Synthesis and antitubercular activity of lipophilic moxifloxacin and gatifloxacin derivatives

被引：51
|
作者：
de Almeida, Mauro V.
Saraiva, Mauricio F.
de Souza, Marcus V. N.
da Costa, Cristiane F.
Vicente, Felipe R. C.
Lourenco, Maria C. S.
机构：
[1] Univ Fed Juiz Fora, Inst Ciencias Exatas, Dept Quim, BR-36036330 Juiz De Fora, MG, Brazil
[2] Fundacao Oswaldo Cruz, Inst Tecnol Farmacos Far Manguinhos, BR-21041250 Rio De Janeiro, Brazil
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 20期
关键词：
Fluoroquinolones; M; tuberculosis; moxifloxacin; gatifloxacin; diamines; N-alkyl chains; antitubercular; structure-activity relationships;
D O I：
10.1016/j.bmcl.2007.07.073
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Fluoroquinolone (FQ) has a broad spectrum of activity against several bacteria, mycobacteria, parasites, and other diseases. Moxifloxacin and gatifloxacin are a new generation of fluoroquinolone agents with improved activity against Gram-negative and positive bacteria. As lipophilicity is an important consideration in the design and activity of novel antibacterial agents, we report in this work the synthesis and biological evaluation of 12 lipophilic moxifloxacin or gatifloxacin derivatives, by reaction of 1-cyclo-propyl-6,7-difluoro-1,4-dihydro-8-methoxy-4-oxoquinoline-3-carboxylic acid 13 with severals N-monoalkyl 1,2-ethanediamine or 1,3-propanediamine. (c) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码：5661 / 5664
页数：4
相关论文
共 50 条
  • [1] SYNTHESIS AND ANTITUBERCULAR ACTIVITY OF PYRIDAZINONE DERIVATIVES
    Husain, Asif
    Ahmad, Aftab
    Bhandari, Anil
    Ram, Veerma
    JOURNAL OF THE CHILEAN CHEMICAL SOCIETY, 2011, 56 (03): : 778 - 780
  • [2] SYNTHESIS AND ANTITUBERCULAR ACTIVITY OF OFLOXACIN DERIVATIVES
    Dundar, Yasemin
    Ulger, Mahmut
    Kaynak Onurdag, Fatma
    Okten, Suzan
    Onkol, Tijen
    REVUE ROUMAINE DE CHIMIE, 2018, 63 (04) : 265 - 272
  • [3] Synthesis and Antitubercular Activity of Berberine Derivatives
    Anita Mahapatra
    Vijay Maheswari
    Nitin Pal Kalia
    Vikrant S. Rajput
    Inshad Ali Khan
    Chemistry of Natural Compounds, 2014, 50 : 321 - 325
  • [4] Synthesis and Antitubercular Activity of Berberine Derivatives
    Mahapatra, Anita
    Maheswari, Vijay
    Kalia, Nitin Pal
    Rajput, Vikrant S.
    Khan, Inshad Ali
    CHEMISTRY OF NATURAL COMPOUNDS, 2014, 50 (02) : 321 - 325
  • [5] Design, synthesis and antitubercular activity of diarylmethyinaphthol derivatives
    Das, Saial Kumar
    Panda, Gautam
    Chaturvedi, Vinita
    Manju, Y. S.
    Galkwad, Anil K.
    Sinha, Sudhir
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2007, 17 (20) : 5586 - 5589
  • [6] Synthesis and antitubercular activity of novel thiazolidinone derivatives
    Oza, H
    Joshi, D
    Parekh, H
    INDIAN JOURNAL OF CHEMISTRY SECTION B-ORGANIC CHEMISTRY INCLUDING MEDICINAL CHEMISTRY, 1998, 37 (08): : 822 - 824
  • [7] The methoxyfluoroquinolones: Gatifloxacin and moxifloxacin
    Stein, GE
    INFECTIONS IN MEDICINE, 2000, 17 (08) : 564 - 570
  • [8] Synthesis and Antitubercular Activity of Novel Amino Acid Derivatives
    Da Costa, Cristiane F.
    Pinheiro, Alessandra C.
    De Almeida, Mauro V.
    Lourenco, Maria C. S.
    De Souza, Marcus V. N.
    CHEMICAL BIOLOGY & DRUG DESIGN, 2012, 79 (02) : 216 - 222
  • [9] SYNTHESIS AND ANTITUBERCULAR ACTIVITY OF 4-THIAZOLIDINONE DERIVATIVES
    SOLANKEE, AN
    KAPADIA, KM
    DESAI, CM
    JOURNAL OF THE INDIAN CHEMICAL SOCIETY, 1992, 69 (11) : 783 - 784
  • [10] Synthesis and Antitubercular Activity of Some Novel Thiazolidinone Derivatives
    Malipeddi, Himaja
    Karigar, Asif A.
    Malipeddi, Venkata Ramana
    Sikarwar, Mukesh S.
    TROPICAL JOURNAL OF PHARMACEUTICAL RESEARCH, 2012, 11 (04) : 611 - 620
12345