Table 2.
Structure and activity of 2-(5-alkoxybenzimidazol-2-ylthio)-N-phenylacetamide derivatives in human neutrophils and FPR1/FPR2-transfected HL-60 cells
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---|---|---|---|---|---|---|
Compound | R1 | R2 | R3 | Ca2+ mobilization EC50 (μM) and efficacy (%)a | ||
FPR1 | FPR2 | Neutrophils | ||||
AG-11/22 |
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H | OCH2CH3 | 6.9 (50) | 14.3 (35) | 3.9 (60) |
AG-11/23 |
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H | OCH3 | 2.2 (70) | N.A. | 2.6 (80) |
AG-11/24 |
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H | OCH2CH3 | 14.2 (65) | 3.7 (40) | 5.6 (75) |
AG-11/25 |
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H | OCH3 | 2.1 (110) | 10.4 (70) | 1.5 (105) |
AG-11/26 |
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CH3 | OCH3 | 7.5 (90) | 11.0 (45) | 17.8 (75) |
See legend for Table 1