Synthesis and Antiviral Activities of New Pyrazolo[4,3‐c]quinolin‐3‐ones and Their Ribonucleoside Derivatives

Mara R. P. de Oliveira Departamento de Química Orgânica, Instituto de Química, Universidade Federal do Rio de Janeiro, Ilha do Fundão, Rio de Janeiro, CEP 21945‐970, Brazil

Thatyana R. Alves Departamento de Química Orgânica, Instituto de Química, Universidade Federal Fluminense, Outeiro de São João Batista s/n°, Centro, Niterói, Rio de Janeiro, CEP 24210‐150, Brazil

Angelo C. Pinto Departamento de Química Orgânica, Instituto de Química, Universidade Federal do Rio de Janeiro, Ilha do Fundão, Rio de Janeiro, CEP 21945‐970, Brazil

Helena de S. Pereira Instituto de Biofísica Carlos Chagas Filho, Universidade Federal do Rio de Janeiro, Ilha do Fundão, Rio de Janeiro, CEP 21941‐590, Brazil

Luiz R. Leão‐Ferreira Programa de Neuroimunologia, Departamento de Biologia Celular e Molecular, Instituto de Biologia, Universidade Federal Fluminense, Outeiro de São João Batista s/n°, Centro, Niterói, Rio de Janeiro, CEP 24210‐150, Brazil

Nissin Moussatché Instituto de Biofísica Carlos Chagas Filho, Universidade Federal do Rio de Janeiro, Ilha do Fundão, Rio de Janeiro, CEP 21941‐590, Brazil

Izabel Christina de P. P. Frugulhetti Programa de Neuroimunologia, Departamento de Biologia Celular e Molecular, Instituto de Biologia, Universidade Federal Fluminense, Outeiro de São João Batista s/n°, Centro, Niterói, Rio de Janeiro, CEP 24210‐150, Brazil

Vitor F. Ferreira Departamento de Química Orgânica, Instituto de Química, Universidade Federal Fluminense, Outeiro de São João Batista s/n°, Centro, Niterói, Rio de Janeiro, CEP 24210‐150, Brazil

Maria Cecília B. V. de Souza Departamento de Química Orgânica, Instituto de Química, Universidade Federal Fluminense, Outeiro de São João Batista s/n°, Centro, Niterói, Rio de Janeiro, CEP 24210‐150, BrazilCorrespondence[email protected]

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Abstract

Several new pyrazolo[4,3‐c]quinolin‐3‐one ribonucleosides (5a–g) and their corresponding heterocycle moieties (3a–g) were synthesized and evaluated against vaccinia virus (VV) and herpes simplex virus type 1 (HSV‐1). The derivatives 3c and 3d showed modest inhibitory activity against vaccinia virus reaching 70% at a concentration of 100 µM. All heterocyclic compounds (3a–f) showed a modest inhibition against HSV‐1, reaching the maximal inhibitory effect around 20–30%. The antiviral effects of most of the pyrazolo[4,3‐c]quinolin‐3‐one ribonucleosides (5a–f) on VV and HSV were not impressive.

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Acknowledgments

The fellowship granted to M. R. P. O. from CNPq (Brazil) is gratefully acknowledged. A. C. P., M. C. B. V. S., and V. F. F. are grateful to CNPq for their individual research fellowships. This work was partially supported by CNPq (National Council of Research from Brazil) and FAPERJ.

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Synthesis and Antiviral Activities of New Pyrazolo[4,3‐c]quinolin‐3‐ones and Their Ribonucleoside Derivatives

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Synthesis and Antiviral Activities of New Pyrazolo[4,3‐c]quinolin‐3‐ones and Their Ribonucleoside Derivatives

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