title: Simple dihydrosphyngosine analogues with potent activity against MDR-Mycobacterium tuberculosis.
abstract: Fifteen dihydrosphingosine analogues have been synthesized and tested in vitro against Mycobacterium tuberculosis (MTB). Two ether (3 and 4b) and one diamine (8b) derivatives have displayed high mycobactericidal potency, with similar MIC values of 1.25 microg/mL, against the virulent strain H37Rv, as well as against a clinical isolate resistant to the five first-line anti-TB drugs. The three compounds, tested on other eleven cultured MTB strains with different multi-drug-resistance (MDR) patterns, retained their MIC values for most strains, or even lowered it, as in the case of compound 4b, which, assayed on strain No. 332, also resistant to all first-line anti-TB drugs, attained the MIC value of 0.78 microg/mL.
authors.affiliation: Departamento de Química Farmacéutica, Facultad de Farmacia, CIETUS, Universidad de Salamanca, Spain. olmo@usal.es
authors.forename: Esther
authors.initials: E
authors.lastname: Del Olmo
authors.forename: Gloria María
authors.initials: GM
authors.lastname: Molina-Salinas
authors.forename: Ricardo
authors.initials: R
authors.lastname: Escarcena
authors.forename: Mario
authors.initials: M
authors.lastname: Alves
authors.forename: José L
authors.initials: JL
authors.lastname: López-Pérez
authors.forename: Rogelio
authors.initials: R
authors.lastname: Hernandez-Pando
authors.forename: Salvador
authors.initials: S
authors.lastname: Said-Fernández
authors.forename: Arturo San
authors.initials: AS
authors.lastname: Feliciano
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D024901:Drug Resistance, Multiple, Bacterial; D006801:Humans; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D013110:Sphingosine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D018088:Tuberculosis, Multidrug-Resistant / Q000188:drug therapy
chemical_list: D000900:Anti-Bacterial Agents; D013110:Sphingosine; C005682:safingol