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首页> 外文期刊>RSC Advances >Organocatalytic synthesis and evaluation of 7-chloroquinoline-1,2,3-triazoyl carboxamides as potential antinociceptive, anti-inflammatory and anticonvulsant agent
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Organocatalytic synthesis and evaluation of 7-chloroquinoline-1,2,3-triazoyl carboxamides as potential antinociceptive, anti-inflammatory and anticonvulsant agent

机译：7-氯喹啉-1,2,3-三唑基羧酰胺的有机催化合成和评估作为潜在的抗伤害，消炎和抗惊厥药

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摘要

We describe herein our results on the organocatalytic synthesis and pharmacological properties of 7-chloroquinoline-1,2,3-triazoyl carboxamides. This class of compounds was synthesized in good to excellent yields by the reaction of 4-azido-7-chloroquinoline with a range of beta-oxo-amides in the presence of a catalytic amount of pyrrolidine (5 mol%). The obtained compound 3a was screened for anticonvulsant, antinociceptive and anti-inflammatory activities in vivo. The results demonstrated that compound 3a was effective in decreasing the appearance of seizures induced by pilocarpine and pentylenetetrazole. In addition, compound 3a demonstrated antinoceptive and anti-inflammatory properties for combating acute pain. This protocol is an efficient method for the production of new heterocyclic compounds with pharmacological activities.
机译：我们在本文中描述了我们对7-氯喹啉-1,2,3-三唑基羧酰胺的有机催化合成和药理特性的研究结果。在催化量的吡咯烷（5摩尔％）存在下，通过4-叠氮基-7-氯喹啉与一系列β-氧代酰胺的反应，可以很好地合成这类化合物。筛选所得化合物3a的体内抗惊厥，抗伤害感受和抗炎活性。结果表明，化合物3a可有效减少毛果芸香碱和戊四氮引起的癫痫发作。此外，化合物3a具有对抗急性疼痛的抗伤害和抗炎特性。该方案是生产具有药理活性的新杂环化合物的有效方法。

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