2566-23-6Relevant articles and documents
Continuous micro-production using enzymatic reaction and online monitoring
Moser, Regula,Chappuis, Thierry,Vanoli, Ennio,Crelier, Simon,Naef, Olivier
, p. 799 - 802 (2010)
A micro-reactor coupled to a microfluidic system and an online UV/VIS spectrometer is described. The enzymatic reaction studied is the hydrolysis of the N-benzoyl-l-tyrosine ethyl ester (BTEE) to N-benzoyl-ltyrosine (BT) and ethanol, catalyzed by chymotry
Optimal covalent immobilization of α-chymotrypsin on Fe 3O4-chitosan nanoparticles
Ju, Hen-Yi,Kuo, Chia-Hung,Too, Jui-Rze,Huang, Hsin-Yi,Twu, Yawo-Kuo,Chang, Chieh-Ming J.,Liu, Yung-Chuan,Shieh, Chwen-Jen
, p. 9 - 15 (2012)
This study investigated the immobilization of α-chymotrypsin onto magnetic Fe3O4-chitosan (α-chymotrypsin-Fe 3O4-CS) nanoparticles by covalent binding. The response surface methodology (RSM) with a 3-factor-3-le
Multi-Institution Research and Education Collaboration Identifies New Antimicrobial Compounds
Fuller, Amelia A.,Dounay, Amy B.,Schirch, Douglas,Rivera, Daniel G.,Hansford, Karl A.,Elliott, Alysha G.,Zuegg, Johannes,Cooper, Matthew A,Blaskovich, Mark A. T.,Hitchens, Jacob R.,Burris-Hiday, Sarah,Tenorio, Kristiana,Mendez, Yanira,Samaritoni, J. Geno,O'Donnell, Martin J.,Scott, William L.
, p. 3187 - 3196 (2020/12/21)
New antibiotics are urgently needed to address increasing rates of multidrug resistant infections. Seventy-six diversely functionalized compounds, comprising five structural scaffolds, were synthesized and tested for their ability to inhibit microbial growth. Twenty-six compounds showed activity in the primary phenotypic screen at the Community for Open Antimicrobial Drug Discovery (CO-ADD). Follow-up testing of active molecules confirmed that two unnatural dipeptides inhibit the growth of Cryptococcus neoformans with a minimum inhibitory concentration (MIC) ≤ 8 μg/mL. Syntheses were carried out by undergraduate students at five schools implementing Distributed Drug Discovery (D3) programs. This report showcases that a collaborative research and educational process is a powerful approach to discover new molecules inhibiting microbial growth. Educational gains for students engaged in this project are highlighted in parallel to the research advances. Aspects of D3 that contribute to its success, including an emphasis on reproducibility of procedures, are discussed to underscore the power of this approach to solve important research problems and to inform other coupled chemical biology research and teaching endeavors.
Design, synthesis and evaluation of novel phenyl propionamide derivatives as non-nucleoside hepatitis B virus inhibitors
Qiu, Jingying,Gong, Qineng,Gao, Jian,Chen, Wang,Zhang, Yinpeng,Gu, Xiaoke,Tang, Daoquan
, p. 424 - 434 (2018/01/01)
As an ongoing search for potent non-nucleoside anti-HBV agents with novel structures, we described a series of phenyl propionamide derivatives (3a-b, 4a-e, 7a-g, 8a-h and 9a-b) by pharmacophore fusion strategy in the present work. All the compounds exhibited an anti-HBV activity to some extent. Among them, compounds 8d and 9b displayed most potent anti-HBV activity with IC50 values on HBV DNA replication of 0.46 and 0.14 μM, respectively. And the selective index values of 8d and 9b were more than 217.39 and 153.14, suggesting that 8d and 9b exhibited favorable safety profiles. Interestingly, 8d and 9b possessed significantly antiviral activities against lamivudine and entecavir resistant HBV mutants with IC50 values of 0.77 and 0.32 μM. Notably, preliminary anti-HBV action mechanism studies showed that 8d could inhibit intracellular HBV pgRNA and RT activity of the HBV polymerase. Molecular docking studies suggested that compound 8d could fit into the dimer-dimer interface of HBV core protein by hydrophobic interaction. In addition, in silico prediction of physicochemical properties showed that 8d conformed well to the Lipinski's rule of five, suggesting its potential for use as a drug like molecule. Taken together, 8d possessed significantly anti-HBV activity, low toxicity, diverse anti-HBV mechanism and favorable physicochemical properties, and warranted further investigation as a promising non-nucleoside anti-HBV candidate.
