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http://hdl.handle.net/2445/129848
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DC Field | Value | Language |
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dc.contributor.author | Barniol-Xicota, Marta | - |
dc.contributor.author | Kwak, Seung-Hwa | - |
dc.contributor.author | Lee, So-Deok | - |
dc.contributor.author | Caseley, Emily | - |
dc.contributor.author | Valverde Murillo, Elena | - |
dc.contributor.author | Jiang, Lin-Hua | - |
dc.contributor.author | Kim, Yong-Chul | - |
dc.contributor.author | Vázquez Cruz, Santiago | - |
dc.date.accessioned | 2019-03-06T14:39:43Z | - |
dc.date.available | 2019-03-06T14:39:43Z | - |
dc.date.issued | 2017-01-16 | - |
dc.identifier.issn | 0960-894X | - |
dc.identifier.uri | http://hdl.handle.net/2445/129848 | - |
dc.description.abstract | The adamantane scaffold, despite being widely used in medicinal chemistry, is not devoid of problems. In recent years we have developed new polycyclic scaffolds as surrogates of the adamantane group with encouraging results in multiple targets. As an adamantane scaffold is a common structural feature in several P2X7 receptor antagonists, herein we report the synthesis and pharmacological evaluation of multiple replacement options of adamantane that maintain a good activity profile. Molecular modeling studies support the binding of the compounds to a site close to the central pore, rather than to the ATP-binding site and shed light on the structural requirements for novel P2X7 antagonists. | - |
dc.format.extent | 5 p. | - |
dc.format.mimetype | application/pdf | - |
dc.language.iso | eng | - |
dc.publisher | Elsevier Ltd | - |
dc.relation.isformatof | Versió postprint del document publicat a: https://doi.org/10.1016/j.bmcl.2017.01.039 | - |
dc.relation.ispartof | Bioorganic & Medicinal Chemistry Letters, 2017, vol. 27, p. 759-763 | - |
dc.relation.uri | https://doi.org/10.1016/j.bmcl.2017.01.039 | - |
dc.rights | cc-by-nc-nd (c) Elsevier Ltd, 2017 | - |
dc.rights.uri | http://creativecommons.org/licenses/by-nc-nd/3.0/es | - |
dc.source | Articles publicats en revistes (Farmacologia, Toxicologia i Química Terapèutica) | - |
dc.subject.classification | Receptors cel·lulars | - |
dc.subject.classification | Medicaments | - |
dc.subject.other | Cell receptors | - |
dc.subject.other | Drugs | - |
dc.title | Escape from adamantane: scaffold optimization of novel P2X7 antagonists featuring complex polycycles | - |
dc.type | info:eu-repo/semantics/article | - |
dc.type | info:eu-repo/semantics/acceptedVersion | - |
dc.identifier.idgrec | 667479 | - |
dc.date.updated | 2019-03-06T14:39:43Z | - |
dc.rights.accessRights | info:eu-repo/semantics/openAccess | - |
dc.identifier.pmid | 28126517 | - |
Appears in Collections: | Articles publicats en revistes (Institut de Biomedicina (IBUB)) Articles publicats en revistes (Farmacologia, Toxicologia i Química Terapèutica) |
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667479.pdf | 432.49 kB | Adobe PDF | View/Open |
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