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10.1080/14756366.2017.1326915 http://scihub22266oqcxt.onion/10.1080/14756366.2017.1326915 C5927774!5927774!28612630     free     free     free Deprecated: Implicit conversion from float 233.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 233.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 233.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 233.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534       J+Enzyme+Inhib+Med+Chem 2017 ; 32 (1): 821-31 Nephropedia Template TP {{tp|p=28612630|t=2017. Isoxazol-5(2H)-one: a new scaffold for potent human neutrophil elastase (HNE) inhibitors |pdf=|usr=}}{{28612630}} gab.com Text Isoxazol-5(2H)-one: a new scaffold for potent human neutrophil elastase (HNE) inhibitors JO: J Enzyme Inhib Med Chem http://www.kidney.de/pget.php?&tw=1&pmid=28612630 #FOAvip Human neutrophil elastase (HNE) is an important target for the development of novel and selective inhibitors to treat inflammatory diseases, especially pulmonary pathologies. Here, we report the synthesis, structure?activity relationship analysis, and biological evaluation of a new series of HNE inhibitors with an isoxazol-5(2H)-one scaffold. The most potent compound (2o) had a good balance between HNE inhibitory activity (IC50 value =20?nM) and chemical stability in aqueous buffer (t1/2=8.9?h). Analysis of reaction kinetics revealed that the most potent isoxazolone derivatives were reversible competitive inhibitors of HNE. Furthermore, since compounds 2o and 2s contain two carbonyl groups (2-N-CO and 5-CO) as possible points of attack for Ser195, the amino acid of the active site responsible for the nucleophilic attack, docking studies allowed us to clarify the different roles played by these groups. Twit Text FOAVip Isoxazol-5(2H)-one: a new scaffold for potent human neutrophil elastase (HNE) inhibitors ????J Enzyme Inhib Med Chem http://www.kidney.de/pget.php?&tw=1&pmid=28612630 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=28612630 #FOAvip English Wikipedia <ref>{{Cite pmid|28612630}}</ref> Isoxazol-5(2H)-one: a new scaffold for potent human neutrophil elastase (HNE) inhibitors #MMPMID28612630 Vergelli C; Schepetkin IA; Crocetti L; Iacovone A; Giovannoni MP; Guerrini G; Khlebnikov AI; Ciattini S; Ciciani G; Quinn MT J Enzyme Inhib Med Chem 2017[]; 32 (1): 821-31 PMID28612630show ga Human neutrophil elastase (HNE) is an important target for the development of novel and selective inhibitors to treat inflammatory diseases, especially pulmonary pathologies. Here, we report the synthesis, structure?activity relationship analysis, and biological evaluation of a new series of HNE inhibitors with an isoxazol-5(2H)-one scaffold. The most potent compound (2o) had a good balance between HNE inhibitory activity (IC50 value =20?nM) and chemical stability in aqueous buffer (t1/2=8.9?h). Analysis of reaction kinetics revealed that the most potent isoxazolone derivatives were reversible competitive inhibitors of HNE. Furthermore, since compounds 2o and 2s contain two carbonyl groups (2-N-CO and 5-CO) as possible points of attack for Ser195, the amino acid of the active site responsible for the nucleophilic attack, docking studies allowed us to clarify the different roles played by these groups. äIsoxazol-5(2H)-one: a new scaffold for potent human neutrophil elastas(epmc).pdf DeepDyve Pubget Overpricing