Matches in SemOpenAlex for { <https://semopenalex.org/work/W4320731570> ?p ?o ?g. }
- W4320731570 endingPage "115211" @default.
- W4320731570 startingPage "115211" @default.
- W4320731570 abstract "Amongst different forms of leishmaniasis, visceral leishmaniasis caused by L. donovani is highly mortal. Identification of new hit compounds might afford new starting points to develop novel therapeutics. In this lieu, a rationally designed small library of bestatin analogs-4-quinolone hybrids were prepared and evaluated. Analysis of SAR unveiled distinct profiles for hybrids type 1 and type 2, which might arise from their different molecular targets. Amongst type 1 bestatin analog-4-quinolone hybrids, hybrid 1e was identified as potential hit inhibiting growth of L. donovani promastigotes by 91 and 53% at 50 and 25 μM concentrations, respectively. Meanwhile, hybrid 2j was identified amongst type 2 bestatin analog-4-quinolone hybrids as potential hit compound inhibiting growth of L. donovani promastigotes by 50 and 38% at 50 and 25 μM concentrations, respectively. Preliminary safety evaluation of the promising hit compounds showed that they are 50-100 folds safer against human derived monocytic THP-1 cells relative to the drug erufosine. In silico study was conducted to predict the possible binding of hybrid 1e with methionine aminopeptidases 1 and 2 of L. donovani. Molecular dynamic simulations verified the predicted binding modes and provide more in depth understanding of the impact of hybrid 1e on LdMetAP-1 and LdMetAP-2." @default.
- W4320731570 created "2023-02-15" @default.
- W4320731570 creator A5007980365 @default.
- W4320731570 creator A5008682765 @default.
- W4320731570 creator A5012171127 @default.
- W4320731570 creator A5034436308 @default.
- W4320731570 creator A5034944739 @default.
- W4320731570 creator A5040340882 @default.
- W4320731570 creator A5065962329 @default.
- W4320731570 creator A5078317517 @default.
- W4320731570 creator A5078994362 @default.
- W4320731570 creator A5084793653 @default.
- W4320731570 creator A5090037972 @default.
- W4320731570 creator A5091899482 @default.
- W4320731570 creator A5058103195 @default.
- W4320731570 date "2023-03-01" @default.
- W4320731570 modified "2023-10-14" @default.
- W4320731570 title "Bestatin analogs-4-quinolinone hybrids as antileishmanial hits: Design, repurposing rational, synthesis, in vitro and in silico studies" @default.
- W4320731570 cites W1031578623 @default.
- W4320731570 cites W1991283241 @default.
- W4320731570 cites W1998652314 @default.
- W4320731570 cites W2018416180 @default.
- W4320731570 cites W2036457196 @default.
- W4320731570 cites W2049815105 @default.
- W4320731570 cites W2062607076 @default.
- W4320731570 cites W2085785716 @default.
- W4320731570 cites W2100121002 @default.
- W4320731570 cites W2166550586 @default.
- W4320731570 cites W2222678458 @default.
- W4320731570 cites W2309277975 @default.
- W4320731570 cites W2323468907 @default.
- W4320731570 cites W2412330801 @default.
- W4320731570 cites W2556781592 @default.
- W4320731570 cites W2571503744 @default.
- W4320731570 cites W2593458328 @default.
- W4320731570 cites W2645797961 @default.
- W4320731570 cites W2736621155 @default.
- W4320731570 cites W2766523394 @default.
- W4320731570 cites W2786074364 @default.
- W4320731570 cites W2799333555 @default.
- W4320731570 cites W2811473578 @default.
- W4320731570 cites W2890349729 @default.
- W4320731570 cites W2899515869 @default.
- W4320731570 cites W2901134045 @default.
- W4320731570 cites W2944225234 @default.
- W4320731570 cites W2951512731 @default.
- W4320731570 cites W2959985586 @default.
- W4320731570 cites W2974926176 @default.
- W4320731570 cites W2983316962 @default.
- W4320731570 cites W2988319662 @default.
- W4320731570 cites W2992112979 @default.
- W4320731570 cites W2993277558 @default.
- W4320731570 cites W3002084745 @default.
- W4320731570 cites W3012358147 @default.
- W4320731570 cites W3013498471 @default.
- W4320731570 cites W3018119281 @default.
- W4320731570 cites W3044060270 @default.
- W4320731570 cites W3080876646 @default.
- W4320731570 cites W3113458973 @default.
- W4320731570 cites W3116613266 @default.
- W4320731570 cites W3119952098 @default.
- W4320731570 cites W3123997054 @default.
- W4320731570 cites W3195268212 @default.
- W4320731570 cites W3200075100 @default.
- W4320731570 cites W3212058642 @default.
- W4320731570 cites W4214668673 @default.
- W4320731570 cites W4280492105 @default.
- W4320731570 cites W4282937816 @default.
- W4320731570 cites W4293769572 @default.
- W4320731570 doi "https://doi.org/10.1016/j.ejmech.2023.115211" @default.
- W4320731570 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/36827952" @default.
- W4320731570 hasPublicationYear "2023" @default.
- W4320731570 type Work @default.
- W4320731570 citedByCount "4" @default.
- W4320731570 countsByYear W43207315702023 @default.
- W4320731570 crossrefType "journal-article" @default.
- W4320731570 hasAuthorship W4320731570A5007980365 @default.
- W4320731570 hasAuthorship W4320731570A5008682765 @default.
- W4320731570 hasAuthorship W4320731570A5012171127 @default.
- W4320731570 hasAuthorship W4320731570A5034436308 @default.
- W4320731570 hasAuthorship W4320731570A5034944739 @default.
- W4320731570 hasAuthorship W4320731570A5040340882 @default.
- W4320731570 hasAuthorship W4320731570A5058103195 @default.
- W4320731570 hasAuthorship W4320731570A5065962329 @default.
- W4320731570 hasAuthorship W4320731570A5078317517 @default.
- W4320731570 hasAuthorship W4320731570A5078994362 @default.
- W4320731570 hasAuthorship W4320731570A5084793653 @default.
- W4320731570 hasAuthorship W4320731570A5090037972 @default.
- W4320731570 hasAuthorship W4320731570A5091899482 @default.
- W4320731570 hasConcept C104317684 @default.
- W4320731570 hasConcept C185592680 @default.
- W4320731570 hasConcept C202751555 @default.
- W4320731570 hasConcept C21951064 @default.
- W4320731570 hasConcept C2775905019 @default.
- W4320731570 hasConcept C2776555147 @default.
- W4320731570 hasConcept C2778689377 @default.
- W4320731570 hasConcept C2779922871 @default.
- W4320731570 hasConcept C2781333301 @default.