Matches in SemOpenAlex for { <https://semopenalex.org/work/W2052500196> ?p ?o ?g. }
- W2052500196 endingPage "5434" @default.
- W2052500196 startingPage "5419" @default.
- W2052500196 abstract "4-Aminoquinolone piperidine amides (AQs) were identified as a novel scaffold starting from a whole cell screen, with potent cidality on Mycobacterium tuberculosis (Mtb). Evaluation of the minimum inhibitory concentrations, followed by whole genome sequencing of mutants raised against AQs, identified decaprenylphosphoryl-β-d-ribose 2'-epimerase (DprE1) as the primary target responsible for the antitubercular activity. Mass spectrometry and enzyme kinetic studies indicated that AQs are noncovalent, reversible inhibitors of DprE1 with slow on rates and long residence times of ∼100 min on the enzyme. In general, AQs have excellent leadlike properties and good in vitro secondary pharmacology profile. Although the scaffold started off as a single active compound with moderate potency from the whole cell screen, structure-activity relationship optimization of the scaffold led to compounds with potent DprE1 inhibition (IC50 < 10 nM) along with potent cellular activity (MIC = 60 nM) against Mtb." @default.
- W2052500196 created "2016-06-24" @default.
- W2052500196 creator A5000473185 @default.
- W2052500196 creator A5004079817 @default.
- W2052500196 creator A5004141498 @default.
- W2052500196 creator A5008578572 @default.
- W2052500196 creator A5008833168 @default.
- W2052500196 creator A5009066976 @default.
- W2052500196 creator A5010531759 @default.
- W2052500196 creator A5011015453 @default.
- W2052500196 creator A5015090682 @default.
- W2052500196 creator A5015643996 @default.
- W2052500196 creator A5018240590 @default.
- W2052500196 creator A5020712978 @default.
- W2052500196 creator A5022577652 @default.
- W2052500196 creator A5023317950 @default.
- W2052500196 creator A5026468998 @default.
- W2052500196 creator A5027356006 @default.
- W2052500196 creator A5027715013 @default.
- W2052500196 creator A5028450220 @default.
- W2052500196 creator A5028625390 @default.
- W2052500196 creator A5030201796 @default.
- W2052500196 creator A5030751811 @default.
- W2052500196 creator A5031247182 @default.
- W2052500196 creator A5032292082 @default.
- W2052500196 creator A5032560846 @default.
- W2052500196 creator A5036473045 @default.
- W2052500196 creator A5036896295 @default.
- W2052500196 creator A5038669019 @default.
- W2052500196 creator A5040090562 @default.
- W2052500196 creator A5042155186 @default.
- W2052500196 creator A5044097768 @default.
- W2052500196 creator A5045698605 @default.
- W2052500196 creator A5046709270 @default.
- W2052500196 creator A5048188169 @default.
- W2052500196 creator A5048932567 @default.
- W2052500196 creator A5049627260 @default.
- W2052500196 creator A5054500278 @default.
- W2052500196 creator A5056766581 @default.
- W2052500196 creator A5060853327 @default.
- W2052500196 creator A5061594597 @default.
- W2052500196 creator A5065714552 @default.
- W2052500196 creator A5069018304 @default.
- W2052500196 creator A5069299314 @default.
- W2052500196 creator A5070368745 @default.
- W2052500196 creator A5073823398 @default.
- W2052500196 creator A5078612453 @default.
- W2052500196 creator A5082630436 @default.
- W2052500196 creator A5082885356 @default.
- W2052500196 creator A5083446220 @default.
- W2052500196 creator A5085957231 @default.
- W2052500196 creator A5087666815 @default.
- W2052500196 date "2014-06-11" @default.
- W2052500196 modified "2023-10-15" @default.
- W2052500196 title "4-Aminoquinolone Piperidine Amides: Noncovalent Inhibitors of DprE1 with Long Residence Time and Potent Antimycobacterial Activity" @default.
- W2052500196 cites W1502955574 @default.
- W2052500196 cites W1976256007 @default.
- W2052500196 cites W2010852549 @default.
- W2052500196 cites W2016408686 @default.
- W2052500196 cites W2039286264 @default.
- W2052500196 cites W2044917835 @default.
- W2052500196 cites W2063654019 @default.
- W2052500196 cites W2075222652 @default.
- W2052500196 cites W2085367819 @default.
- W2052500196 cites W2087292427 @default.
- W2052500196 cites W2089068540 @default.
- W2052500196 cites W2102377211 @default.
- W2052500196 cites W2106016791 @default.
- W2052500196 cites W2110483912 @default.
- W2052500196 cites W2126989272 @default.
- W2052500196 cites W2320887812 @default.
- W2052500196 doi "https://doi.org/10.1021/jm5005978" @default.
- W2052500196 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/24871036" @default.
- W2052500196 hasPublicationYear "2014" @default.
- W2052500196 type Work @default.
- W2052500196 sameAs 2052500196 @default.
- W2052500196 citedByCount "73" @default.
- W2052500196 countsByYear W20525001962015 @default.
- W2052500196 countsByYear W20525001962016 @default.
- W2052500196 countsByYear W20525001962017 @default.
- W2052500196 countsByYear W20525001962018 @default.
- W2052500196 countsByYear W20525001962019 @default.
- W2052500196 countsByYear W20525001962020 @default.
- W2052500196 countsByYear W20525001962021 @default.
- W2052500196 countsByYear W20525001962022 @default.
- W2052500196 countsByYear W20525001962023 @default.
- W2052500196 crossrefType "journal-article" @default.
- W2052500196 hasAuthorship W2052500196A5000473185 @default.
- W2052500196 hasAuthorship W2052500196A5004079817 @default.
- W2052500196 hasAuthorship W2052500196A5004141498 @default.
- W2052500196 hasAuthorship W2052500196A5008578572 @default.
- W2052500196 hasAuthorship W2052500196A5008833168 @default.
- W2052500196 hasAuthorship W2052500196A5009066976 @default.
- W2052500196 hasAuthorship W2052500196A5010531759 @default.
- W2052500196 hasAuthorship W2052500196A5011015453 @default.
- W2052500196 hasAuthorship W2052500196A5015090682 @default.
- W2052500196 hasAuthorship W2052500196A5015643996 @default.
- W2052500196 hasAuthorship W2052500196A5018240590 @default.