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The piridobenzochiajin derivative null which has high anti-bacterial activity and the high biological utilization talent for

机译:具有较高的抗菌活性和较高的生物利用才华的吡啶并苯并恶亚金衍生物无效

摘要

Pyrido-benzothiazine derivatives having the following general formula: CHEM in which R is H or a C1-C6 alkyl or a C1-C6 fluoroalkyl, and R1 is N-alkyl-3-pyrrolidinalkylamine with C1 to C6 alkyls or CHEM where R2 is a C1-C6 alkyl or a C2-C6 alkenyl or an arylalkyl group, possibly substituted by halogen, hydroxy or keto-groups, both in the racemic form and in the optically active form. The invention also comprises the process for the preparation of derivatives of formula (I) starting from 2.4-difluoro-3-chloronitrobenzene. Said derivatives possess a high antibacterial acitvity as well as a high bioavailability to tissues; the invention also refers to pharmaceutical compositions containing them as active components.
机译:具有以下通式的吡啶基-苯并噻嗪衍生物:其中R为H或C1-C6烷基或C1-C6氟烷基,R1为具有C1-C6烷基的N-烷基-3-吡咯烷基烷基胺或其中R 2是外消旋形式和旋光形式的C 1 -C 6烷基或C 2 -C 6烯基或芳基烷基,可能被卤素,羟基或酮基取代。本发明还包括从2.4-二氟-3-氯硝基苯开始制备式(I)的衍生物的方法。所述衍生物具有高抗菌活性以及对组织的高生物利用度。本发明还涉及含有它们作为活性成分的药物组合物。

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