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异吲哚啉酮:对抗惊厥的新希望。

ISATIN: New Hope Against Convulsion.

作者信息

Cheke Rameshwar S, Firke Sandip D, Patil Ravindra R, Bari Sanjay B

机构信息

Department of Pharmaceutical Chemistry, R.C. Patel Institute of Pharmaceutical Education and Research, Shirpur, Dhule, 425405 Maharashtra, India.

Department of Pharmaceutical Chemistry, H.R. Patel Institute of Pharmaceutical Education and Research, Shirpur, Dhule, 425405 Maharashtra, India.

出版信息

Cent Nerv Syst Agents Med Chem. 2018;18(2):76-101. doi: 10.2174/1871524917666171113124112.

DOI:10.2174/1871524917666171113124112
PMID:29141569
Abstract

BACKGROUND

Epilepsy is one in every of the foremost important chronic neurological disorders with high incidence worldwide. Several epileptic patients don't seem to be fully treated with currently available marketed medicines likewise so many drugs have shown unfavorable side effect and drug interaction. Therefore, there are continuing interests to seek out new anticonvulsant drugs.

METHODS

Literature search was carried out to indentify isatin containing derivatives as anticonvulsant drugs.

RESULTS

Common synthetic schemes were studied to design and develop isatin derives anticonvulsant agents. Various structural features essential for the design of isatin compounds were reported. Anticonvulsant activity is evaluated by different tests were identified and their results can be considered for the design of novel isatin derivatives as anticonvulsants.

CONCLUSION

In outline, isatin has been proved to be an excellent hybrid building the molecule with interesting biological activities. Among the prospect of derivatizing the N1, C2 and C3 positions, along with substitution on the aromatic ring, the synthetic modification for isatin is almost endless. Despite the fact that isatin derivatives are well-studied compounds, new derivatives are continually being discovered on the basis of known AEDs, isatin has been fused with other bioactive drug fragments and subsequently investigated as hybrid/dual action drugs and selectively targeted against convulsion.

摘要

背景

癫痫是全球发病率较高的最重要的慢性神经系统疾病之一。目前市售药物并不能完全治愈一些癫痫患者,而且许多药物已显示出不良副作用和药物相互作用。因此,人们一直在持续关注寻找新的抗惊厥药物。

方法

进行文献检索以确定含异吲哚酮的衍生物作为抗惊厥药物。

结果

研究了常见的合成方案以设计和开发异吲哚酮衍生的抗惊厥剂。报道了异吲哚酮化合物设计所需的各种结构特征。通过不同测试评估抗惊厥活性,并确定了结果,这些结果可用于设计新型异吲哚酮衍生物作为抗惊厥剂。

结论

总体而言,异吲哚酮已被证明是一种具有有趣生物活性的出色分子构建杂合体。在N1、C2和C3位置衍生化以及芳香环上进行取代的前景中,异吲哚酮的合成修饰几乎是无穷无尽的。尽管异吲哚酮衍生物是经过充分研究的化合物,但基于已知的抗癫痫药物仍不断发现新的衍生物,异吲哚酮已与其他生物活性药物片段融合,并随后作为杂合/双效药物进行研究,并选择性地针对惊厥。

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