title: An efficient synthesis of aryloxyphenyl cyclopropyl methanones: a new class of anti-mycobacterial agents.
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.
authors.affiliation: Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow-226001, India.
authors.forename: Namrata
authors.initials: N
authors.lastname: Dwivedi
authors.forename: Neetu
authors.initials: N
authors.lastname: Tewari
authors.forename: V K
authors.initials: VK
authors.lastname: Tiwari
authors.forename: Vinita
authors.initials: V
authors.lastname: Chaturvedi
authors.forename: Y K
authors.initials: YK
authors.lastname: Manju
authors.forename: A
authors.initials: A
authors.lastname: Srivastava
authors.forename: A
authors.initials: A
authors.lastname: Giakwad
authors.forename: S
authors.initials: S
authors.lastname: Sinha
authors.forename: R P
authors.initials: RP
authors.lastname: Tripathi
mesh_terms: D000818:Animals; D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D008697:Methane / Q000737:chemistry*; D051379:Mice; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects
chemical_list: D000995:Antitubercular Agents; D008697:Methane