1,2,3-Triazolyl-4-oxoquinolines: A feasible beginning for promising chemical structures to inhibit oseltamivir-resistant influenza A and B viruses

Boechat Fernanda da C. S.; Sacramento Carolina Q.; Cunha Anna C.Sagrillo Fernanda S.Nogueira Christiane M.Fintelman-Rodrigues NataliaSantos-Filho OsvaldoRiscado Cecilia S.Forezi Luana da S. M.Faro Leticia V.Brozeguini LeonardoMarques Isakelly P.Ferreira Vitor F.Souza Thiago Moreno L.de Souza Maria Cecilia B. V.

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1,2,3-Triazolyl-4-oxoquinolines: A feasible beginning for promising chemical structures to inhibit oseltamivir-resistant influenza A and B viruses

机译：1,2,3-Triazolyl-4-oxoquinolines: A feasible beginning for promising chemical structures to inhibit oseltamivir-resistant influenza A and B viruses

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We described the synthesis of a new congener series of 1,2,3-triazolyl-4-oxoquinolines and evaluated their ability to inhibit oseltamivir (OST)-resistant influenza strains. Oxoquinoline derivative 1i was the most potent compound within this series, inhibiting 94 of wild-type (WT) influenza neuraminidase (NA) activity. Compound 1i inhibited influenza virus replication with an EC50 of 0.2 mu M with less cytotoxicity than OST, and also inhibited different OST-resistant NAs. These results suggest that 1,2,3-triazolyl-4-oxoquinolines represent promising lead molecules for further anti-influenza drug design. Published by Elsevier Ltd.

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《Bioorganic and medicinal chemistry》 |2015年第24期|7777-7784|共8页
作者
Boechat Fernanda da C. S.; Sacramento Carolina Q.; Cunha Anna C.Sagrillo Fernanda S.Nogueira Christiane M.Fintelman-Rodrigues NataliaSantos-Filho OsvaldoRiscado Cecilia S.Forezi Luana da S. M.Faro Leticia V.Brozeguini LeonardoMarques Isakelly P.Ferreira Vitor F.Souza Thiago Moreno L.de Souza Maria Cecilia B. V.;
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Univ Fed Fluminense, Inst Quim Outeiro Sao Joao Batista, BR-24020150 Niteroi, RJ, Brazil;

Fundacao Oswaldo Cruz, Inst Oswaldo Cruz, Lab Virus Resp, NIC WHO, BR-21041360 Rio De Janeiro, RJ;

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正文语种英语
中图分类药学;
关键词
1; 2; 3-Triazole; 4-Oxoquinoline; Influenza viruses; Neuraminidase inhibitors; Oseltamivir carboxylate; Antiviral resistance;

1,2,3-Triazolyl-4-oxoquinolines: A feasible beginning for promising chemical structures to inhibit oseltamivir-resistant influenza A and B viruses

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