Search Results - "Crosby, Ian T"
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Probing Structural Requirements of Positive Allosteric Modulators of the M4 Muscarinic Receptor
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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2
Synthesis and Pharmacological Evaluation of M4 Muscarinic Receptor Positive Allosteric Modulators Derived from VU10004
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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3
Antiviral agents 3. Discovery of a novel small molecule non-nucleoside inhibitor of Hepatitis B Virus (HBV)
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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4
Homology Modeling and Docking Evaluation of Aminergic G Protein-Coupled Receptors
Published in Journal of chemical information and modeling (26-04-2010)“…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
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
Published in Acta crystallographica. Section E, Structure reports online (06-09-2008)“…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
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
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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9
A three-dimensional model of the human immunodeficiency virus type 1 integration complex
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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Synthesis of 8-Chloro-11-(4-(3-(p-tolyloxy)propyl)piperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepine
Published in MolBank (01-03-2006)“…n/a…”
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11
Di- tert -butyl N -[2,6-bis(methoxymethoxy)phenyl]iminodiacetate
Published in Acta crystallographica. Section E, Structure reports online (01-04-2009)“…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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12
Status of GPCR Modeling and Docking as Reflected by Community-wide GPCR Dock 2010 Assessment
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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13
Probing Structural Requirements of Positive Allosteric Modulators of the M 4 Muscarinic Receptor
Published in Journal of medicinal chemistry (24-10-2013)Get full text
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14
Synthesis and Pharmacological Evaluation of M 4 Muscarinic Receptor Positive Allosteric Modulators Derived from VU10004
Published in ACS chemical neuroscience (17-06-2015)Get full text
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15
2,2,7-Trichloro-3,4-dihydronaphthalen-1(2 H )-one
Published in Acta crystallographica. Section E, Structure reports online (01-09-2009)“…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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16
2,2,7-Trichloro-3,4-dihydro-naphthalen-1(2H)-one
Published in Acta crystallographica. Section E, Structure reports online (26-08-2009)“…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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17
Di-tert-butyl N-[2,6-bis-(methoxy-meth-oxy)phen-yl]imino-diacetate
Published in Acta crystallographica. Section E, Structure reports online (25-03-2009)“…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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18
JL13, a clozapine‐like potential antipsychotic agent, reduces sympathetic cutaneous vasomotor alerting responses (SCVARs) in rats, but the drug is less potent than clozapine
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
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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Synthesis of 8-chloro-11-(4-(3-(p-tolyloxy)propyl)piperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepine
Published in MolBank (01-12-2005)“…n/a…”
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