Synthesis and In Vitro Antibacterial Evaluation of Mannich Base Nitrothiazole Derivatives

被引:1
|
作者
Dube, Phelelisiwe S. [1 ]
Hart, Dylan [1 ]
Legoabe, Lesetja J. [1 ]
Jordaan, Audrey [2 ]
Warner, Digby F. [2 ,3 ,4 ]
Beteck, Richard M. [1 ]
机构
[1] North West Univ, Ctr Excellence Pharmaceut Sci, ZA-2520 Potchefstroom, South Africa
[2] Univ Cape Town, Dept Pathol, SAMRC NHLS UCT Mol Mycobacteriol Res Unit, ZA-7925 Observatory, South Africa
[3] Univ Cape Town, Inst Infect Dis & Mol Med, ZA-7701 Rondebosch, South Africa
[4] Univ Cape Town, Fac Hlth Sci, Welcome Ctr Infect Dis Res Africa CIDRI Africa, ZA-7701 Rondebosch, South Africa
基金
英国医学研究理事会; 新加坡国家研究基金会; 英国惠康基金;
关键词
nitrothiazole; Mannich bases; antitubercular activity; tuberculosis; Mycobacterium tuberculosis; MYCOBACTERIUM-TUBERCULOSIS;
D O I
10.3390/M1793
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Nitrothiazole derivatives have been reported to exhibit activity against aerobic, anaerobic, and microaerophilic bacteria. This activity profile makes the nitrothiazole compound class an ideal lead source against Mycobacterium tuberculosis, which flourishes in varied environments with different oxygen concentrations. In this work, we investigated six nitrothiazole derivatives for antitubercular activity. The compounds exhibited potent activity, with compounds 9 and 10 possessing an equipotent MIC90 value of 0.24 mu M. The compounds were investigated for cytotoxicity against HEK293 cells and hemolysis against red blood cells, and they demonstrated no cytotoxicity nor hemolytic effects, suggesting they possess inherent antitubercular activity.
引用
收藏
页数:8
相关论文
共 50 条
  • [1] Design, synthesis and biological evaluation of novel flavone Mannich base derivatives as potential antibacterial agents
    Xian-Hai Lv
    Hao Liu
    Zi-Li Ren
    Wei Wang
    Feng Tang
    Hai-Qun Cao
    Molecular Diversity, 2019, 23 : 299 - 306
  • [2] Design, synthesis and biological evaluation of novel flavone Mannich base derivatives as potential antibacterial agents
    Lv, Xian-Hai
    Liu, Hao
    Ren, Zi-Li
    Wang, Wei
    Tang, Feng
    Cao, Hai-Qun
    MOLECULAR DIVERSITY, 2019, 23 (02) : 299 - 306
  • [3] ANTIBACTERIAL ACTIVITIES OF NITROTHIAZOLE DERIVATIVES
    HOF, H
    ZAK, O
    SCHWEIZER, E
    DENZLER, A
    JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY, 1984, 14 (01) : 31 - 39
  • [4] Synthesis and antitumor activity evaluation of coumarin Mannich base derivatives
    He, Bing
    Ding, Le
    Tan, Hong-zhou
    Liu, Cheng-bo
    He, Li-qin
    CHEMICAL BIOLOGY & DRUG DESIGN, 2024, 103 (01)
  • [5] SYNTHESIS AND ANTIBACTERIAL EVALUATION OF SOME NOVEL MANNICH BASES OF BENZIMIDAZOLE DERIVATIVES
    Ahmadi, A.
    BULLETIN OF THE CHEMICAL SOCIETY OF ETHIOPIA, 2016, 30 (03) : 421 - 425
  • [6] Synthesis of Mannich base derivatives of berberine and evaluation of their anticancer and antioxidant effects
    Mistry, Bhupendra
    Patel, Rahul V.
    Keum, Young Soo
    Noorzai, Rafi
    Gansukh, Enkhtaivan
    Kim, Doo Hwan
    JOURNAL OF CHEMICAL RESEARCH, 2016, (02) : 73 - 77
  • [7] Synthesis and Antitumor Evaluation of a Novel Class of Chalcone Mannich Base Derivatives
    He, Bing
    Tan, Hong-zhou
    Liu, Cheng-bo
    Wu, Hong
    He, Li-qin
    CHEMICAL BIOLOGY & DRUG DESIGN, 2025, 105 (03)
  • [8] Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation
    Paucar, Rocio
    Martin-Escolano, Ruben
    Moreno-Viguri, Elsa
    Azqueta, Amaya
    Cirauqui, Nuria
    Marin, Clotilde
    Sanchez-Moreno, Manuel
    Perez-Silanes, Silvia
    BIOORGANIC & MEDICINAL CHEMISTRY, 2019, 27 (17) : 3902 - 3917
  • [9] Synthesis and In Vitro Cytotoxic Activity Evaluation of Novel Mannich Bases and Modified AZT Derivatives Possessing Mannich Base Moieties via Click Chemistry
    Tran Khac Vu
    Patil, Sachin Prakash
    Park, Yoo Jin
    Do Thi Thao
    LETTERS IN DRUG DESIGN & DISCOVERY, 2013, 10 (07) : 585 - 593
  • [10] Lipophilic quinolone derivatives: Synthesis and in vitro antibacterial evaluation
    Sadowski, Elodie
    Bercot, Beatrice
    Chauffour, Aurelie
    Gomez, Catherine
    Varon, Emmanuelle
    Mainardis, Mary
    Sougakoff, Wladimir
    Mayer, Claudine
    Sachon, Emmanuelle
    Anquetin, Guillaume
    Aubry, Alexandra
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2022, 55