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
  • [21] SYNTHESIS AND IN VITRO AND IN VIVO ANTIMALARIAL ACTIVITY OF NOVEL 4-ANILINOQUINOLINE MANNICH BASE DERIVATIVES
    Singh, Bhupendra
    Chetia, Dipak
    Puri, S. K.
    Prakash, Anil
    MEDICINAL CHEMISTRY RESEARCH, 2010, 19 : S59 - S60
  • [22] Synthesis and in vitro study of novel Mannich bases as antibacterial agents
    Joshi, S
    Khosla, N
    Khare, D
    Sharda, R
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2005, 15 (01) : 221 - 226
  • [23] A step towards development of promising trypanocidal agents: Synthesis, characterization and in vitro biological evaluation of ferrocenyl Mannich base-type derivatives
    Paucar, Rocio
    Martin-Escolano, Ruben
    Moreno-Viguri, Elsa
    Cirauqui, Nuria
    Rangel Rodrigues, Carlos
    Marin, Clotilde
    Sanchez-Moreno, Manuel
    Perez-Silanes, Silvia
    Ravera, Mauro
    Gabano, Elisabetta
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2019, 163 : 569 - 582
  • [24] Synthesis, characterization and antibacterial studies of transition metal complexes of Mannich base
    Balakrishnan, K
    ASIAN JOURNAL OF CHEMISTRY, 2005, 17 (03) : 1935 - 1940
  • [25] Synthesis and In Vitro Antibacterial Evaluation of Some Novel Annulated Quinazolinone Derivatives
    A. I. El-Shenawy
    Russian Journal of General Chemistry, 2018, 88 : 1712 - 1719
  • [26] Synthesis and In Vitro Antibacterial Evaluation of Some Novel Annulated Quinazolinone Derivatives
    El-Shenawy, A. I.
    RUSSIAN JOURNAL OF GENERAL CHEMISTRY, 2018, 88 (08) : 1712 - 1719
  • [27] Synthesis and biological evaluation of 1, 3-dihydroxyxanthone mannich base derivatives as anticholinesterase agents
    Qin, Jiangke
    Lan, Wenli
    Liu, Zhong
    Huang, Jun
    Tang, Huang
    Wang, Hengshan
    CHEMISTRY CENTRAL JOURNAL, 2013, 7
  • [28] Synthesis and biological evaluation of 1, 3-dihydroxyxanthone mannich base derivatives as anticholinesterase agents
    Jiangke Qin
    Wenli Lan
    Zhong Liu
    Jun Huang
    Huang Tang
    Hengshan Wang
    Chemistry Central Journal, 7
  • [29] Facile synthesis and stereochemical investigation of Mannich base derivatives: Evaluation of antioxidant property and antituberculostic potency
    Parthiban, Paramasivam
    Subalakshmi, Viswalingam
    Balasubramanian, Krishnamurthy
    Islam, Md. Nurul
    Choi, Jae Sue
    Jeong, Yeon Tae
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2011, 21 (08) : 2287 - 2296
  • [30] Synthesis and Biological Activity of Benzodihydrofuran Neolignans and Their Mannich Base Derivatives
    Shi, Ling
    Wang, Caifang
    Xu, Yu
    Wang, Qiu'an
    CHINESE JOURNAL OF ORGANIC CHEMISTRY, 2015, 35 (07) : 1537 - 1543