title: Efficient synthesis of new (R)-2-amino-1-butanol derived ureas, thioureas and acylthioureas and in vitro evaluation of their antimycobacterial activity.
abstract: The synthesis of 22 structurally diverse urea, thiourea and acylthiourea derivatives containing the (R)-2-amino-1-butanol motif has been performed. The evaluation of their in vitro activity against Mycobacterium tuberculosis (H37Rv and strain 43) showed promising results in the case of the acylthiourea derivatives (MIC range 0.36-7.46 μM for H37Rv strain).
authors.affiliation: Institute of Organic Chemistry with Centre of Phytochemistry, Bulgarian Academy of Sciences, Bl. 9, Acad. G. Bonchev Str., Sofia 1113, Bulgaria. gmdob@orgchm.bas.bg
authors.forename: Georgi M
authors.initials: GM
authors.lastname: Dobrikov
authors.forename: Violeta
authors.initials: V
authors.lastname: Valcheva
authors.forename: Yana
authors.initials: Y
authors.lastname: Nikolova
authors.forename: Iva
authors.initials: I
authors.lastname: Ugrinova
authors.forename: Evdokia
authors.initials: E
authors.lastname: Pasheva
authors.forename: Vladimir
authors.initials: V
authors.lastname: Dimitrov
mesh_terms: D000215:Acylation; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D057809:HEK293 Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D008826:Microbial Sensitivity Tests; D008956:Models, Chemical; D015394:Molecular Structure; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D013890:Thiourea / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D014508:Urea / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000900:Anti-Bacterial Agents; D000995:Antitubercular Agents; D014508:Urea; D013890:Thiourea