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. Author manuscript; available in PMC: 2012 Sep 1.
Published in final edited form as: Future Med Chem. 2011 Nov;3(15):1909–1934. doi: 10.4155/fmc.11.136

Table 6.

Synthetic compounds.

Scaffold (early leads) Selected lead compound(s) IC50 (μM)† EC50 (μM)‡ HWB In vivo activity Ref.
MK-886 (indole) 25
graphic file with name nihms338344t25.jpg 		0.007 0.49
8.0 		NI§ ND [76]
26
graphic file with name nihms338344t26.jpg 		0.003 0.27
5.8 		NI ND
Phenanthrene imidazoles 27
(MF63)
graphic file with name nihms338344t27.jpg 		0.001 0.42 1.3 Analgesic/antipyretic in guinea pigs and mPGES-1 KI mice (ED50= 100 mg/kg in guinea pig hyperalgesia model) [92,94]
28
graphic file with name nihms338344t28.jpg 		0.001 0.02 0.2 Analgesic in guinea pigs (ED50= 30 mg/kg) [95]
29
(MK-7285)
graphic file with name nihms338344t29.jpg 		0.0009 0.01 0.14 Analgesic in guinea pigs (ED50= 14 mg/kg) [95]
Biaryl imidazole 30
graphic file with name nihms338344t30.jpg 		0.001 0.013
0.160 		1.6 ND [97]
31 (pirinixic acid)
graphic file with name nihms338344t31.jpg 		32 (YS121)
graphic file with name nihms338344t32.jpg 		3.4 12 2 Anti-inflammatory in carrageenan-induced rat pleurisy model [99,101]
33
graphic file with name nihms338344t33.jpg 		1.3 6 ND ND [99]
34
graphic file with name nihms338344t34.jpg 		0.94 ND ND ND [100]
35
graphic file with name nihms338344t35.jpg 		1.2 ND ND ND [102]
36
graphic file with name nihms338344t36.jpg 		0.9 ND ND ND
Trisubstituted benzene 37
graphic file with name nihms338344t37.jpg 		1.1 ND ND ND [102]
2-mercaptohexanoic acids 38
graphic file with name nihms338344t38.jpg 		1.7 ND ND ND [103]
39
graphic file with name nihms338344t39.jpg 		2.2 ND ND ND
40
graphic file with name nihms338344t40.jpg 		2.2 ND ND ND [103]
Licofelone (arylpyrrolizines) 41
graphic file with name nihms338344t41.jpg 		2.1 ND ND ND [104]
Benzo[g]indol-3-carboxylates 42
graphic file with name nihms338344t42.jpg 		0.6 2 ND Anti-inflammatory in carrageenan- induced mouse paw edema and rat pleurisy models [106]
Oxicam 43
graphic file with name nihms338344t43.jpg 		45
graphic file with name nihms338344t44.jpg 		0.016 0.42 5 ND [107]
↓
44 (IC50 = 0.11 μM; EC50 = 0.46 μM)
graphic file with name nihms338344t45.jpg 		(PF-9184)
46 (trisubstituted ureas; 88% enzyme inhibition at 10 μM)
graphic file with name nihms338344t46.jpg 		47
graphic file with name nihms338344t47.jpg 		0.002 0.34 2.1 ND [110]
Carbazole benzamides 48 (AF3442)
graphic file with name nihms338344t48.jpg 		0.06 0.41 (LPS-stimulated monocytes) 29 ND [111]
†

IDetermined by cell-free assays measuring the conversion of prostaglandin E2 to prostaglandin E2 in vitro.

‡

Determined by cell-based assays measuring the production of prostaglandin E2 by cells.

§

NI: No significant inhibition up to 30 or 33 μM.

In the presence of 50% FBS.

AA: Arachidonic acid; HWB: Human whole-blood; LPS: Lipopolysaccharide; ND: Not determined.