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

被引：5

作者：

Xu, Xuemei ^{[1
]}

Luo, Zaigang ^{[1
]}

He, Kuai ^{[1
]}

Zhang, Mingyang ^{[1
]}

机构：

[1] AnHui Univ Sci & Technol, Coll Chem Engn, Huainan 232001, Anhui, Peoples R China

来源：

ADVANCES IN CHEMICAL, MATERIAL AND METALLURGICAL ENGINEERING, PTS 1-5 | 2013年 / 634-638卷

关键词：

HIV-1; integrase inhibitors; quinolone acid; polyhydroxylated aromatic; strand transfer; NITROGEN;

D O I：

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

中图分类号：

TQ [化学工业];

学科分类号：

0817 ;

摘要：

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 mu M.

引用

页码：1116 / 1119

页数：4

共 50 条

[1] Synthesis of polyhydroxylated aromatics having amidation of piperazine nitrogen as HIV-1 integrase inhibitor
Yang, Leifu
Xu, Xuemei
Huang, Yali
Zhang, Bin
Zeng, Chengchu
He, Hongqiu
Wang, Cunxin
Hu, Liming
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2010, 20 (18) : 5469 - 5471
[2] Nitrogen-containing polyhydroxylated aromatics as HIV-1 integrase inhibitors: synthesis, structure-activity relationship analysis, and biological activity
Yu, Shenghui
Zhang, Linna
Yan, Shifeng
Wang, Peng
Sanchez, Tino
Christ, Frauke
Debyser, Zeger
Neamati, Nouri
Zhao, Guisen
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2012, 27 (05) : 628 - 640
[3] Design and synthesis of novel nitrogen-containing polyhydroxylated aromatics as HIV-1 integrase inhibitors from caffeic acid phenethyl ester
Wang, Peng
Liu, Chuan
Sanches, Tino
Zhong, Yuan
Liu, Bo
Xiong, Junlong
Neamati, Nouri
Zhao, Guisen
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2009, 19 (16) : 4574 - 4578
[4] Synthesis and biological evaluation of HIV-1 integrase inhibitors.
Gervay-Hague, J
Meadows, DC
Hadd, MJ
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2003, 225 : U179 - U179
[5] Naphthoxazepine inhibitors of HIV-1 integrase: Synthesis and biological evaluation
Garofalo, Antonio
Grande, Fedora
Brizzi, Antonella
Aiello, Francesca
Dayam, Raveendra
Neamati, Nouri
CHEMMEDCHEM, 2008, 3 (06) : 986 - 990
[6] Design, synthesis, and biological evaluation of chicoric acid analogs as inhibitors of HIV-1 integrase
Charvat, Trevor T.
Lee, Deborah J.
Robinson, W. Edward
Chamberlin, A. Richard
BIOORGANIC & MEDICINAL CHEMISTRY, 2006, 14 (13) : 4552 - 4567
[7] Synthesis and Biological Activities of Quinoline Derivatives as HIV-1 Integrase Inhibitors
Luo Zai-gang
Zeng Cheng-chu
Wang Fang
He Hong-qiu
Wang Cun-xin
Du Hong-guang
Hu Li-ming
CHEMICAL RESEARCH IN CHINESE UNIVERSITIES, 2009, 25 (06) : 841 - 845
[8] Synthesis and Biological Activities of Quinoline Derivatives as HIV-1 Integrase Inhibitors
LUO Zai-gang1
2. College of Science
Chemical Research in Chinese Universities, 2009, 25 (06) : 841 - 845
[9] Synthesis and biological evaluation of geminal disulfones as HIV-1 integrase inhibitors
Meadows, DC
Mathews, TB
North, TW
Hadd, MJ
Kuo, CL
Neamati, N
Gervay-Hague, J
JOURNAL OF MEDICINAL CHEMISTRY, 2005, 48 (14) : 4526 - 4534
[10] Novel quinolinonyl diketo acid derivatives as HIV-1 integrase inhibitors: Design, synthesis, and biological activities
Di Santo, Roberto
Costi, Roberta
Roux, Alessandra
Miele, Gaetano
Crucitti, Giuliana Cuzzucoli
Iacovo, Alberto
Rosi, Federica
Lavecchia, Antonio
Marinelli, Luciana
Di Giovanni, Carmen
Novellino, Ettore
Palmisano, Lucia
Andreotti, Mauro
Amici, Roberta
Galluzzo, Clementina Maria
Nencioni, Lucia
Palamara, Anna Teresa
Pommier, Yves
Marchand, Christophe
JOURNAL OF MEDICINAL CHEMISTRY, 2008, 51 (15) : 4744 - 4750

← 1 2 3 4 5 →