Synthesis of Novel Fluorene Bisamide Derivatives via Ugi Reaction and Evaluation their Biological Activity against Mycobacterium species

通过Ugi反应合成新型芴双酰胺衍生物及其对分枝杆菌的生物活性评价

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作者:Ali Hossein Rezayan, Safoura Hariri, Parisa Azerang, Ghazaleh Ghavami, Isabel Portugal, Soroush Sardari

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).

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