1185869-40-2Relevant academic research and scientific papers
Antiviral activity of 4-oxoquinoline-3-carboxamide derivatives against bovine herpesvirus type 5
Pinto, Ana Maria V.,Leite, José Paulo G.,Marinho, Robson S.S.,Forezi, Luana da S.M.,Batalha, Pedro N.,Boechat, Fernanda da C.S.,Cunha, Anna C.,Silva, David O.,Gama, Ivson L.,Faro, Letícia V.,de Souza, Maria C.B.V.,Paix?o, Izabel Christina P.
, p. 13 - 20 (2020/10/21)
Background: Bovine herpesvirus type 5 is an important agent of meningoencephalitis in cattle and has been identified in outbreaks of bovine neurological disease in several Brazilian states. In recent years, oxoquinoline derivatives have become an important focus in antiviral drug research. Methods: The cytotoxicity and anti BoHV-5RJ42/01 activity of a set of synthetic 4-oxoquinoline derivatives 4a-k were assayed on Madin-Darby Bovine Kidney cell and antiviral activity by plaque reduction assay. Results: The most promising substance (4h) exhibited CC50 and EC50 values of 1,239 μM ±5.5 and 6.0 μM ±1.5, respectively, with an SI =206. Two other compounds 4j (CC50 = 35 μM ±2 and EC50 = 24 μM ±7.0) and 4k (CC50= 55 μM ±2 and EC50 = 24 μM ±5.1) presented similar inhibitory profile and selectivity indexes of 1.4 and 2.9, respectively. The results of the time-of-addition studies revealed expressive reduction of virus production (≥80%) in different stages of virus replication cycle except for compound 4h that slightly inhibited virus yield in the first 2 h post infection, but it showed expressive virus inhibition after this time. Conclusions: All three compounds slightly interact with the virus on the virucidal assay and they are not able to block virus attachment and penetration. Antiviral effect of oxoquinoline 4h was more prominent than acyclovir which leads us to suggest compound 4h as a promising molecule for further anti-BoHV-5 drug design.
Synthesis, antiviral activity and molecular modeling of oxoquinoline derivatives
Santos, Fernanda da C.,Abreu, Paula,Castro, Helena C.,Paixao, Izabel C.P.P.,Cirne-Santos, Claudio C.,Giongo, Viveca,Barbosa, Juliana E.,Simonetti, Bruno R.,Garrido, Valeria,Bou-Habib, Dumith Chequer,Silva, David de O.,Batalha, Pedro N.,Temerozo, Jairo R.,Souza, Thiago M.,Nogueira, Christiane M.,Cunha, Anna C.,Rodrigues, Carlos R.,Ferreira, Vitor F.,de Souza, Maria C.B.V.
scheme or table, p. 5476 - 5481 (2009/12/09)
In the present article, we describe the synthesis, anti-HIV1 profile and molecular modeling evaluation of 11 oxoquinoline derivatives. The structure-activity relationship analysis revealed some stereoelectronic properties such as LUMO energy, dipole momen
