Synthesis and biological evaluation of trans 6-methoxy-1,1-dimethyl-2-phenyl-3-aryl-2,3-dihydro-1H-inden-4-yloxyalkylamine derivatives against drug susceptible,non-replicating M. tuberculosis H37Rv and clinical multidrug resistant strains |
| |
| Authors: | Shailesh Kumar Atma P Dwivedi Vivek Kr Kashyap AK Saxena AK Dwivedi Ranjana Srivastava Devi P Sahu |
| |
| Affiliation: | 1. Medicinal and Process Chemistry Division, CSIR, Central Drug Research Institute, Lucknow 226001, India;2. Microbiology Division, CSIR, Central Drug Research Institute, Lucknow 226001, India;3. Pharmaceutics Division, CSIR, Central Drug Research Institute, Lucknow 226001, India |
| |
| Abstract: | Synthesis of a library of novel trans 6-methoxy-1,1-dimethyl-2-phenyl-3-aryl-2,3-dihydro-1H-inden-4-yloxy alkyl amines and their antimycobacterial activity against drug sensitive and multidrug resistant strains of Mycobacterium tuberculosis have been reported. All the new compounds in the series exhibited MIC between 1.56 and 6.25 μg/ml. Two compounds 1i and 1j with low MIC and low cytotoxicity showed significant reduction in CFU in infected mouse macrophages at 1× MIC concentration. The compound 1i inhibited the growth of M. tuberculosis in mice at 100 mg/kg dose with 1.35 log10 reduction of CFU in lungs tissue and was active against non-replicating Mycobacterium tuberculosis under anaerobic condition. |
| |
| Keywords: | |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
