title: Enantiopure antituberculosis candidates synthesized from (-)-fenchone.
abstract: The synthesis of new enantiopure N-acyl compounds derived from (-)-fenchone has been performed. The evaluation of their in vitro activity against Mycobacterium tuberculosis H37Rv showed for most of them moderate activity. The structures bearing sulfonamide functionality have comparable activity to ethambutol and possess low cytotoxicity.
authors.affiliation: Institute of Organic Chemistry with Centre of Phytochemistry, Bulgarian Academy of Sciences, Bl. 9, Acad. G. Bonchev Str., Sofia 1113, Bulgaria. Electronic address: gmdob@orgchm.bas.bg.
authors.forename: Georgi M
authors.initials: GM
authors.lastname: Dobrikov
authors.affiliation: Stephan Angeloff Institute of Microbiology, Bulgarian Academy of Sciences, Bl. 26, Acad. G. Bonchev Str., Sofia 1113, Bulgaria.
authors.forename: Violeta
authors.initials: V
authors.lastname: Valcheva
authors.affiliation: Institute of Organic Chemistry with Centre of Phytochemistry, Bulgarian Academy of Sciences, Bl. 9, Acad. G. Bonchev Str., Sofia 1113, Bulgaria.
authors.forename: Yana
authors.initials: Y
authors.lastname: Nikolova
authors.affiliation: Institute of Molecular Biology "Roumen Tsanev", Bulgarian Academy of Sciences, Bl. 21, Acad. G. Bonchev Str., Sofia 1113, Bulgaria.
authors.forename: Iva
authors.initials: I
authors.lastname: Ugrinova
authors.affiliation: Institute of Molecular Biology "Roumen Tsanev", Bulgarian Academy of Sciences, Bl. 21, Acad. G. Bonchev Str., Sofia 1113, Bulgaria.
authors.forename: Evdokia
authors.initials: E
authors.lastname: Pasheva
authors.affiliation: Institute of Organic Chemistry with Centre of Phytochemistry, Bulgarian Academy of Sciences, Bl. 9, Acad. G. Bonchev Str., Sofia 1113, Bulgaria.
authors.forename: Vladimir
authors.initials: V
authors.lastname: Dimitrov
mesh_terms: D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001892:Camphanes; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004977:Ethambutol / Q000494:pharmacology; D057809:HEK293 Cells; D006801:Humans; D008826:Microbial Sensitivity Tests; D008968:Molecular Conformation; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D009636:Norbornanes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000737:chemistry
chemical_list: D000995:Antitubercular Agents; D001892:Camphanes; D009636:Norbornanes; D013449:Sulfonamides; C027327:fenchone; D004977:Ethambutol
keywords: Amides; Antimycobacterial; Chiral; Fenchone; Tuberculosis