synthesis and biological evaluation of propargyl acetate derivatives as anti-mycobacterial agents炔丙基乙酸酯衍生物的合成和生物评价anti-mycobacterial代理.pdfVIP

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synthesis and biological evaluation of propargyl acetate derivatives as anti-mycobacterial agents炔丙基乙酸酯衍生物的合成和生物评价anti-mycobacterial代理.pdf

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synthesis and biological evaluation of propargyl acetate derivatives as anti-mycobacterial agents炔丙基乙酸酯衍生物的合成和生物评价anti-mycobacterial代理

Azerang et al. DARU Journal of Pharmaceutical Sciences 2012, 20:90 /content/20/1/90 RESEARCH ARTICLE Open Access Synthesis and biological evaluation of propargyl acetate derivatives as anti-mycobacterial agents 1 2 1* 3,4 4 3 Parisa Azerang , Ali Hossein Rezayan , Soroush Sardari , Farzad Kobarfard , Mitra Bayat and Kimia Tabib Abstract Background: The emergence of multidrug-resistant strains of Mycobacterium tuberculosis (Mtb) has intensified efforts to discover novel drugs for tuberculosis (TB) treatment. Targeting the persistent state of Mtb, a condition in which Mtb is resistant to conventional drug therapies, is of particular interest. Methods: This study is focused on propargyl acetate derivatives. Eight molecules were designed based on propargyl alcohols and different acid anhydrides. Results: All the synthesized compounds and commercially available ones were evaluated for anti-tuberculosis activity. Conclusions: Inhibitors against Mtb have been identified and characterized for further development into potential novel anti-tubercular drugs. Keywords: Mycobacterium tuberculosis, BCG, Propargyl alcohol, Acetylenic compounds (propargyl acetate derivatives) Background infectious disease caused by mycobacteria, mainly Mycobac- Tuberculosis (TB) is a deadly infectious disease and is terium tuberculosis (Mtb) [5]. The success of mycobacteria the leading cause of death worldwide, killing around 2 in producing disease relies entirely on its ability to utilize million people annually, primarily in developing coun- macrophages for its repl