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10.1016/j.bmcl.2014.09.067 http://scihub22266oqcxt.onion/10.1016/j.bmcl.2014.09.067 C4255153!4255153 !25452003     free     free     free Warning: file_get_contents(https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&id=25452003 &cmd=llinks): Failed to open stream: HTTP request failed! HTTP/1.1 429 Too Many Requests in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 215 Deprecated: Implicit conversion from float 209.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 209.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 209.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 209.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 243.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 243.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 243.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 243.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Warning: imagejpeg(C:\Inetpub\vhosts\kidney.de\httpdocs\phplern\25452003 .jpg): Failed to open stream: No such file or directory in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 117       Bioorg+Med+Chem+Lett 2014 ; 24 (24 ): 5840-5844 Nephropedia Template TP {{tp|p=25452003 |t=2014. ?F508-CFTR correctors: synthesis and evaluation of thiazole-tethered imidazolones, oxazoles, oxadiazoles, and thiadiazoles |pdf=|usr=}}{{25452003 }} gab.com Text F508-CFTR correctors: synthesis and evaluation of thiazole-tethered imidazolones, oxazoles, oxadiazoles, and thiadiazoles JO: Bioorg Med Chem Lett http://www.kidney.de/pget.php?&tw=1&pmid=25452003 #FOAvip The most common mutation causing cystic fibrosis (CF) is deletion of phenylalanine residue 508 in the cystic fibrosis transmembrane regulator conductance (CFTR) protein. Small molecules that are able to correct the misfolding of defective ?F508-CFTR have considerable promise for therapy. Reported here are the design, preparation, and evaluation of five more hydrophilic bisazole analogs of previously identified bithiazole CF corrector 1. Interestingly, bisazole ?F508-CFTR corrector activity was not increased by incorporation of more H-bond acceptors (O or N), but correlated best with the overall bisazole molecular geometry. The structure activity data, together with molecular modeling, suggested that active bisazole correctors adopt a U-shaped conformation, and that corrector activity depends on the molecule's ability to access this molecular geometry. Twit Text FOAVip F508-CFTR correctors: synthesis and evaluation of thiazole-tethered imidazolones, oxazoles, oxadiazoles, and thiadiazoles ????Bioorg Med Chem Lett http://www.kidney.de/pget.php?&tw=1&pmid=25452003 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=25452003 #FOAvip English Wikipedia <ref>{{Cite pmid|25452003 }}</ref> ?F508-CFTR correctors: synthesis and evaluation of thiazole-tethered imidazolones, oxazoles, oxadiazoles, and thiadiazoles #MMPMID25452003 Ye L ; Hu B ; El-Badri F ; Hudson BM ; Phuan PW ; Verkman AS ; Tantillo DJ ; Kurth MJ Bioorg Med Chem Lett 2014[Dec]; 24 (24 ): 5840-5844 PMID25452003 show ga The most common mutation causing cystic fibrosis (CF) is deletion of phenylalanine residue 508 in the cystic fibrosis transmembrane regulator conductance (CFTR) protein. Small molecules that are able to correct the misfolding of defective ?F508-CFTR have considerable promise for therapy. Reported here are the design, preparation, and evaluation of five more hydrophilic bisazole analogs of previously identified bithiazole CF corrector 1. Interestingly, bisazole ?F508-CFTR corrector activity was not increased by incorporation of more H-bond acceptors (O or N), but correlated best with the overall bisazole molecular geometry. The structure activity data, together with molecular modeling, suggested that active bisazole correctors adopt a U-shaped conformation, and that corrector activity depends on the molecule's ability to access this molecular geometry. |Cystic Fibrosis Transmembrane Conductance Regulator/*chemistry/metabolism [MESH] |Cystic Fibrosis/metabolism/pathology [MESH] |Humans [MESH] |Imidazoles/*chemistry/metabolism [MESH] |Kinetics [MESH] |Molecular Conformation [MESH] |Oxadiazoles/*chemistry/metabolism [MESH] |Oxazoles/*chemistry/metabolism [MESH] |Protein Binding [MESH] |Structure-Activity Relationship [MESH] |Thermodynamics [MESH] |Thiadiazoles/*chemistry/metabolism [MESH] |Thiazoles/chemistry [MESH]?F508-CFTR correctors: synthesis and evaluation of thiazole-tethered (epmc).pdf DeepDyve Pubget Overpricing