40107-10-6Relevant articles and documents
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, Natalia,Santos-Filho, Osvaldo,Riscado, Cecília S.,Forezi, Luana Da S.M.,Faro, Letícia V.,Brozeguini, Leonardo,Marques, Isakelly P.,Ferreira, Vitor F.,Souza, Thiago Moreno L.,De Souza, Maria Cecília B.V.
, p. 7777 - 7784 (2015)
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 μM 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.
Invariant and variable intermolecular interactions in functionalized malonic acid half-esters: X-ray, Hirshfeld surface and PIXEL energy analyses
Venkatesan, Perumal,Thamotharan, Subbiah,Kumar, Rajendran Ganesh,Ilangovan, Andivelu
, p. 904 - 915 (2015/02/19)
A series of functionalized malonic acid half-ester derivatives (parent compound MHE-1), with variations in functional groups at different positions on the aromatic ring, have been synthesized and crystal structures are determined at room temperature (296
Oxoquinoline acyclonucleoside phosphonate analogues as a new class of specific inhibitors of human immunodeficiency virus type 1
Faro, Leticia V.,De Almeida, Jessica M.,Cirne-Santos, Claudio C.,Giongo, Viveca A.,Castello-Branco, Luis R.,Oliveira, Ingrid De B.,Barbosa, Juliana E.F.,Cunha, Anna C.,Ferreira, Vitor F.,De Souza, Marcos C.,Paixao, Izabel C.N.P.,De Souza, Maria Cecilia B.V.
scheme or table, p. 5055 - 5058 (2012/08/28)
The emergence of a multidrug-resistant HIV-1 strain and the toxicity of anti-HIV-1 compounds approved for clinical use are the most significant problems facing antiretroviral therapies. Therefore, it is crucial to find new agents to overcome these issues. In this study, we synthesized a series of new oxoquinoline acyclonucleoside phosphonate analogues (ethyl 1- [(diisopropoxyphosphoryl)methyl]-4-oxo-1,4-dihydroquinoline-3-carboxylates 3a-3k), which contained different substituents at the C6 or C7 positions of the oxoquinoline nucleus and an N1-bonded phosphonate group. We subsequently investigated these compounds' in vitro inhibitory effects against HIV-1-infected peripheral blood mononuclear cells (PBMCs). The most active compounds were the fluoro-substituted derivatives 3f and 3g, which presented excellent EC 50 values of 0.4 ± 0.2 μM (3f) and 0.2 ± 0.005 μM (3g) and selectivity index values (SI) of 6240 and 14675, respectively.
