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Your search keyword '"Feng, Enguang"' showing total 3 results
Start Over Author "Feng, Enguang" Journal journal of medicinal chemistry
3 results on '"Feng, Enguang"'

1. Structure-Based Design and Synthesis of C-1- and C-4-Modified Analogs of Zanamivir as Neuraminidase Inhibitors

Author

Feng, Enguang, primary, Shin, Woo-Jin, additional, Zhu, Xuelian, additional, Li, Jian, additional, Ye, Deju, additional, Wang, Jiang, additional, Zheng, Mingyue, additional, Zuo, Jian-Ping, additional, No, Kyoung Tai, additional, Liu, Xian, additional, Zhu, Weiliang, additional, Tang, Wei, additional, Seong, Baik-Lin, additional, Jiang, Hualiang, additional, and Liu, Hong, additional

Published
2013
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2. Design and Synthesis of Small Molecule RhoA Inhibitors: A New Promising Therapy for Cardiovascular Diseases?

Author

Deng, Jing, primary, Feng, Enguang, additional, Ma, Sheng, additional, Zhang, Yan, additional, Liu, Xiaofeng, additional, Li, Honglin, additional, Huang, Huang, additional, Zhu, Jin, additional, Zhu, Weiliang, additional, Shen, Xu, additional, Miao, Liyan, additional, Liu, Hong, additional, Jiang, Hualiang, additional, and Li, Jian, additional

Published
2011
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3. Structure-Based Designand Synthesis of C-1-and C-4-Modified Analogs of Zanamivir as Neuraminidase Inhibitors.

Author

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, and Liu, Hong

Subjects
*NEURAMINIDASE, *CHEMICAL synthesis, *BINDING sites, *MOLECULAR models, *DRUG design, *PHARMACOKINETICS
Abstract

In order to exploit the 430-cavity in the active sitesof 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 9fexerts the most potency, with IC50value of0.013, 0.001, and 0.09 μM against H3N2, H5N1, and H1N1, whichis similar to that of zanamivir (H3N2 IC50= 0.0014 μM,H5N1 IC50= 0.012 μM, H1N1 IC50= 0.001μM). Pharmacokinetic studies of compound 9finrats showed a much longer plasma half-life (t1/2) than that of zanamivir following administration (po dose).Molecular modeling provided information about the binding model betweenthe new inhibitors and neuraminidase, with the elongated groups atthe C-1-position being projected toward the 430-loop region. Thisstudy may represent a novel starting point for the future developmentof improved antiflu agents. [ABSTRACT FROM AUTHOR]

Published
2013
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