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. Author manuscript; available in PMC: 2011 Nov 1.
Published in final edited form as: Eur J Med Chem. 2010 Sep 15;45(11):5406–5419. doi: 10.1016/j.ejmech.2010.09.001

Table 1.

Structure and receptor specificity of compounds under investigation

A. Compounds with 2-(benzimidazol-2-ylthio)-N-phenylacetamide scaffold [from [12]].
graphic file with name nihms237478u1.jpg
Compound R1 R2 Specificity
AG-09/1 4-NO2 5-OMe FPR1
AG-09/2 4-OEt 5-OMe FPR1
AG-09/11 H H N.A.
AG-09/13 4-OMe 5-OEt FPR1
AG-09/17 3,4-diOMe 5-OMe FPR1/FPR2
AG-09/18 H 5-OMe FPR1
AG-09/19 3-OMe 5-OMe FPR1
AG-09/20 4-Cl 5-OMe FPR1/FPR2
AG-09/21 4-Br 5-OMe FPR1
AG-09/22 2-OMe 5-OMe FPR1/FPR2
AG-09/25 3-Br H N.A.
AG-09/26 3-NO2, 4-Cl 4-Me N.A.
AG-09/28 4-NO2 H N.A.
AG-09/30 3-CF3 5-Me N.A.
B. Compounds with N-phenethyl-N′-phenylurea scaffold [from [12]].
graphic file with name nihms237478u2.jpg
Compound R1 R2 Specificity
AG-26 4-Cl OMe FPR2
AG-09/36 H H N.A.
AG-09/37 H OMe FPR2
AG-09/38 4-F OMe FPR2
AG-09/41 2,4-diCl OMe N.A.
AG-09/42 4-Br OMe FPR2
AG-09/45 4-F Me N.A.
AG-09/52 2-NO2 Cl N.A.
AG-09/54 3-Me Cl N.A.
C. Compounds with piperazine scaffold [from [12]].
graphic file with name nihms237478u3.jpg
Compound R1 R2 Specificity
AG-09/03 4-Br 4-F FPR2
AG-09/04 4-Br 3-Cl FPR2
AG-09/55 H H N.A.
AG-09/56 H 2-Cl N.A.
AG-09/64 3-Cl,4-F H N.A.
AG-09/71 2-Br H N.A.
AG-09/72 3-Br H N.A.
AG-09/73 4-Br H FPR2
AG-09/74 4-Br 4-Cl FPR2
AG-09/75 4-Br 3-Cl, 4-Me FPR2
AG-09/76 4-Br 2-Me, 3-Cl FPR2
AG-09/77 4-Br 2-Me, 5-Cl FPR2
AG-09/82 4-Br 3-OMe FPR2
AG-09/91 graphic file with name nihms237478t1.jpg N.A.
D. Compounds with acetohydrazide scaffold [from [12]].
graphic file with name nihms237478u4.jpg
Compound R1 R2 Specificity
AG-09/92 NO2 graphic file with name nihms237478t2.jpg FPR2
AG-09/93 NO2 graphic file with name nihms237478t3.jpg FPR2
AG-09/95 NO2 graphic file with name nihms237478t4.jpg N.A.
AG-09/96 NO2 graphic file with name nihms237478t5.jpg FPR2
AG-09/97 NO2 graphic file with name nihms237478t6.jpg N.A.
AG-09/99 OMe graphic file with name nihms237478t7.jpg N.A.
AG-09/101 graphic file with name nihms237478t8.jpg FPR2
AG-09/102 graphic file with name nihms237478t9.jpg N.A.
AG-09/7 graphic file with name nihms237478t10.jpg FPR2
E. Specific FPR2 agonists with 1-(2-indolylcarbonyl)-4-(1-benzimidazolyl)piperidine scaffolds [from [16]].
graphic file with name nihms237478u5.jpg
Compound R Specificity
F-5 Me FPR2
F-6 Et FPR2
F-7 iBu FPR2
F-8 CF3 FPR2
F-9 Ph FPR2
F. Specific FPR2 agonists with pyrazolone scaffold [from [9,31]].
graphic file with name nihms237478u6.jpg
Compound R1 R2 Specificity
B-25 Me 4-Br FPR2
B-35 Me 4-SMe FPR2
B-42 Et 4-Cl FPR2
B-43 iPro 4-Cl FPR1/FPR2
G. Specific FPR2 agonists with 1-(2-indolylcarbonyl)-3-(1-benzimidazolyl)pyrrolidine and related scaffolds [from [16]].
graphic file with name nihms237478u7.jpg
Compound R X Specificity
F-10 OMe CH FPR2
F-13 F CH FPR2
F-14 Cl CH FPR2
F-15 Br CH FPR2
F-16 OCF3 CH FPR2
F-17 Et CH FPR2
F-18 OMe N FPR2
H. Compounds with 4-benzylpyridazin-3-one scaffold [from [17]].
graphic file with name nihms237478u8.jpg
Compound R1 R2 Specificity
C-14a 3-OMe NH-C6H4-Br (p) FPR1/FPR2
C-14b 3-OMe NH-C6H4-Br (m) N.A.
C-14e 3-OMe NH-C6H4-I (p) FPR1/FPR2
C-14f 3-OMe NH-C6H4-F (p) FPR1
C-14h 3-OMe NH-C6H4-CH3 (p) FPR1/FPR2
C-14m 3-OMe graphic file with name nihms237478t11.jpg FPR1
C-14n 3-OMe NH-C6H4-CF3 (p) FPR1/FPR2
C-14r 3-OMe N(CH3)-C6H4-Br (p) N.A.
C-14x 4-OMe NH-C6H4-Br (p) FPR2
C-6c graphic file with name nihms237478t12.jpg N.A.
graphic file with name nihms237478u9.jpg
Compound X Specificity
C-17b CH(CH3)CONH FPR1
C-18a CH2 N.A.
C-23 (CH2)2NH N.A.
I. Structures of other FPR1/FPR2 agonists.
Compound Structure Specificity
AG-14 graphic file with name nihms237478t13.jpg FPR111
AG-22 graphic file with name nihms237478t14.jpg FPR1/FPR212
AG-09/5 graphic file with name nihms237478t15.jpg FPR212
AG-09/6 graphic file with name nihms237478t16.jpg FPR212
AG-09/8 graphic file with name nihms237478t17.jpg FPR212
AG-09/9 graphic file with name nihms237478t18.jpg FPR1/FPR212
AG-09/10 graphic file with name nihms237478t19.jpg FPR1/FPR212
Quin-C1 graphic file with name nihms237478t20.jpg FPR27
S-1 graphic file with name nihms237478t21.jpg FPR211
S-2 graphic file with name nihms237478t22.jpg FPR211
1910-5441 graphic file with name nihms237478t23.jpg FPR18 (activity for FPR2 is unknown)
fMLF graphic file with name nihms237478t24.jpg FPR1/FPR217
WKYMVm graphic file with name nihms237478t25.jpg FPR1/FPR217