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Bioorg Med Chem Lett ; 15(20): 4526-30, 2005 Oct 15.
Article in English | MEDLINE | ID: mdl-16087335

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 microg/mL. The most active compounds showed activity against MDR strains and two of them (14 and 16) showed marginal enhancement of MST in mice.


Subject(s)
Antitubercular Agents/chemical synthesis , Antitubercular Agents/pharmacology , Methane/chemistry , Animals , Antitubercular Agents/chemistry , Mice , Microbial Sensitivity Tests , Mycobacterium tuberculosis/drug effects
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