原创力文档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
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
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