Synthesis and pharmacological activity of 21-esters of prednisolone with glycine and glutamic acid

Translated from Khimiko-farmatsevitcheskii Zhurnal, Vol. 25, No. 4, pp. 16–18, April, 1991.     

谷氨酸硫酸镧固体配合物的合成,性质及抗癌活性

合成了新的谷氨酸硫酸镧固体配合物,并确定了该配合物的组成为Ｌａ２（Ｇｌｕ）４（ＳＯ４）３·８Ｈ２Ｏ．并对其荧光光谱、摩尔电导及抗癌活性进行了研究．结果表明,该配合物对Ｋ５６２（红白血病）、Ｈ２２（小鼠肝癌）和ＳＷ４８０（人结肠癌）有显著的抑制作用     

Synthesis and pharmacological properties of novel glycine antagonists

The NMDA receptor is an ionotropic receptor complex widely distributed in the central nervous system and its activation, particularly in hypoxic conditions such as stroke, traumatic head injury and hypoglycemia, results in a massive influx of calcium ions into the post-synaptic neurones, leading to cell death through the activation of several neurotoxic cascades. The NMDA receptor is a unique ionotropic receptor complex because its activation requires the simultaneous binding of glutamate and glycine and selective antagonists at the glycine binding site are endowed with a better side-effect profile than competitive NMDA antagonists. Then, considerable efforts have been devoted to find potent and selective ligands, resulting in the identification of several classes of glycine antagonists. The research at Glaxo Wellcome has been aimed at the identification of novel in vivo active glycine antagonists, and led to the synthesis and pharmacological characterization of a number of novel, potent and systemically active compounds belonging to different chemical classes.     

Synthesis and pharmacological activity of 3-carboxypicolinic acid amides

A series of substituted amides of 3-carboxypicolinic acid have been synthesized via the interaction of quinolinic acid anhydride with alkyl(aryl)amines. Their structures were studied by ¹H and ¹³C NMR spectroscopy. The direction of the reaction was explained by quantum-chemistry methods. Three compounds demonstrated hemostatic activity. Two substances exhibited anticoagulant properties. Most substances also exhibited weak bacteriostatic activity.     

Search for lipoxygenase inhibitors and study of their pharmacological activity

Translated from Khimiko-farmatsevticheskii Zhurnal, Vol. 23, No. 9, pp. 1084–1088, September 1989.     

吡唑类化合物的合成与药理活性研究*

目的:合成吡唑类衍生物并研究其抗流感病毒活性。方法:以1-甲氧甲酰基-5-氨基-1H-吡唑-3-甲酸乙酯为原料,同氯乙酰氯和取代哌嗪反应得到含氮化合物;同硫氰酸钠、酰氯反应得到酰氨基硫脲。结果与结论:合成了7个新化合物;其中部分化合物具有一定抗流感病毒活性。     

氨基噻唑衍生物的合成与药理活性研究

目的:合成氨基噻唑类衍生物并研究其抗流感病毒活性。方法:以氨基噻唑类化合物为母核,合成一系列神经氨酸酶抑制剂,通过在体方法检测其对流感病毒的抑制活性。结果与结论:合成了6个新化合物,其中部分化合物具有一定的抗流感病毒活性。