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
收藏
页码：1116 / 1119
页数：4
相关论文
共 50 条
  • [41] Boronic acid-containing diarylpyrimidine derivatives as novel HIV-1 NNRTIs: Design, synthesis and biological evaluation
    Feng, Da
    Wei, Fenju
    Sun, Yanying
    Sharma, Prem Prakash
    Zhang, Tao
    Lin, Hao
    Rathi, Brijesh
    De Clercq, Erik
    Pannecouque, Christophe
    Kang, Dongwei
    Zhan, Peng
    Liu, Xinyong
    CHINESE CHEMICAL LETTERS, 2021, 32 (12) : 4053 - 4057
  • [42] Geometrically and conformationally restrained cinnamoyl compounds as inhibitors of HIV-1 integrase: Synthesis, biological evaluation, and molecular modeling
    Artico, M
    Di Santo, R
    Costi, R
    Novellino, E
    Greco, G
    Massa, S
    Tramontano, E
    Marongiu, ME
    De Montis, A
    La Colla, P
    JOURNAL OF MEDICINAL CHEMISTRY, 1998, 41 (21) : 3948 - 3960
  • [43] Design, synthesis and biological evaluation of novel tricyclic HIV-1 integrase inhibitors by modification of its pyridine ring
    Metobo, Sammy E.
    Jin, Haolun
    Tsiang, Manuel
    Kim, Choung U.
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2006, 16 (15) : 3985 - 3988
  • [44] Discovery of HIV-1 Integrase Inhibitors: Pharmacophore Mapping, Virtual Screening, Molecular Docking, Synthesis, and Biological Evaluation
    Bhatt, Hardik
    Patel, Paresh
    Pannecouque, Christophe
    CHEMICAL BIOLOGY & DRUG DESIGN, 2014, 83 (02) : 154 - 166
  • [45] Synthesis and biological evaluation of 5-fluoroquinolone-3-carboxylic acids as potential HIV-1 integrase inhibitors
    He, Qiu-Qin
    Zhang, Xuan
    Yang, Liu-Meng
    Zheng, Yong-Tang
    Chen, Fener
    JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2013, 28 (04) : 671 - 676
  • [46] QSAR Study on Diketo Acid and Carboxamide Derivatives as Potent HIV-1 Integrase Inhibitor
    Adebimpe, Arodola Olayide
    Dash, Radha Charan
    Soliman, Mahmoud E. S.
    LETTERS IN DRUG DESIGN & DISCOVERY, 2014, 11 (05) : 618 - 627
  • [47] HIV-1 integrase strand transfer inhibitors (INSTIs): Design, synthesis and biological activity
    Ferro, S.
    Barreca, M. L.
    De Luca, L.
    Rao, A.
    Monforte, A. M.
    Michiels, M.
    Witvrouw, M.
    Debyser, Z.
    Chimirri, A.
    PROCEEDINGS OF THE 5TH JOINT MEETING ON MEDICINAL CHEMISTRY, 2007, : 11 - 15
  • [48] Design, Synthesis, and Docking Studies of Thioimidazolyl Diketoacid Derivatives Targeting HIV-1 Integrase
    Karimi, Nafiseh
    Roudsari, Rouhollah Vahabpour
    Hajimahdi, Zahra
    Zarghi, Afshin
    MEDICINAL CHEMISTRY, 2022, 18 (05) : 616 - 628
  • [49] Synthesis and HIV-1 integrase inhibitory activities of catechol and bis-catechol derivatives
    Dupont, R
    Jeanson, L
    Mouscadet, JF
    Cotelle, P
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2001, 11 (24) : 3175 - 3178
  • [50] Newer tetracycline derivatives: Synthesis, anti-HIV, antimycobacterial activities and inhibition of HIV-1 integrase
    Sriram, Dharmarajan
    Yogeeswari, Perumal
    Senchani, Geetha
    Banerjee, Debjani
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2007, 17 (08) : 2372 - 2375
12345