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

Iranian Journal of Pharmaceutical Research

关键词: multi-component reaction;    Ugi reaction;    Mycobacterium bovis;    fluorene bisamide derivatives;    brine shrimp toxicity study;   

DOI  :  

学科分类：社会科学、人文和艺术（综合）

来源: Shaheed Beheshti Medical University * School of Pharmacy

【 摘 要 】

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 to. 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 1.95μg/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).

【 授权许可】

CC BY