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Biological targets for isatin and its analogues: Implications for therapy

机译:伊斯兰素及其类似物的生物靶标:对治疗的意义

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Isatin and its metabolites are constituents of many natural substances. They are also components of many synthetic compounds exhibiting a wide range of effects, including antiviral activity, antitumor and antiangiogenic activity, antibacterial, antitubercular, antifungal, antiaptotic, anticonvulsant and anxyolytic activities. Isatin itself is an endogenous oxidized indole with a wide spectrum of behavioral and metabolic effects. It has a distinct and discontinuous distribution in the brain, peripheral tissues and body fluids and isatin binding sites are widely distributed also. Its output is increased during stress. Its most potent known in vitro actions are as an antagonist of atrial natriuretic peptide (ANP) function and NO signaling. As we understand more about its function and sites of action we may be able to develop new pharmacological agents to mimic or counteract its activity. We consider here the most promising biological targets for various isatin analogues and/or metabolites, which are employed for the development of various groups of therapeutics. It is also possible that the level of endogenous isatin may influence the in vivo pharmacological activity of compounds possessing the isatin moiety.
机译:Isatin及其代谢物是许多天然物质的成分。它们还是许多具有广泛作用的合成化合物的成分,这些作用包括抗病毒活性,抗肿瘤和抗血管生成活性,抗菌,抗结核,抗真菌,抗凋亡,抗惊厥和抗焦虑活性。 Isatin本身是一种内源性氧化吲哚,具有广泛的行为和代谢作用。它在脑,外周组织和体液中具有明显且不连续的分布,并且伊斯汀结合位点也广泛分布。在压力期间其输出增加。它最有效的体外作用是作为心钠素(ANP)功能和NO信号的拮抗剂。随着我们对它的功能和作用部位的更多了解,我们也许能够开发出新的药理剂来模拟或抵消其活性。在这里,我们考虑了各种伊斯兰类似物和/或代谢物的最有前途的生物学目标,这些目标被用于开发各种治疗药物。内源性Isatin的水平也可能会影响具有isatin部分的化合物的体内药理活性。

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