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. Author manuscript; available in PMC: 2013 Dec 13.
Published in final edited form as: J Med Chem. 2007 Aug 16;50(18):10.1021/jm070284z. doi: 10.1021/jm070284z

Table 1.

Inhibitory Activities of Hydroxyethylene Isostere-Based Compounds against Wild-Type HIV-1 Protease

graphic file with name nihms162795u1.jpg
Compd R1 R2 Ki (nM)
12a graphic file with name nihms162795t1.jpg H (5R) 131.4
13a graphic file with name nihms162795t1.jpg H (5S) 0.85
13c graphic file with name nihms162795t1.jpg 3,4-di-F (5S) 2.13
13d graphic file with name nihms162795t1.jpg 3-CF3 (5S) 2.62
13e graphic file with name nihms162795t1.jpg 3-Ac (5S) 0.98
14a graphic file with name nihms162795t2.jpg H (5S) 2.04
15a graphic file with name nihms162795t3.jpg H (5S) 3.51
16a graphic file with name nihms162795t4.jpg H (5S) 8.05
16e graphic file with name nihms162795t4.jpg 3-Ac (5S) 35.11
16f graphic file with name nihms162795t4.jpg 4-Ac (5S) 39.87
21a graphic file with name nihms162795t5.jpg H (5R) 4731
22a graphic file with name nihms162795t5.jpg H (5S) 7.28
22d graphic file with name nihms162795t5.jpg 3-CF3 (5S) 21.63
23a graphic file with name nihms162795t6.jpg H (5S) 657
24a graphic file with name nihms162795t7.jpg H (5R) 1800
25d graphic file with name nihms162795t8.jpg 3-CF3 (5S) 41.09