当前位置： SCI文献检索 > JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Structure-activity relationship studies and discovery of a potent transient receptor potential vanilloid (TRPV1) antagonist 4-[3-chloro-5-[(1S)-1,2-dihydroxyethyl]-2-pyridyl]-N-[5-(trifluoromethyl)-2-pyridyl]-3,6-dihydro-2H-pyridine-1-carboxamide (V116517

Structure-activity relationship studies and discovery of a potent transient receptor potential vanilloid (TRPV1) antagonist 4-[3-chloro-5-[(1S)-1,2-dihydroxyethyl]-2-pyridyl]-N-[5-(trifluoromethyl)-2-pyridyl]-3,6-dihydro-2H-pyridine-1-carboxamide (V116517

Abstract：

:A series of novel tetrahydropyridinecarboxamide TRPV1 antagonists were prepared and evaluated in an effort to optimize properties of previously described lead compounds from piperazinecarboxamide series. The compounds were evaluated for their ability to block capsaicin and acid-induced calcium influx in CHO cells expressing human TRPV1. The most potent of these TRPV1 antagonists were further characterized in pharmacokinetic, efficacy, and body temperature studies. On the basis of its pharmacokinetic, in vivo efficacy, safety, and toxicological properties, compound 37 was selected for further evaluation in human clinical trials.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Tafesse L,Kanemasa T,Kurose N,Yu J,Asaki T,Wu G,Iwamoto Y,Yamaguchi Y,Ni C,Engel J,Tsuno N,Patel A,Zhou X,Shintani T,Brown K,Hasegawa T,Shet M,Iso Y,Kato A,Kyle DJ

doi

10.1021/jm500818a

subject

Has Abstract

pub_date

2014-08-14 00:00:00

pages

6781-94

issue

15

eissn

0022-2623

issn

1520-4804

journal_volume

57

pub_type

杂志文章

相关文献

JOURNAL OF MEDICINAL CHEMISTRY文献大全
  • Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.

    abstract：:Structural modifications requiring novel synthetic chemistry were made to the morpholine acetal human neurokinin-1 (hNK-1) receptor antagonist 4, and this resulted in the discovery of 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-ox o-1 ,2,4-triazol-5-yl)methyl morpholine (17). This m...

    journal_title：Journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1021/jm980299k

    authors： Hale JJ,Mills SG,MacCoss M,Finke PE,Cascieri MA,Sadowski S,Ber E,Chicchi GG,Kurtz M,Metzger J,Eiermann G,Tsou NN,Tattersall FD,Rupniak NM,Williams AR,Rycroft W,Hargreaves R,MacIntyre DE

    更新日期：1998-11-05 00:00:00

  • Structure-activity relationships for the antileishmanial and antitrypanosomal activities of 1'-substituted 9-anilinoacridines.

    abstract：:Members of the class of 9-anilinoacridine topoisomerase II inhibitors bearing lipophilic electron-donating 1'-anilino substituents are active against both the promastigote and amastigote forms of the parasite Leishmania major. A series of analogues of the known 1'-NHhexyl lead compound were prepared and evaluated agai...

    journal_title：Journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1021/jm970232h

    authors： Gamage SA,Figgitt DP,Wojcik SJ,Ralph RK,Ransijn A,Mauel J,Yardley V,Snowdon D,Croft SL,Denny WA

    更新日期：1997-08-01 00:00:00

  • Cyclic nitrone free radical traps: isolation, identification, and synthesis of 3,3-dimethyl-3,4-dihydroisoquinolin-4-ol N-oxide, a metabolite with reduced side effects.

    abstract：:A C-4 hydroxylated metabolite (2, 3,3-dimethyl-3,4-dihydroisoquinolin-4-ol N-oxide) of the previously described cyclic nitrone free radical trap 1 (3,3-dimethyl-3,4-dihydroisoquinoline N-oxide, a cyclic analog of phenyl-tert-butylnitrone (PBN)) was isolated, identified, and synthesized. The metabolite (2), though a le...

    journal_title：Journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1021/jm960244n

    authors： Thomas CE,Bernardelli P,Bowen SM,Chaney SF,Friedrich D,Janowick DA,Jones BK,Keeley FJ,Kehne JH,Ketteler B,Ohlweiler DF,Paquette LA,Robke DJ,Fevig TL

    更新日期：1996-12-06 00:00:00

  • 2-Phenylquinoline S. aureus NorA Efflux Pump Inhibitors: Evaluation of the Importance of Methoxy Group Introduction.

    abstract：:Antimicrobial resistance (AMR) represents a hot topic in drug discovery. Besides the identification of new antibiotics, the use of nonantibiotic molecules to block resistance mechanisms is a powerful alternative. Bacterial efflux pumps exert an early step in AMR development by allowing bacteria to grow at subinhibitor...

    journal_title：Journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1021/acs.jmedchem.8b00791

    authors： Felicetti T,Cannalire R,Pietrella D,Latacz G,Lubelska A,Manfroni G,Barreca ML,Massari S,Tabarrini O,Kieć-Kononowicz K,Schindler BD,Kaatz GW,Cecchetti V,Sabatini S

    更新日期：2018-09-13 00:00:00

  • Synthesis, structure, and antitumor activity of a novel tetranuclear titanium complex.

    abstract：:The coordination complex cyclo-tetrakis[bis(1-phenyl-3-methyl-4-benzoylpyrazolon-5-ato++ +)mu-o xotitanium(IV)] has been synthesized and characterized with IR and NMR spectroscopies and X-ray diffraction. The core of this species consists of an eight-membered Ti-mu-oxo ring with alternate short-long Ti-O bond lengths....

    journal_title：Journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1021/jm990539b

    authors： Caruso F,Rossi M,Tanski J,Sartori R,Sariego R,Moya S,Diez S,Navarrete E,Cingolani A,Marchetti F,Pettinari C

    更新日期：2000-10-05 00:00:00

  • Structural studies of metyrapone: a potent inhibitor of cytochrome P-450.

    abstract：:The crystal and molecular structure of metyrapone, a powerful inhibitor of certain cytochromes P-450, is described. Cytochrome P-450 enzymes are involved in metabolic processes, including those activating insecticides, drugs, and carcinogens. Metyrapone inhibits both the adrenal cytochrome P-450 catalyzing 11-beta-hyd...

    journal_title：Journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1021/jm00363a008

    authors： Rossi M

    更新日期：1983-09-01 00:00:00

  • Synthesis and adrenergic activity of ring-fluorinated phenylephrines.

    abstract：:2-Fluoro-, 4-fluoro-, and 6-fluorophenylephrine (6-FPE) were synthesized from the corresponding fluorinated 3-hydroxybenzaldehydes. New routes to 2-fluoro- and 6-fluoro-3-hydroxybenzaldehydes were developed based on regioselective lithiation of 2- and 4-[(dimethyl-tert-butylsilyl)oxy]fluorobenzene ortho to fluorine. A...

    journal_title：Journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1021/jm00160a030

    authors： Kirk KL,Olubajo O,Buchhold K,Lewandowski GA,Gusovsky F,McCulloh D,Daly JW,Creveling CR

    更新日期：1986-10-01 00:00:00

  • An Orally Bioavailable, Indole-3-glyoxylamide Based Series of Tubulin Polymerization Inhibitors Showing Tumor Growth Inhibition in a Mouse Xenograft Model of Head and Neck Cancer.

    abstract：:A number of indole-3-glyoxylamides have previously been reported as tubulin polymerization inhibitors, although none has yet been successfully developed clinically. We report here a new series of related compounds, modified according to a strategy of reducing aromatic ring count and introducing a greater degree of sat...

    journal_title：Journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1021/acs.jmedchem.5b01312

    authors： Colley HE,Muthana M,Danson SJ,Jackson LV,Brett ML,Harrison J,Coole SF,Mason DP,Jennings LR,Wong M,Tulasi V,Norman D,Lockey PM,Williams L,Dossetter AG,Griffen EJ,Thompson MJ

    更新日期：2015-12-10 00:00:00

  • Structure-activity relationships of analogues of thapsigargin modified at O-11 and O-12.

    abstract：:A number of analogues of thapsigargin have been synthesized by alkylating or acylating O-11 and O-12 in the lactol obtained by reducing thapsigargicin. Introduction of alpha-disposed substituents decreased the Ca(2+)-ATPase inhibitory potency of the analogue, whereas the enzyme was more tolerant toward beta-disposed s...

    journal_title：Journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1021/jm00002a009

    authors： Nielsen SF,Thastrup O,Pedersen R,Olsen CE,Christensen SB

    更新日期：1995-01-20 00:00:00

  • Thrombin inhibitors. 2. Amide derivatives of N alpha-substituted L-arginine.

    abstract：:A series of N alpha-(arylsulfonyl)-L-arginine amide derivatives with substituted or unsubstituted naphthalene and heterocyclic compounds as the N alpha-substituent was prepared and tested as inhibitors of the clotting activity of thrombin. N-n-Butyl and N-n-butyl-N-methyl derivatives of N alpha-dansyl-L-arginine amide...

    journal_title：Journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1021/jm00182a004

    authors： Kikumoto R,Tamao Y,Ohkubo K,Tezuka T,Tonomura S,Okamoto S,Funahara Y,Hijikata A

    更新日期：1980-08-01 00:00:00

  • Sultam hydroxamates as novel matrix metalloproteinase inhibitors.

    abstract：:In this communication we describe the design, synthesis, and evaluation of novel sultam hydroxamates 4 as MMP-2, -9, and -13 inhibitors. Compound 26 was found to be an active inhibitor (MMP-2 IC(50) = 1 nM) with 1000-fold selectivity over MMP-1 and good oral bioavailability (F = 43%) in mouse. An X-ray crystal structu...

    journal_title：Journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1021/jm049833g

    authors： Cherney RJ,Mo R,Meyer DT,Hardman KD,Liu RQ,Covington MB,Qian M,Wasserman ZR,Christ DD,Trzaskos JM,Newton RC,Decicco CP

    更新日期：2004-06-03 00:00:00

  • Discovery of antimycobacterial spiro-piperidin-4-ones: an atom economic, stereoselective synthesis, and biological intervention.

    abstract：:An atom economic and stereoselective synthesis of several spiro-piperidin-4-ones through 1,3-dipolar cycloaddition of azomethine ylides generated in situ from isatin and alpha-amino acids viz . proline, phenylglycine, and sarcosine to a series of 1-methyl-3,5-bis[(E)-arylmethylidene]tetrahydro-4(1H)-pyridinones is des...

    journal_title：Journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1021/jm800545k

    authors： Kumar RR,Perumal S,Senthilkumar P,Yogeeswari P,Sriram D

    更新日期：2008-09-25 00:00:00

  • Synthesis and preliminary biological evaluation of high-drug-load paclitaxel-antibody conjugates for tumor-targeted chemotherapy.

    abstract：:The goal of this study was to design paclitaxel (PTX)-monoclonal antibody (mAb) prodrug conjugates (PTXMAbs) with the ability to deliver therapeutically significant doses of the drug to the tumor while avoiding the previously observed solubility limitations of conjugates with PTX:mAb molar ratios of >3. New PTX conjug...

    journal_title：Journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1021/jm900899g

    authors： Quiles S,Raisch KP,Sanford LL,Bonner JA,Safavy A

    更新日期：2010-01-28 00:00:00

  • Synthesis and biological evaluation of alkenyldiarylmethane HIV-1 non-nucleoside reverse transcriptase inhibitors that possess increased hydrolytic stability.

    abstract：:Non-nucleoside inhibitors of HIV reverse transcriptase (NNRTIs), albeit not the mainstays of HIV/AIDS treatment, have become increasingly important in highly active antiretroviral therapy (HAART) due to their unique mechanism of action. Several years ago our group identified the alkenyldiarylmethanes (ADAMs) as a pote...

    journal_title：Journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1021/jm070382k

    authors： Cullen MD,Deng BL,Hartman TL,Watson KM,Buckheit RW Jr,Pannecouque C,Clercq ED,Cushman M

    更新日期：2007-10-04 00:00:00

  • 2-Phenylindoles. Effect of N-benzylation on estrogen receptor affinity, estrogenic properties, and mammary tumor inhibiting activity.

    abstract：:Hydroxy-2-phenylindoles carrying substituted benzyl groups and similar substituents at the nitrogen were synthesized and tested for their ability to displace estradiol from its receptor. All of the derivatives tested exhibited high binding affinities for the calf uterine estrogen receptor, with RBA values ranging from...

    journal_title：Journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1021/jm00384a022

    authors： von Angerer E,Strohmeier J

    更新日期：1987-01-01 00:00:00

  • Methylene-gem-difluorocyclopropane analogues of nucleosides: synthesis, cyclopropene-methylenecyclopropane rearrangement, and biological activity.

    abstract：:Alkylation-elimination of adenine and 2-amino-6-chloropurine with gem-difluorocyclopropane dibromide 10 gave E- and Z-methylene-gem-difluorocyclopropanes 11a, 11b, 12a, and 12b and gem-difluorocyclopropenes 13a and 13b. Debenzylation of intermediates 11a, 11b, 12a, and 12b afforded E- and Z-methylenecyclopropanes 4a, ...

    journal_title：Journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1021/jm010191w

    authors： Wang R,Ksebati MB,Corbett TH,Kern ER,Drach JC,Zemlicka J

    更新日期：2001-11-08 00:00:00

  • Imidazo[1,2-a]pyridine Derivatives as Aldehyde Dehydrogenase Inhibitors: Novel Chemotypes to Target Glioblastoma Stem Cells.

    abstract：:Glioblastoma multiforme (GBM) is the deadliest form of brain tumor. It is known for its ability to escape the therapeutic options available to date thanks to the presence of a subset of cells endowed with stem-like properties and ability to resist to cytotoxic treatments. As the cytosolic enzyme aldehyde dehydrogenase...

    journal_title：Journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1021/acs.jmedchem.9b01910

    authors： Quattrini L,Gelardi ELM,Coviello V,Sartini S,Ferraris DM,Mori M,Nakano I,Garavaglia S,La Motta C

    更新日期：2020-05-14 00:00:00

  • NMR structural studies of the supramolecular adducts between a liver cytosolic bile acid binding protein and gadolinium(III)-chelates bearing bile acids residues: molecular determinants of the binding of a hepatospecific magnetic resonance imaging contras

    abstract：:The binding affinities of a selected series of Gd(III) chelates bearing bile acid residues, potential hepatospecific MRI contrast agents, to a liver cytosolic bile acid transporter, have been determined through relaxivity measurements. The Ln(III) complexes of compound 1 were selected for further NMR structural analys...

    journal_title：Journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1021/jm070397i

    authors： Assfalg M,Gianolio E,Zanzoni S,Tomaselli S,Russo VL,Cabella C,Ragona L,Aime S,Molinari H

    更新日期：2007-11-01 00:00:00

  • Substituted halogenated arylsulfonamides: a new class of sigma receptor binding tumor imaging agents.

    abstract：:The discovery of a series of novel halogenated arylsulfonamides (HAS) as new sigma receptor binding tumor imaging agents is described. Several substituted halogenated sulfonamides have been prepared and characterized. Target compounds were examined for their affinity for sigma1 and sigma2 receptor subtypes using guine...

    journal_title：Journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1021/jm9800447

    authors： John CS,Lim BB,Vilner BJ,Geyer BC,Bowen WD

    更新日期：1998-07-02 00:00:00

  • Molecular modeling and molecular dynamics simulation of the human A2B adenosine receptor. The study of the possible binding modes of the A2B receptor antagonists.

    abstract：:A molecular model of the human A(2B) adenosine receptor containing seven transmembrane alpha helices connected by three intracellular and three extracellular hydrophilic loops had been constructed. A molecular docking of seven structurally diverse xanthine antagonists of the A(2B) receptor was performed, and the diffe...

    journal_title：Journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1021/jm049418o

    authors： Ivanov AA,Baskin II,Palyulin VA,Piccagli L,Baraldi PG,Zefirov NS

    更新日期：2005-11-03 00:00:00

  • 4-Methyl-3-(arylsulfonyl)furoxans: a new class of potent inhibitors of platelet aggregation.

    abstract：:A series of 4-methyl-3-(arylthio)furoxans were synthesized by oxidation of 1-(arylthio)-2-methylglyoxymes with dinitrogen tetroxide. Reduction with trimethyl phosphite of the furoxan derivatives afforded the corresponding furazans, while oxidation with an equimolar amount of 30% hydrogen peroxide in acetic acid or wit...

    journal_title：Journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1021/jm00095a028

    authors： Calvino R,Fruttero R,Ghigo D,Bosia A,Pescarmona GP,Gasco A

    更新日期：1992-08-21 00:00:00

  • Transition state mimetics of the Plasmodium export element are potent inhibitors of Plasmepsin V from P. falciparum and P. vivax.

    abstract：:Following erythrocyte invasion, malaria parasites export a catalogue of remodeling proteins into the infected cell that enable parasite development in the human host. Export is dependent on the activity of the aspartyl protease, plasmepsin V (PMV), which cleaves proteins within the Plasmodium export element (PEXEL; Rx...

    journal_title：Journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1021/jm500797g

    authors： Sleebs BE,Gazdik M,O'Neill MT,Rajasekaran P,Lopaticki S,Lackovic K,Lowes K,Smith BJ,Cowman AF,Boddey JA

    更新日期：2014-09-25 00:00:00

  • Discovery of 4-[(2S)-2-{[4-(4-chlorophenoxy)phenoxy]methyl}-1-pyrrolidinyl]butanoic acid (DG-051) as a novel leukotriene A4 hydrolase inhibitor of leukotriene B4 biosynthesis.

    abstract：:Both in-house human genetic and literature data have converged on the identification of leukotriene 4 hydrolase (LTA(4)H) as a key target for the treatment of cardiovascular disease. We combined fragment-based crystallography screening with an iterative medicinal chemistry effort to optimize inhibitors of LTA(4)H. Lig...

    journal_title：Journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1021/jm900838g

    authors： Sandanayaka V,Mamat B,Mishra RK,Winger J,Krohn M,Zhou LM,Keyvan M,Enache L,Sullins D,Onua E,Zhang J,Halldorsdottir G,Sigthorsdottir H,Thorlaksdottir A,Sigthorsson G,Thorsteinnsdottir M,Davies DR,Stewart LJ,Zembower DE

    更新日期：2010-01-28 00:00:00

  • Discovery of novel non-peptide CCR1 receptor antagonists.

    abstract：:Ligands for the CCR1 receptor (MIP-1alpha and RANTES) have been implicated in a number of chronic inflammatory diseases, most notably multiple sclerosis and rheumatoid arthritis. Because these ligands share a common receptor, CCR1, we sought to discover antagonists for this receptor as an approach to treating these di...

    journal_title：Journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1021/jm990316l

    authors： Ng HP,May K,Bauman JG,Ghannam A,Islam I,Liang M,Horuk R,Hesselgesser J,Snider RM,Perez HD,Morrissey MM

    更新日期：1999-11-04 00:00:00

  • Pyrrolopyrimidine Derivatives as Novel Inhibitors of Multidrug Resistance-Associated Protein 1 (MRP1, ABCC1).

    abstract：:Five series of pyrrolo[3,2-d]pyrimidines were synthesized and evaluated with respect to potency and selectivity toward multidrug resistance-associated protein 1 (MRP1, ABCC1). This transport protein is a major target to overcome multidrug resistance in cancer patients. We investigated differently substituted pyrrolopy...

    journal_title：Journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1021/acs.jmedchem.5b01644

    authors： Schmitt SM,Stefan K,Wiese M

    更新日期：2016-04-14 00:00:00

  • Prodrug-inspired probes selective to cathepsin B over other cysteine cathepsins.

    abstract：:Cathepsin B (CTB) is a cysteine protease believed to be an important therapeutic target or biomarker for several diseases including aggressive cancer, arthritis, and parasitic infections. The development of probes capable of assessing CTB activity in cell lysates, living cells, and animal models of disease are needed ...

    journal_title：Journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1021/jm500544p

    authors： Chowdhury MA,Moya IA,Bhilocha S,McMillan CC,Vigliarolo BG,Zehbe I,Phenix CP

    更新日期：2014-07-24 00:00:00

  • Nitric oxide synthases activation and inhibition by metallacarborane-cluster-based isoform-specific affectors.

    abstract：:A small library of boron-cluster- and metallacarborane-cluster-based ligands was designed, prepared, and tested for isoform-selective activation or inhibition of the three nitric oxide synthase isoforms. On the basis of the concept of creating a hydrophobic analogue of a natural substrate, a stable and nontoxic basic ...

    journal_title：Journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1021/jm300805x

    authors： Kaplánek R,Martásek P,Grüner B,Panda S,Rak J,Masters BS,Král V,Roman LJ

    更新日期：2012-11-26 00:00:00

  • Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels.

    abstract：:Transient receptor potential canonical 3/6/7 (TRPC3/6/7) are highly homologous receptor-operated nonselective cation channels. Despite their physiological significance, very few selective and potent agonists are available for functional examination of these channels. Using a cell-based high throughput screening approa...

    journal_title：Journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1021/acs.jmedchem.7b00304

    authors： Qu C,Ding M,Zhu Y,Lu Y,Du J,Miller M,Tian J,Zhu J,Xu J,Wen M,Er-Bu A,Wang J,Xiao Y,Wu M,McManus OB,Li M,Wu J,Luo HR,Cao Z,Shen B,Wang H,Zhu MX,Hong X

    更新日期：2017-06-08 00:00:00

  • Specific nonpeptide photoprobes as tools for the structural study of the angiotensin II AT(1) receptor.

    abstract：:The aim of this work was to obtain photoactivatable nonpeptide antagonists of the angiotensin II AT(1) receptor. Based on structure-function relationships, two chemical structures as well as appropriate synthetic schemes were chosen as a frame for the design of radiolabeled azido probes. The feasibility of the strateg...

    journal_title：Journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1021/jm991050l

    authors： Nouet S,Dodey PR,Bondoux MR,Pruneau D,Luccarini JM,Groblewski T,Larguier R,Lombard C,Marie J,Renaut PP,Leclerc G,Bonnafous JC

    更新日期：1999-11-04 00:00:00

  • 6-(3,4-dichlorophenyl)-1-[(methyloxy)methyl]-3-azabicyclo[4.1.0]heptane: a new potent and selective triple reuptake inhibitor.

    abstract：:A pharmacophore model for triple reuptake inhibitors and the new class of 1-(aryl)-6-[alkoxyalkyl]-3-azabicyclo[3.1.0]hexanes were recently reported. Further investigation in this area led to the identification of a new series of potent and selective triple reuptake inhibitors endowed with good developability characte...

    journal_title：Journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1021/jm100481d

    authors： Micheli F,Cavanni P,Andreotti D,Arban R,Benedetti R,Bertani B,Bettati M,Bettelini L,Bonanomi G,Braggio S,Carletti R,Checchia A,Corsi M,Fazzolari E,Fontana S,Marchioro C,Merlo-Pich E,Negri M,Oliosi B,Ratti E,Read K

    更新日期：2010-07-08 00:00:00