Table 1.
A. Compounds with 2-(benzimidazol-2-ylthio)-N-phenylacetamide scaffold [from [12]]. | |||
---|---|---|---|
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]]. | |||
---|---|---|---|
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]]. | |||
---|---|---|---|
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 | N.A. |
D. Compounds with acetohydrazide scaffold [from [12]]. | |||
---|---|---|---|
Compound | R1 | R2 | Specificity |
AG-09/92 | NO2 | FPR2 | |
AG-09/93 | NO2 | FPR2 | |
AG-09/95 | NO2 | N.A. | |
AG-09/96 | NO2 | FPR2 | |
AG-09/97 | NO2 | N.A. | |
AG-09/99 | OMe | N.A. | |
AG-09/101 | FPR2 | ||
AG-09/102 | N.A. | ||
AG-09/7 | FPR2 |
E. Specific FPR2 agonists with 1-(2-indolylcarbonyl)-4-(1-benzimidazolyl)piperidine scaffolds [from [16]]. | ||
---|---|---|
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]]. | |||
---|---|---|---|
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]]. | |||
---|---|---|---|
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]]. | |||
---|---|---|---|
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 | 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 | N.A. |
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 | FPR111 | |
AG-22 | FPR1/FPR212 | |
AG-09/5 | FPR212 | |
AG-09/6 | FPR212 | |
AG-09/8 | FPR212 | |
AG-09/9 | FPR1/FPR212 | |
AG-09/10 | FPR1/FPR212 | |
Quin-C1 | FPR27 | |
S-1 | FPR211 | |
S-2 | FPR211 | |
1910-5441 | FPR18 (activity for FPR2 is unknown) | |
fMLF | FPR1/FPR217 | |
WKYMVm | FPR1/FPR217 |