Cavalli A,Andrisano V,Bottegoni G,Rampa A

    更新日期：2014-05-06 00:00:00

  • Structure-based drug design: Synthesis and biological evaluation of quinazolin-4-amine derivatives as selective Aurora A kinase inhibitors.

    abstract：:Aurora kinases play critical roles in the regulation of the cell cycle and mitotic spindle assembly. Aurora A kinase, a member of the Aurora protein family, is frequently highly expressed in tumors, and selective Aurora A inhibition serves as a significant component of anticancer therapy. However, designing highly sel...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.08.053

    authors： Long L,Wang YH,Zhuo JX,Tu ZC,Wu R,Yan M,Liu Q,Lu G

    更新日期：2018-09-05 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, antiproliferative activity and inhibition of tubulin polymerization by anthracenone-based oxime derivatives.

    abstract：:A series of anthracenone-based oxime ethers and -esters were synthesized in order to evaluate their antiproliferative activity. Several investigated compounds displayed strong antiproliferative activity against K562 leukemia cells and proved to be strong inhibitors of tubulin polymerization. In this context, anthracen...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2010.04.019

    authors： Surkau G,Böhm KJ,Müller K,Prinz H

    更新日期：2010-08-01 00:00:00

  • Chemistry, biosynthesis and biological activity of terpenoids and meroterpenoids in bacteria and fungi isolated from different marine habitats.

    abstract：:The marine environment with its vast biological diversity encompasses many organisms that produce bioactive natural products. Marine microorganisms are rich sources of compounds from many structural classes with a multitude of biological activities. The biosynthesis of microbial natural products depends on a variety o...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2020.112957

    authors： Gozari M,Alborz M,El-Seedi HR,Jassbi AR

    更新日期：2021-01-15 00:00:00

  • Design, synthesis, and antiviral activity of novel rutin derivatives containing 1, 4-pentadien-3-one moiety.

    abstract：:Rutin (compound 5) and some compounds (compounds 1-4 and 6) were isolated from Artemisia princeps Pamp (A. princeps Pamp.) and a series of novel rutin derivatives containing 1,4-pentadien-3-one moiety were designed and synthesized. The target compounds were characterized by proton nuclear magnetic resonance spectrosco...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.01.017

    authors： Han Y,Ding Y,Xie D,Hu D,Li P,Li X,Xue W,Jin L,Song B

    更新日期：2015-03-06 00:00:00

  • Identification of an oxime-containing C-glucosylarene as a potential inhibitor of sodium-dependent glucose co-transporter 2.

    abstract：:Treatment of hyperglycemia with drugs that block renal glucose reabsorption via inhibition of sodium-dependent glucose cotransporter 2 (SGLT2) is a novel approach to diabetes management. In this study, twenty-seven aryl C-glycosides bearing a C=N/C-N linkage at the glucosyl C6 position were designed, synthesized and e...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2017.11.019

    authors： Yuan MC,Yeh TK,Chen CT,Song JS,Huang YC,Hsieh TC,Huang CY,Huang YL,Wang MH,Wu SH,Yao CH,Chao YS,Lee JC

    更新日期：2018-01-01 00:00:00

  • Structural features and functional activities of benzimidazoles as NOD2 antagonists.

    abstract：:NOD1 and NOD2 are pattern recognition receptors that have important roles in innate immune responses. Although their overactivation has been linked to a number of diseases, NOD2 in particular remains a virtually unexploited target in this respect, with only one structural class of antagonist reported. To gain insight ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.112089

    authors： Guzelj S,Gobec M,Urbančič D,Mlinarič-Raščan I,Corsini E,Jakopin Ž

    更新日期：2020-03-15 00:00:00

  • Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-{[2-(2-methoxyphenoxy)ethyl]amino}propan-2-ol and its enantiomers. Part 1.

    abstract：:The synthesis of (2RS)-1-(1H-indol-4-yloxy)-3-{[2-(2-methoxyphenoxy)ethyl]amino}propan-2-ol ((RS)-9) and its enantiomers has been described and tested for electrocardiographic, antiarrhythmic, hypotensive and spasmolytic activities as well as for alpha(1)-, alpha(2)- and beta(1)-adrenoceptors' binding affinities. All ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2008.05.019

    authors： Groszek G,Bednarski M,Dybała M,Filipek B

    更新日期：2009-02-01 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

  • Comparative study on antioxidant capacity of flavonoids and their inhibitory effects on oleic acid-induced hepatic steatosis in vitro.

    abstract：:Nonalcoholic fatty liver disease (NAFLD) is the most common liver disease and its incidence is rising worldwide. We compared the antioxidant capacity of seventeen flavonoids with their inhibitory effects on oleic acid-induced triglyceride (TG) over-accumulation in HepG2 cells. The results showed significant correlatio...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2011.07.031

    authors： Zhang D,Xie L,Jia G,Cai S,Ji B,Liu Y,Wu W,Zhou F,Wang A,Chu L,Wei Y,Liu J,Gao F

    更新日期：2011-09-01 00:00:00

  • Synthesis and antibacterial activities of novel pleuromutilin derivatives with a substituted pyrimidine moiety.

    abstract：:The alarming growth of multidrug-resistant bacteria such as methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococci (VRE) has become a major global health hazard. Therefore, urgent demand for new antibiotics with a unique mechanism of action is very necessary. The present study reports ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.11.054

    authors： Yi Y,Xu X,Liu Y,Xu S,Huang X,Liang J,Shang R

    更新日期：2017-01-27 00:00:00

  • Clubbed triazoles: a novel approach to antitubercular drugs.

    abstract：:In last few decades, though significant progress has been made in the treatment and control strategies of tubercular infections by introducing new diagnostic and monitoring tools and combination therapy, it still continues to be a severe problem. Thus with the aim of developing novel molecules with improved potency fo...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2006.12.001

    authors： Shiradkar M,Suresh Kumar GV,Dasari V,Tatikonda S,Akula KC,Shah R

    更新日期：2007-06-01 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

  • 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 and anticancer activity of new dihydropyrimidinone derivatives.

    abstract：:A series of dihydropyrimidinone derivatives bearing various N-heterocyclic moieties was designed and synthesized. Twelve new compounds were screened for their cytotoxic activity using 60 cancer cell lines according to NCI (USA) protocol. Compound 19 showed a significant activity against NCI-H460, SK-MEL-5, and HL-60 (...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.07.004

    authors： Mostafa AS,Selim KB

    更新日期：2018-08-05 00:00:00

  • Design, synthesis and biological evaluation of 3,4-diaryl-1,2,5-oxadiazole-2/5-oxides as highly potent inhibitors of tubulin polymerization.

    abstract：:Structure-activity relationships for rigid analogues of combretastatin A-4 (CA-4) were investigated, leading to the discovery of a series of 3,4-diaryl-1,2,5-oxadiazole-N-oxides. Among them, 7n' and 7n'' showed remarkable antiproliferative activities against three cancer cell lines in nanomolar concentrations. Interes...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2019.05.036

    authors： Hong Y,Zhao Y,Yang L,Gao M,Li L,Man S,Wang Z,Guan Q,Bao K,Zuo D,Wu Y,Zhang W

    更新日期：2019-09-15 00:00:00

  • Design of antineoplastic agents based on the '2-phenylnaphthalene-type' structural pattern--synthesis and biological activity studies of 11H-indolo[3.2-c]quinoline derivatives.

    abstract：:Designed as a new group of planar molecule containing the proposed 2-phenylnaphthalene-type structure, a number of 11H-indolo[3.2-c]quinoline derivatives were synthesized and evaluated biologically. Several compounds were found to possess cytotoxic activity against the growth of human promyelocytic leukemia cells (HL-...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/s0223-5234(02)01420-4

    authors： He L,Chang HX,Chou TC,Savaraj N,Cheng CC

    更新日期：2003-01-01 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

  • Design, synthesis and docking studies of some novel (R)-2-(4'-chlorophenyl)-3-(4'-nitrophenyl)-1,2,3,5-tetrahydrobenzo[4,5] imidazo [1,2-c]pyrimidin-4-ol derivatives as antitubercular agents.

    abstract：:Filamenting temperature-sensitive mutant (FtsZ) is a novel target for the treatment of tuberculosis. A series of (R)-2-(4'-chlorophenyl)-3-(4'-nitrophenyl)-1,2,3,5-tetrahydrobenzo[4,5] imidazo[1,2-c]pyrimidin-4-ol derivatives were designed and docked on the FtsZ protein crystal structure (PDB Id: 1RLU, resolution 2.08...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.06.019

    authors： Barot KP,Jain SV,Gupta N,Kremer L,Singh S,Takale VB,Joshi K,Ghate MD

    更新日期：2014-08-18 00:00:00

  • Synthesis of polyfluoroalkyl sp2-iminosugar glycolipids and evaluation of their immunomodulatory properties towards anti-tumor, anti-leishmanial and anti-inflammatory therapies.

    abstract：:Immunomodulatory glycolipids, among which α-galactosylceramide (KRN7000) is an iconic example, have shown strong therapeutic potential in a variety of conditions ranging from cancer and infection to autoimmune or neurodegenerative diseases. A main difficulty for those channels is that they often provoke a cytokine sto...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2019.111604

    authors： Sánchez-Fernández EM,García-Moreno MI,Arroba AI,Aguilar-Diosdado M,Padrón JM,García-Hernández R,Gamarro F,Fustero S,Sánchez-Aparicio JE,Masgrau L,García Fernández JM,Ortiz Mellet C

    更新日期：2019-11-15 00:00:00

  • Synthesis and biological evaluation of new [1,2,4]triazino[5,6-b]indol-3-ylthio-1,3,5-triazines and [1,2,4]triazino[5,6-b]indol-3-ylthio-pyrimidines against Leishmania donovani.

    abstract：:A series of [1,2,4]triazino[5,6-b]indol-3-ylthio-1,3,5-triazines and [1,2,4]triazino[5,6-b]indol-3-ylthio-pyrimidines were synthesized and screened for their in vitro antileishmanial activity against Leishmania donovani. Among all, 8 compounds have shown more than 90% inhibition against promastigotes and IC50 in the r...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2010.02.015

    authors： Gupta L,Sunduru N,Verma A,Srivastava S,Gupta S,Goyal N,Chauhan PM

    更新日期：2010-06-01 00:00:00

  • The design of 8-hydroxyquinoline tetracyclic lactams as HIV-1 integrase strand transfer inhibitors.

    abstract：:A novel series of HIV-1 integrase strand transfer inhibitors were designed using the venerable two-metal binding pharmacophore model and incorporating structural elements from two different literature scaffolds. This manuscript describes a number of 8-hydroxyquinoline tetracyclic lactams with exceptional antiviral act...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.03.038

    authors： Velthuisen EJ,Johns BA,Temelkoff DP,Brown KW,Danehower SC

    更新日期：2016-07-19 00:00:00

  • Inhibition of 17β-HSD1: SAR of bicyclic substituted hydroxyphenylmethanones and discovery of new potent inhibitors with thioether linker.

    abstract：:Estradiol is the most potent estrogen in humans. It is known to be involved in the development and proliferation of estrogen dependent diseases such as breast cancer and endometriosis. The last step of its biosynthesis is catalyzed by 17β-hydroxysteroid dehydrogenase type 1 (17β- HSD1) which consequently is a promisin...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.05.074

    authors： Abdelsamie AS,Bey E,Hanke N,Empting M,Hartmann RW,Frotscher M

    更新日期：2014-07-23 00:00:00

  • Rational design of reversible inhibitors for trehalose 6-phosphate phosphatases.

    abstract：:In some organisms, environmental stress triggers trehalose biosynthesis that is catalyzed collectively by trehalose 6-phosphate synthase, and trehalose 6-phosphate phosphatase (T6PP). T6PP catalyzes the hydrolysis of trehalose 6-phosphate (T6P) to trehalose and inorganic phosphate and is a promising target for the dev...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2017.02.001

    authors： Liu C,Dunaway-Mariano D,Mariano PS

    更新日期：2017-03-10 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

  • 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