. Author manuscript; available in PMC: 2011 May 13.

Published in final edited form as: J Med Chem. 2010 May 13;53(9):3602–3610. doi: 10.1021/jm901872v

Table 1.

Inhibition of PLA₂ by fluoroketones.^a

No	Structure	GVIA iPLA₂		GIVA cPLA₂		GV sPLA₂
No	Structure	% Inhibition	X_I(50)	% Inhibition	X_I(50)	% Inhibition
2		99.4 ± 0.1	0.0014 ± 0.0001	N.D.		28 ± 1
6a		99.4 ± 0.0	0.0022 ± 0.0001	32.6 ± 4.0		61.8 ± 6.7
6b		98.4 ± 0.3	0.0030 ± 0.0002	N.D.		N. D.
19		94.3 ± 1.5	0.0390 ± 0.0024	44.8 ± 3.7		67.3 ± 7.7
20		97.0 ± 1.3	0.0258 ± 0.0016	82.0 ± 1.2		65.8 ± 1.8
10		96.0 ± 0.8	0.0313 ± 0.0025	59.0 ± 3.6		N. D.
12a		99.1 ± 0.5	0.0036 ± 0.0001	N. D.		N. D.
12b		84.4 ± 2.1	0.0262 ± 0.0006	N. D.		41.9 ± 4.4
21		95.5 ± 0.4	0.0192 ± 0.0007	41.4 ± 3.4		67.0 ± 6.4
22		80.6 ± 2.5	0.0574 ± 0.0030	57.0 ± 1.9		33.9 ± 18.4
23		96.4 ± 0.6	0.0066 ± 0.0005	N. D.		76.9 ± 5.3
12c		98.3 ± 0.2	0.0084 ± 0.0006	76.1 ± 1.8		71.7 ± 3.6
12d		95.8 ± 1.3	0.0136 ± 0.0006	43.7 ± 3.2		76.9 ± 2.2
12e		99.4 ± 0.1	0.0029 ± 0.0001	91.5 ± 0.9	0.022 ± 0.001	61.4 ± 5.3
12f		99.4 ± 0.1	0.0024 ± 0.0001	88.8 ± 0.7		63.0 ± 6.2
12g		99.9 ± 0.1	0.0002 ± 0.0000	80.8 ± 1.5		36.8 ± 7.9
12h		99.8 ± 0.0	0.0006 ± 0.0000	77.1 ± 1.8		58.4 ± 5.7
12i		99.7 ± 0.2	0.0010 ± 0.0001	55.8 ± 2.1		46.3 ± 10.0
18a		97.6 ± 0.2	0.0025 ± 0.0001	52.1 ± 2.2		N. D.
18b		98.8 ± 0.2	0.0013 ± 0.0000	66.0 ± 3.7		N. D.
24		100 ± 0.1	0.0005 ± 0.0000	68.4 ± 1.5		39.1 ± 12.6
25		100.0 ± 0.1	0.0005 ± 0.0000	79.9 ± 1.0		36.1 ± 8.2

Average percent inhibition and standard error (n=3) reported for each compound at 0.091 mole fraction. X_I(50) values determined for inhibitors with greater than 90% inhibition. N.D. signifies compounds with less than 25% inhibition (or no detectable inhibition).