63478-10-4Relevant articles and documents
Synthesis and Antimicrobial Activity of Burkholderia-Related 4-Hydroxy-3-methyl-2-alkenylquinolines (HMAQs) and Their N-Oxide Counterparts
Caulet, Armand,Coulon, Pauline M. L.,Déziel, Eric,Gauthier, Charles,Groleau, Marie-Christine,Piochon, Marianne
supporting information, p. 2145 - 2154 (2020/07/27)
The Burkholderia genus offers a promising potential in medicine because of the diversity of biologically active natural products encoded in its genome. Some pathogenic Burkholderia spp. biosynthesize a specific class of antimicrobial 2-alkyl-4(1H)-quinolo
Rational Design, Synthesis, and Biological Evaluation of Heterocyclic Quinolones Targeting the Respiratory Chain of Mycobacterium tuberculosis
Hong, W. David,Gibbons, Peter D.,Leung, Suet C.,Amewu, Richard,Stocks, Paul A.,Stachulski, Andrew,Horta, Pedro,Cristiano, Maria L. S.,Shone, Alison E.,Moss, Darren,Ardrey, Alison,Sharma, Raman,Warman, Ashley J.,Bedingfield, Paul T. P.,Fisher, Nicholas E.,Aljayyoussi, Ghaith,Mead, Sally,Caws, Maxine,Berry, Neil G.,Ward, Stephen A.,Biagini, Giancarlo A.,O’Neill, Paul M.,Nixon, Gemma L.
supporting information, p. 3703 - 3726 (2017/05/19)
A high-throughput screen (HTS) was undertaken against the respiratory chain dehydrogenase component, NADH:menaquinone oxidoreductase (Ndh) of Mycobacterium tuberculosis (Mtb). The 11000 compounds were selected for the HTS based on the known phenothiazine Ndh inhibitors, trifluoperazine and thioridazine. Combined HTS (11000 compounds) and in-house screening of a limited number of quinolones (50 compounds) identified ～100 hits and four distinct chemotypes, the most promising of which contained the quinolone core. Subsequent Mtb screening of the complete in-house quinolone library (350 compounds) identified a further ～90 hits across three quinolone subtemplates. Quinolones containing the amine-based side chain were selected as the pharmacophore for further modification, resulting in metabolically stable quinolones effective against multi drug resistant (MDR) Mtb. The lead compound, 42a (MTC420), displays acceptable antituberculosis activity (Mtb IC50 = 525 nM, Mtb Wayne IC50 = 76 nM, and MDR Mtb patient isolates IC50 = 140 nM) and favorable pharmacokinetic and toxicological profiles.
Synthesis, structural investigations and ethylene polymerization of titanium complexes with tripodal oxazoline ligands
Hafeez, Muhammad,Lippert, Sonja,Bauer, Tobias,Kretschmer, Winfried P.
, p. 957 - 966 (2015/05/05)
Abstract A series of tripodal nitrogen containing ligands including amidine and aminopyridines with extra oxazoline functionality were synthesized. The corresponding titanium complexes bearing such ligands were synthesized by diethylamine elimination rout
