当前位置： SCI文献检索 > BIOORGANIC & MEDICINAL CHEMISTRY LETTERS期刊下所有文献 > Heterocyclic aminopyrrolidine derivatives as melatoninergic agents.

Heterocyclic aminopyrrolidine derivatives as melatoninergic agents.

Abstract：

:A series of chiral heterocyclic aminopyrrolidine derivatives was synthesized as novel melatoninergic ligands. Binding affinity assays were performed on cloned human MT(1) and MT(2) receptors, stably expressed in NIH3T3 cells. Compound 16 was identified as an orally bioavailable agonist at MT(1) and MT(2) melatonin receptors with low vasoconstrictive activity.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Sun LQ,Chen J,Mattson RJ,Epperson JR,Deskus JA,Li WS,Takaki K,Hodges DB,Iben L,Mahle CD,Ortiz A,Molstad D,Ryan E,Yeleswaram K,Xu C,Luo G

doi

10.1016/j.bmcl.2003.09.030

subject

Has Abstract

pub_date

2003-12-15 00:00:00

pages

4381-4

issue

24

eissn

0960-894X

issn

1464-3405

pii

S0960894X03010047

journal_volume

13

pub_type

杂志文章

相关文献

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS文献大全
  • Syntheses and evaluation of substituted aromatic hydroxamates and hydroxamic acids that target Mycobacterium tuberculosis.

    abstract：:Tuberculosis (TB) continues to remain one of the most threatening diseases in the world. With the emergence of multi-drug resistant (MDR) and extensively drug resistant (XDR) strains, the need to develop new therapies is dire. The syntheses of a focused library of hydroxamates and hydroxamic acids is described, as wel...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2015.04.099

    authors： Majewski MW,Cho S,Miller PA,Franzblau SG,Miller MJ

    更新日期：2015-11-01 00:00:00

  • A tetradecapeptide somatostatin dicarba-analog: Synthesis, structural impact and biological activity.

    abstract：:We described here the first tetradecapeptide somatostatin-analogue where the disulfide bridge has been replaced by a carbon-carbon double bond. This analogue was prepared using microwave assisted ring closing metathesis (RCM) using the 2nd generation Grubbs as catalyst. Under our optimized conditions the cyclization b...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2013.11.065

    authors： Martín-Gago P,Ramón R,Aragón E,Fernández-Carneado J,Martin-Malpartida P,Verdaguer X,López-Ruiz P,Colás B,Cortes MA,Ponsati B,Macias MJ,Riera A

    更新日期：2014-01-01 00:00:00

  • Expanding the chemical space of human serine racemase inhibitors.

    abstract：:Serine racemase, the enzyme responsible for d-serine synthesis in the central nervous system, has been identified as a potential therapeutic target to treat N-methyl-d-aspartate receptors-related pathologies. The search for specific inhibitors of the enzyme has revealed that serine racemase is a difficult target, with...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2015.07.081

    authors： Dellafiora L,Marchetti M,Spyrakis F,Orlandi V,Campanini B,Cruciani G,Cozzini P,Mozzarelli A

    更新日期：2015-10-01 00:00:00

  • Discovery of novel benzylidene-1,3-thiazolidine-2,4-diones as potent and selective inhibitors of the PIM-1, PIM-2, and PIM-3 protein kinases.

    abstract：:Novel substituted benzylidene-1,3-thiazolidine-2,4-diones (TZDs) have been identified as potent and highly selective inhibitors of the PIM kinases. The synthesis and SAR of these compounds are described, along with X-ray crystallographic, anti-proliferative, and selectivity data. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2012.05.098

    authors： Dakin LA,Block MH,Chen H,Code E,Dowling JE,Feng X,Ferguson AD,Green I,Hird AW,Howard T,Keeton EK,Lamb ML,Lyne PD,Pollard H,Read J,Wu AJ,Zhang T,Zheng X

    更新日期：2012-07-15 00:00:00

  • 6,7-dihydroxyisoquinoline-3-carboxylic acids are potent inhibitors on the binding of insulin-like growth factor (IGF) to IGF-binding proteins: optimization of the 1-position benzoyl side chain.

    abstract：:A series of 1-benzoyl isoquinolines, based on compound 1, was synthesized and evaluated for their ability to displace IGF-I from its complex with IGF-binding protein-3. Successful modifications of 1 included the replacement of the 3,4-dihydroxybenzoyl group with a substituted benzyl group. These alternations culminate...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(03)00321-4

    authors： Zhu YF,Wilcoxen K,Gross T,Connors P,Strack N,Gross R,Huang CQ,McCarthy JR,Xie Q,Ling N,Chen C

    更新日期：2003-06-02 00:00:00

  • Successful bridging from a peptide to a non peptide antagonist at the human tachykinin NK-2 receptor.

    abstract：:Non peptide products have been found to show nanomolar binding and functional affinities at the human tachykinin NK-2 receptor. The new antagonists do not possess stereogenic centers and their thermal behaviour in solution is featured by a peculiar set of conformational stereoisomers. A macroscopic viewpoint is prefer...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(02)00539-5

    authors： Altamura M,Canfarini F,Catalioto RM,Guidi A,Pasqui F,Renzetti AR,Triolo A,Maggi CA

    更新日期：2002-10-21 00:00:00

  • Palbinone and triterpenes from Moutan Cortex (Paeonia suffruticosa, Paeoniaceae) stimulate glucose uptake and glycogen synthesis via activation of AMPK in insulin-resistant human HepG2 Cells.

    abstract：:Moutan Cortex is a well-known herb in traditional Korean, Chinese, and Japanese anti-diabetic formulae. In the current study, we investigated the metabolic effects of isolated triterpenes (1-7) in HepG2 cells under high glucose conditions. These compounds remakably stimulated AMP-activated protein kinase (AMPK), GSK-3...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2009.08.048

    authors： Ha do T,Tuan DT,Thu NB,Nhiem NX,Ngoc TM,Yim N,Bae K

    更新日期：2009-10-01 00:00:00

  • Design, synthesis and antibacterial activity of 3-methylenepyrrolidine formyl hydroxyamino derivatives as novel peptide deformylase inhibitors.

    abstract：:The synthesis and antibacterial activity of 3-methylenepyrrolidine formyl hydroxyamino derivatives are reported. The antibacterial activities of these derivatives were evaluated to discover SAR at P(1') and P(3') positions, and most of these derivatives exhibit better in vitro antibacterial activity than existing drug...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2010.11.102

    authors： Shi W,Ma H,Duan Y,Aubart K,Fang Y,Zonis R,Yang L,Hu W

    更新日期：2011-02-01 00:00:00

  • 1H-imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors: separation of desired cellular activity from undesired tissue accumulation through optimization of basic nitrogen pka.

    abstract：:Based on the theoretical understanding of the in vivo lysosomotropism, by adjusting the pk(a) of basic nitrogen containing cathepsin S inhibitors, a set of compounds with pk(a) 6-8 were identified to have excellent cell based Lip10 activity, yet avoiding undesired sequestration in spleen. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2010.12.065

    authors： Arbuckle W,Baugh M,Belshaw S,Bennett DJ,Bruin J,Cai J,Cameron KS,Claxton C,Dempster M,Everett K,Fradera X,Hamilton W,Jones PS,Kinghorn E,Long C,Martin I,Robinson J,Westwood P

    更新日期：2011-02-01 00:00:00

  • Makomotindoline from Makomotake, Zizania latifolia infected with Ustilago esculenta.

    abstract：:Makomotindoline (1) was isolated from Makomotake, Zizania latifolia infected with Ustilago esculenta. The structure was determined by the interpretation of spectroscopic data and synthesis. Makomotindoline (1), its l-Glc isomer (2) and its aglycon (3) were synthesized and their effects on rat glioma cells showed adver...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2012.05.021

    authors： Suzuki T,Choi JH,Kawaguchi T,Yamashita K,Morita A,Hirai H,Nagai K,Hirose T,Omura S,Sunazuka T,Kawagishi H

    更新日期：2012-07-01 00:00:00

  • Synthesis and evaluation of new iRGD peptide analogs for tumor optical imaging.

    abstract：:Recently, a disulfide-based cyclic RGD peptide called iRGD, that is, c(CRGDKGPDC), has been reported to interact with both integrin and neuropilin-1 receptors for cellular and deep tissue penetration to improve the imaging sensitivity and therapeutic efficacy. In this study, two new near-infrared fluorescent iRGD conj...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2010.12.112

    authors： Ye Y,Zhu L,Ma Y,Niu G,Chen X

    更新日期：2011-02-15 00:00:00

  • Growth inhibition of human cancer cells in vitro by T-type calcium channel blockers.

    abstract：:This paper describes the preliminary biological results that novel T-type calcium channel blockers inhibit the growth of human cancer cells by blocking calcium influx into the cell, based on unknown mechanism on the cell cycle responsible for cellular proliferation. Among the selected compounds from compound library, ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2006.07.046

    authors： Lee JY,Park SJ,Park SJ,Lee MJ,Rhim H,Seo SH,Kim KS

    更新日期：2006-10-01 00:00:00

  • Tyrosine phosphorylation of β-catenin affects its subcellular localization and transcriptional activity of β-catenin in Hela and Bcap-37 cells.

    abstract：:In order to investigate the relationship between tyrosine phosphorylation of β-catenin and transcriptional activity of β-catenin in Hela and Bcap-37 cells, genistein (a tyrosine kinase inhibitor) was used to inhibit tyrosine phosphorylation in cells. Our results showed the total β-catenin protein levels were mainly eq...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2014.03.078

    authors： Qian HY,Zhang DG,Wang HW,Pei DS,Zheng JN

    更新日期：2014-06-01 00:00:00

  • Synthesis, absolute configuration and antimuscarinic activity of the enantiomers of [1-(2,2-diphenyl-[1,3]dioxolan-4-yl)-ethyl]-dimethyl-amine.

    abstract：:Methylation of the carbon atom C of compound 1, a potent and not selective muscarinic antagonist, was carried out. The resulting diastereomers were separated and the corresponding racemate further resolved to give four enantiomers, which were tested both as hydrogen oxalate and methiodide salts. The pharmacological re...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(00)00647-8

    authors： Gulini U,Angeli P,Marucci G,Buccioni M,Giardinà D,Antolini L,Franchini S,Sorbi C,Brasili L

    更新日期：2001-01-22 00:00:00

  • Thrombin inhibitors based on a propargylglycine template.

    abstract：:A series of novel arylsulfonylpropargylglycinamide derivatives was investigated as thrombin inhibitors in which the SAR was focused on substituents at the acetylenic terminus. Several compounds in this series were identified as potent thrombin inhibitors (Ki up to 5 nM) that are highly selective over trypsin and other...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(99)00125-0

    authors： Lee K,Hwang SY,Park CW

    更新日期：1999-04-05 00:00:00

  • Lead optimization of an acylhydrazone scaffold possessing antiviral activity against Lassa virus.

    abstract：:Previously we reported the optimization of antiviral scaffolds containing benzimidazole and related heterocycles possessing activity against a variety of arenaviruses. These series of compounds were discovered through an HTS campaign of a 400,000 small molecule library using lentivirus-based pseudotypes incorporated w...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2013.08.103

    authors： Burgeson JR,Gharaibeh DN,Moore AL,Larson RA,Amberg SM,Bolken TC,Hruby DE,Dai D

    更新日期：2013-11-01 00:00:00

  • P4 capped amides and lactams as HCV NS3 protease inhibitors with improved potency and DMPK profile.

    abstract：:SAR studies on the extension of P3 unit of Boceprevir (1, SCH 503034) with amides and lactams and their synthesis is described. Extensive SAR studies resulted in the identification of 36 bearing 4, 4-dimethyl lactam as the new P4 cap unit with improved potency (K(i)( *)=15nM, EC 90=70nM) and pharmacokinetic properties...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2009.11.094

    authors： Nair LG,Sannigrahi M,Bogen S,Pinto P,Chen KX,Prongay A,Tong X,Cheng KC,Girijavallabhan V,George Njoroge F

    更新日期：2010-01-15 00:00:00

  • A highly catalytically active γ-carbonic anhydrase from the pathogenic anaerobe Porphyromonas gingivalis and its inhibition profile with anions and small molecules.

    abstract：:Carbonic anhydrases (CAs, EC 4.2.1.1) belonging to the γ-class are present in archaea, bacteria and plants but, except the Methanosarcina thermophila enzymes CAM and CAMH, they were poorly characterized so far. Here we report a new such enzyme (PgiCA), the γ-CA from the oral cavity pathogenic bacterium Porphyromonas g...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2013.05.063

    authors： Del Prete S,Vullo D,De Luca V,Carginale V,Scozzafava A,Supuran CT,Capasso C

    更新日期：2013-07-15 00:00:00

  • Design and synthesis of new bis-pyridinium oxime reactivators for acetylcholinesterase inhibited by organophosphorous nerve agents.

    abstract：:New bis-pyridinium oxime reactivators connected with a CH(2)CH(2)OCH(2)CH(2) linker between two pyridinium rings were designed and synthesized. In the test of their potency to reactivate AChE inhibited by cyclosarin, the bis-pyridinium oxime 6b achieved reactivation potency higher than 10% at the lower concentration 1...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2005.03.060

    authors： Kim TH,Kuca K,Jun D,Jung YS

    更新日期：2005-06-02 00:00:00

  • Synthesis and biological evaluations of novel bendazac lysine analogues as potent anticataract agents.

    abstract：:Novel bendazac analogues and their salts have been designed and prepared. The resulting compounds (13c-d, 15c, 17c) showed very good aqueous solubility (>100 mg/mL). An in vitro assay showed that most of the resulting compounds had potent protective activity against the oxidative damage. Particularly, compound 13d was...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2010.02.061

    authors： Shen H,Gou S,Shen J,Zhu Y,Zhang Y,Chen X

    更新日期：2010-04-01 00:00:00

  • Targeting tyrosine kinase: Development of acridone - pyrrole - oxindole hybrids against human breast cancer.

    abstract：:Based on the molecular modelling studies, a rational modification of the lead molecule was made to develop highly potent compounds showing anti-cancer activity against human breast cancer cell lines MCF 7, MDA-MB-468 and T-47D. The most potent compounds have Log P and total polar surface area 4.4-5.4 and 59.8 Å, respe...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2018.11.021

    authors： Kaur M,Singh P

    更新日期：2019-01-01 00:00:00

  • Synthesis and biological evaluation of 3-phenethylazetidine derivatives as triple reuptake inhibitors.

    abstract：:We report the synthesis of 3-phenethylazetidine derivatives 2 and their biological activities against 5-HT, NE and DA transporters as well as microsomal stability, CYP inhibition, and hERG inhibition profiles. Compound 2at showed most potent triple reuptake inhibitor with good selectivity as a candidate for depression...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2014.06.026

    authors： Yun J,Han M,Song C,Cheon SH,Choi K,Hahn HG

    更新日期：2014-08-01 00:00:00

  • Synthesis and biological evaluation of L- and D-configuration 1,3-dioxolane 5-azacytosine and 6-azathymine nucleosides.

    abstract：:Novel L- and D-configuration dioxolane 5-azacytosine and 6-azathymine nucleosides have been synthesized and evaluated for biological activity. (-)-(2S,4S)-1-[2-(Hydroxymethyl)-1,3-dioxolan-4-yl]-5-azacytosine (6) showed significant activity against HBV, whereas the D-configuration analogue (14) has been found to exhib...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(00)00418-2

    authors： Luo MZ,Liu MC,Mozdziesz DE,Lin TS,Dutschman GE,Gullen EA,Cheng YC,Sartorelli AC

    更新日期：2000-09-18 00:00:00

  • Synthesis of conjugates between oxazolidinone antibiotics and a pyochelin analogue.

    abstract：:Pseudomonas aeruginosa is a Gram-negative pathogenic bacterium responsible for severe infections, and it is naturally resistant to many clinically approved antibiotic families. Oxazolidinone antibiotics are active against many Gram-positive bacteria, but are inactive against P. aeruginosa. Increasing the uptake of oxa...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2017.09.039

    authors： Paulen A,Hoegy F,Roche B,Schalk IJ,Mislin GLA

    更新日期：2017-11-01 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

  • Biological evaluation of tanshindiols as EZH2 histone methyltransferase inhibitors.

    abstract：:EZH2 is the core subunit of Polycomb repressive complex 2 catalyzing the methylation of histone H3 lysine-27 and closely involved in tumorigenesis. To discover small molecule inhibitors for EZH2 methyltransferase activity, we performed an inhibitor screen with catalytically active EZH2 protein complex and identified t...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2014.04.010

    authors： Woo J,Kim HY,Byun BJ,Chae CH,Lee JY,Ryu SY,Park WK,Cho H,Choi G

    更新日期：2014-06-01 00:00:00

  • Inhaled Janus Kinase (JAK) inhibitors for the treatment of asthma.

    abstract：:Multiple asthma-relevant cytokines including IL-4, IL-5, IL-13, and TSLP depend upon JAKs for signaling. JAK inhibition may, therefore, offer a novel intervention strategy for patients with disease refractory to current standards of care. Multiple systemically delivered JAK inhibitors have been approved for human use ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章,评审

    doi：10.1016/j.bmcl.2019.126658

    authors： Zak M,Dengler HS,Rajapaksa NS

    更新日期：2019-10-15 00:00:00

  • Inhibition of human cytomegalovirus protease by enedione derivatives of thieno[2,3-d]oxazinones through a novel dual acylation/alkylation mechanism.

    abstract：:Enedione derivatives of thieno[2,3-d]oxazinones are nanomolar inhibitors of CMV protease which act through a novel dual acylation of the catalytic serine and alkylation of the protease cysteine 161 via a Michael addition to the enedione moiety of the inhibitor. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(99)00005-0

    authors： Pinto IL,Jarvest RL,Clarke B,Dabrowski CE,Fenwick A,Gorczyca MM,Jennings LJ,Lavery P,Sternberg EJ,Tew DG,West A

    更新日期：1999-02-08 00:00:00

  • 2'-Deoxy-2'(S)-ethinyl oligonucleotides: a modification which selectively stabilizes oligoadenylate pairing to DNA complements.

    abstract：:Oligonucleotides consisting of 2'-deoxy-2'(S)-ethinyl-thymidine,-uridine, and -adenosine have been prepared. Whereas the modified pyrimidine oligonucleotides uniformly lead to weaker pairing affinity with DNA and RNA complements, the corresponding adenine oligonucleotides show enhanced thermal stability in duplexes wi...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(98)00060-2

    authors： Buff R,Hunziker J

    更新日期：1998-03-03 00:00:00

  • Antitrypanosomal and antioxidant properties of 4-hydroxycoumarins derivatives.

    abstract：:In the present communication we prepared a series of six 4-hydroxycoumarin derivatives, isosters of quercetin, recognized as an antioxidant natural compound, with the aim of evaluating the antitrypanosomal activity against Trypanosoma cruzi, the parasite responsible for Chagas disease, and the antioxidant properties. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2012.07.013

    authors： Pérez-Cruz F,Serra S,Delogu G,Lapier M,Maya JD,Olea-Azar C,Santana L,Uriarte E

    更新日期：2012-09-01 00:00:00