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Feng, Enguang,Shin, Woo-Jin,Zhu, Xuelian,Li, Jian,Ye, Deju,Wang, Jiang,Zheng, Mingyue,Zuo, Jian-Ping,No, Kyoung Tai,Liu, Xian,Zhu, Weiliang,Tang, Wei,Seong, Baik-Lin,Jiang, Hualiang,Liu, Hong American Chemical Society 2013 Journal of medicinal chemistry Vol.56 No.3
<P>In order to exploit the 430-cavity in the active sites of neuraminidases, 22 zanamivir analogs with C-1 and C-4 modification were synthesized, and their inhibitory activities against both group-1 (H5N1, H1N1) and group-2 neuraminidases (H3N2) were determined. Compound <B>9f</B> exerts the most potency, with IC<SUB>50</SUB> value of 0.013, 0.001, and 0.09 μM against H3N2, H5N1, and H1N1, which is similar to that of zanamivir (H3N2 IC<SUB>50</SUB> = 0.0014 μM, H5N1 IC<SUB>50</SUB> = 0.012 μM, H1N1 IC<SUB>50</SUB> = 0.001 μM). Pharmacokinetic studies of compound <B>9f</B> in rats showed a much longer plasma half-life (<I>t</I><SUB>1/2</SUB>) than that of zanamivir following administration (po dose). Molecular modeling provided information about the binding model between the new inhibitors and neuraminidase, with the elongated groups at the C-1-position being projected toward the 430-loop region. This study may represent a novel starting point for the future development of improved antiflu agents.</P><P><B>Graphic Abstract</B> <IMG SRC='http://pubs.acs.org/appl/literatum/publisher/achs/journals/content/jmcmar/2013/jmcmar.2013.56.issue-3/jm3009713/production/images/medium/jm-2012-009713_0009.gif'></P><P><A href='http://pubs.acs.org/doi/suppl/10.1021/jm3009713'>ACS Electronic Supporting Info</A></P>
Qingyu Zhang,Xiaoling Duan,Siyi Tang,Cunwen Wang,Weiguo Wang,Weiliang Feng,Tielin Wang 대한환경공학회 2023 Environmental Engineering Research Vol.28 No.1
In this study, a series of acid-base bi-functional catalysts were prepared by mixing different amounts of basic amino acids (AAs) and phosphotungstic acid (PTA), which exhibited the excellent performance in catalyzing conversion of oleic acid (OA) for the biodiesel production. The physicochemical properties of the catalysts were characterized and analyzed using modern testing techniques and characterization methods such as XRD, FT-IR, XPS, SEM, TEM, and Hammett titration. The various influence parameters were optimized using the central composite design based the response surface methodology, where the maximum biodiesel yield of 97.0% was achieved at the MeOH/OA molar ratio of 5.9, the catalyst loading of 8%, reaction time of 6 h, and reaction temperature of 65℃. Furthermore, the stability and reusability of the prepared catalyst were also demonstrated. At last, the possible catalytic mechanism of the prepared catalyst was comprehensively described.