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.
MeSH terms
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Amides / chemistry
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Amides / pharmacology*
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Animals
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Benzimidazoles / chemical synthesis
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Benzimidazoles / pharmacology*
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Binding Sites
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CHO Cells / drug effects
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Cricetinae
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Cricetulus
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Humans
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Models, Chemical
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Quinolines / chemistry
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Quinolines / pharmacology*
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Radioligand Assay
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Receptors, CXCR3 / antagonists & inhibitors*
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Receptors, CXCR3 / metabolism
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Structure-Activity Relationship
Substances
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Amides
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Benzimidazoles
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Quinolines
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Receptors, CXCR3