当前位置： SCI文献检索 > BIOORGANIC & MEDICINAL CHEMISTRY LETTERS期刊下所有文献 > Novel N1-(benzyl)cinnamamidine derived NR2B subtype-selective NMDA receptor antagonists.

Novel N1-(benzyl)cinnamamidine derived NR2B subtype-selective NMDA receptor antagonists.

Abstract：

:Novel (E)-N(1)-(benzyl)cinnamamidines were prepared and evaluated as NR2B subtype NMDA receptor ligands. Excellent affinity was achieved by appropriate substitution of either phenyl ring. The 2-methoxybenzyl compound 1h had approximately 1,000-fold lower IC(50) in NR2B than NR2A-containing cells. Replacement of the styryl unit by 2-naphthyl was well tolerated.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Curtis NR,Diggle HJ,Kulagowski JJ,London C,Grimwood S,Hutson PH,Murray F,Richards P,Macaulay A,Wafford KA

doi

10.1016/s0960-894x(02)01060-0

subject

Has Abstract

pub_date

2003-02-24 00:00:00

pages

693-6

issue

4

eissn

0960-894X

issn

1464-3405

pii

S0960894X02010600

journal_volume

13

pub_type

杂志文章

相关文献

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS文献大全
  • Synthesis and biological evaluation of a new series of N-acyldiamines as potential antibacterial and antifungal agents.

    abstract：:In continuation of our efforts to find new antimicrobial compounds, series of fatty N-acyldiamines were prepared from fatty methyl esters and 1,2-ethylenediamine, 1,3-propanediamine or 1,4-butanediamine. The synthesized compounds were screened for their antibacterial activity against Gram-positive bacteria (Staphyloco...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2014.08.047

    authors： Ferreira BDS,de Almeida AM,Nascimento TC,de Castro PP,Silva VL,Diniz CG,Le Hyaric M

    更新日期：2014-10-01 00:00:00

  • Biotinylated-spiperone ligands for quantum dot labeling of the dopamine D2 receptor in live cell cultures.

    abstract：:We have synthesized 3 analogs of the dopamine D2 receptor (D2 DR) antagonist spiperone that can be conjugated to streptavidin-coated quantum dots via a pegylated biotin derivative. Using fluorescent imaging we demonstrate that substitution on the spiro position is tolerated, whilst the length and rigidity of a spacer ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.02.024

    authors： Tomlinson ID,Kovtun O,Crescentini TM,Rosenthal SJ

    更新日期：2019-04-15 00:00:00

  • Novel 3,5-diaryl pyrazolines as human acyl-CoA:cholesterol acyltransferase inhibitors.

    abstract：:A series of pyrazoline derivatives were prepared for evaluating their acyl-CoA:cholesterol acyltransferase activities. 3-(3,5-Di-tert-butyl-4-hydroxyphenyl)-5-(multi-substituted 4-hydroxyphenyl)-2-pyrazolines 4a-i were shown in vitro inhibitory activity on hACAT-1 and -2. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2004.03.079

    authors： Jeong TS,Kim KS,An S,Cho KH,Lee S,Lee WS

    更新日期：2004-06-07 00:00:00

  • Respiratory syncytial virus fusion inhibitors. Part 4: optimization for oral bioavailability.

    abstract：:A series of benzimidazole-based inhibitors of respiratory syncytial virus (RSV) fusion were optimized for antiviral potency, membrane permeability and metabolic stability in human liver microsomes. 1-Cyclopropyl-1,3-dihydro-3-[[1-(4-hydroxybutyl)-1H-benzimidazol-2-yl]methyl]-2H-imidazo[4,5-c]pyridin-2-one (6m, BMS-433...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2006.11.063

    authors： Yu KL,Sin N,Civiello RL,Wang XA,Combrink KD,Gulgeze HB,Venables BL,Wright JJ,Dalterio RA,Zadjura L,Marino A,Dando S,D'Arienzo C,Kadow KF,Cianci CW,Li Z,Clarke J,Genovesi EV,Medina I,Lamb L,Colonno RJ,Yang Z,Kr

    更新日期：2007-02-15 00:00:00

  • Inhibition of human cytomegalovirus protease N(o) with monocyclic beta-lactams.

    abstract：:Monocyclic beta-lactams have been identified as potent and selective inhibitors of the human cytomegalovirus protease (HCMV) N(o). Two series of these inhibitors are described, a peptidyl series of compounds and non-peptidic molecules featuring lower molecular weights. The SAR work that lead to the discovery of these ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(98)00240-6

    authors： Déziel R,Malenfant E

    更新日期：1998-06-02 00:00:00

  • Antifungal trichothecene sesquiterpenes obtained from the culture broth of marine-derived Trichoderma cf. brevicompactum and their structure-activity relationship.

    abstract：:Two new trichothecene sesquiterpenes, trichobreols D (1) and E (2), were isolated from the culture broth of marine-derived Trichoderma cf. brevicompactum together with trichobreol A (3). The structures of 1 and 2 were assigned on the basis of their spectroscopic data. Compound 1 inhibited the growth of two yeast-like ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2020.127375

    authors： Yamazaki H,Yagi A,Takahashi O,Yamaguchi Y,Saito A,Namikoshi M,Uchida R

    更新日期：2020-09-01 00:00:00

  • Rapid cleavage of cyclic tertiary amides of Kemp's triacid: effects of ring structure.

    abstract：:The piperidyl and prolyl amides of Kemp's triacid (7 and 8, respectively) have been prepared and their rates of intramolecular acylolysis measured as a function of pD. The piperidyl derivative 7 reacts approximately four-times faster (e.g., t(1/2)=3 min at 20 degrees C and pD7.7) than the previously reported pyrrolidy...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2004.06.024

    authors： Dougan ML,Chin JL,Solt K,Hansen DE

    更新日期：2004-08-16 00:00:00

  • Nitrone derivatives of trolox as neuroprotective agents.

    abstract：:Synthesis of nitrone derivatives of trolox is described. Their biological evaluation was performed in vitro for scavenging different free radicals, inhibiting Fe(2+)-induced lipid peroxidation, and in vivo in a permanent middle cerebral artery occlusion model in mice. New compounds exert pharmacological activities com...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2005.04.043

    authors： Balogh GT,Vukics K,Könczöl A,Kis-Varga A,Gere A,Fischer J

    更新日期：2005-06-15 00:00:00

  • InCl3 mediated one-pot multicomponent synthesis, anti-microbial, antioxidant and anticancer evaluation of 3-pyranyl indole derivatives.

    abstract：:A simple and convenient method for the one-pot three-component synthesis of 3-pyranyl indoles has been accomplished by tandem Knoevenagel-Michael reaction of 3-cyanoacetyl indole, various aromatic aldehydes and malononitrile catalyzed by InCl(3) in ethanol under reflux conditions. The newly synthesized 3-pyranyl indol...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2010.07.039

    authors： Lakshmi NV,Thirumurugan P,Noorulla KM,Perumal PT

    更新日期：2010-09-01 00:00:00

  • Antifungal Sordarins. Part 4: synthesis and structure--activity relationships of 3',4'-fused alkyl-tetrahydrofuran derivatives.

    abstract：:A series of Sordarin derivatives bearing alkyl substituted tetrahydrofuran rings fused to C3'-C4' bond of the sugar moiety have been prepared and their antifungal properties evaluated. Most of them show remarkable antifungal activity against Candida spp and Cryptococcus neoformans. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(02)00293-7

    authors： Bueno JM,Chicharro J,Fiandor JM,Gómez de las Heras F,Huss S

    更新日期：2002-07-08 00:00:00

  • Discovery of substituted (4-phenyl-1H-imidazol-2-yl)methanamine as potent somatostatin receptor 3 agonists.

    abstract：:We report SAR studies on a novel non-peptidic somatostatin receptor 3 (SSTR3) agonist lead series derived from (4-phenyl-1H-imidazol-2-yl)methanamine. This effort led to the discovery of a highly potent low molecular weight SSTR3 agonist 5c (EC50=5.2 nM, MW=359). The results from molecular overlays of 5c onto the L-12...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2015.06.087

    authors： Lai Z,He S,Sherer EC,Wu Z,Yu Y,Ball R,Hong Q,Yang DX,Guo L,Li D,Tuang Q,Chicchi GG,Trusca D,Tsao KL,Zhou YP,Howard AD,Nargund RP,Hagmann WK

    更新日期：2015-09-01 00:00:00

  • Synthesis of novel 2-pyrazoline analogues with potent anti-inflammatory effect mediated by inhibition of phospholipase A2: Crystallographic, in silico docking and QSAR analysis.

    abstract：:Oxidative-stress induces inflammatory diseases. Further, infections caused by drug-resistant microbial strains are on the rise. This necessitates the discovery of novel small-molecules for intervention therapy. A series of 3-(2,3-dichlorophenyl)-1-(aryl)prop-2-en-1-ones are synthesized as intermediates via Claisen-Sch...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2017.06.063

    authors： Lokeshwari DM,Achutha DK,Srinivasan B,Shivalingegowda N,Krishnappagowda LN,Kariyappa AK

    更新日期：2017-08-15 00:00:00

  • The first synthesis of [(11)C]SB-216763, a new potential PET agent for imaging of glycogen synthase kinase-3 (GSK-3).

    abstract：:SB-216763 is a novel, potent and selective glycogen synthase kinase-3 (GSK-3) inhibitor with an IC(50) value of 34 nM. [(11)C]SB-216763 (3-(2,4-dichlorophenyl)-4-(1-[(11)C]methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione), a new potential PET agent for imaging of GSK-3, was first designed and synthesized in 20-30% decay cor...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2010.11.026

    authors： Wang M,Gao M,Miller KD,Sledge GW,Hutchins GD,Zheng QH

    更新日期：2011-01-01 00:00:00

  • Design, synthesis and evaluation of 4-substituted anthra[2,1-c][1,2,5]thiadiazole-6,11-dione derivatives as novel non-camptothecin topoisomerase I inhibitors.

    abstract：:Previously, 4-tosylanthra[1,2-c][1,2,5]thiadiazole-6,11-dione (1) was identified as a novel non-camptothecin topoisomerase I (Top1) inhibitor by structure-based virtual screening. Herein, a series of 4-substituted derivatives were designed and synthesized. Most of them showed potent Top1 inhibitory activity. Their in ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2017.03.039

    authors： Dong G,Fang Y,Liu Y,Liu N,Wu S,Zhang W,Sheng C

    更新日期：2017-05-01 00:00:00

  • Synthesis and SAR of potent and orally bioavailable tert-butylpyrrolidine archetype derived melanocortin subtype-4 receptor modulators.

    abstract：:Discovery of a series of tert-butyl pyrrolidine derived, potent and orally bioavailable melanocortin receptor subtype-4 (MC4R) selective modulators is disclosed. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2008.04.049

    authors： Guo L,Ye Z,Ujjainwalla F,Sings HL,Sebhat IK,Huber J,Weinberg DH,Tang R,MacNeil T,Tamvakopoulos C,Peng Q,MacIntyre E,van der Ploeg LH,Goulet MT,Wyvratt MJ,Nargund RP

    更新日期：2008-06-01 00:00:00

  • Synthesis and preliminary evaluation of mono-[123I]iodohypericin monocarboxylic acid as a necrosis avid imaging agent.

    abstract：:Hypericin monocarboxylic acid was synthesized in an overall yield of 25% in four steps and radiolabelled with iodine-123 in good yield (>75%). The resulting mono-[(123)I]iodohypericin monocarboxylic acid was evaluated in normal mice and in rats with ethanol induced liver necrosis. In this model, tracer concentration i...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2007.04.083

    authors： Fonge H,Jin L,Wang H,Ni Y,Bormans G,Verbruggen A

    更新日期：2007-07-15 00:00:00

  • Design, synthesis and RON receptor tyrosine kinase inhibitory activity of new head groups analogs of LCRF-0004.

    abstract：:New heteroarylcarboxamide head groups substituted with two aromatic rings analogs of thieno[3,2-b]pyridine-based kinase inhibitor LCRF-0004 were designed and synthesized. Potent inhibitors of RON tyrosine kinase with various level of selectivity for c-Met RTK were obtained. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2015.07.080

    authors： Raeppel F,Raeppel SL,Therrien E

    更新日期：2015-09-15 00:00:00

  • Synthesis, cytotoxicity and topoisomerase II inhibitory activity of lomefloxacin derivatives.

    abstract：:A novel series of amide derivatives of lomefloxacin were synthesized and evaluated for their topoisomerase I and II inhibitory activity as well as cytotoxicity against a panel of five human cancer cell lines. Of the compounds prepared compounds 9d and 9g exhibited strong inhibition against topoisomerase II at 100μM. I...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2013.03.037

    authors： Zhou Y,Xu X,Sun Y,Wang H,Sun H,You Q

    更新日期：2013-05-15 00:00:00

  • Synthesis, anti-inflammatory and antimicrobial evaluation of novel 1-acetyl-3,5-diaryl-4,5-dihydro (1H) pyrazole derivatives bearing urea, thiourea and sulfonamide moieties.

    abstract：:A series of novel 1-acetyl-3-(3,4-dimethoxypheny)-5-(4-(3-(arylureido/arylthioureido/arylsulfonamido) phenyl)-4,5-dihydropyrazole derivatives of biological interest have been prepared by sequential cyclization of 1-(4-nitrophenyl)-3-(3,4-dimethoxyphenyl)-pro-2-ene-1 with hydrazine hydrate, reduction followed by reacti...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2012.08.118

    authors： Keche AP,Hatnapure GD,Tale RH,Rodge AH,Kamble VM

    更新日期：2012-11-01 00:00:00

  • LAT1 activity of carboxylic acid bioisosteres: Evaluation of hydroxamic acids as substrates.

    abstract：:Large neutral amino acid transporter 1 (LAT1) is a solute carrier protein located primarily in the blood-brain barrier (BBB) that offers the potential to deliver drugs to the brain. It is also up-regulated in cancer cells, as part of a tumor's increased metabolic demands. Previously, amino acid prodrugs have been show...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2016.09.001

    authors： Zur AA,Chien HC,Augustyn E,Flint A,Heeren N,Finke K,Hernandez C,Hansen L,Miller S,Lin L,Giacomini KM,Colas C,Schlessinger A,Thomas AA

    更新日期：2016-10-15 00:00:00

  • Structure--activity relationships of the peptide deformylase inhibitor BB-3497: modification of the P2' and P3' side chains.

    abstract：:Structural modifications to the peptide deformylase inhibitor BB-3497 are described. In this paper, we describe the initial SAR around this lead for modifications to both the P2' and P3' side chains. Enzyme inhibition and antibacterial activity data revealed that a variety of substituents are tolerated at the P2' and ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(03)00533-x

    authors： Davies SJ,Ayscough AP,Beckett RP,Clements JM,Doel S,Pratt LM,Spavold ZM,Thomas SW,Whittaker M

    更新日期：2003-08-18 00:00:00

  • Synthesis and evaluation of prodrugs of corticotropin-releasing factor-1 (CRF1) receptor antagonist BMS-665053 leading to improved oral bioavailability.

    abstract：:A series of phosphate and ester-based prodrugs of anilinopyrazinone 1 (BMS-665053) containing either a methylene or an (acyloxy)alkoxy linker was prepared and evaluated in rat pharmacokinetic studies with the goal of improving the oral bioavailability of the parent (1). The prodrugs, in general, had improved aqueous s...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2017.02.015

    authors： Hartz RA,Vrudhula VM,Ahuja VT,Grace JE,Lodge NJ,Bronson JJ,Macor JE

    更新日期：2017-03-15 00:00:00

  • Structure-activity relationship of a series of cyclohexylpiperidines bearing an amide side chain as antagonists of the human melanocortin-4 receptor.

    abstract：:A series of cyclohexylpiperazines was synthesized as potent and selective antagonists of the human MC4 receptor. Compound 14t displayed binding affinity (Ki) of 4.2 and 1100 nM at MC4R and MC3R, respectively. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2005.05.017

    authors： Tran JA,Pontillo J,Arellano M,Fleck BA,Tucci FC,Marinkovic D,Chen CW,Saunders J,Foster AC,Chen C

    更新日期：2005-07-15 00:00:00

  • On-resin macrocyclization of peptides via intramolecular SnAr reactions.

    abstract：:On-resin macrocyclization via an SNAr reaction is employed in the synthesis of tocinoic acid analogs. Specifically, an N-terminal nitrofluorobenzene is attacked by a nucleophilic C-terminal sidechain. The remaining nitro group can be reduced and acylated. NMR is used to compare the conformation of the new macrocyclic ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(99)00356-x

    authors： Fotsch C,Kumaravel G,Sharma SK,Wu AD,Gounarides JS,Nirmala NR,Petter RC

    更新日期：1999-08-02 00:00:00

  • Diphenyl ethers as androgen receptor antagonists for the topical suppression of sebum production.

    abstract：:A series of diphenyl ethers was prepared and evaluated for androgen receptor antagonist activity in human androgen receptor binding and cellular functional assays. Analogs with potent in vitro activities were evaluated for topical in vivo efficacy in the Golden Syrian Hamster ear model. Several compounds showed reduct...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2009.02.104

    authors： Mitchell LH,Hu LY,Nguyen M,Fakhoury S,Smith Y,Iula D,Kostlan C,Carroll M,Dettling D,Du D,Pocalyko D,Wade K,Lefker B

    更新日期：2009-04-15 00:00:00

  • Identification of arylsulfonamides as ExoU inhibitors.

    abstract：:ExoU is a potent virulence factor of Pseudomonas aeruginosa and is considered a potential therapeutic target. In order to discover novel ExoU inhibitors, we screened an in-house chemical library utilizing a yeast-based screening system. Some sulfonamides displayed significant activity without nonspecific cytotoxicity....

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2014.06.064

    authors： Kim D,Baek J,Song J,Byeon H,Min H,Min KH

    更新日期：2014-08-15 00:00:00

  • The binding of cocaine to cyclodextrins.

    abstract：:Cocaine binds into beta-cyclodextrin, but not detectably into alpha- or gamma-cyclodextrin, in water solution. NMR studies indicate the geometry of the complex, which is confirmed by molecular mechanics calculations and binding studies on cocaine analogues and cyclodextrin dimers. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(00)00371-1

    authors： Nesna N,Lou J,Breslow R

    更新日期：2000-09-04 00:00:00

  • Exploring amino acids derivatives as potent, selective, and direct agonists of sphingosine-1-phosphate receptor subtype-1.

    abstract：:In the quest to discover a potent and selective class of direct agonists to the sphingosine-1-phosphate receptor, we explored the carboxylate functional group as a replacement to previously reported lead phosphates. This has led to the discovery of potent and selective direct agonists with moderate to substantial in v...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2012.11.053

    authors： Evindar G,Deng H,Bernier SG,Doyle E,Lorusso J,Morgan BA,Westlin WF

    更新日期：2013-01-15 00:00:00

  • Polyether ionophores-promising bioactive molecules for cancer therapy.

    abstract：:The natural polyether ionophore antibiotics might be important chemotherapeutic agents for the treatment of cancer. In this article, the pharmacology and anticancer activity of the polyether ionophores undergoing pre-clinical evaluation are reviewed. Most of polyether ionophores have shown potent activity against the ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章,评审

    doi：10.1016/j.bmcl.2012.09.046

    authors： Huczyński A

    更新日期：2012-12-01 00:00:00

  • Discovery of 4-aminomethylphenylacetic acids as γ-secretase modulators via a scaffold design approach.

    abstract：:Starting from literature examples of nonsteroidal anti-inflammatory drugs (NSAIDs)-type carboxylic acid γ-secretase modulators (GSMs) and using a scaffold design approach, we identified 4-aminomethylphenylacetic acid 4 with a desirable γ-secretase modulation profile. Scaffold optimization led to the discovery of a nov...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2011.10.047

    authors： Xin Z,Peng H,Zhang A,Talreja T,Kumaravel G,Xu L,Rohde E,Jung MY,Shackett MN,Kocisko D,Chollate S,Dunah AW,Snodgrass-Belt PA,Arnold HM,Taveras AG,Rhodes KJ,Scannevin RH

    更新日期：2011-12-15 00:00:00