Substituted hydrazinecarbothioamide as potent antitubercular agents: Synthesis and quantitative structure-activity relationship (QSAR)

被引：16
|
作者：
Singh, Supriya [1 ]
Mandal, Pintu K. [1 ]
Singh, Nagendra [1 ]
Misra, Anup K. [1 ]
Singh, Shubhra [2 ]
Chaturvedi, Vinita [2 ]
Sinha, Sudhir [2 ]
Saxena, Anil K. [1 ]
机构：
[1] Cent Drug Res Inst, Med & Proc Chem Div, Lucknow 226001, Uttar Pradesh, India
[2] Cent Drug Res Inst, Drug Target Discovery & Dev Div, Lucknow 226001, Uttar Pradesh, India
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 08期
关键词：
Tuberculosis; Hydrazinecarbothioamides; QSAR; Synthesis; MYCOBACTERIUM-TUBERCULOSIS; MACROPHAGES; AVIUM;
D O I：
10.1016/j.bmcl.2010.02.081
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of novel substituted hydrazinecarbothioamides was synthesized and evaluated for anti-TB activity. Three most active compounds viz. 1, 6 and 12 were found to exhibit minimum inhibitory concentration (MIC) of 0.4 mu g/mL, whereas four compounds viz. 3, 5, 10 and 11 showed comparatively lesser activity with MIC value of 0.8 mu g/mL against Mycobacterium tuberculosis strain. A highly significant QSAR equation explaining 81.8% variance is described. (C) 2010 Elsevier Ltd. All rights reserved.
引用
收藏
页码：2597 / 2600
页数：4
相关论文
共 50 条
  • [1] SUBSTITUTED HYDRAZINECARBOTHIOAMIDE AS POTENT ANTITUBERCULAR AGENTS: SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIP (QSAR)
    Singh, Nagendra
    Singh, Supriya
    Saxena, Anil. K.
    MEDICINAL CHEMISTRY RESEARCH, 2010, 19 : S91 - S91
  • [2] Design, Synthesis, and Structure-Activity Relationship Studies of Tryptanthrins As Antitubercular Agents
    Hwang, Jae-Min
    Oh, Taegwon
    Kaneko, Takushi
    Upton, Anna M.
    Franzblau, Scott G.
    Ma, Zhenkun
    Cho, Sang-Nae
    Kim, Pilho
    JOURNAL OF NATURAL PRODUCTS, 2013, 76 (03): : 354 - 367
  • [3] Cinnamic Derivatives as Antitubercular Agents: Characterization by Quantitative Structure-Activity Relationship Studies
    Teixeira, Catia
    Ventura, Cristina
    Gomes, Jose R. B.
    Gomes, Paula
    Martins, Filomena
    MOLECULES, 2020, 25 (03):
  • [4] Synthesis and structure-activity relationship of 8-substituted protoberberine derivatives as a novel class of antitubercular agents
    Li, Ying-Hong
    Fu, Hai-Gen
    Su, Feng
    Gao, Li-Mei
    Tang, Sheng
    Bi, Chong-Wen
    Li, Yu-Huan
    Wang, Yan-Xiang
    Song, Dan-Qing
    CHEMISTRY CENTRAL JOURNAL, 2013, 7
  • [5] Synthesis, evaluation and quantitative structure-activity relationship (QSAR) analysis of Wogonin derivatives as cytotoxic agents
    Bian, Jinlei
    Li, Tinghan
    Weng, Tianwei
    Wang, Jubo
    Chen, Yu
    Li, Zhiyu
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2017, 27 (04) : 1012 - 1016
  • [6] Biodegradation and Quantitative Structure-Activity Relationship (QSAR)
    Sabljic, Aleksandar
    Nakagawa, Yoshiaki
    NON-FIRST ORDER DEGRADATION AND TIME-DEPENDENT SORPTION OF ORGANIC CHEMICALS IN SOIL, 2014, 1174 : 57 - +
  • [7] Sorption and Quantitative Structure-Activity Relationship (QSAR)
    Sabljic, Aleksandar
    Nakagawa, Yoshiaki
    NON-FIRST ORDER DEGRADATION AND TIME-DEPENDENT SORPTION OF ORGANIC CHEMICALS IN SOIL, 2014, 1174 : 85 - +
  • [8] Quantitative structure-activity relationship study of antitubercular fluoroquinolones
    Minovski, Nikola
    Vracko, Marjan
    Solmajer, Tom
    MOLECULAR DIVERSITY, 2011, 15 (02) : 417 - 426
  • [9] Quantitative structure-activity relationship models for potent DNA alkylating agents
    Hannongbua, Supa
    Saparpakorn, Patchreenart
    Kim, Jae-Hyoun
    MOLECULAR & CELLULAR TOXICOLOGY, 2009, 5 (03) : 81 - 81
  • [10] Three-dimensional quantitative structure-activity relationships for a large series of potent antitubercular agents
    Andrade, Carolina Horta
    Salum, Livia de Barros
    Mesquita Pasqualoto, Kerly Fernanda
    Ferreira, Elizabeth Igne
    Andricopulo, Adriano Defini
    LETTERS IN DRUG DESIGN & DISCOVERY, 2008, 5 (06) : 377 - 387
12345