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http://hdl.handle.net/10261/88203
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dc.contributor.author | Martínez Gil, Ana | - |
dc.contributor.author | Castro, Ana | - |
dc.contributor.author | Gil, Carmen | - |
dc.contributor.author | Miralpeix, Montserrat | - |
dc.contributor.author | Segarra, Víctor | - |
dc.contributor.author | Doménech, Teresa | - |
dc.contributor.author | Beleta, Jorge | - |
dc.contributor.author | Palacios, José M. | - |
dc.contributor.author | Ryder, Hamish | - |
dc.contributor.author | Miró, Xavier | - |
dc.contributor.author | Bonet-Costa, Carles | - |
dc.contributor.author | Casacuberta, Josep M. | - |
dc.contributor.author | Azorín, Ferran | - |
dc.contributor.author | Piña, Benjamín | - |
dc.contributor.author | Puigdomènech, Pere | - |
dc.date.accessioned | 2013-12-04T11:34:41Z | - |
dc.date.available | 2013-12-04T11:34:41Z | - |
dc.date.issued | 2000 | - |
dc.identifier | doi: 10.1021/jm990382n | - |
dc.identifier | issn: 0022-2623 | - |
dc.identifier | e-issn: 1520-4804 | - |
dc.identifier.citation | Journal of Medicinal Chemistry 43: 683- 689 (2000) | - |
dc.identifier.uri | http://hdl.handle.net/10261/88203 | - |
dc.description.abstract | The synthesis of a new family of benzyl derivatives of 2,1,3-benzo- and benzothieno[3,2-a]-thiadiazine 2,2-dioxides was achieved. The biological data revealed the first heterocyclic family of compounds with PDE 7 inhibitory properties appearing to be a new objective for the treatment of T-cell- dependent disorders. The IC50 values or percent inhibition values of the compounds against PDE 7 were calculated by testing them against human recombinant PDE 7 expressed in S. cerevisiae. In this expression system the only cyclic nucleotide hydrolyzing activity present in cell extracts corresponded to human PDE 7. Isoenzyme selectivity PDE 7 versus PDE 4 and PDE 3 was also measured. Considering simultaneously inhibition of the three different isoenzymes, monobenzyl derivatives 15 and 23 showed interesting PDE 7 potency (around 10 μM); although not statistically significant, a trend toward selectivity with respect to PDE 3 and PDE 4 was obtained. Benzothiadiazine 16, although less potent at PDE 7 (IC50 = 25 μM), also showed a trend of selectivity toward PDE 3 and PDE 4. These compounds are considered the best leads for further optimization. | - |
dc.language.iso | eng | - |
dc.publisher | American Chemical Society | - |
dc.rights | closedAccess | - |
dc.title | Benzyl derivatives of 2,1,3-benzo- and benzothieno[3,2-a]thiadiazine 2,2-dioxides: First phosphodiesterase 7 inhibitors | - |
dc.type | artículo | - |
dc.identifier.doi | 10.1021/jm990382n | - |
dc.date.updated | 2013-12-04T11:34:41Z | - |
dc.description.version | Peer Reviewed | - |
dc.type.coar | http://purl.org/coar/resource_type/c_6501 | es_ES |
item.openairecristype | http://purl.org/coar/resource_type/c_18cf | - |
item.fulltext | No Fulltext | - |
item.cerifentitytype | Publications | - |
item.openairetype | artículo | - |
item.languageiso639-1 | en | - |
item.grantfulltext | none | - |
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