2. Academic Validation
  3. 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

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

  • Bioorg Med Chem Lett. 2013 Apr 15;23(8):2404-7. doi: 10.1016/j.bmcl.2013.02.030.
Shailesh Kumar 1,  Atma P Dwivedi,  Vivek Kr Kashyap,  A K Saxena,  A K Dwivedi,  Ranjana Srivastava,  Devi P Sahu
Affiliations

Affiliation

  • 1 Medicinal and Process Chemistry Division, CSIR, Central Drug Research Institute, Lucknow 226001, India. drskum10@gmail.com
PMID: 23474387 DOI: 10.1016/j.bmcl.2013.02.030
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 100mg/kg dose with 1.35 log10 reduction of CFU in lungs tissue and was active against non-replicating Mycobacterium tuberculosis under anaerobic condition.

Figures