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Novel Binary Compounds Derived from 1,2,4-Thiadiazole

机译:1,2,4-噻二唑衍生的新型二元化合物

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The design of multifunctional pharmaceuticals with a broad spectrum of activity that are capable of interacting with several targets is one of the promising directions of contemporary medicinal chemistry. Recently, molecules containing pharmacophoric thia-diazole fragment and showing interesting pharmaceutical properties [1], including neuroprotective [2], have attracted much attention as promising therapeutics. In continuation of our studies, we developed a method of synthesis of 1,2,4-thiadiazole derivatives containing biogenic amines as a second pharmacophore or nitroxy group as a nitrogen oxide NO producer. We showed recently that N,N-disubstituted 5-amino-3-(2-nitroxypropyl)-l,2,4-thiadiazoles are efficient blocators of glutamate-stimulated ~(45)Ca~(2+) uptake [3] and, therefore, can affect pathological processes in different neurodegenerative diseases [4].
机译:具有多种活性且能够与多个靶标相互作用的多功能药物的设计是当代药物化学的有希望的方向之一。最近,含有药效团噻二唑片段并显示出令人关注的药物特性的分子[1],包括神经保护剂[2],作为有前途的治疗方法引起了广泛的关注。在继续研究的过程中,我们开发了一种合成1,2,4-噻二唑衍生物的方法,该衍生物含有生物胺作为第二药效基团或硝基氧基作为氮氧化物NO的产生剂。我们最近发现,N,N-二取代的5-氨基-3-(2-硝基氧丙基)-1,2,4-噻二唑是谷氨酸刺激的〜(45)Ca〜(2+)吸收的有效结合剂[3]和因此,可以影响不同神经退行性疾病的病理过程[4]。

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