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Lead identification of 2-iminobenzimidazole antagonists of the chemokine receptor CXCR3 |
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| Authors: | 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 |
| Affiliation: | Abbott Bioresearch Center, Medicinal Chemistry, 381 Plantation Street, Worcester, MA 01605, USA. martin.hayes@abbott.com |
| 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. |
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