Author/Authors :
Namrata Dwivedi، نويسنده , , Neetu Tewari، نويسنده , , V.K. Tiwari، نويسنده , , Vinita Chaturvedi، نويسنده , , Y.K. Manju، نويسنده , , A. Srivastava، نويسنده , , A. Giakwad، نويسنده , , S. Sinha، نويسنده , , R.P Tripathi، نويسنده ,
Abstract :
An efficient, high yield and one-pot synthesis of phenyl cyclopropyl methanones by reaction of different aryl alcohols with 4′-fluoro-4-chloro-butyrophenone in THF/DMF in the presence of NaH/TBAB is reported. Most of the methanones were further reduced to respective alcohols or methylenes. All the compounds were evaluated for their anti-tubercular activities against M. tuberculosis H37Rv in vitro displaying MICs ranging from 25 to 3.125 μg/mL. The most active compounds showed activity against MDR strains and two of them (14 and 16) showed marginal enhancement of MST in mice.
Keywords :
Tetrabutylammonium bromide , Phenyl cyclopropyl methanones , Wolf–Kishner reduction , Tuberculosis
