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Open Access Research article

Synthesis and biological evaluation of propargyl acetate derivatives as anti-mycobacterial agents

Parisa Azerang1, Ali Hossein Rezayan2, Soroush Sardari1*, Farzad Kobarfard34, Mitra Bayat4 and Kimia Tabib3

Author Affiliations

1 Drug Design and Bioinformatics Unit, Medical Biotechnology Department, Biotechnology Research Center, Pasteur Institute, Tehran, Iran 13164

2 Department of Life Science Engineering, Faculty of New Science and Technology, University of Tehran, Tehran, Iran

3 Department of Medicinal Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran

4 Phytochemistry Research Centre, Shahid Beheshti University of Medical Sciences, Tehran, Iran

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DARU Journal of Pharmaceutical Sciences 2012, 20:90  doi:10.1186/2008-2231-20-90

Published: 11 December 2012

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)