通过骨架跃迁发现 ADAMTS-5（聚集蛋白聚糖酶-2）抑制剂的苯并咪唑系列。
Discovery of a benzimidazole series of ADAMTS-5 (aggrecanase-2) inhibitors by scaffold hopping.
机构信息
Pharmaceutical Research Center, Asahi Kasei Pharma Corporation, 632-1 Mifuku, Izunokuni-shi, Shizuoka 410-2321, Japan.
Pharmaceutical Research Center, Asahi Kasei Pharma Corporation, 632-1 Mifuku, Izunokuni-shi, Shizuoka 410-2321, Japan.
出版信息
Eur J Med Chem. 2014 Jan;71:250-8. doi: 10.1016/j.ejmech.2013.10.075. Epub 2013 Nov 15.
We describe a medicinal chemistry approach to generate a series of benzimidazoles bearing thiazolidin-4-one using scaffold hopping from thiazole 1, our previously described thiazole. Our goal was to discover a potent and permeable small-molecule ADAMTS-5 inhibitor. The results suggest that small compound 22 shows promise as a potent small-molecule ADAMTS-5 inhibitor with good permeability.
我们描述了一种从噻唑 1（我们之前描述的噻唑）进行支架跳跃生成一系列含有噻唑烷-4-酮的苯并咪唑的药物化学方法。我们的目标是发现一种有效的、可渗透的小分子 ADAMTS-5 抑制剂。结果表明，小分子化合物 22 具有成为一种有效的、可渗透的小分子 ADAMTS-5 抑制剂的潜力。
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