Table 3.
Activity of acyl analogs 17 and 18 against varicella-zoster virus (VZV) in human embryonic lung (HEL) cells..
| Compounds | R | R1 | EC50 (μM)a |
MCC (μM)b | |
|---|---|---|---|---|---|
| TK+ |
TK- |
||||
| OKA | 07–1 | ||||
| 17a | Biphenylethyl | Methyl | 2.6 | 2.0 | 35 |
| 17d | 2-naphtyl | >4 | >4 | 20 | |
| 17e | 1-naphtyl | >20 | >20 | 100 | |
| 17f | 2-naphtylmethyl | >4 | >4 | 20 | |
| 17g | 1-naphtylmethyl | >20 | >20 | 100 | |
| 17h | Biphenylmethyl | >20 | >20 | 100 | |
| 17i | Phenyloxybenzyl | >4 | >4 | 20 | |
| 18a | Cyclohexyl | >4 | >4 | 20 | |
| 18b | Phenyl | 20 | 20 | >100 | |
| 18c | Morpholinethyl | >4 | >4 | 20 | |
| 18d | t-butyloxy | >4 | >4 | 20 | |
| Acyclovir | 3.8 | 145 | >440 | ||
| Brivudin | 0.026 | 143 | >300 | ||
a
Effective concentration required to reduce virus plaque formation by 50%. Virus input was 20 plaque forming units (PFU).
b
Minimum cytotoxic concentration that causes a microscopically detectable alteration of cell morphology.