苯并[d]异噻唑-1,1-二氧化物衍生物作为5-脂氧合酶和微粒体前列腺素E(2)合酶-1的双重功能抑制剂
Benzo[d]isothiazole 1,1-dioxide derivatives as dual functional inhibitors of 5-lipoxygenase and microsomal prostaglandin E(2) synthase-1.
作者信息
Shang Erchang, Wu Yiran, Liu Pei, Liu Ying, Zhu Wei, Deng Xiaobing, He Chong, He Shan, Li Cong, Lai Luhua
机构信息
BNLMS, State Key Laboratory for Structural Chemistry of Unstable and Stable Species, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China.
BNLMS, State Key Laboratory for Structural Chemistry of Unstable and Stable Species, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China; Center for Quantitative Biology, Peking University, Beijing 100871, China.
出版信息
Bioorg Med Chem Lett. 2014 Jun 15;24(12):2764-7. doi: 10.1016/j.bmcl.2014.04.006. Epub 2014 Apr 13.
A series of 6-nitro-3-(m-tolylamino) benzo[d]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 23.6μM. One of the most potential compounds, 3g, inhibits 5-LOX and mPGES-1 with IC50 values of 0.6μM, 2.1μM, respectively.
合成了一系列6-硝基-3-(间甲苯基氨基)苯并[d]异噻唑1,1-二氧化物类似物，并评估了它们对5-脂氧合酶(5-LOX)和微粒体前列腺素E2合酶(mPGES-1)的抑制活性。这些化合物能够抑制这两种酶，IC50值范围为0.15至23.6μM。其中最具潜力的化合物之一3g，对5-LOX和mPGES-1的IC50值分别为0.6μM、2.1μM。
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