Title of article :
Synthesis of Novel Fluorene Bisamide Derivatives via Ugi Reaction and Evaluation their Biological Activity against Mycobacterium species
Author/Authors :
Rezayan, Ali Hossein Department of Life Science Engineering - Faculty of New Sciences and Technologies - University of Tehran, ,Tehran, Iran , Hariri, Safoura Drug Design and Bioinformatics Unit - Department of Medical Biotechnology - Biotechnology Research Center - Pasteur Institute of Iran, Tehran, Iran , Azerang, Parisa Drug Design and Bioinformatics Unit - Department of Medical Biotechnology - Biotechnology Research Center - Pasteur Institute of Iran, Tehran, Iran , Ghavami, Ghazaleh Drug Design and Bioinformatics Unit - Department of Medical Biotechnology - Biotechnology Research Center - Pasteur Institute of Iran, Tehran, Iran , Portugal, Isabel iMed.ULisboa - Instituto de Investigação do Medicamento - Faculdade de Farmácia da Universidade de Lisboa - Av. das Forcas Armadas 1649-019 Lisboa, Portugal , Sardari, Soroush Drug Design and Bioinformatics Unit - Department of Medical Biotechnology - Biotechnology Research Center - Pasteur Institute of Iran, Tehran, Iran
Abstract :
A series of new fluorene bisamide derivatives were synthesized through multi-component
Ugi reaction and tested for their in-vitro anti-mycobacterial activity. The structures of the
products 5a-w were deduced from their IR, 1H NMR, and 13C NMR spectra. Elemental
analyses (CHN) for novel compounds (5a, 5d, 5f, 5h, 5k, 5l, 5p, 5s, 5t, 5v, 5w) was done.
These compounds were evaluated as anti-bacterial agents against Mycobacterium bovis and M.
tuberculosis, while their activity expressed as the minimum inhibitory concentration (MIC) in
μg/mL. Among the twenty-three synthesized compounds, 5a was found to be the most active
compound in vitro with MIC of 1.95 μg/mL against Mycobactrium bovis and compound 5k
showed greatest potency against sensitive and resistant strains of M. tuberculosis (H37Rv,
IHMT149/09, HPV115/08, and HPV65/08).
Keywords :
brine shrimp toxicity study , fluorene bisamide derivatives , Mycobacterium bovis , Ugi reaction , multi-component reaction
Journal title :
Astroparticle Physics
