Benzo[d]isothiazole 1,1-dioxide derivatives as dual functional inhibitors of 5-lipoxygenase and microsomal prostaglandin E2 synthase-1 |
| |
| Institution: | 1. BNLMS, State Key Laboratory for Structural Chemistry of Unstable and Stable Species, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China;2. Center for Quantitative Biology, Peking University, Beijing 100871, China;3. Peking-Tsinghua Center for Life Sciences, Peking University, Beijing 100871, China;1. Department of Cardiology, Beijing Anzhen Hospital, Capital Medical University, Beijing, China;1. Centre of Excellence for Pharmaceutical Sciences, North-West University, Private Bag X6001, Potchefstroom 2520, South Africa;2. Pharmaceutical Chemistry, School of Pharmacy, North-West University, Private Bag X6001, Potchefstroom 2520, South Africa;1. CNR-IBF, Consiglio Nazionale delle Ricerche – Istituto di Biofisica, Via Celoria, 26, I-20133 Milan, Italy;2. Fondazione IRCCS Istituto Nazionale dei Tumori, Via Amadeo, 42, I-20133, Milano, Italy;3. Dipartimento di Chimica, Università di Milano, Via Venezian, 21, I-20133 Milano, Italy;1. Department of Orthopedics, Heilongjiang Province Hospital, Harbin 150036, Heilongjiang Province, China;2. Department of Orthopedics, Harbin Medical University Cancer Hospital, Harbin 150081, Heilongjiang Province, China;3. Department of Orthopedics, Traditional Chinese Medicine Hospital of Harbin, Harbin 150000, Heilongjiang Province, China;4. Department of Orthopedics, Affiliated Hospital of Putian University, Putian 351100, Fujian Province, China |
| |
| Abstract: | A series of 6-nitro-3-(m-tolylamino) benzod]isothiazole 1,1-dioxide analogues were synthesized and evaluated for their inhibition activity against 5-lipoxygenase (5-LOX) and microsomal prostaglandin E2 synthase (mPGES-1). These compounds can inhibit both enzymes with IC50 values ranging from 0.15 to 23.6 μM. One of the most potential compounds, 3g, inhibits 5-LOX and mPGES-1 with IC50 values of 0.6 μM, 2.1 μM, respectively. |
| |
| Keywords: | 5-Lipoxygenase Dual functional inhibitor |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
