TABLE 2.
Spectrum of antiviral activities of 1,6-naphthyridine and 7,8-dihydroisoquinoline representatives
| Virus (strain)a | Antiviral activity (IC50 [μM]) and selectivity index (SI)b
|
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Controlc
|
A1
|
B1
|
B2
|
B3
|
||||||
| IC50 | SI | IC50 | SI | IC50 | SI | IC50 | SI | IC50 | SI | |
| Influenza virus A | 25 ± 2 | >16 | >10 | <1 | 169 ± 31 | 1 | >32 | <1 | >344 | >1 |
| Influenza virus B | 23 ± 3 | >36 | 10 ± 1.6 | 2 | 158 ± 10 | >2 | 23 ± 8 | 2 | >344 | >1 |
| RSV (A2) | 8.2 ± 4.1 | 17 | 19 ± 13 | <1 | 118 ± 25 | <1 | 178 ± 13 | <1 | >344 | <1 |
| RV/2 (GPH) | 4.4 ± 1.2 | >7 | <0.03 | >400 | 31 ± 1.4 | 3 | 11 ± 2.5 | 3 | 74 ± 7 | 2 |
| AV/1 (65098) | 9.9 ± 1.7 | 13 | 13 ± 0.6 | 1 | >282 | <1 | 64 ± 12 | 1.5 | 136 ± 14 | <1 |
| PIV/3 (14702) | 12.3 ± 0.4 | 10 | 28.1 ± 3 | <1 | 282 ± 141 | <1 | 127 ± 32 | <1 | >344 | <1 |
| HIV RFd | 0.018 | >404 | >31 | <1 | >181 | <1 | >51 | <1 | >34 | <1 |
| HIV IIIBd | 0.028 | >388 | >31 | <1 | ND | ND | ND | ND | >34 | <1 |
| HIV ROJOc | 0.004 | >769 | 12.4 | 1.5 | 127 | >1.4 | 9.2 | 2 | 30 | 9 |
| HIV TEKIe | 0.004 | >1,250 | 0.93 | 22 | ND | ND | ND | ND | 139 | 2 |
Cell lines used for antiviral activity evaluation were MDCK for influenza viruses A and B, MA-104 for RSV and PIV/3, and A549 for RV/2 and AV/1.
In vitro selectivity index value, which is the ratio of CC50 to IC50. ND, not determined.
Control: influenza viruses A and B, RSV, and PIV/3, ribavirin; AV/1, HPMPA; RV/2, pirodavir; HIV RF and IIIB strains, dideoxycytosine; HIV ROJO and TEKI strains, zidovudine.
Anti-HIV activity was evaluated in CEM-SS cells. Experiments were performed in triplicate. Standard deviation was less than 10%.
Anti-HIV activity was evaluated in PBMC. Experiments were performed in triplicate. Standard deviation was less than 10%.