Evaluation of anti-tubercular activity of nicotinic and isoniazid analogues

被引:227
|
作者
Lourenco, Maria C. S. [2 ]
Souza, Marcus V. N. de [1 ]
Pinheiro, Alessandra C. [1 ]
Ferreira, Marcelle de L. [1 ]
Goncalves, Raoni S. B. [1 ]
Nogueira, Thais Cristina M. [1 ]
Peralta, Monica A. [1 ]
机构
[1] FioCruz Fdn Oswaldo Cruz, Inst Tecnol & Farmacos Far Manguinhos, Rua Sizenando Nabuco 100, BR-21041250 Rio De Janeiro, Brazil
[2] Inst Pesquisas Clin Evandro Chagas, Dept Bacteriol, Rio De Janeiro, Brazil
关键词
tuberculosis; isoniazid; nicotinic acid; analogs;
D O I
10.3998/ark.5550190.0008.f18
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Several nicotinic and isoniazid derivatives, most of them containing nitro groups were synthesized by our group, and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H(37)Rv using the Alamar Blue susceptibility test and the activity expressed as the minimum inhibitory concentration ( MIC) in mg/mL. The compound 11d exhibited the best result (1.2 mu g/mL) when compared with first line drugs such as isoniazid (INH) and rifampicin (RIP). Therefore this class of compounds could be a good starting point to develop new lead compounds in the treatment of multi-drug resistant tuberculosis.
引用
收藏
页码:181 / 191
页数:11
相关论文
共 50 条
  • [31] Anti-tubercular Activity of Ruthenium (II) Complexes with Polypyridines
    Hadda, Taibi Ben
    Akkurt, Mehmet
    Baba, Mohamed Filali
    Daoudi, Maria
    Bennani, Brahim
    Kerbal, Abdelali
    Chohan, Zahid H.
    JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2009, 24 (02) : 457 - 463
  • [32] Synthesis and anti-tubercular evaluation of 4-quinolylhydrazones
    Savini, L
    Chiasserini, L
    Gaeta, A
    Pellerano, C
    BIOORGANIC & MEDICINAL CHEMISTRY, 2002, 10 (07) : 2193 - 2198
  • [33] Computational, crystallographic studies, cytotoxicity and anti-tubercular activity of substituted 7-methoxy-indolizine analogues
    Venugopala, Katharigatta Narayanaswamy
    Chandrashekharappa, Sandeep
    Pillay, Melendhran
    Abdallah, Hassan H.
    Mahomoodally, Fawzi M.
    Bhandary, Subhrajyoti
    Chopra, Deepak
    Attimarad, Mahesh
    Aldhubiab, Bandar E.
    Nair, Anroop B.
    Sreeharsha, Nagaraja
    Morsy, Mohamed A.
    Pottathil, Shinu
    Venugopala, Rashmi
    Odhav, Bharti
    Mlisana, Koleka
    PLOS ONE, 2019, 14 (06):
  • [34] Synthesis and in vitro antimicrobial and anti-tubercular evaluation of some quinoline-based azitidinone and thiazolidinone analogues
    Bhupendra M. Mistry
    Smita Jauhari
    Medicinal Chemistry Research, 2013, 22 : 635 - 646
  • [35] Synthesis and in vitro antimicrobial and anti-tubercular evaluation of some quinoline-based azitidinone and thiazolidinone analogues
    Mistry, Bhupendra M.
    Jauhari, Smita
    MEDICINAL CHEMISTRY RESEARCH, 2013, 22 (02) : 635 - 646
  • [36] Non-Enzymatic Radical Activation of the Potent Anti-Tubercular Isoniazid by Cu(II)
    Zhu, Ben-Zhan
    Qin, Li
    FREE RADICAL BIOLOGY AND MEDICINE, 2016, 100 : S34 - S34
  • [37] Synthesis and evaluation of in vitro anti-microbial and anti-tubercular activity of 2-styryl benzimidazoles
    Shingalapur, Ramya V.
    Hosamani, Kallappa M.
    Keri, Rangappa S.
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2009, 44 (10) : 4244 - 4248
  • [38] MODIFICATION OF AN ANTI-TUBERCULAR MOLECULE
    BARRY, VC
    BELTON, JG
    KELLY, RM
    TWOMEY, D
    NATURE, 1950, 166 (4216) : 303 - 305
  • [39] 'Kits' of anti-tubercular drugs
    Aggarwal, P
    Handa, R
    Wali, JP
    NATIONAL MEDICAL JOURNAL OF INDIA, 1996, 9 (03): : 143 - 144
  • [40] A NEW ANTI-TUBERCULAR SUBSTANCE
    KLEIN, S
    MEDICINA EXPERIMENTALIS, 1963, 9 (04): : 283 - &