New progress of COX-2 selective inhibitor anti-inflammatory and analgesic drug project

Arthritis is a common chronic disease, which is listed as the number one disability disease in the world According to the latest statistics, there are 355 million arthritis patients in the world China's incidence rate of arthritis was 120 million, with an incidence of about 13% as of 2015 The incidence rate of the disease increased gradually, and the incidence of young people increased gradually China spends more than 13.5 billion yuan on the total cost of arthritis treatment every year, and there is a huge market of anti-inflammatory drugs and painkillers Guangzhou Institute of biology has made important progress in the research and development of new COX-2 selective inhibitors, anti-inflammatory and analgesic drugs (source: Guangzhou Institute of biomedicine and health, Chinese Academy of Sciences) Selective COX-2 inhibitors are a group of new NSAID Compared with the traditional non selective NSAID, drugs like drugs like drugs like drugs like drugs like drugs like drugs like COX-2 cause fewer gastrointestinal complications Therefore, since its invention in the 1990s, they have been used more and more widely in clinical practice Dr Zhang Yanmei, senior R & D personnel of Guangzhou Institute of biomedicine and health, Chinese Academy of Sciences, and Dr John J Talley, a famous American pharmaceutical chemist, formed a project team to jointly develop the COX-2 selective inhibitor anti-inflammatory and analgesic drug project and made new progress The related research results were recently published in the Journal of pharmaceutical chemistry Chemistry) Compound sf-1001 is a new COX-2 selective inhibitor with independent intellectual property rights The results of biological activity test showed that the compound had better drug properties and the prospect of further research and development The IC50 value of sf-1001 is greater than 10 um for COX-1 and 0.018 um for COX-2 The IC50 value of celecoxib to COX-1 is more than 10um, and the IC50 value of celecoxib to COX-2 is 0.050um It can be seen that the compound is an effective selective inhibitor of COX-2 Compound sf-1001 has good bioavailability, and its bioavailability and half-life (T1 / 2 = 12.5h) are better than celecoxib In addition, the dispersion volume of sf-1001 is 0.34, which is much better than that of celecoxib (1.944) Compared with the similar drugs celecoxib, rofecoxib and valdecoxib, compound sf-1001 is locally distributed in the pathogenic tissues in vivo, so it can significantly reduce the cardiotoxicity and nephrotoxicity caused by the Xibu drugs This is the characteristic of selective benzopyran COX-2 inhibitors Therefore, sf-1001 can be developed into an effective and low toxic anti-inflammatory and analgesic drug In addition, the compound was characterized on three different animal models, which has a strong anti-inflammatory and analgesic activity, and the effect is better than the first-line clinical drug celecoxib The preparation of compound sf-1001 is relatively simple, and researchers have also developed the synthesis method of s-configuration compound, which is economical and efficient Paper link: https://