Hayes Martin E, Breinlinger Eric C, Wallace Grier A, Grongsaard Pintipa, Miao Wenyan, McPherson Michael J, Stoffel Robert H, Green David W, Roth Gregory P
Abbott Bioresearch Center, Medicinal Chemistry, 381 Plantation Street, Worcester, MA 01605, USA.
Bioorg Med Chem Lett. 2008 Apr 1;18(7):2414-9. doi: 10.1016/j.bmcl.2008.02.049. Epub 2008 Feb 26.
Modification of a 2-iminobenzimidazole series derived from an HTS hit resulted in compounds with improved in-vitro species selectivity. Incorporation of an 8-quinoline amide and conformational rigidification of an aliphatic tether furnished potent compounds suitable for further lead optimization.
对源自高通量筛选命中化合物的2-亚氨基苯并咪唑系列进行修饰，得到了体外物种选择性提高的化合物。引入8-喹啉酰胺并使脂肪族连接链构象刚性化，得到了适合进一步先导优化的强效化合物。
