Výsledky vyhledávání - "Shawn Maddaford"

Autor: Stephen G, Nuara, Jim C, Gourdon, Shawn, Maddaford, Philippe, Huot

Publikováno v: Naunyn-Schmiedeberg's archives of pharmacology. 394(12)

Antagonising serotonin (5-HT) type 2A receptors (5-HTFive 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-lesioned marmosets exhibiting dyskinesia and psychosis-like behaviours (PLBs) were administered L-3,4-dihydroxyphenylalanine (L-DOPA) in com

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::570d120a613e004733dc3022ba3958d3
https://pubmed.ncbi.nlm.nih.gov/34550406

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Effect of the glycine transporter 1 inhibitor ALX-5407 on dyskinesia, psychosis-like behaviours and parkinsonism in the MPTP-lesioned marmoset

Autor: Shawn Maddaford, Philippe Huot, Imane Frouni, Sébastien Belliveau, Stephen G. Nuara, Jim C. Gourdon

Publikováno v: European Journal of Pharmacology. 910:174452

Dyskinesia and psychosis are complications encountered in advanced Parkinson's disease (PD) following long-term therapy with L-3,4-dihydroxyphenylalanine (L-DOPA). Disturbances in the glutamatergic system have been associated with both dyskinesia and

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a6eee6c57557a7953f0cfd9ccb982f16
https://doi.org/10.1016/j.ejphar.2021.174452

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Discovery of a potent, orally bioavailable and highly selective human neuronal nitric oxide synthase (nNOS) inhibitor, N-(1-(piperidin-4-yl)indolin-5-yl)thiophene-2-carboximidamide as a pre-clinical development candidate for the treatment of migraine

Autor: Jailall Ramnauth, Taras Rybak, Gabriela Mladenova, Frank Porreca, Shawn Maddaford, Subhash C. Annedi, Dongqin Zhang, John S. Andrews, Peter Dove, Sarah Silverman, Paul Renton, Suman Rakhit

Publikováno v: European Journal of Medicinal Chemistry. 55:94-107

We recently reported a series of 1,6-disubstituted indoline-based thiophene amidine compounds (5) as selective neuronal nitric oxide synthase (nNOS) inhibitors to mitigate the cardiovascular liabilities associated with hERG K+ channel inhibition (IC5

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bb520ec9cc451caf145bb1fb5eccc02d
https://doi.org/10.1016/j.ejmech.2012.07.006

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Novel, druglike 1,7-disubstituted 2,3,4,5-tetrahydro-1H-benzo[b]azepine-based selective inhibitors of human neuronal nitric oxide synthase (nNOS)

Autor: Frank Porreca, John S. Andrews, Michele Cossette, Suman Rakhit, Peter Dove, Subhash C. Annedi, Shawn Maddaford, Jailall Ramnauth

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 22:2510-2513

A novel class of 1,7-disubstituted 2,3,4,5-tetrahydro-1H-benzo[b]azepine derivatives was designed, synthesized and evaluated as human nitric oxide synthase (NOS) inhibitors. Structure–activity relationship studies based on various basic amine side

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9683700cee49c941cc50ddd78cfd9469
https://doi.org/10.1016/j.bmcl.2012.02.004

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Discovery of N-(3-(1-Methyl-1,2,3,6-tetrahydropyridin-4-yl)-1H-indol-6-yl) thiophene-2-carboximidamide as a Selective Inhibitor of Human Neuronal Nitric Oxide Synthase (nNOS) for the Treatment of Pain

Autor: Jailall Ramnauth, Shawn Maddaford, Frank Porreca, David H. Lee, Suman Rakhit, Gabriela Mladenova, Dongqin Zhang, David Bunton, Subhash C. Annedi, John S. Andrews, Lee Christie

Publikováno v: Journal of Medicinal Chemistry. 54:7408-7416

3,6-Disubstituted indole derivatives were designed, synthesized, and evaluated as inhibitors of human nitric oxide synthase (NOS). Bulky amine containing substitution on the 3-position of the indole ring such as an azabicyclic system showed better se

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ca922b416e67bfab33e7740065e46ad7
https://doi.org/10.1021/jm201063u

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1,5-Disubstituted indole derivatives as selective human neuronal nitric oxide synthase inhibitors

Autor: Paul Renton, Joanne Speed, Shawn Maddaford, Subhash C. Annedi, Jailall Ramnauth, Suman Rakhit, John Andrews

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 21:5301-5304

A series of 1,5-disubstituted indole derivatives was designed, synthesized and evaluated as inhibitors of human nitric oxide synthase. A variety of flexible and restricted basic amine side chain substitutions was explored at the 1-position of the ind

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6fdbc0c27580e4d210fe1a3137ba25f1
https://doi.org/10.1016/j.bmcl.2011.07.022

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Design, Synthesis, and Biological Evaluation of 3,4-Dihydroquinolin-2(1H)-one and 1,2,3,4-Tetrahydroquinoline-Based Selective Human Neuronal Nitric Oxide Synthase (nNOS) Inhibitors

Autor: Frank Porreca, Subhash C. Annedi, Peter Dove, David H. Lee, Milena De Felice, Gabriela Mladenova, Salvatore Zinghini, Joanne Speed, Concettina Catalano, Jailall Ramnauth, Sheela Nair, Shawn Maddaford, John S. Andrews, Paul Renton, Sarah Silverman, Suman Rakhit

Publikováno v: Journal of Medicinal Chemistry. 54:5562-5575

Neuronal nitric oxide synthase (nNOS) inhibitors are effective in preclinical models of many neurological disorders. In this study, two related series of compounds, 3,4-dihydroquinolin-2(1H)-one and 1,2,3,4-tetrahydroquinoline, containing a 6-substit

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1f7ffd3f452a96b03ad44d3269cfb826
https://doi.org/10.1021/jm200648s

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Triptan-induced enhancement of neuronal nitric oxide synthase in trigeminal ganglion dural afferents underlies increased responsiveness to potential migraine triggers

Autor: David W. Dodick, Frank Porreca, Juliana Geremias Chichorro, Milena De Felice, Ian D. Meng, Michael H. Ossipov, Josephine Lai, Shawn Maddaford, Ruizhong Wang, John S. Andrews, Gregory Dussor, Suman Rakhit

Publikováno v: Brain. 133:2475-2488

Migraine is a common neurological disorder often treated with triptans. Triptan overuse can lead to increased frequency of headache in some patients, a phenomenon termed medication overuse headache. Previous preclinical studies have demonstrated that

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f666343fc255a4cf442199cc8c9467c2
https://doi.org/10.1093/brain/awq159

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Novel 2-aminobenzothiazoles as selective neuronal nitric oxide synthase inhibitors

Autor: John S. Andrews, Subhash C. Annedi, Suman Rakhit, Shawn Maddaford, Jailall Ramnauth, Joanne Patman, Paul Renton, Namrta Bhardwaj

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 17:2540-2544

A series of substituted 2-aminobenzothiazole compounds have been synthesized and evaluated as nitric oxide synthase (NOS) inhibitors. Compound 14 shows activity in the nM range and is selective for the human neuronal NOS isoform. We have also evaluat

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::16c069bbfc64f0788c199e84a4b91648
https://doi.org/10.1016/j.bmcl.2007.02.011

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