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38 results on '"Feng, Enguang"'

5. 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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11. Development of a novel class of B-RafV600E-selective inhibitors through virtual screening and hierarchical hit optimization

Author

Kong, Xiangqian, primary, Qin, Jie, additional, Li, Zeng, additional, Vultur, Adina, additional, Tong, Linjiang, additional, Feng, Enguang, additional, Rajan, Geena, additional, Liu, Shien, additional, Lu, Junyan, additional, Liang, Zhongjie, additional, Zheng, Mingyue, additional, Zhu, Weiliang, additional, Jiang, Hualiang, additional, Herlyn, Meenhard, additional, Liu, Hong, additional, Marmorstein, Ronen, additional, and Luo, Cheng, additional

Published
2012
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12. Structural and Functional Analysis of Laninamivir and its Octanoate Prodrug Reveals Group Specific Mechanisms for Influenza NA Inhibition

Author

Vavricka, Christopher J., primary, Li, Qing, additional, Wu, Yan, additional, Qi, Jianxun, additional, Wang, Mingyang, additional, Liu, Yue, additional, Gao, Feng, additional, Liu, Jun, additional, Feng, Enguang, additional, He, Jianhua, additional, Wang, Jinfang, additional, Liu, Hong, additional, Jiang, Hualiang, additional, and Gao, George F., additional

Published
2011
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14. 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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33. 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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35. GoldICatalyzed OnePot Tandem CouplingCyclization: An Efficient Synthesis of PyrroloPyrido2,1bbenzod1,3oxazin 1ones

Author

Zhou, Yu, Zhai, Yun, Ji, Xun, Liu, Guannan, Feng, Enguang, Ye, Deju, Zhao, Linxiang, Jiang, Hualiang, and Liu, Hong

Abstract

A highly efficient method has been developed for the onepot synthesis of multiring heterocyclic compounds such as pyrrolopyrido2,1bbenzod1,3oxazin1ones from oaminobenzyl alcohols viaa goldIcatalyzed tandem couplingcyclization reaction. Significantly, the strategy presents a straightforward and efficient approach to construct novel tricyclic or polycyclic molecular architectures in which two new CN bonds and one CO bond are formed in a onepot reaction operation from two simple starting materials. Moreover, a broad spectrum of substrates can participate in the process effectively to produce the desired products in good yields.

Published
2010
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37. Metal-free synthesis of 2-substituted (N, O, C) benzothiazoles via an intramolecular C-S bond formation.

Author

Feng E, Huang H, Zhou Y, Ye D, Jiang H, and Liu H

Subjects
Benzothiazoles chemistry, Combinatorial Chemistry Techniques, Cyclization, Molecular Structure, Stereoisomerism, Benzothiazoles chemical synthesis
Abstract

An efficient, economical, and convenient method was developed for the preparation of 2-substituted (N, O, C) benzothiazoles from N'-substituted-N-(2-halophenyl)thioureas, O'-substituted-N-(2-halophenyl) carbamothioates, or N-(2-halophenyl) thioamides via a base-promoted cyclization in dioxane without any transition metal. A one-pot variant combining the synthesis of the thiourea and the cyclization was also demonstrated. High yields were obtained, and a variety of functional groups were tolerated under these conditions. Transition-metal-free, mild reactive conditions, wide application scope, and shorter reaction times make this method superior to the reported methods for the synthesis of 2-substituted benzothiazoles and suitable for combinatorial format.

Published
2010
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38. Highly alpha-selective synthesis of sialyl spirohydantoins by regiospecific domino condensation/O-->N acyl migration/N-sialylation of carbodiimides with peracetylated sialic acid.

Author

Zhang D, Ye D, Feng E, Wang J, Shi J, Jiang H, and Liu H

Subjects
Acetylation, Organic Chemistry Phenomena, Spiro Compounds chemistry, Carbodiimides chemistry, Hydantoins chemical synthesis, Sialic Acids chemistry
Abstract

A novel and efficient process for the synthesis of alpha-sialyl spirohydantoin analogues via one-pot sequential reaction involving various carbodiimides and peracetylated Neu5Ac is reported. BF(3) x Et(2)O mediating intramolecular N-sialylation with excellent alpha-selectivity is first demonstrated.

Published
2010
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