Potential anti-tubercular agents: Hexahydro-3-phenyl indazol-2-yl(pyridin-4-yl)methanones from anti-tubercular drug isoniazid and bis(substituted-benzylidene)cycloalkanones

被引:10
作者
Napoleon, Ayyakannu Arumugam [1 ]
Khan, Fazlur-Rahman Nawaz [1 ,2 ]
Jeong, Euh Duck [2 ]
Chung, Eun Hyuk [2 ]
机构
[1] VIT Univ, Sch Adv Sci, Div Organ Chem, Organ & Med Chem Res Lab, Vellore 632014, Tamil Nadu, India
[2] Korea Basic Sci Inst, Busan Ctr, Busan 618230, South Korea
关键词
Benzylidene cyclohexanones; Hexahydro-3-phenyl indazol-2-yl(pyridin-4-yl)methanones; Isoniazid; Anti-tubercular activity; ANTIMYCOBACTERIAL ACTIVITY; PHARMACOLOGICAL EVALUATION; PYRAZOLINE DERIVATIVES;
D O I
10.1016/j.cclet.2015.01.008
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
A series of indazol-2-yl(pyridin-4-yOmethanones, 4 were acquired from 2,6-bisbenzylidene cyclohex-anones, 3 and anti-tubercular drug (isoniazid), and their anti-tubercular impacts were screened. Among the test compounds used against Mycobacterium tuberculosis H37 Ra cell line in the microplate alamar blue assay, the compounds 4g-j revealed moderate anti-tubercular activity with MIC 12.5 mu g/mL, comparable to standard drugs (streptomycin, MIC, 6.25 mu g/mL, pyrazinamide, isoniazid and ciprofloxacin with MICs of 3.125 mu g/mL). (C) 2015 Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences. Published by Elsevier B.V. All rights reserved.
引用
收藏
页码:567 / 571
页数:5
相关论文
共 31 条
[1]   Synthesis, spectral studies and antiamoebic activity of new 1-N-substituted thiocarbamoyl-3-phenyl-2-pyrazolines [J].
Abid, Mohammad ;
Bhat, Abdul Roouf ;
Athar, Fareeda ;
Azam, Amir .
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2009, 44 (01) :417-425
[2]   Design, synthesis, in vitro evaluation of tetrahydropyrimidine-isatin hybrids as potential antibacterial, antifungal and anti-tubercular agents [J].
Akhaja, Tarunkumar Nanjibhai ;
Raval, Jignesh Priyakant .
CHINESE CHEMICAL LETTERS, 2012, 23 (04) :446-449
[3]  
Ali Mohamed A, 2007, Acta Pol Pharm, V64, P435
[4]   Synthesis and pharmacological evaluation of pyrazoline derivatives as new anti-inflammatory and analgesic agents [J].
Amir, Mohammad ;
Kumar, Harish ;
Khan, Suroor A. .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2008, 18 (03) :918-922
[5]  
Babu VH, 2004, INDIAN J HETEROCY CH, V13, P253
[6]  
Bhatt AH, 2001, INDIAN J CHEM B, V40, P57
[7]  
BLOOM BR, 1992, ANNU REV IMMUNOL, V10, P453, DOI 10.1146/annurev.iy.10.040192.002321
[8]   Potential cytotoxic and apoptosis inducing agents: synthesis and evaluation of methoxy-substituted chalcones against human lung and cervical cancers [J].
Ethiraj, K. R. ;
Aranjani, Jesil Mathew ;
Khan, F. Nawaz .
MEDICINAL CHEMISTRY RESEARCH, 2013, 22 (11) :5408-5417
[9]   Synthesis and cytotoxicity study of pyrazoline derivatives of methoxy substituted naphthyl chalcones [J].
Ethiraj, K. R. ;
Nithya, P. ;
Krishnakumar, V. ;
Mathew, A. Jesil ;
Khan, F. Nawaz .
RESEARCH ON CHEMICAL INTERMEDIATES, 2013, 39 (04) :1833-1841
[10]   Synthesis of Methoxy-substituted Chalcones and in vitro Evaluation of their Anticancer Potential [J].
Ethiraj, Kannatt Radhakrishnan ;
Aranjani, Jesil Mathew ;
Khan, Fazlur-Rahman Nawaz .
CHEMICAL BIOLOGY & DRUG DESIGN, 2013, 82 (06) :732-742