Search Results - "Crosby, Ian T"

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    Probing Structural Requirements of Positive Allosteric Modulators of the M4 Muscarinic Receptor by Huynh, Tracey, Valant, Celine, Crosby, Ian T, Sexton, Patrick M, Christopoulos, Arthur, Capuano, Ben

    Published in Journal of medicinal chemistry (24-10-2013)
    “…The M4 mAChR is implicated in several CNS disorders and possesses an allosteric binding site for which ligands modulating the affinity and/or efficacy of ACh…”
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    Synthesis and Pharmacological Evaluation of M4 Muscarinic Receptor Positive Allosteric Modulators Derived from VU10004 by Huynh, Tracey, Valant, Celine, Crosby, Ian T, Sexton, Patrick M, Christopoulos, Arthur, Capuano, Ben

    Published in ACS chemical neuroscience (17-06-2015)
    “…The M4 mAChR is implicated in several CNS disorders and possesses an allosteric binding site for which ligands modulating the affinity and/or efficacy of ACh…”
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    Antiviral agents 3. Discovery of a novel small molecule non-nucleoside inhibitor of Hepatitis B Virus (HBV) by Crosby, Ian T., Bourke, David G., Jones, Eric D., Jeynes, Tyrone P., Cox, Susan, Coates, Jonathan A.V., Robertson, Alan D.

    Published in Bioorganic & medicinal chemistry letters (15-03-2011)
    “…The discovery of a small molecule non-nucleoside inhibitor of Hepatitis B Virus is described. During our work on conocurvone derived naphthoquinone ‘trimers’…”
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    Homology Modeling and Docking Evaluation of Aminergic G Protein-Coupled Receptors by McRobb, Fiona M, Capuano, Ben, Crosby, Ian T, Chalmers, David K, Yuriev, Elizabeth

    “…We report the development of homology models of dopamine (D2, D3, and D4), serotonin (5-HT1B, 5-HT2A, 5-HT2B, and 5-HT2C), histamine (H1), and muscarinic (M1)…”
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    Homobivalent Ligands of the Atypical Antipsychotic Clozapine: Design, Synthesis, and Pharmacological Evaluation by McRobb, Fiona M, Crosby, Ian T, Yuriev, Elizabeth, Lane, J. Robert, Capuano, Ben

    Published in Journal of medicinal chemistry (23-02-2012)
    “…To date all typical and atypical antipsychotics target the dopamine D2 receptor. Clozapine represents the best-characterized atypical antipsychotic, although…”
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    8-Chloro-5-(4-phenethylpiperazin-1--yl)pyrido[2,3-b][1,5]benzoxazepine by Capuano, Ben, Crosby, Ian T, Forsyth, Craig M, Lloyd, Edward J, Vom, Amelia, Yuriev, Elizabeth

    “…As part of an anti-psychotic drug discovery program, we report the crystal structure of the title compound, C(24)H(23)ClN(4)O. The mol-ecule has a tricyclic…”
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    Synthesis and SAR study of 4-arylpiperidines and 4-aryl-1,2,3,6-tetrahydropyridines as 5-HT2C agonists by Conway, Richard J., Valant, Celine, Christopoulos, Arthur, Robertson, Alan D., Capuano, Ben, Crosby, Ian T.

    Published in Bioorganic & medicinal chemistry letters (01-04-2012)
    “…A series of substituted 4-arylpiperidines and a smaller family of 4-aryl-1,2,3,6-tetrahydropyridines were synthesized and their biological activity at the…”
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    Antiviral agents 2. Synthesis of trimeric naphthoquinone analogues of conocurvone and their antiviral evaluation against HIV by Crosby, Ian T., Bourke, David G., Jones, Eric D., de Bruyn, Paula J., Rhodes, David, Vandegraaff, Nick, Cox, Susan, Coates, Jonathan A.V., Robertson, Alan D.

    Published in Bioorganic & medicinal chemistry (01-09-2010)
    “…The synthesis of a new series of conocurvone analogues is presented that explores the importance of the pyran rings of conocurvone, their degree of…”
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    A three-dimensional model of the human immunodeficiency virus type 1 integration complex by Wielens, Jerome, Crosby, Ian T, Chalmers, David K

    Published in Journal of computer-aided molecular design (01-05-2005)
    “…While the general features of HIV-1 integrase function are understood, there is still uncertainty about the composition of the integration complex and how…”
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    Di- tert -butyl N -[2,6-bis(methoxymethoxy)phenyl]iminodiacetate by Capuano, Ben, Crosby, Ian T., Forsyth, Craig M., Khakham, Yelena, Manallack, David T.

    “…The title molecule, C20H31NO8, has pseudo-C2 symmetry about the C—N bond, with the bis(tert-butoxycarbonyl)amino group twisted from the benzene ring…”
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    Status of GPCR Modeling and Docking as Reflected by Community-wide GPCR Dock 2010 Assessment by Kufareva, Irina, Rueda, Manuel, Katritch, Vsevolod, Stevens, Raymond C., Abagyan, Ruben

    Published in Structure (London) (10-08-2011)
    “…The community-wide GPCR Dock assessment is conducted to evaluate the status of molecular modeling and ligand docking for human G protein-coupled receptors. The…”
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    2,2,7-Trichloro-3,4-dihydronaphthalen-1(2 H )-one by Capuano, Ben, Crosby, Ian T., Forsyth, Craig M., Shin, James K.

    “…The title compound, C10H7Cl3O, obtained as a major byproduct from a classical Schmidt reaction. The cyclohexyl ring is distorted from a classical chair…”
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    2,2,7-Trichloro-3,4-dihydro-naphthalen-1(2H)-one by Capuano, Ben, Crosby, Ian T, Forsyth, Craig M, Shin, James K

    “…The title compound, C(10)H(7)Cl(3)O, obtained as a major byproduct from a classical Schmidt reaction. The cyclohexyl ring is distorted from a classical chair…”
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    Di-tert-butyl N-[2,6-bis-(methoxy-meth-oxy)phen-yl]imino-diacetate by Capuano, Ben, Crosby, Ian T, Forsyth, Craig M, Khakham, Yelena, Manallack, David T

    “…The title mol-ecule, C(20)H(31)NO(8), has pseudo-C2 symmetry about the C-N bond, with the bis-(tert-butoxy-carbon-yl)amino group twisted from the benzene ring…”
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    JL13, a clozapine‐like potential antipsychotic agent, reduces sympathetic cutaneous vasomotor alerting responses (SCVARs) in rats, but the drug is less potent than clozapine by Blessing, William W., Capuano, Ben, Crosby, Ian T., Taylor, David A.

    Published in The FASEB journal (01-03-2008)
    “…Clozapine is an atypical antipsychotic drug used to treat schizophrenia. However clozapine has serious side effects and there is a search for new…”
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    New hybrids of clozapine and haloperidol and their isosteric analogues: synthesis, X-ray crystallography, conformational analysis and preliminary pharmacological evaluation by Capuano, Ben, Crosby, Ian T., Forsyth, Craig M., McRobb, Fiona M., Moudretski, Vladimir V., Taylor, David A., Vom, Amelia, Yuriev, Elizabeth

    Published in Structural chemistry (01-06-2010)
    “…Schizophrenia is a debilitating mental disorder which affects approximately 1% of the world’s population. Clozapine is an atypical antipsychotic showing…”
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