Skip to main content
. Author manuscript; available in PMC: 2017 Jan 1.
Published in final edited form as: Expert Opin Ther Pat. 2016;26(3):297–308. doi: 10.1517/13543776.2016.1153065

Table 3.

Activity of representative dipeptidyl inhibitors (I): α-hydroxyphosphonates

R R1 Z IC50 (μM) EC50 (μM)
18 H Isobutyl CH(OH)P(O)(OC2H5)2 11.5 0.8
19 CH(OH)P(O)(OCH3)2 20.2 3.5
20 CH(OH)P(O)(OH)2 ND 7.5
21 Cyclohexylmethyl CH(OH)P(O)(OC2H5)2 3.5 0.25
22 CH(OH)P(O)(OCH3)2 8.3 2.8
23 CH(OH)P(O)(OC4H9)2 ND 0.5
24 CH(OH)P(O)(OCH2CF3)2 6.5 0.35
25 CH(OH)P(O)(OCH2C6H5)2 ND 0.6
26 m-Cl CH(OH)P(O)(OC2H5)2 >10 0.06
27 o-Cl >10 0.2
28 o-F >10 >2
29 m-Br 6.5 0.15