Table 1.
Inhibition of integrase activities (3′-processing and strand transfer) of dihydropyrimidine α,γ-diketobutanoic acid derivatives.
Compound No. | IC50 (μM) ± S.D. |
|
---|---|---|
3′- processing Strand transfer (ST) | ||
46 | 16.9 ± 3.4 | 0.19 ± 0.12 |
47 | 17.4 ± 2.1 | 1.3 ± 0.1 |
48 | 19.1 ± 4.0 | 0.64 ± 0.16 |
49 | 35 ± 8 | 1.1 ± 0.4 |
50 | 72 ± 4.5 | 5.6 ± 4.6 |
51 | 16.3 ± 3.5 | 1.3 ± 0.5 |
52 | 16.6 ± 2.4 | 1.3 ± 0.5 |
53 | 22.5 ± 2.0 | 0.85 ± 0.12 |
54 | 21.1 ± 1.2 | 2.23 ± 0.27 |
55 | 29.3 ± 3.5 | 0.92 ± 0.14 |
56 | 30.7 ± 2.7 | 2.27 ± 0.28 |
57 | 22 ± 4 | 2.8 ± 0.9 |