Výsledky vyhledávání - "Konrad, Feichtinger"

Tetrahydroquinoline-based tricyclic amines as potent and selective agonists of the 5-HT 2C receptor

Autor: Minh Le, Albert S. Ren, Andrew J. Grottick, Graeme Semple, Kevin Whelan, Kelli Chase, Carleton R. Sage, Bilal Al Doori, Jenny Dong, Michelle Kasem, Chunrui Wu, Konrad Feichtinger, Jing Wei, Thomas O. Schrader, Huong T. Dang, Joel Gatlin

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 26:5877-5882

The syntheses, structure-activity relationships (SARs), and biological activities of tetrahydroquinoline-based tricyclic amines as 5-HT2C receptor agonists are reported. An early lead containing a highly unique 6,6,7-ring system was optimized for bot

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::1b144b9a662f28a39e38044641e2169c
https://doi.org/10.1016/j.bmcl.2016.11.016

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Novel (R)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,n]naphthyridines as potent and selective agonists of the 5-HT2C receptor

Autor: Clayton Hutton, Andrew J. Grottick, Graeme Semple, Konrad Feichtinger, Thomas O. Schrader, Jeremy Barden, Chunyan Liu, Kevin Whelan, Xiuwen Zhu, Chuan Chen, Chunrui Wu, John Frazer, Huong T. Dang, Joel Gatlin, Alvaro Ortiz, Minh Le, Albert S. Ren, Michelle Kasem, Kelli Chase

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 38:127872

A series of novel (R)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,n]naphthyridines were identified as potent and selective agonists of the 5-HT2C receptor. Optimizations performed on a previously reported series of racemic tetrahydroquinoline-based

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::9f72df697c29fc0f3668d49cfdc3fed8
https://doi.org/10.1016/j.bmcl.2021.127872

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Discovery of a lead series of potent benzodiazepine 5-HT2C receptor agonists with high selectivity in functional and binding assays

Autor: Albert S. Ren, Kevin Whelan, Konrad Feichtinger, Xiuwen Zhu, Michael Morgan, David J. Unett, Graeme Semple, Andrew J. Grottick, Amy Siu-Ting Wong, Michelle Kasem, Huong T. Dang, Juerg Lehman, Minh Le, Thomas O. Schrader, John Frazer, Carleton R. Sage

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 30:126929

A series of potential new 5-HT2 receptor scaffolds based on a simplification of the clinically studied, 5-HT2CR agonist vabicaserin, were designed. An in vivo feeding assay early in our screening process played an instrumental part in the lead identi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::a0c6c9d2b6e9f953cfc42198cdb93d7b
https://doi.org/10.1016/j.bmcl.2019.126929

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Identification of fused bicyclic heterocycles as potent and selective 5-HT2A receptor antagonists for the treatment of insomnia

Autor: Marc Decaire, Graeme Semple, Yifeng Xiong, Andrew J. Grottick, Woo H. Yoon, Kevin Whelan, Sonja Strah-Pleynet, Martin C. Cherrier, Brett Ullman, John Frazer, Hussien A. Al-Shamma, Jin-Sun Karoline Choi, Konrad Feichtinger, Erin K. Sanabria

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 22:1870-1873

A series of fused bicyclic heterocycles was identified as potent and selective 5-HT 2A receptor antagonists. Optimization of the series resulted in compounds that had improved PK properties, favorable CNS partitioning, good pharmacokinetic properties

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d847b773d26b55ba6e956b096b7717df
https://doi.org/10.1016/j.bmcl.2012.01.080

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Triurethane-Protected Guanidines and Triflyldiurethane-Protected Guanidines: New Reagents for Guanidinylation Reactions

Autor: Kenneth S. Matthews, Murray Goodman, Heather L. Sings, Tracy J. Baker, Konrad Feichtinger

Publikováno v: The Journal of Organic Chemistry. 63:8432-8439

New guanidinylation reagents are reported. These reagents consist of N,N‘,N‘‘-tri-Boc-guanidine (1) and N,N‘,N‘‘-tri-Cbz-guanidine (2), which allow for the facile conversion of alcohols to substituted guanidines. A series of arginine anal

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::c42bf5d116a91b119f55cd3912d8b186
https://doi.org/10.1021/jo9814344

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Synthesis and in vivo evaluation of phenethylpiperazine amides: selective 5-hydroxytryptamine(2A) receptor antagonists for the treatment of insomnia

Autor: Marc Decaire, Woo H. Yoon, Sonja Strah-Pleynet, Martin C. Cherrier, Yifeng Xiong, Andrew J. Grottick, Yun Shan, Konrad Feichtinger, Jin-Sun Karoline Choi, Peter I. Dosa, Erin K. Hauser, Graeme Semple, Bradley Teegarden, Brett Ullman, Hussien A. Al-Shamma, John Frazer, Kevin Whelan

Publikováno v: Journal of medicinal chemistry. 53(15)

Recent developments in sleep research suggest that antagonism of the serotonin 5-HT(2A) receptor may improve sleep maintenance insomnia. We herein report the discovery of a series of potent and selective serotonin 5-HT(2A) receptor antagonists based

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::be1f12cc27afd5f40417fd45e6654d93
https://pubmed.ncbi.nlm.nih.gov/20684606

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