Výsledky vyhledávání - "Douglas M. Park"

Identification of biaryl sulfone derivatives as antagonists of the histamine H3 receptor: Discovery of (R)-1-(2-(4′-(3-methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine (APD916)

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 22:71-75

The design of a new clinical candidate histamine-H(3) receptor antagonist for the potential treatment of excessive daytime sleepiness (EDS) is described. Phenethyl-R-2-methylpyrrolidine containing biphenylsulfonamide compounds were modified by replac

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::5d0d99a5060605090b0ee3524c5cbb2d
https://doi.org/10.1016/j.bmcl.2011.11.075

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Design and Evaluation of Novel Biphenyl Sulfonamide Derivatives with Potent Histamine H3 Receptor Inverse Agonist Activity

Publikováno v: Journal of Medicinal Chemistry. 52:5603-5611

Antagonism of the histamine-H(3) receptor is one tactic being explored to increase wakefulness for the treatment of disorders such as excessive daytime sleepiness (EDS) as well as other sleep or cognitive disorders. Phenethyl-R-2-methylpyrrolidine co

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::91140b3031229283d3f2a52afb1585eb
https://doi.org/10.1021/jm900857n

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Discovery and SAR of new benzazepines as potent and selective 5-HT2C receptor agonists for the treatment of obesity

Autor: Jeffrey A. Schultz, William Thomsen, Robert R. Webb, Emily B. Prieto, Hazel R. Saldana, James Tsai, Rita R. Chen, Nigel Robert Arnold Beeley, Jeffrey Smith, Brian M. Smith, Scott A. Estrada, Kevin Whelan, Charles A Gilson, Dipanjan Sengupta, Charlemagne S. Gallardo, Frederique Menzaghi, Douglas M. Park

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 15:1467-1470

We report on the synthesis, biological evaluation and structure–activity relationships for a series of 3-benzazepine derivatives as 5-HT2C receptor agonists. The compounds were evaluated in functional assays measuring [3H] phosphoinositol turnover

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ff028e8cdb4c992bcfd3798687be7ae2
https://doi.org/10.1016/j.bmcl.2004.12.080

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Identification of biaryl sulfone derivatives as antagonists of the histamine H₃ receptor: discovery of (R)-1-(2-(4'-(3-methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine (APD916)

Publikováno v: Bioorganicmedicinal chemistry letters. 22(1)

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::35cf1f9e058b59b88466844ada85b945
https://pubmed.ncbi.nlm.nih.gov/22172695

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Discovery and structure-activity relationship of (1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a selective serotonin 5-HT2C receptor agonist for the treatment of obesity

Publikováno v: Journal of medicinal chemistry. 51(2)

The synthesis and SAR of a novel 3-benzazepine series of 5-HT2C agonists is described. Compound 7d (lorcaserin, APD356) was identified as one of the more potent and selective compounds in vitro (pEC50 values in functional assays measuring [(3)H]phosp

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::023ac9ea3dfbee3121f4be18befd7671
https://pubmed.ncbi.nlm.nih.gov/18095642

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Akademický článek

Design and Evaluation of Novel Biphenyl Sulfonamide Derivatives with Potent Histamine H3Receptor Inverse Agonist Activity.

Publikováno v: Journal of Medicinal Chemistry; Sep2009, Vol. 52 Issue 18, p5603-5611, 9p

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Akademický článek

Discovery and Structure−Activity Relationship of (1R)-8-Chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a Selective Serotonin 5-HT2CReceptor Agonist for the Treatment of Obesity.

Publikováno v: Journal of Medicinal Chemistry; Dec2007, Vol. 51 Issue 2, p305-313, 9p

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