咪唑并[1,2-[公式：见正文]]哒嗪类化合物的合成及作为 TNF-[公式：见正文]产生抑制剂的生物评价。
Synthesis and biological evaluation of imidazo[1,2-[Formula: see text]]pyridazines as inhibitors of TNF-[Formula: see text] production.
机构信息
Department of Chemistry, Post Graduate and Research Centre, Padmashri Vikhe Patil College of Arts, Science and Commerce, Pravaranagar, A/P Loni, Tal. Rahata, Dist., Ahmednagar, 413713, India.
Department of Medicinal Chemistry, Piramal Enterprises Limited 1, Nirlon Complex, Off Western Exp. Highway, Near NSE Complex, Goregaon East, Mumbai, Maharashtra, 400 063, India.
出版信息
Mol Divers. 2018 Aug;22(3):545-560. doi: 10.1007/s11030-017-9798-8. Epub 2017 Dec 2.
Tumor necrosis factor-alpha (TNF-[Formula: see text] is an important pro-inflammatory cytokine responsible for a diverse range of inflammatory diseases including rheumatoid arthritis. In the present manuscript, our medicinal chemistry efforts on the design, synthesis and TNF-[Formula: see text] evaluation of a series of 3, 6-disubstituted imidazo[1,2-b]pyridazine is described. The best compounds were 3-pyridyl and (4-(methylsulfonyl)phenyl) analogs 8q and 8w, showing inhibition of TNF-[Formula: see text] production with IC[Formula: see text]values of 0.9 and 0.4 [Formula: see text]M, respectively. The identified leads have potential for further development for treatment of inflammatory diseases.
肿瘤坏死因子-α（TNF-[Formula: see text]）是一种重要的促炎细胞因子，可引发多种炎症性疾病，包括类风湿关节炎。在本手稿中，我们描述了一系列 3,6-二取代的咪唑并[1,2-b]哒嗪的设计、合成和 TNF-[Formula: see text]评估的药物化学研究。最佳化合物为 3-吡啶基和（4-（甲磺酰基）苯基）类似物 8q 和 8w，其对 TNF-[Formula: see text]产生的抑制作用的 IC[Formula: see text]值分别为 0.9 和 0.4 [Formula: see text]M。鉴定出的先导化合物具有进一步开发用于治疗炎症性疾病的潜力。
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