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2, 6- disubstituted cyclohexane (alcohol) of analgesic activity design, synthesis and anti-inflammatory

Author: YuWeiShe
Tutor: ZhaoLinXiang
School: Shenyang Pharmaceutical University
Course: Medicinal Chemistry
Keywords: synthesis 2-(E)-substituted benzylidene-6-(N-substituted aminomethyl) cyclohexanones 2-(E)-substituted benzylidene -6-(N-substituted aminomethyl)-1- aryl-cyclohexanols anti-inflammation analgesia
CLC: R91
Type: Master's thesis
Year: 2007
Downloads: 35
Quote: 0
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Abstract


In order to study mechanism and SAR of 2-(E)-substituted benzylidene cyclohexanone Mannich bases and 2-(E)-substituted benzylidene-6-(N-substituted aminomethyl)-1-aryl-cyclohexanols, aminomethyl group were modified with substituted phenylamine. Ten 2-(E)-substituted benzylidene-6-(N-substituted aminomethyl)cyclohexanones(A-1～A-10)and tweleve 2-(E)-substituted benzylidene -6-(N-substituted aminomethyl)-1-aryl- cyclohexanols(G-1～G-12)were designed and synthesized, which structure have been characterized by the application of ~1H-NMR snd MS spectra.The anti-inflammatory activity of target compounds were evaluated with the model of xylene-induced ear edema in mice. The results showed that G-1 has the best activity of anti-inflammatory with inhibition of 66.67％. Compare with ibuprofen as positive compounds, A-1, A-2, A-4, A-8 and G-4 have significant activities with inhibition of 41.50％～56.35％.The analgesic activity of target compounds were evaluated with the model of acetic acid inducing mice’s writhing. The results showed that, comparing with ibuprofen as positive compounds, A-1, A-3, A-8, A-9, A-10, G-3, G-5, G-8, G-9 have significant activities with inhibition of 80.89％-84.53％.The primary SAR was showed as follows: from target compounds of 2-(E)-substituted benzylidene-6-(N-substituted aminomethyl)cyclohexanones(A-1～A-10) to 2-(E)-substituted benzylidene -6-(N-substituted aminomethyl)-1-aryl- cyclohexanols(G-1～G-12), the analgesic activity has not been enhanced, and the anti-inflammatory activity has been weakened.

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