- 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
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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
- Cao, Xu,Wang, Shi-Ben,Deng, Xian-Qing,Liu, Da-Chuan,Quan, Zhe-Shan
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p. 1829 - 1838
(2014/05/06)
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- Synthesis and anticonvulsant activity of some 7-alkoxy-2H-1,4-benzothiazin- 3(4H)-ones and 7-alkoxy-4H-[1,2,4]triazolo[4,3-d]benzo[b][1,4]thiazines
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A series of 7-alkoxy-2H-1,4-benzothiazin-3(4H)-ones and a new series of 7-alkoxy-4H-[1,2,4]triazolo[4,3-d]benzo[b][1,4]thiazine derivatives were synthesized using 5-methoxybenzo[d]thiazol-2-amine as starting material. The structures of the compounds were
- Zhang, Li-Qiu,Guan, Li-Ping,Wei, Cheng-Xi,Deng, Xian-Qing,Quan, Zhe-Shan
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experimental part
p. 326 - 331
(2011/02/25)
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- SYNTHESIS AND REACTIVITY OF CYCLIC QUINONIMINES OF THE 2H-1,4-BENZOTHIAZINE SERIES
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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.
- Crescenzi, Orlando,Prota, Giuseppe,Schultz, Thomas M.,Wolfram, Leszek J.
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- Inhibitors of cyclic AMP phosphodiesterase. 1. Analogues of cilostamide and anagrelide
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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.
- Jones,Venuti,Alvarez,Bruno,Berks,Prince
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p. 295 - 303
(2007/10/02)
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- Alkanolaminoxy derivatives of 3,4-dihydro-2H-1,4-benzothiazin-3-one, their production process, and their pharmaceutical use
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Object of the invention is a class of new organic compounds derived from 1,4-benzothiazine through substitution of an hydrogen atom in position 6, 7 or 8 by an oxypropanolammine radical monosubstituted in N and furthermore a series of new phenyl derivatives of 1,4-benzothiazine, obtained as intermediate in the synthesis of oxypropanolammine derivatives, and process for obtained the new compounds in form suitable for the preparation of pharmaceutical compositions having antihypertensive, vasodilating and antiarrhythmic activity.
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