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. Author manuscript; available in PMC: 2016 Jun 5.
Published in final edited form as: Medchemcomm. 2015 Jun 5;6:1278–1284. doi: 10.1039/C5MD00198F

Table 1.

Inhibition of UT-A1 and UT-B urea transport by 2,7-disubstituted fluorenoneanalogs.

Structure Functional group UT- A1 IC50 (μM) UT-B IC50 (μM)
graphic file with name nihms697800t1.jpg 1 >50 >50
graphic file with name nihms697800t2.jpg R
2 H >50 >50
3 COCH3 1 1.5
4 COCH2CH3 15 5
5 COCH(CH3) 2 18 50
6 CO(CH2) 2CH3 >50 >50
7 COCF3 10 7.5
8 CONH2 2 1.2
9 SO2CH3 1.5 2.5
10 SO2(CH2)3 >50 >50
11 COCH2Br 30 10
12 COCH2OH 20 25
13 COCH2O(CH2)2OMe >50 50
14 COCH2N3 20 30
15 COCH2OBn >50 >50
16 CO(CH) 2CO2H 30 >50
graphic file with name nihms697800t3.jpg X
17 CNHOH 12 25
18 CHOH >50 20
20 SO2 15 2
graphic file with name nihms697800t4.jpg R
21 H >50 >50
22 COCH3 18 20
23 COCH2OBn >50 >50
24 SO2CH3 >50 30