99281-72-8Relevant academic research and scientific papers
Vinyl Sulfone-Based Inhibitors of Nonstructural Protein 2 Block the Replication of Venezuelan Equine Encephalitis Virus
Zhang, Huaisheng,Harmon, Moeshia,Radoshitzky, Sheli R.,Soloveva, Veronica,Kane, Christopher D.,Duplantier, Allen J.,Ogungbe, Ifedayo Victor
, p. 2139 - 2145 (2020/12/17)
Emerging infectious diseases like those caused by arboviruses such as Venezuelan equine encephalitis virus (VEEV) pose a serious threat to public health systems. Development of medical countermeasures against emerging infectious diseases are of utmost importance. In this work, an acrylate and vinyl sulfone-based chemical series was investigated as promising starting scaffolds against VEEV and as inhibitors of the cysteine protease domain of VEEV's nonstructural protein 2 (nsP2). Primary screen and dose response studies were performed to evaluate the potency and cytotoxicity of the compounds. The results provide structural insights into a new class of potent nonpeptidic covalent inhibitors of nsP2 cysteine protease represented by compound 11 (VEEV TrD, EC50= 2.4 μM (HeLa), 1.6 μM (Vero E6)). These results may facilitate the evolution of the compounds into selective and broad-spectrum anti-alphaviral drug leads.
Stereoselective dihydroxylation reactions of γ-amino-α,β- unsaturated esters via their aryl ketimine derivatives
Oh, Joon Seok,Jeon, Jongho,Park, Do Yeon,Kim, Young Gyu
, p. 770 - 771 (2007/10/03)
OsO4-catalysed dihydroxylation reactions of the aryl ketimine derivatives of (E)-γ-amino-α,β-unsaturated esters gave anti selectivity ranging from 6.7:1 to 19:1, whereas the opposite syn selectivity was consistently observed with those of (Z)-γ
