Výsledky vyhledávání - "Ngan B, Phung"

Bridged Piperidine Analogues of a High Affinity Naphthalene-Based P2Y

Autor: Zhiwei, Wen, Veronica, Salmaso, Young-Hwan, Jung, Ngan B, Phung, Varun, Gopinatth, Qasim, Shah, Alexandra T, Patterson, John C R, Randle, Zhoumou, Chen, Daniela, Salvemini, David I, Lieberman, Gregory S, Whitehead, Tadeusz P, Karcz, Donald N, Cook, Kenneth A, Jacobson

Publikováno v: J Med Chem

High affinity phenyl-piperidine P2Y(14)R antagonist 1 (PPTN) was modified with piperidine bridging moieties to probe receptor affinity and hydrophobicity. Various 2-azanorbornane, nortropane, isonortropane, isoquinuclidine, and ring-opened cyclopenty

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::da62c41535c927994c70d1b42266cae7
https://pubmed.ncbi.nlm.nih.gov/35113556

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Structure–Activity Relationship of Heterocyclic P2Y14 Receptor Antagonists: Removal of the Zwitterionic Character with Piperidine Bioisosteres

Autor: Kenneth A. Jacobson, Donald N. Cook, Tadeusz P Karcz, John C R Randle, John M. Bennett, Varun Gopinatth, Zhiwei Wen, Ngan B. Phung, Daniela Salvemini, Young-Hwan Jung, David I. Lieberman, Veronica Salmaso, Zhoumou Chen

Publikováno v: Journal of Medicinal Chemistry. 64:5099-5122

A known zwitterionic, heterocyclic P2Y14R antagonist 3a was substituted with diverse groups on the central phenyl and terminal piperidine moieties, following a computational selection process. The most potent analogues contained an uncharged piperidi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c8619de0d7c2d74a8325f516dd55228e
https://doi.org/10.1021/acs.jmedchem.1c00164

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P2Y14 Receptor Antagonists Reverse Chronic Neuropathic Pain in a Mouse Model

Autor: Kenneth A. Jacobson, Fatma Mufti, Ngan B. Phung, Luigino Antonio Giancotti, Daniela Salvemini, Young-Hwan Jung, Jinha Yu, Zhoumou Chen

Publikováno v: ACS Medicinal Chemistry Letters. 11:1281-1286

Eight P2Y14R antagonists, including three newly synthesized analogues, containing a naphthalene or phenyl-triazolyl scaffold were compared in a mouse model of chronic neuropathic pain (sciatic constriction). P2Y14R antagonists rapidly (≤30 min) rev

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::5294955a197573842d2dc091376c94e0
https://doi.org/10.1021/acsmedchemlett.0c00115

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Structure-Activity Relationship of Heterocyclic P2Y

Autor: Young-Hwan, Jung, Veronica, Salmaso, Zhiwei, Wen, John M, Bennett, Ngan B, Phung, David I, Lieberman, Varun, Gopinatth, John C R, Randle, Zhoumou, Chen, Daniela, Salvemini, Tadeusz P, Karcz, Donald N, Cook, Kenneth A, Jacobson

Publikováno v: J Med Chem

A known zwitterionic, heterocyclic P2Y(14)R antagonist 3a was substituted with diverse groups on the central phenyl and terminal piperidine moieties, following a computational selection process. The most potent analogues contained an uncharged piperi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::2538a8e3308d6a52460a78072272a801
https://pubmed.ncbi.nlm.nih.gov/33787273

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Structure activity relationship of 3-nitro-2-(trifluoromethyl)-2H-chromene derivatives as P2Y

Autor: Young-Hwan, Jung, Shanu, Jain, Varun, Gopinatth, Ngan B, Phung, Zhan-Guo, Gao, Kenneth A, Jacobson

Publikováno v: Bioorg Med Chem Lett

Various 6-alkynyl analogues of a known 3-nitro-2-(trifluoromethyl)-2H-chromene antagonist 3 of the G(q)-coupled P2Y(6) receptor (P2Y(6)R) were synthesized using a Sonogashira reaction to replace a 6-iodo group. The analogues were tested in a function

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::6e0b3bced1f28e29dfac11377d1858be
https://pubmed.ncbi.nlm.nih.gov/33831560

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Exploration of Alternative Scaffolds for P2Y(14) Receptor Antagonists Containing a Biaryl Core

Autor: Steven Dudas, Zhan-Guo Gao, Jinha Yu, Zhiwei Wen, Tadeusz P Karcz, John M. Bennett, Kenneth A. Jacobson, Sierra Duca, Ngan B. Phung, Daniela Salvemini, Young-Hwan Jung, Veronica Salmaso, Donald N. Cook, Zhoumou Chen

Publikováno v: J Med Chem

Various heteroaryl and bicyclo-aliphatic analogues of zwitterionic biaryl P2Y(14) receptor (P2Y(14)R) antagonists were synthesized, and affinity was measured in P2Y(14)R-expressing Chinese hamster ovary cells by flow cytometry. Given this series’ l

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::07e1e7f295e8914ed6cd6052e64fe4cb
https://europepmc.org/articles/PMC8040948/

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Structure-activity relationships of pyrimidine nucleotides containing a 5′-α,β-methylene diphosphonate at the P2Y6 receptor

Autor: Kiran S. Toti, Anna Junker, Ngan B. Phung, Shanu Jain, Paola Oliva, Varun Gopinatth, Kenneth A. Jacobson, Mirko Scortichini, Clemens Dobelmann

Publikováno v: Bioorg Med Chem Lett

The G(q)-coupled P2Y(6) receptor (P2Y(6)R) is a component of the purinergic signaling system and functions in inflammatory, cardiovascular and metabolic processes. UDP, the native P2Y(6)R agonist and P2Y(14)R partial agonist, is subject to hydrolysis

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b3e4645d3ce1a9053edf4f52e5bdc546
https://doi.org/10.1016/j.bmcl.2021.128137

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