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对映体纯席夫碱的镇痛潜力的合成与研究:一种机理方法。

Synthesis and Investigation of the Analgesic Potential of Enantiomerically Pure Schiff Bases: A Mechanistic Approach.

机构信息

Department of Pharmacy, University of Malakand Dir (Lower) at Chakdara, Chakdara 18800, KPK, Pakistan.

Department of Pharmacy, Shaheed Benazir Bhutto University Sheringal Dir (Upper), Dir 18000, KPK, Pakistan.

出版信息

Molecules. 2022 Aug 15;27(16):5206. doi: 10.3390/molecules27165206.

DOI:10.3390/molecules27165206
PMID:36014445
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9416351/
Abstract

Schiff bases are a class of organic compounds with azomethine moiety, exhibiting a wide range of biological potentials. In this research, six chiral Schiff bases, three ‘S’ series (H1−H3) and three ‘R’ series (H4−H6), were synthesized. The reaction was neat, which means without a solvent, and occurred at room temperature with a high product yield. The synthesized compounds were evaluated for analgesic potential in vivo at doses of 12.5 and 25 mg/kg using acetic-acid-induced writhing assay, formalin test, tail immersion and hot plate models, followed by investigating the possible involvement of opioid receptors. The compounds H2 and H3 significantly (*** p < 0.001) reduced the writhing frequency, and H3 and H5 significantly (*** p < 0.001) reduced pain in both phases of the formalin test. The compounds H2 and H5 significantly (*** p < 0.001) increased latency at 90 min in tail immersion, while H2 significantly (*** p < 0.001) increased latency at 90 min in the hot plate test. The ‘S’ series Schiff bases, H1−H3, were found more potent than the ‘R’ series compounds, H4−H6. The possible involvement of opioid receptors was also surveyed utilizing naloxone in tail immersion and hot plate models, investigating the involvement of opioid receptors. The synthesized compounds could be used as alternative analgesic agents subjected to further evaluation in other animal models to confirm the observed biological potential.

摘要

席夫碱是一类含有亚胺部分的有机化合物,具有广泛的生物潜力。在这项研究中,合成了六个手性席夫碱,三个“S”系列(H1-H3)和三个“R”系列(H4-H6)。反应是在没有溶剂的条件下进行的,在室温下进行,产率很高。用醋酸诱导扭体试验、福氏试验、尾浸和热板模型评价了合成化合物的体内镇痛潜力,剂量为 12.5 和 25mg/kg,然后研究了阿片受体可能的参与情况。化合物 H2 和 H3 显著(***p<0.001)减少扭体频率,H3 和 H5 显著(***p<0.001)减少福氏试验两个阶段的疼痛。化合物 H2 和 H5 显著(***p<0.001)增加尾浸 90 分钟时的潜伏期,而 H2 显著(***p<0.001)增加热板试验 90 分钟时的潜伏期。“S”系列席夫碱 H1-H3 比“R”系列化合物 H4-H6 更有效。还利用纳洛酮在尾浸和热板模型中调查了阿片受体的可能参与情况,研究了阿片受体的参与情况。这些合成化合物可以作为替代镇痛剂,在其他动物模型中进一步评估,以确认观察到的生物学潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6245/9416351/d1fb79d537e8/molecules-27-05206-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6245/9416351/0da387e2d69d/molecules-27-05206-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6245/9416351/c1d99c3b8fc9/molecules-27-05206-sch002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6245/9416351/d1fb79d537e8/molecules-27-05206-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6245/9416351/0da387e2d69d/molecules-27-05206-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6245/9416351/c1d99c3b8fc9/molecules-27-05206-sch002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6245/9416351/d1fb79d537e8/molecules-27-05206-g001.jpg

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