@article{PAR00010525, title = {{H}ydrophobicity of imidazole derivatives correlates with improved activity against human methanogenic archaea}, author = {{K}helaifia, {S}. and {B}runel, {J}. {M}. and {R}aoult, {D}idier and {D}rancourt, {M}.}, editor = {}, language = {{ENG}}, abstract = {{M}ethanogenic archaea are involved in periodontitis in humans. {T}hey have also been implicated in digestive tract pathologies and obesity. {T}hese microorganisms are broadly resistant to antibiotics, except for metronidazole and ornidazole. {I}n this study, eight imidazole derivatives were synthesised and their in vitro cytotoxicity and activity against six species of methanogenic archaea, including {M}ethanobrevibacter smithii, {M}ethanobrevibacter oralis, {M}ethanosphaera stadtmanae, {M}ethanobacterium beijingense, {M}ethanosaeta concilii and {M}ethanomassiliicoccus luminyensis, were tested. {W}hilst the effective half-maximum cytotoxic concentrations ({EC}50 values) of all compounds were <= 50 mg/{L}, minimum inhibitory concentrations ({MIC}s) were 0.05-0.8 mg/{L} for most methanogenic archaea and 0.1-1 mg/{L} for {M}. stadtmanae. {T}hese results indicated a >20-400 therapeutic index ({EC}50/{MIC}) for these compounds, which compared with metronidazole exhibited 1-log increased activity against methanogenic archaea cultured from the human microbiota. {T}hese compounds are therefore promising molecules for the treatment of methanogenic archaea-related infections.}, keywords = {{H}uman methanogenic archaea ; {M}icrobiota ; {A}nti-archaea agents ; {S}usceptibility testing ; {I}n vitro activity ; {M}etronidazole derivative}, booktitle = {}, journal = {{I}nternational {J}ournal of {A}ntimicrobial {A}gents}, volume = {41}, numero = {6}, pages = {544--547}, ISSN = {0924-8579}, year = {2013}, DOI = {10.1016/j.ijantimicag.2013.02.013}, URL = {https://www.documentation.ird.fr/hor/{PAR}00010525}, }