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新型吡啶并-[2,3-c]-1,2-噻嗪1,1-二氧化物衍生物组中的药理活性。

Pharmacological activity in the group of new pyrido-[2,3-c]-1,2 thiazine 1,1-dioxide derivatives.

作者信息

Kowalczyk-Bronisz S H

出版信息

Arch Immunol Ther Exp (Warsz). 1980;28(5):783-90.

PMID:7212984
Abstract

Influence of 25 newly synthesized pyrido-1,2 thiazine 1,1-dioxide derivatives on immunological response and on induced inflammatory processes was studied. Marked immunostimulative activity (PFC) of 4,6-dimethyl-8-phenyl-2H-pyrido-[2,3-c]-thiazine dioxide (preparation X) was noted. Strong immunosuppressive activity connected with antiinflammatory activity (xylene, carrageenin and granulation test) was observed after the animals had been treated with 2-2'-(dimethyl-aminoethyl)-4,6-dimethyl-7-methoxy-8-phenyl-2H-pyrido-[2,3-c]-1, 2 thiazine 1,1-dioxide (preparation VIII) as well as 2,4,6-trimethyl-8-3H-thiazine dioxide (preparation XX). Mechanism of the activity of these compounds is discussed. In the group of the tested derivatives, relatively limited dependence between biological effects and chemical structure of the compounds was demonstrated.

摘要

研究了25种新合成的吡啶并-1,2-噻嗪1,1-二氧化物衍生物对免疫反应和诱导炎症过程的影响。注意到4,6-二甲基-8-苯基-2H-吡啶并-[2,3-c]-噻嗪二氧化物(制剂X)具有显著的免疫刺激活性(PFC)。在用2-2'-(二甲基氨基乙基)-4,6-二甲基-7-甲氧基-8-苯基-2H-吡啶并-[2,3-c]-1,2-噻嗪1,1-二氧化物(制剂VIII)以及2,4,6-三甲基-8-3H-噻嗪二氧化物(制剂XX)处理动物后,观察到与抗炎活性(二甲苯、角叉菜胶和肉芽形成试验)相关的强免疫抑制活性。讨论了这些化合物的活性机制。在测试的衍生物组中,证明了化合物的生物学效应与化学结构之间相对有限的相关性。

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