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Background  Herpes simplex virus type-1 (HSV-1) is the primary cause of facial lesions (mouth, lips, and eyes) in humans. The widespread use of acyclovir and nucleoside analogues has led to emergence of HSV strains that are resistant to these drugs. Recently, non-nucleoside anti-HSV compounds have received considerable attention. 1,6-Naphthyridines are a class of heterocyclic compounds that exhibit a broad spectrum of biological activities such as inhibitor of HIV-1 integrase, HCMV, FGF receptor-1 tyrosine kinase, and the enzyme acetylcholinesterase. We previously reported the synthesis, SAR studies, and evaluation anti-HSV-1 activity of 3 H -benzo[ b ]pyrazolo[3,4- h ]-1,6-naphthyridines. In the course of our search for new 1,6-naphthyridines derivatives with potential activity against HSV-1, we have synthesized and evaluated new 3 H -benzo[ b ]pyrazolo[3,4- h ]-1,6-naphthyridines  (1a-k)  and 3 H -pyrido[2,3- b ]pyrazolo[3,4- h ]-1,6-naphthyridines  (2a-c) .    Results  A known synthetic approach was used for preparing new 3 H -benzo[ b ]pyrazolo[3,4- h ]-1,6-naphthyridines  (1a-k)  and 3 H -pyrido[2,3- b ]pyrazolo[3,4- h ]-1,6-naphthyridines  (2a-c) , starting from ethyl 4-chloro-1-phenyl-1 H -pyrazolo[3,4- b ]pyridine-5-carboxylate  (7) . All compounds were identified by FTIR,  1 H NMR, and mass spectrometry. The antiviral effect on HSV-1 virus replication was determined.    Conclusions  The compounds  1d ,  1f ,  1g , and  1h  exhibited the highest anti-HSV-1 activity. In general, 3 H -benzo[ b ]pyrazolo[3,4- h ]-1,6-naphthyridines were more effective inhibitors than their corresponding 3 H -pyrido[2,3- b ]pyrazolo[3,4- h ]-1,6-naphthyridines. The compound  1h  reduced the virus yield in 91% at 50 μM and exhibited a low cytotoxicity (CC 50  600 μM).

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