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. 2010 Feb;77(2):159–170. doi: 10.1124/mol.109.060673

TABLE 2.

Structure and activity of benzimidazole derivatives

Median effective concentration values (EC50) were determined by nonlinear regression analysis of the dose-response curves (5–6 points) generated using GraphPad Prism 5 with 95% confidential interval (P < 0.05). Efficacy (in parentheses) is expressed as a percentage of the response induced by 5 nM fMLF (FPR1) or 5 nM WKYMVm (FPR2).

graphic file with name zmo002106053g001.jpg

No. R1 R2 R3 R4 R5 R6 Ca2+ Mobilization EC50 and Efficacy
FPR1
 FPR2
 PMN
RBL-2H3 HL-60 RBL-2H3 HL-60
μM (%)
AG-09/1 H H NO2 H H O-CH3 2.4 (140) 3.4 (120) N.A. N.A. 0.4 (130)
AG-09/2 H H O-C2H5 H H O-CH3 15.8 (110) 21.5 (120) N.A. N.A. 5.8 (105)
AG-09/11 H H H H H H N.A. N.A. N.A. N.A. N.A.
AG-09/12 H H O-CH3 H H H N.A. N.A. N.A. N.A. N.A.
AG-09/13 H H O-CH3 H H O-C2H5 1.6 (80) 19.1 (40) N.A. N.A. 0.6 (100)
AG-09/14 H H O-(CH2)3CH3 H H O-CH3 N.A. N.A. N.A. N.A. 1.2 (40)
AG-09/15 H H O-(CH2)3CH3 H H O-C2H5 N.A. N.A. N.A. N.A. NA
AG-09/16 H H O-CH3 H H O-CH3 7.0 (95) 1.7 (65) 17.0 (40) 5.1 (25) 0.3 (165)
AG-09/17 H O-CH3 O-CH3 H H O-CH3 3.1 (60) 3.7 (55) 9.4 (25) 4.7 (50) 2.6 (150)
AG-09/18 H H H H H O-CH3 30.7 (65) 5.0 (80) N.A. N.A. 3.5 (135)
AG-09/19 H O-CH3 H H H O-CH3 3.2 (90) 1.5 (40) N.A. N.A. 0.5 (160)
AG-09/20 H H Cl H H O-CH3 1.7 (130) 1.6 (90) 5.0 (75) 6.0 (85) 0.7 (90)
AG-09/21 H H Br H H O-CH3 8.1 (120) 3.3 (100) N.A. N.A. 1.8 (140)
AG-09/22 Cl H H H H O-CH3 13.3 (65) 4.5 (110) 17.5 (40) 10.0 (70) 0.7 (115)
AG-09/23 H NO2 H H H O-CH3 8.0 (50) 3.5 (95) 14.9 (40) 10.8 (45) 0.2 (95)
AG-09/24 O-CH3 H H H H O-CH3 8.1 (40) 3.8 (80) 21.0 (35) 13.5 (55) 0.8 (95)
AG-09/25 H Br H H H H N.A. N.A. N.A. N.A. N.A.
AG-09/26 H NO2 Cl H CH3 H N.A. N.A. N.A. N.A. N.A.
AG-09/27 H NO2 H CH3 H H N.A. N.A. N.A. N.A. N.A.
AG-09/28 H H NO2 H H H N.A. N.A. N.A. N.A. N.A.
AG-09/29 CH3 CH3 H H H O-CH3 N.A. N.A. N.A. N.A. N.A.
AG-09/30 H CF3 H H H CH3 N.A. N.A. N.A. N.A. N.A.
AG-09/31 H Cl Cl H H O-CH3 N.A. N.A. N.A. N.A. N.A.
AG-09/32 H H graphic file with name zmo002106053g005.jpg H H O-CH3 N.A. N.A. N.A. N.A. N.A.
AG-09/33 H H O-CF3 H H H N.A. N.A. N.A. N.A. N.A.
AG-09/34 H Cl graphic file with name zmo002106053g006.jpg H H H N.A. N.A. N.A. N.A. N.A.
AG-09/35 H CO-O-CH(CH3)2 H CH3 H H N.A. N.A. N.A. N.A. N.A.

N.A., very low response (efficacy <20% of positive control) or no activity (no Ca2+ flux response was observed during the 3 min after addition of compounds under investigation).