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Synthesis and Preliminary Biological Evaluation of Capsaicin Derivatives as Potential Analgesic Drugs

[ Vol. 6 , Issue. 4 ]


Hai Qian, Zhixian Fu, Wenlong Huang, Huibin Zhang, Jinpei Zhou, Liang Ge, Rui Lin, Haiyan Lin and Xiaowen Hu   Pages 205 - 210 ( 6 )


A series of capsaicin derivatives were designed and synthesized, including 10 compounds which are the combination of capsaicin and dihydro capsaicin with ibuprofen through bridge chain. Preliminary biological tests suggested that some compounds had both anti-inflammatory activity and analgesic activity. And their pungency was lower. Based on these results, some of these molecules can be considered as lead candidates for the further development of analgesic drugs.


Analgesic drugs, capsaicin derivatives, TRPV1 agonist, dihydro capsaicin, ibuprofen, transient receptor poten-tial vanilloid subtype 1, diabetic neuropathy, 2-(4-isobutylphenyl)propanoyl chloride 2, SOCl2, wiping test, NMR, CDCl3, MHz spectrometer, HP1100 analyzer, Model of Xylene-Inducing Mouse Auricle Swelling, Model of Mouse Acetic Acid Writhing Test, CH2Cl2, ethyl acetate, Na2SO4, silica gel column, Human embryonic kidney, (HEK)-293, glutamine, fluorescent probe for Ca2+, 96-well plates, Fura-2/AM, Krebs, –, Ringer, Hepes (KRH) buffer, CMC-Na aqueous solution, p-xylene


School of Pharmacy, China Pharmaceutical University, Nanjing 210009, People's Republic of China.

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