Skip to main content
. Author manuscript; available in PMC: 2011 Nov 11.
Published in final edited form as: J Med Chem. 2010 Nov 11;53(21):7804–7824. doi: 10.1021/jm100947x

Table 2.

Inhibition of NOS isozymes by synthetic compounds 8–34.

Compounds Ki (μM)a
Selectivityb
nNOS eNOS iNOS n/e n/i
L-NNAc 0.57 0.75 4.55 1.3 8
(±)-8 47.94 121.62 609.43 2.5 13
(±)-9 3.98 172.91 437.76 43 110
(±)-10 304.96 849.21 2,522.8 3 8
(±)-11 13.47 1,696 651.85 126 48
(±)-12 6.94 340.83 25.24 49 4
(±)-13 15.68 241.7 308.1 15 20
(±)-14 14.45 2,906 166.1 201 11.5
(±)-15 13.86 1,453 298.55 105 21.5
(±)-16 20.57 1,453 416.61 71 20
(±)-17 12.85 625.42 234.06 49 18
(±)-18 20.93 460.16 253.43 22 12
(±)-19 17.92 108.69 209.01 6 12
(±)-20 24.4 170.52 285.54 7 12
(±)-21 0.61 262.74 32.03 431 52.5
(±)-22 0.53 118.34 44.85 223 85
(±)-23 0.25 95.18 44.11 380 176
(±)-24 0.74 61.19 40.42 83 55
(±)-25 0.87 78.75 27.35 90.5 31
(±)-26 0.74 108.55 58.72 147 79
(±)-27 0.66 201.61 83.9 305.5 127
(±)-28 0.414 63.22 23.76 153 57
(±)-29 0.483 76.13 44.23 158 92
(±)-30 0.589 16.47 20.46 28 35
(±)-31 1.891 58.14 75.36 31 40
(±)-32 0.088 123.90 18.17 1408 206.5
(±)-33 0.119 44.09 22.59 370.5 190
(±)-34 0.048 49.07 26.59 1022 554
a

The apparent Ki values are represented as the mean of two or more independent experiments preformed in duplicate with five or six data points each and correlation coefficients of 0.88–0.99. The experimental standard deviations were less than 10%.

b

n/e and n/i are the selectivity ratio of Ki (eNOS or iNOS) to Ki (nNOS).

c

L-NNA: L-Nω-nitroarginine, a positive control.