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. Author manuscript; available in PMC: 2007 Oct 16.
Published in final edited form as: Antiviral Res. 2007 Mar 30;75(3):198–209. doi: 10.1016/j.antiviral.2007.03.005

Table 2.

Anti-HIV activity and enzymatic hydrolysis of DAPD prodrugs

Anti-HIV Activity(a) Enzymatic Hydrolysis(b)
# R EC50 (μM) %
graphic file with name nihms-29192-t0006.jpg 8 NHEt 0.41 ± 0.25 0.7
9 NMe2 0.87 ± 0.33 1.0
10 NHi-Pr 5.40 ± 5.20 1.1
14 NHBn 44.90 ± 27.9 0.0
DAPD(c) NH2 6.90 ± 4.70 89.0
(a)

in human PBM cells unless otherwise indicated. Based on three replicate assays

(b)

percentage conversion of DAPD prodrugs to DXG by adenosine deaminase (bovine spleen) after 240 min. in pH 7.4 buffer solution at 37 ± 0.5 °C

(c)

DAPD was used as the positive control