Characterization of new PPARγ agonists: Benzimidazole derivatives—importance of positions 5 and 6, and computational studies on the binding mode

M Goebel, G Wolber, P Markt, B Staels, T Unger…

文献索引：Goebel, Matthias; Wolber, Gerhard; Markt, Patrick; Staels, Bart; Unger, Thomas; Kintscher, Ulrich; Gust, Ronald Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 16 p. 5885 - 5895

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被引用次数: 21

摘要

In this and previous studies we investigated the importance of partial structures of Telmisartan on PPARγ activation. The biphenyl-4-ylmethyl moiety at N1 and residues at C2 of the central benzimidazole were identified to be essential for receptor activation and potency of receptor binding. Now we focused our attention on positions 5 and 6 of the central benzimidazole and introduced bromine (3b–5/6, 3c), phenylcarbonyl (3d–5/6), ...