AHMU Scholars Publish a Paper in the Internationally Renowned Journal J. Med. Chem.


Recently, Professor Shi Jingbo and Professor Liu Xinhuafrom Anhui Medical University, served as the first author and correspondent author respectively, with Anhui Medical University as author’s affiliation, published the paper Novel Pyrazolo [4,3-d] pyrimidine as Potent and Orally Active Inducible Nitric Oxide Synthase (iNOS) Dimerization Inhibitor with Efficacy in Rheumatoid Arthritis Mouse Model” online in the Journal of Medicinal Chemistry (DOI: 10.1021/acs.jmedchem. 9b00039).
In this study, the researchers carried out a systematic structural optimization and design byusingpyrazolo[4,3-d] pyrimidine compounds as the scaffolding structure with activity screening, and found the highly active iNOS dimerization inhibitor D27. In vitro findings showed that compound D27 could effectively inhibit the activity of iNOS (IC50=1.12μM). Preliminary mechanism studies indicated that compound D27 could affect the enzyme activity of iNOS protein by interfering with the formation of dimericiNOS, and inhibit the secretion of NO inflammatory factor.The anti-inflammatory effect of compound D27 showed good activity in adjuvant arthritis in rat models, suggesting that this compound may be an effective candidate compound for the treatment of inflammatory diseases by inhibiting iNOS dimerization, which provided a new idea for studying potential targets of anti-inflammatory drugs.
The Journal of Medicinal Chemistry affiliated with the American Chemical Society is a top journal in the field of pharmaceutical chemistry. This paper is the first research result published by the provincial university as the only author’s affiliation in the journal. It is also the new progress in the design and synthesis study of anti-tumor and anti-inflammatory lead compounds, which has been committed by the pharmaceutical chemistry team of the School of Pharmacy of Anhui Medical University for many years.