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Evaluation of Anti‐inflammatory and Analgesic Effects of Synthesized Derivatives of Ibuprofen
Author(s) -
Wang Jingjie,
Dai Dongyan,
Qiu Qianqian,
Deng Xin,
Lin Haiyan,
Qian Hai,
Huang Wenlong
Publication year - 2015
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12316
Subject(s) - ibuprofen , analgesic , pharmacology , trpv1 , transient receptor potential channel , cyclooxygenase , capsaicin , nociception , chemistry , receptor , anti inflammatory , medicine , biochemistry , enzyme
Inflammatory and pain are major areas for drug discovery. Current analgesic drugs often cause a number of side‐effects. In the present study, we modified carboxylic acid group of ibuprofen, one of non‐steroidal anti‐inflammatory drugs, based on the common structure of transient receptor potential vanilloid type 1 antagonists which are considered as new candidates for analgesic drugs, and synthesized several derivatives of ibuprofen. Comprehensive evaluations of the pharmacological properties of these compounds were investigated. Compound 17 showed weak cyclooxygenase inhibition and exhibited strong transient receptor potential vanilloid type 1 antagonistic activity. It was found to be capable of blocking noxious thermal nociception and capsaicin‐induced nociception in mice. Besides, 17 showed less ulcerogenic action than ibuprofen did and had no hyperthermia side‐effect compared with common transient receptor potential vanilloid type 1 antagonists. Therefore, it suggested that 17 could be used as a safe alternative analgesic candidate for pain treatment.