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. Author manuscript; available in PMC: 2012 May 15.
Published in final edited form as: Bioorg Med Chem Lett. 2011 Mar 21;21(10):2980–2985. doi: 10.1016/j.bmcl.2011.03.048

Table 1.

Activity of quinoline urea analogues against OX1R and OX2R.

graphic file with name nihms283908t1.jpg
No. R1 R2 R3 R4 X Ke (nM)
OX1a OX2b
1 45±12 1194
5 682.6±231 >10,000
9 H H NO2 N >10,000 nt
10 H Me NO2 CH >10,000 nt
11 Cl Me NO2 CH >10,000 nt
12 Me Me NO2 CH >10,000 nt
13 OMe Me NO2 CH >10,000 nt
14 H Me H H CH >10,000 >10,000
15 H Me Me Me CH 356.7±89 >10,000
16 Me Me Me Me CH 2561±266 >10,000
17 OMe Me Me Me CH 3945±2517 >10,000
18 H Me H Hexanoyl CH >10,000 >10,000
19 H Me H 3-Ph-propyl CH 3278±639 >10,000
20 H Me Me 3-Ph-propyl CH >10,000 >10,000
21 H Me H Hexyl CH >10,000 >10,000
22 H Me Me Hexyl CH 398±16 >10,000
23 H H Me Me N 46.3±8 >10,000
a

values are the mean of at least three independent experiments in duplicate.

b

values are the mean of at least two independent experiments in duplicate.

nt = not tested.