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. 2016 May 9;7(7):702–707. doi: 10.1021/acsmedchemlett.6b00135

Table 2. Profile of Compounds 9i, 9k–9t, and Atazanavir.

                    Rat PKc
Compound X R1 R2 R3 R4 R5 R6 Enzymea IC50 (nM) Antiviralb IC95 (nM) Cl (mL/min/kg) %F
atazanavir               0.04 17 nd nd
9i C H H H H H Moc 27 120 36 19
9k C F H H H H Moc 12 95 36 37
9l C F H H H H H 3.1 230 nd nd
9m N H H H H H Moc 14 330 81 <5
9n N F H H H H Moc 3.5 94 11 15
9o N F H H H H H 9.9 150 13 59
9p C F F H H F H 6.4 75 45 30
9q C F F F H F H 8.2 61 22 14
9r N F F H H F H 2.4 66 16 37
9s N F F F H F H 2.4 130 nd nd
9t (MK-8718) N F Cl F H F H 0.8 49 11 25
a

Assay for inhibition HIV protease as described in the Supporting Information (n = 2).

b

Assay for inhibition of viral infection as described in the Supporting Information (n = 2).

c

For compounds 9i–9n: 1 mpk IV (60% PEG 400/water), 5 mpk PO (0.5% methylcellulose). n = 2 rats. For compounds 9o–9t: 2 mpk IV (1:1 DMSO/PEG400), 10 mpk PO (10% tween 80/water). n = 2 rats.