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http://hdl.handle.net/2445/128385
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DC Field | Value | Language |
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dc.contributor.author | Leiva Martínez, Rosana | - |
dc.contributor.author | Seira Castán, Constantí | - |
dc.contributor.author | McBride, Andrew | - |
dc.contributor.author | Binnie, Margaret | - |
dc.contributor.author | Luque Garriga, F. Xavier | - |
dc.contributor.author | Bidon-Chanal Badia, Axel | - |
dc.contributor.author | Webster, Scott P. | - |
dc.contributor.author | Vázquez Cruz, Santiago | - |
dc.date.accessioned | 2019-02-18T15:23:50Z | - |
dc.date.available | 2019-02-18T15:23:50Z | - |
dc.date.issued | 2015-08-05 | - |
dc.identifier.issn | 0960-894X | - |
dc.identifier.uri | http://hdl.handle.net/2445/128385 | - |
dc.description.abstract | The adamantane scaffold is found in several marketed drugs and in many investigational 11b-HSD1 inhibitors. Interestingly, all the clinically approved adamantane derivatives are C-1 substituted. We demonstrate that, in a series of paired adamantane isomers, substitution of the adamantane in C-2 is preferred over the substitution at C-1 and is necessary for potency at human 11b-HSD1. Furthermore, the introduction of an oxygen atom in the hydrocarbon scaffold of adamantane is deleterious to 11b-HSD1 inhibition. Molecular modeling studies provide a basis to rationalize these features. | - |
dc.format.extent | 4 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.2015.07.097 | - |
dc.relation.ispartof | Bioorganic & Medicinal Chemistry Letters, 2015, vol. 25, num. 19, p. 4250-4253 | - |
dc.relation.uri | https://doi.org/10.1016/j.bmcl.2015.07.097 | - |
dc.rights | cc-by-nc-nd (c) Elsevier Ltd, 2015 | - |
dc.rights.uri | http://creativecommons.org/licenses/by-nc-nd/3.0/es | - |
dc.source | Articles publicats en revistes (Nutrició, Ciències de l'Alimentació i Gastronomia) | - |
dc.subject.classification | Biologia | - |
dc.subject.classification | Farmacologia | - |
dc.subject.classification | Medicaments antivírics | - |
dc.subject.classification | Síntesi orgànica | - |
dc.subject.classification | Investigació farmacèutica | - |
dc.subject.classification | Cromatografia | - |
dc.subject.classification | Isomerització | - |
dc.subject.classification | Reaccions químiques | - |
dc.subject.other | Biology | - |
dc.subject.other | Pharmacology | - |
dc.subject.other | Antiviral agents | - |
dc.subject.other | Organic synthesis | - |
dc.subject.other | Pharmaceutical research | - |
dc.subject.other | Chromatography | - |
dc.subject.other | Isomerization | - |
dc.subject.other | Chemical reactions | - |
dc.title | Novel 11β-HSD1 inhibitors: C-1 versus C-2 substitution and effect of the introduction of an oxygen atom in the adamantane scaffold | - |
dc.type | info:eu-repo/semantics/article | - |
dc.type | info:eu-repo/semantics/acceptedVersion | - |
dc.identifier.idgrec | 654095 | - |
dc.date.updated | 2019-02-18T15:23:50Z | - |
dc.rights.accessRights | info:eu-repo/semantics/openAccess | - |
dc.identifier.pmid | 26306982 | - |
Appears in Collections: | Articles publicats en revistes (Farmacologia, Toxicologia i Química Terapèutica) Articles publicats en revistes (Nutrició, Ciències de l'Alimentació i Gastronomia) |
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654095.pdf | 327.71 kB | Adobe PDF | View/Open |
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