61948-59-2Relevant articles and documents
Design, synthesis and biological evaluation of 2-aminoquinazolin-4(3H)-one derivatives as potential SARS-CoV-2 and MERS-CoV treatments
Lee, Jun Young,Shin, Young Sup,Jeon, Sangeun,Lee, Se In,Noh, Soojin,Cho, Jung-Eun,Jang, Min Seong,Kim, Seungtaek,Song, Jong Hwan,Kim, Hyoung Rae,Park, Chul Min
supporting information, (2021/03/15)
Despite the rising threat of fatal coronaviruses, there are no general proven effective antivirals to treat them. 2-Aminoquinazolin-4(3H)-one derivatives were newly designed, synthesized, and investigated to show the inhibitory effects on SARS-CoV-2 and MERS-CoV. Among the synthesized derivatives, 7-chloro-2-((3,5-dichlorophenyl)amino)quinazolin-4(3H)-one (9g) and 2-((3,5-dichlorophenyl)amino)-5-hydroxyquinazolin-4 (3H)-one (11e) showed the most potent anti-SARS-CoV-2 activities (IC50 50 50 > 25 μM). In addition, both compounds showed acceptable results in metabolic stabilities, hERG binding affinities, CYP inhibitions, and preliminary PK studies.
Design, synthesis and evaluation of phenethylaminoheterocycles as K v1.5 inhibitors
Johnson, James A.,Xu, Ningning,Jeon, Yoon,Finlay, Heather J.,Kover, Alexander,Conder, Mary L.,Sun, Huabin,Li, Danshi,Levesque, Paul,Hsueh, Mei-Mann,Harper, Timothy W.,Wexler, Ruth R.,Lloyd, John
, p. 3018 - 3022 (2014/06/24)
Phenethylaminoheterocycles have been prepared and assayed for inhibition of the Kv1.5 potassium ion channel as a potential approach to the treatment of atrial fibrillation. A diverse set of heterocycles were identified as potent Kv1.
ACYCLIC IKUR INHIBITORS
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Page/Page column 92, (2010/11/26)
A compound of formula I wherein R1, R2, R3, R4 and R5 are described herein.
