91375-75-6Relevant articles and documents
Synthesis and anticonvulsant activity evaluation of 7-alkoxy-2, 4-dihydro-1H-benzo[b][1,2,4]triazolo[4,3-d][1,4]thiazin-1-ones in various murine experimental seizure models
Cao, Xu,Wang, Shi-Ben,Deng, Xian-Qing,Liu, Da-Chuan,Quan, Zhe-Shan
, p. 1829 - 1838 (2014/05/06)
A novel series of 7-alkoxy-2,4-dihydro-1H-benzo [b][1,2,4]triazolo[4,3-d] [1,4]-thiazin-1-ones have been synthesized and tested for their anticonvulsant activity using the maximal electroshock (MES) method. The majority of the compounds prepared were effe
SYNTHESIS AND REACTIVITY OF CYCLIC QUINONIMINES OF THE 2H-1,4-BENZOTHIAZINE SERIES
Crescenzi, Orlando,Prota, Giuseppe,Schultz, Thomas M.,Wolfram, Leszek J.
, p. 21 - 24 (2007/10/02)
Periodate oxidation of cysteinylhydroquinone ethyl ester, 4, led to the 2H-1,4-benzothiazine 6, evidently via rearrangement of the intermediate quinonimine 1a.The relatively more stable quinonimine 1b could be obtained in crystalline form by oxidation of the dihydrobenzothiazine 8.In solution, 1b exhibits a marked tendency to undergo acid- or base-catalyzed isomerization to the highly unstable 7-hydroxy-2H-1,4-benzothiazine, 3.Once formed, the latter can either give rise to the trimer 2 by an imine-enamine type condensation, or undergo oxidation with formation of the lactam 9 or of the Δ2,2'-bi(2H-1,4-benzothiazine) dye 10.
Inhibitors of cyclic AMP phosphodiesterase. 1. Analogues of cilostamide and anagrelide
Jones,Venuti,Alvarez,Bruno,Berks,Prince
, p. 295 - 303 (2007/10/02)
Evaluation of a series of lactam heterocyclic analogues of cilostamide as inhibitors of cyclic AMP phosphodiesterase derived from both human platelets and rat heart in comparison with their corresponding methoxy-substituted heterocycles has revealed that the N-cyclohexyl-N-methyl-4-oxybutyramide side chain of 2 is an important lipophilic and/or steric pharmacophore. Attachment of this side chain to the parent heterocycle of the potent cyclic AMP phosphodiesterase inhibitor anagrelide afforded the hybrid structure RS-82856, shown to be more potent than either of its progenitors as an inhibitor of cyclic AMP phosphodiesterase or of ADP-induced platelet aggregation. The available in vitro data suggest that 1 possesses potentially useful antithrombotic and cardiotonic properties.