当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Design, synthesis and evaluation of diarylpiperazine derivatives as potent anti-tubercular agents.

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 evaluated their in-vitro anti-tubercular activity. Among the reported sixteen diarylpiperazines, eleven analogues exhibited significant anti-tubercular activity against Mycobacterium tuberculosis H37Rv strain with MIC values below 6.25 μg/mL and good selectivity index. Structure activity relationship studies concluded that, ortho-para directing group (except para chloro) substitution on ortho and para position of piperazine attached phenyl ring favored anti-tubercular activity.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Penta A,Franzblau S,Wan B,Murugesan S

doi

10.1016/j.ejmech.2015.10.024

subject

Has Abstract

pub_date

2015-11-13 00:00:00

pages

238-44

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(15)30306-8

journal_volume

105

pub_type

杂志文章

相关文献

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY文献大全
  • Indole based antimalarial compounds targeting the melatonin pathway: Their design, synthesis and biological evaluation.

    abstract：:Malaria, one of the most severe global diseases, infects nearly 300 million people causing death of about a million population annually. Herein we have reported design, synthesis and biological evaluation of potent antimalarial compounds that target melatonin hormone as a potential pathway for the inhibition of the pa...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2019.02.019

    authors： Luthra T,Nayak AK,Bose S,Chakrabarti S,Gupta A,Sen S

    更新日期：2019-04-15 00:00:00

  • Inhibitors of the kynurenine pathway.

    abstract：:Strokes (intracranial thomboses or haemorrhaging) cause death and disability, but effective treatments are lacking. The metabolism of tryptophan leads to the generation of quinolinic acid, an agonist potentially neurotoxic at glutamate receptors, and kynurenic acid, an antagonist at the same population of receptors. T...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/s0223-5234(00)00121-5

    authors： Stone TW

    更新日期：2000-02-01 00:00:00

  • Synthesis, local anaesthetic and antiarrhythmic activities of N-alkyl derivatives of proline anilides.

    abstract：:We describe here the design, synthesis and evaluation of in vivo local anaesthetic and antiarrhythmic activities of a series of N-alkylproline anilides. Most of the compounds demonstrated surface anaesthetic activity higher than that of lidocaine, ropivacaine and bupivacaine. We established that the local anaesthetic ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.02.003

    authors： Kalinin DV,Pantsurkin VI,Syropyatov BY,Kalinina SA,Rudakova IP,Vakhrin MI,Dolzhenko AV

    更新日期：2013-05-01 00:00:00

  • Synthesis, brain antihypoxic activity and cell neuroprotection of 1-substituted-3,7-dimethylxanthines.

    abstract：:Five newly synthesised original compounds were investigated for acute toxicity, influence on hexobarbital sleeping time, effect on the locomotor activity, and brain antihypoxic activity. Two of the compounds were tested in a model of glutamate induced neurotoxicity in the brain cell culture using a cell viability test...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/s0223-5234(00)01172-7

    authors： Zlatkov A,Peikov P,Rodriguez-Alvarez J,Danchev N,Nikolova I,Mitkov J

    更新日期：2000-10-01 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

  • Design, synthesis and biological evaluation of monobactams as antibacterial agents against gram-negative bacteria.

    abstract：:A series of monobactam derivatives were prepared and evaluated for their antibacterial activities against susceptible and resistant Gram-negative strains, taking Aztreonam and BAL30072 as the leads. Six conjugates (12a-f) bearing PIH-like siderophore moieties were created to enhance the bactericidal activities against...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.01.024

    authors： Fu HG,Hu XX,Li CR,Li YH,Wang YX,Jiang JD,Bi CW,Tang S,You XF,Song DQ

    更新日期：2016-03-03 00:00:00

  • Synthesis, physicochemical properties and antimicrobial evaluation of new (E)-chalcones.

    abstract：:In a wide search program towards new and efficient antimicrobial agents, a series of 40 substituted chalcones have been synthesized and tested for their in vitro antibacterial and antifungal activities. The structures of these compounds have been investigated by nuclear magnetic resonance spectroscopy and mass spectro...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2007.05.006

    authors： Nowakowska Z,Kedzia B,Schroeder G

    更新日期：2008-04-01 00:00:00

  • Synthesis of new N3-substituted dihydropyrimidine derivatives as L-/T- type calcium channel blockers.

    abstract：:Cardiovascular diseases (CVDs) are the main cause of deaths worldwide. Up-to-date, hypertension is the most significant contributing factor to CVDs. Recent clinical studies recommend calcium channel blockers (CCBs) as effective treatment alone or in combination with other medications. Being the most clinically useful ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2017.03.080

    authors： Teleb M,Zhang FX,Farghaly AM,Aboul Wafa OM,Fronczek FR,Zamponi GW,Fahmy H

    更新日期：2017-07-07 00:00:00

  • Structure-activity analysis of CJ-15,801 analogues that interact with Plasmodium falciparum pantothenate kinase and inhibit parasite proliferation.

    abstract：:Survival of the human malaria parasite Plasmodium falciparum is dependent on pantothenate (vitamin B5), a precursor of the fundamental enzyme cofactor coenzyme A. CJ-15,801, an enamide analogue of pantothenate isolated from the fungus Seimatosporium sp. CL28611, was previously shown to inhibit P. falciparum proliferat...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2017.08.050

    authors： Spry C,Sewell AL,Hering Y,Villa MVJ,Weber J,Hobson SJ,Harnor SJ,Gul S,Marquez R,Saliba KJ

    更新日期：2018-01-01 00:00:00

  • Spirostanols obtained by cyclization of pseudosaponin derivatives and comparison of anti-platelet agglutination activities of spirostanol glycosides.

    abstract：:Naturally occurring saponins 3 and 4 have a normal type F ring and alpha-arranged CH(3)-21 group. Treatments of pseudosaponin peracetates 18 and 19 derived from 3 and 4, respectively, with alcoholic KOH, followed by acidification with acetic acid, gave spirostanols 20 and 22 having iso type F rings as major products. ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/s0223-5234(00)00151-3

    authors： Tobari A,Teshima M,Koyanagi J,Kawase M,Miyamae H,Yoza K,Takasaki A,Nagamura Y,Saito S

    更新日期：2000-05-01 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

  • 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

  • Novel 4-anilinoquinazoline derivatives featuring an 1-adamantyl moiety as potent EGFR inhibitors with enhanced activity against NSCLC cell lines.

    abstract：:With the aim of overcoming gefitinib resistance, a series of novel quinazoline derivatives bearing an adamantyl group on the aniline ring were synthesized as potent epidermal growth factor receptor (EGFR) inhibitors. Most of these analogues are comparable to gefitinib in their ability to inhibit non-small cell lung ca...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.01.045

    authors： Yu H,Li Y,Ge Y,Song Z,Wang C,Huang S,Jin Y,Han X,Zhen Y,Liu K,Zhou Y,Ma X

    更新日期：2016-03-03 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

  • Dimeric aryl-substituted imidazoles may inhibit ALT cancer by targeting the multimeric G-quadruplex in telomere.

    abstract：:In 10-15% of cancers, telomere maintenance is provided by a telomerase-independent mechanism known as alternative lengthening of telomere (ALT), making telomerase inhibitors ineffective on these cancers. Ligands that stabilize telomeric G-quadruplex (G4) are considered to be able to inhibit either the ALT process or d...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2019.111891

    authors： Hu MH,Lin XT,Liu B,Tan JH

    更新日期：2020-01-15 00:00:00

  • Synthesis and neuromuscular blocking activity of 16beta-piperidinosteroidal derivatives.

    abstract：:The synthesis and pharmacological profiles of some new steroidal mono- and bisquaternary ammonium derivatives have been described. The compounds featured have been conceptually derived structurally from two lead structures: pancuronium bromide 1 and chandonium iodide 2. In vitro and in vivo neuromuscular blocking stud...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/s0223-5234(00)01205-8

    authors： Jindal DP,Piplani P,Fajrak H,Prior C,Marshall IG

    更新日期：2001-02-01 00:00:00

  • Reversal of P-gp and BCRP-mediated MDR by tariquidar derivatives.

    abstract：:With an aim to generate non-toxic, specific and highly potent multidrug resistance (MDR) modulators, a novel series of anthranilic acid amide-substituted tariquidar derivatives were synthesized. The new compounds were evaluated for their cytotoxicity toward normal human colon fibroblasts (CCD18-Co), human gastric epit...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.06.049

    authors： Li XQ,Wang L,Lei Y,Hu T,Zhang FL,Cho CH,To KK

    更新日期：2015-08-28 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

  • 1,5-Diphenylpenta-2,4-dien-1-ones as potent and selective monoamine oxidase-B inhibitors.

    abstract：:A series of (2E,4E)-1-(2-hydroxyphenyl)-5-phenylpenta-2,4-dien-1-ones (3a-r) and (2Z,4E)-3-hydroxy-1-(2-hydroxyphenyl)-5-phenylpenta-2,4-dien-1-ones (6a-l) were synthesized and evaluated in vitro as inhibitors of the two human Monoamine oxidase (hMAO) isoforms, MAO-A and MAO-B. Most of the compounds showed a selective...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2012.11.006

    authors： Desideri N,Fioravanti R,Proietti Monaco L,Biava M,Yáñez M,Ortuso F,Alcaro S

    更新日期：2013-01-01 00:00:00

  • Benzyloxynitrostyrene analogues - A novel class of selective and highly potent inhibitors of monoamine oxidase B.

    abstract：:This study examines a series of novel 3-benzyloxy-β-nitrostyrene analogues as a novel class of inhibitors of the monoamine oxidase (MAO) enzymes. MAO inhibitors are considered useful for the treatment of depression and Parkinson's disease, and have recently attracted attention as potential therapeutic agents for a ran...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.11.016

    authors： Van der Walt MM,Terre'Blanche G,Petzer JP,Petzer A

    更新日期：2017-01-05 00:00:00

  • Antitumor activity and carrier properties of novel hemocyanins coupled to a mimotope of GD2 ganglioside.

    abstract：:Conjugation to carrier proteins is a way to improve the immunogenicity of peptides. Such is the case for peptides mimicking carbohydrate tumor-associated antigens in cancer vaccine development. The most used protein for this purpose is the keyhole limpet hemocyanin (KLH) from Megathura crenulata. Its limited bioavaila...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.02.082

    authors： Palacios M,Tampe R,Del Campo M,Zhong TY,López MN,Salazar-Onfray F,Becker MI

    更新日期：2018-04-25 00:00:00

  • Design and synthesis of potent and selective P2X₃ receptor antagonists derived from PPADS as potential pain modulators.

    abstract：:Pyridoxalphosphate-6-azophenyl-2',4'-disulfonate (7a, PPADS), a nonselective P2X receptor antagonist, was extensively modified to develop more stable, potent, and selective P2X₃ receptor antagonists as potential antinociceptive agents. Based on the results of our previous report, all strong anionic groups in PPADS inc...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.10.026

    authors： Cho JH,Jung KY,Jung Y,Kim MH,Ko H,Park CS,Kim YC

    更新日期：2013-01-01 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

  • Synthesis and evaluation of thymidine kinase 1-targeting carboranyl pyrimidine nucleoside analogs for boron neutron capture therapy of cancer.

    abstract：:A library of sixteen 2nd generation amino- and amido-substituted carboranyl pyrimidine nucleoside analogs, designed as substrates and inhibitors of thymidine kinase 1 (TK1) for potential use in boron neutron capture therapy (BNCT) of cancer, was synthesized and evaluated in enzyme kinetic-, enzyme inhibition-, metabol...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.05.042

    authors： Agarwal HK,Khalil A,Ishita K,Yang W,Nakkula RJ,Wu LC,Ali T,Tiwari R,Byun Y,Barth RF,Tjarks W

    更新日期：2015-07-15 00:00:00

  • Synthesis, characterization, oxidative degradation, antibacterial activity and acetylcholinesterase/butyrylcholinesterase inhibitory effects of some new phosphorus(V) hydrazides.

    abstract：:Some new phosphorus(V) hydrazides 1a-12a were synthesized and characterized by (1)H, (13)C, (31)P NMR, IR spectroscopy and elemental analysis. Moreover, the interaction of Cu(M)(2)·nH(2)O with 1a, 3a and 7a gave 4,4'-bis(morpholine)diazene (1b). In fact, in these reactions, copper(II) ions acted as oxidizing agent. Th...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2010.08.025

    authors： Gholivand K,Hosseini Z,Farshadian S,Naderi-Manesh H

    更新日期：2010-11-01 00:00:00

  • Synthesis of novel bioactive derivatives of 3-(4-chlorophenyl)-2-hydrazino-5,6,7,8-tetrahydrobenzo(b)thieno[2,3-d]pyrimidine-4(3H)-ones.

    abstract：:A series of triazolo[4,3-a]tetrahydrobenzo(b)thieno[3,2-e]pyrimidine-5(4H)-ones (12a-n) were synthesized and evaluated for CNS depressant, skeletal muscle relaxant and anticonvulsant activities by photoactometer, Rotarod and pentylenetetrazole induced the convulsions method respectively in Swiss albino mice. Diazepam ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2009.05.027

    authors： Gupta SV,Baheti K,Bora R,Dekhane D,Chhabría M,Shingare M,Pawar S,Shishoo CJ,Thore SN

    更新日期：2009-11-01 00:00:00

  • Synthesis of novel 2-(1-adamantanylcarboxamido)thiophene derivatives. Selective cannabinoid type 2 (CB2) receptor agonists as potential agents for the treatment of skin inflammatory disease.

    abstract：:A set of CB2R ligands, based on the thiophene scaffold, was synthesized and evaluated in in vitro assays. Compounds 8c-i, k, l, bearing the 3-carboxylate and 2-(adamantan-1-yl)carboxamido groups together with apolar alkyl/aryl substituents at 5-position or at 4- and 5-positions of the thiophene ring possess high CB2R ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.09.070

    authors： Mugnaini C,Rabbito A,Brizzi A,Palombi N,Petrosino S,Verde R,Di Marzo V,Ligresti A,Corelli F

    更新日期：2019-01-01 00:00:00

  • (5aR)-5a-C-Pentyl-4-epi-isofagomine: A powerful inhibitor of lysosomal β-galactosidase and a remarkable chaperone for mutations associated with GM1-gangliosidosis and Morquio disease type B.

    abstract：:This report is about the identification, synthesis and initial biological characterization of derivatives of 4-epi-isofagomine as pharmacological chaperones (PC) for human lysosomal β-galactosidase. The two epimers of 4-epi-isofagomine carrying a pentyl group at C-5a, namely (5aR)- and (5aS)-5a-C-pentyl-4-epi-isofagom...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.09.095

    authors： Front S,Biela-Banaś A,Burda P,Ballhausen D,Higaki K,Caciotti A,Morrone A,Charollais-Thoenig J,Gallienne E,Demotz S,Martin OR

    更新日期：2017-01-27 00:00:00

  • Oxo-heterocyclic fused naphthalimides as antitumor agents: synthesis and biological evaluation.

    abstract：:Three series of novel oxo-heterocyclic fused naphthalimide derivatives (8a-8f, 13a-13d, 17a-17d) were prepared. The newly-synthesized compounds, and their thio-heterocyclic fused analogs (1a-1c, 2a-2d, 3a-3c) exhibited potent antiproliferative activity correlated well with their structure. Further research demonstrate...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2012.12.039

    authors： Tan S,Yin H,Chen Z,Qian X,Xu Y

    更新日期：2013-04-01 00:00:00

  • Activation of anti-oxidant Nrf2 signaling by enone analogues of curcumin.

    abstract：:Inflammation and oxidative stress are common in many chronic diseases. Targeting signaling pathways that contribute to these conditions may have therapeutic potential. The transcription factor Nrf2 is a major regulator of phase II detoxification and anti-oxidant genes as well as anti-inflammatory and neuroprotective g...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2017.11.048

    authors： Deck LM,Hunsaker LA,Vander Jagt TA,Whalen LJ,Royer RE,Vander Jagt DL

    更新日期：2018-01-01 00:00:00