Synthesis and Biological Evaluation of Quinolone Acid Derivatives Having Polyhydroxylated Aromatics as HIV-1 Integrase Inhibitions

Xue Mei Xu; Zai Gang Luo; Kuai He; Ming Yang Zhang

doi:10.4028/www.scientific.net/AMR.634-638.1116

Paper Titles

Study on Synthesis of 2-(1-Tert-Butoxycarbonylamino-2-Methyl-Butyl)-Thiazole-4-Carboxylic Acid Methyl Ester
p.1099

Study on Synthesis of 2,2-Dimethyl-3-Hydroxy-7-Octynoic Acid
p.1103

Study on Synthesis of N-Methyldipeptide N-Ns-N(Me)-L-Ala-N(Me)-L-lle-O^tBu
p.1108

Synthesis and Anti-HIV Integrase Inhibitory Activity of β-Diketo Derivatives of Mono-Substituted Calix[4]arene
p.1112

Synthesis and Biological Evaluation of Quinolone Acid Derivatives Having Polyhydroxylated Aromatics as HIV-1 Integrase Inhibitions
p.1116

The Application of Silk Fibroin in Tissue Engineering and Drug Carrier Area
p.1120

The Preparation and Research of the Aerogel-Type Wood Composite Material
p.1124

The Effect of KHCO₃ on Photosynthesis of Eggplant Seedlings
p.1129

Synthesis and In Vitro Anti-Breast Cancer Activity of Trametenolic Acid B Derivatives
p.1135

HomeAdvanced Materials ResearchAdvanced Materials Research Vols. 634-638Synthesis and Biological Evaluation of Quinolone...

Synthesis and Biological Evaluation of Quinolone Acid Derivatives Having Polyhydroxylated Aromatics as HIV-1 Integrase Inhibitions

Abstract:

A small chemical library of quinolone acid derivatives were synthesized as potential HIV-1 integrase inhibitors and evaluated their inhibition to the strand transfer process of HIV-1 integrase. Their structures were characterized by NMR, MS and HRMS. The result indicates that quinolone acid derivatives having 3,4,5-trihydroxylated aromatic substituent on the N-1 position of quinolone ring exhibit good inhibition with IC50 of 2.6 μM.

You might also be interested in these eBooks

Advances in Chemical, Material and Metallurgical Engineering

View Preview

Info:

Periodical:

Advanced Materials Research (Volumes 634-638)

Pages:

1116-1119

DOI:

https://doi.org/10.4028/www.scientific.net/AMR.634-638.1116

Citation:

Cite this paper

Online since:

January 2013

Authors:

Xue Mei Xu, Zai Gang Luo, Kuai He, Ming Yang Zhang

Keywords:

HIV-1, Integrase Inhibitors, Polyhydroxylated Aromatic, Quinolone Acid, Strand Transfer

Export:

RIS, BibTeX

Price:

Permissions CCC:

Request Permissions

Permissions PLS:

Request Permissions

Сopyright:

Citation:

References

[1] Y. Pommier, A. A. Johnson, C. Marchand. Nat. ReV. Drug Discov. 4(2005), p.236.

Google Scholar

[2] R. Dayam, N. Neamati, Curr. Pharm. Des. 9(2003), p.1789.

Google Scholar

[3] O. Tabarrini, S. Massari, D. Daelemans, M. Stevens, G. Manfroni, S. Sabatini, J. Balzarini, V. Cecchetti, C. Pannecouque, A. Fravolini. J. Med. Chem. 51(2008), p.5454.

DOI: 10.1021/jm701585h

Google Scholar

[4] V. Cecchetti, C. Parolin, S. Moro, T. Pecere, E. Filipponi, A. Calistri, O. Tabarrini, B. Gatto, M. Palumbo, A. Fravolini, G. Palu. J. Med. Chem. 43(2000), p.3799.

DOI: 10.1021/jm9903390

Google Scholar

[5] S. Motohide, M. Takahisa, A. Hisateru, M. Takashi, Y. Masaki, I. Yoshiharu, K. Hiroshi, M. Yuji, W. Wataru, Y. Kazunobu, I. Satoru, K. Eiichi, M. Masao and S. Hisashi. J. Med. Chem. 49(2006), p.1506.

Google Scholar

[6] P. Wang, C. Liu, T. Sanches, Y. Zhong, B. Liu, J. Xiong, N. Neamati, G. Zhao. Bioorg. Med. Chem. Lett. 19(2009), p.4574.

Google Scholar

[7] A. Mazumder, A. Gazit, A. Levitzki, M. Nicklaus, J. Yung, G. Kohlhagen, Y. Pommiers. Biochemistry, 34(1995), p.15111.

DOI: 10.1021/bi00046a018

Google Scholar

[8] L. F. Yang, X. M. Xu, Y. L. Huang, B. Zhang, C. C. Zeng, H. Q. He, C. X. Wang and L. M. Hu, Bioorg. Med. Chem. Lett. 20(2010), p.5469.

Google Scholar

[9] H. Q. He, X. H. Ma, B. Liu, W. Z. Chen, C. X. Wang, S. H. Cheng. Acta. Pharma-cologica. Sinica. 29(2008), p.397.

Google Scholar

[10] L. M. Hu, S. Yan, Z. G. Luo, X. Han, Y. J. Wang, Z. Y. Wang and C. C. Zeng: submitted to Molecules (2012).

Google Scholar