Recently, the pharmaceutical chemistry research team led by Professor Liu Xinhua of the School of Pharmacy of AHMU has successfully designed and synthesized a novel and high-efficiency NLRP3 inflammasome inhibitor, which shows significant therapeutic effects in the animal model with inflammatory bowel diseases.
The inflammatory bowel diseases include Crohn’s disease and ulcerative colitis. According to statistics, there are 7 million patients with inflammatorybowel diseases in the world, and the incidence is still rising, but there is no specific cure for the diseases. In order to develop new drugs for the treatment of inflammatory bowel diseases, an inhibitor screening model targeting NLRP3 inflammosomehas been established. With the help of compound libraries in Anhui Province, the active scaffold has been screened out. Then, the target- and mechanism-based drug design was applied to optimize the synthesis of high efficiency NLRP3 inhibitor compound 47. The compound has significant anti-inflammatory activity and druggability, shows a significant therapeutic effect on the mouse inflammatory bowel disease model, and has potential and value for further development. This study provides a new approach for the design of new drugs for inflammatory bowel disease targeting NLRP3 inflammasome.
For the above research results, Chinese invention patent protection has been applied for, and an academic paper was published in Journal of Medicinal Chemistry, a top journal in the field of medicinal chemistry, with Chen Liuzeng and Zhang Xingxing as the co-first authors. Professor Liu Xinhua and Researcher Dr. RuanBanfeng of Hefei University are the co-corresponding authors, our school being the first author unit.
Paper link：https://pubs.acs.org/doi/10.1021/acs.jmedchem.1c01007