趋化因子受体CXCR3的2-亚氨基苯并咪唑拮抗剂的先导化合物鉴定
Lead identification of 2-iminobenzimidazole antagonists of the chemokine receptor CXCR3.
作者信息
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
机构信息
Abbott Bioresearch Center, Medicinal Chemistry, 381 Plantation Street, Worcester, MA 01605, USA.
出版信息
Bioorg Med Chem Lett. 2008 Apr 1;18(7):2414-9. doi: 10.1016/j.bmcl.2008.02.049. Epub 2008 Feb 26.
PMID:18337097
Abstract
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.
摘要
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。
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