Výsledky vyhledávání - "Honnappa Jayakumar"

Synthesis and SAR of N-Benzoyl-?-Biphenylalanine Derivatives: Discovery of TR-14035, A Dual α4β7/α4β1 Integrin Antagonist

Autor: Ila Sircar, Sumihiro Nomura, Bradley Teegarden, Dawn M. Nowlin, Jason R Mah, Griffith Ronald C, Samuel Connell, Honnappa Jayakumar, Kristjan S. Gudmundsson, Elias Lazarides, Pina M. Cardarelli, Richard Martin, Jimmy Liang

Publikováno v: Bioorganic & Medicinal Chemistry. 10:2051-2066

alpha(4)beta(1) and alpha(4)beta(7) integrins are key regulators of physiologic and pathologic responses in inflammation and autoimmune disease. The effectiveness of anti-integrin antibodies to attenuate a number of inflammatory/immune conditions pro

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::f8f85d85089696b745ea8a723445a8a3
https://doi.org/10.1016/s0968-0896(02)00021-4

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Discovery and structure-activity relationship of 3-methoxy-N-(3-(1-methyl-1H-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide (APD791): a highly selective 5-hydroxytryptamine2A receptor inverse agonist for the treatment of arterial thrombosis

Publikováno v: Journal of medicinal chemistry. 53(11)

Serotonin, which is stored in platelets and is released during thrombosis, activates platelets via the 5-HT(2A) receptor. 5-HT(2A) receptor inverse agonists thus represent a potential new class of antithrombotic agents. Our medicinal program began wi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1cbe094a664ee0ae0e520ee19db34d9a
https://pubmed.ncbi.nlm.nih.gov/20455563

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Discovery of 1-[3-(4-bromo-2-methyl-2h-pyrazol-3-yl)-4-methoxyphenyl]-3-(2,4-difluorophenyl)urea (nelotanserin) and related 5-hydroxytryptamine2A inverse agonists for the treatment of insomnia

Publikováno v: Journal of medicinal chemistry. 53(5)

Insomnia affects a growing portion of the adult population in the U.S. Most current therapeutic approaches to insomnia primarily address sleep onset latency. Through the 5-hydroxytryptamine(2A) (5-HT(2A)) receptor, serotonin (5-HT) plays a role in th

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::91185de5dbe3d3961b3976cd2b827093
https://pubmed.ncbi.nlm.nih.gov/20143782

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Solubilized phenyl-pyrazole ureas as potent, selective 5-HT(2A) inverse-agonists and their application as antiplatelet agents

Autor: Peter I. Dosa, Marc Decaire, Martin Casper, Juerg Lehmann, Katie Elwell, Juan Ramirez, Yifeng Xiong, John W. Adams, Amy Siu-Ting Wong, Graeme Semple, Karoline Choi, Honnappa Jayakumar, Jeremy G. Richman, Bradley Teegarden, William Thomsen, Robert R. Webb, Sonja Strah-Pleynet

Publikováno v: Bioorganicmedicinal chemistry letters. 19(18)

Potent 5-HT 2A inverse-agonists containing phenyl-pyrazole ureas with an amino side chain were identified. Optimization of this series resulted in selective compounds that proved effective in modulating 5HT-induced amplification of ADP-stimulated hum

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::481b10fcdb4966e398fe2f6adf23b27b
https://pubmed.ncbi.nlm.nih.gov/19665894

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Synthesis and SAR of N-benzoyl-L-biphenylalanine derivatives: discovery of TR-14035, a dual alpha(4)beta(7)/alpha(4)beta(1) integrin antagonist

Autor: Ila, Sircar, Kristjan S, Gudmundsson, Richard, Martin, Jimmy, Liang, Sumihiro, Nomura, Honnappa, Jayakumar, Bradley R, Teegarden, Dawn M, Nowlin, Pina M, Cardarelli, Jason R, Mah, Samuel, Connell, Ronald C, Griffith, Elias, Lazarides

Publikováno v: Bioorganicmedicinal chemistry. 10(6)

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::63eb18faf2504a69fae29d7c28ce74fe
https://pubmed.ncbi.nlm.nih.gov/11937364

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