Synthesis and anti-HSV-1 evaluation of new 3H-benzo[b]pyrazolo[3,4-h]-1,6-naphthyridines and 3H-pyrido[2,3-b]pyrazolo[3,4-h]-1,6-naphthyridines

Organic and Medicinal Chemistry Letters

Table 1 Anti-HSV-1 activity of 3H-benzo[b]pyrazolo[3,4-h]-1,6-naphthyridines (1a-k) and 3H-pyrido[2,3-b]pyrazolo[3,4-h]-1,6-naphthyridines (2a-c)

Compound	R	% of inhibition of virus yield (HSV-1)
1a	H	20,6
1b	9-OCH₃	50,0
1c	9-CH₃	68,0
1d	9-Cl	80,0
1e	8-Cl	60,0
1f	9-NO₂	80,0
1g	8-NO₂	87,0
1h	9-F	91,0
1i	8-F	65,0
1j	9-Br	30,0
1k	8-Br	30,0
2a	7-CH₃	11,0
2b	8-CH₃	ND
2c	9-CH₃	65,0
ACV	-	96.0 ± 1.0

The experimental concentration of 1a-k and 2a-c was 50 μM and for ACV 10 μM.
Results are presented as the mean of triplicate experiments.
ACV has been included for comparison purposes.