75332-44-4Relevant academic research and scientific papers
Rational modifications on a benzylidene-acrylohydrazide antiviral scaffold, synthesis and evaluation of bioactivity against Chikungunya virus
Giancotti, Gilda,Cancellieri, Michela,Balboni, Andrea,Giustiniano, Mariateresa,Novellino, Ettore,Delang, Leen,Neyts, Johan,Leyssen, Pieter,Brancale, Andrea,Bassetto, Marcella
supporting information, p. 56 - 68 (2018/03/06)
Chikungunya virus is a re-emerging arbovirus transmitted to humans by Aedes mosquitoes, responsible for an acute febrile illness associated with painful and debilitating arthralgia, which can persist for several months or become chronic. Over the past few years, infection with this virus has spread worldwide with a previously unknown virulence. No specific antiviral treatments nor vaccines are currently available against this important pathogen. Starting from the structure of a class of selective anti-CHIKV agents previously identified in our research group, different modifications to this scaffold were rationally designed, and 69 novel small-molecule derivatives were synthesised and evaluated for their inhibition of Chikungunya virus replication in Vero cells. Further structure-activity relationships associated with this class of antiviral agents were elucidated for the original scaffolds, and novel antiviral compounds with EC50 values in the low micromolar range were identified. This work provides the foundation for further investigation of these new structures as antivirals against Chikungunya virus.
Exquisite synthesis of a designed PAR-1 antagonist
Miao, Hua-Ming,Zhao, Gui-Long,Zhang, Lin-Shan,Shao, Hua,Wang, Jian-Wu
, p. 1981 - 1993 (2012/01/04)
The synthesis of a designed, sterically congested geminal dimethyl-bearing PAR-1 antagonist was achieved by a route of ten steps, with the oxidation of an electron-rich benzaldehyde, the construction of a tertiary alkyl azide, and the selective hydrogenolysis of a 1,5-fused tetrazole to generate the cyclic amidine with Raney-Ni being the key steps. The selective hydrogenolysis of 1,5-fused tetrazole to generate the cyclic amidine with Raney-Ni was discovered and may be generally used for the synthesis of structurally unusual cyclic amidines. Several unsuccessful attempts to construct the desired geminal dimethyl-bearing cyclic amidine were also discussed. Copyright
QUINAZOLINE DERIVATIVES AS RAF KINASE MODULATORS AND METHODS OF USE THEREOF
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Page/Page column 176, (2009/10/22)
Compounds according to formula (I), compositions and methods are provided for modulating the activity of RAF kinases, including BRAF kinase and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by RAF kinases. Formula (I): or a pharmaceutically acceptable salt, solvate, clathrate of hydrate thereof, wherein X is O or S(O)t; Ra is O or S.
The synthesis and mesomorphism of di-, tetra- and hexa-catenar liquid crystals based on 2,2′-bipyridine
Rowe, Kathryn E.,Bruce, Duncan W.
, p. 331 - 341 (2007/10/03)
2,2′-Bipyridines are known to coordinate to a wide variety of metal centres. In this paper, liquid-crystalline two-chained (dicatenar), four-chained (tetracatenar) and six-chained (hexacatenar) bipyridines are synthesised and their mesomorphism is described. For the tetracatenar bipyridines, a full homologous series, from tetramethoxy to tetratetradecyloxy, was synthesised, and the phase diagram showed a classic progression from nematic and smectic C phases at short chain length, through a cubic phase to a columnar phase.
