脂肪酯类isatin衍生物的合成、酶抑制及对接研究

IF 2.3 4区 化学 Q3 CHEMISTRY, MULTIDISCIPLINARY
Rifhat Sultana, Obaid-ur-Rahman Abid, Saira Bibi, Mohsin Ali, Syed Maeen Badshah, Shoaib Khan, Zaheed Ahmed
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引用次数: 0

摘要

以脂肪族酰肼和取代的isatin为原料,合成了一系列isatin 4(A - e)、5(A - e)、6(A - b)的亚胺衍生物。对合成产物进行了光谱分析,并对其脲酶和α-葡萄糖苷酶的抑制活性进行了评价。化合物3a、3b、4b、5a、5b、5c和6a的IC50值分别为50.40±0.21、46.19±0.21、46.03±1.22、43.33±0.62、50.67±0.13、45.78±3.53、50.34±1.92[µM],与标准化合物24.14µM相比,具有较好的脲酶抑制效果。而化合物3b、4a、5a、5b和5c对α-葡萄糖苷酶的抑制作用较好,IC50值分别为133.08±0.24、162.15±0.32、128.56±2.42、136.70±3.22和145.33±0.32[µM]。对接研究也支持了这一结果。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Synthesis, enzyme inhibition and docking studies of isatin derivatives from aliphatic esters

Synthesis, enzyme inhibition and docking studies of isatin derivatives from aliphatic esters

Synthesis, enzyme inhibition and docking studies of isatin derivatives from aliphatic esters

A series of imine derivatives of isatin 4(a–e), 5(a–e), 6(a–b) were synthesized using aliphatic hydrazides and substituted isatins. Synthesized products were analyzed by spectroanalytical techniques and evaluated for urease and α-glucosidase inhibition activities. Compounds 3a, 3b, 4b, 5a, 5b, 5c and 6a with an IC50 values 50.40 ± 0.21, 46.19 ± 0.21, 46.03 ± 1.22, 43.33 ± 0.62, 50.67 ± 0.13, 45.78 ± 3.53, 50.34 ± 1.92 [µM] respectively exhibited excellent urease inhibition results compared to the standard [24.14 µM]. However with respect to α-glucosidase inhibition activity, the compounds 3b, 4a, 5a, 5b, and 5c with IC50 values 133.08 ± 0.24, 162.15 ± 0.32, 128.56 ± 2.42, 136.70 ± 3.22 and 145.33 ± 0.32 [µM] respectively showed good inhibition. Results were also supported by docking studies.

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来源期刊
CiteScore
4.40
自引率
8.30%
发文量
230
审稿时长
5.6 months
期刊介绍: JICS is an international journal covering general fields of chemistry. JICS welcomes high quality original papers in English dealing with experimental, theoretical and applied research related to all branches of chemistry. These include the fields of analytical, inorganic, organic and physical chemistry as well as the chemical biology area. Review articles discussing specific areas of chemistry of current chemical or biological importance are also published. JICS ensures visibility of your research results to a worldwide audience in science. You are kindly invited to submit your manuscript to the Editor-in-Chief or Regional Editor. All contributions in the form of original papers or short communications will be peer reviewed and published free of charge after acceptance.
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