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10.1016/j.bmcl.2021.128202 http://scihub22266oqcxt.onion/10.1016/j.bmcl.2021.128202 34139325!ä!34139325 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 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 Deprecated: Implicit conversion from float 267.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 267.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 267.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 267.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 267.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534       Bioorg+Med+Chem+Lett 2021 ; 47 (ä): 128202 Nephropedia Template TP {{tp|p=34139325|t=2021. Development of potent and selective Cathepsin C inhibitors free of aortic binding liability by application of a conformational restriction strategy |pdf=|usr=}}{{34139325}} gab.com Text Development of potent and selective Cathepsin C inhibitors free of aortic binding liability by application of a conformational restriction strategy JO: Bioorg Med Chem Lett http://www.kidney.de/pget.php?&tw=1&pmid=34139325 #FOAvip Cathepsin C plays a key role in the activation of several degradative enzymes linked to tissue destruction in chronic inflammatory and autoimmune diseases. Therefore, Cathepsin C inhibitors could potentially be effective therapeutics for the treatment of diseases such as chronic obstructive pulmonary disease (COPD) or acute respiratory distress syndrome (ARDS). In our efforts towards the development of a novel series of Cathepsin C inhibitors, we started working around AZD5248 (1), an alpha-amino acid based scaffold having potential liability of aortic binding. A novel series of amidoacetonitrile based Cathepsin C inhibitors were developed by the application of a conformational restriction strategy on 1. In particular, this work led to the development of a potent and selective Cathepsin C inhibitor 3p, free of aortic binding liability. Twit Text FOAVip Development of potent and selective Cathepsin C inhibitors free of aortic binding liability by application of a conformational restriction strategy ????Bioorg Med Chem Lett http://www.kidney.de/pget.php?&tw=1&pmid=34139325 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=34139325 #FOAvip English Wikipedia <ref>{{Cite pmid|34139325}}</ref> Development of potent and selective Cathepsin C inhibitors free of aortic binding liability by application of a conformational restriction strategy #MMPMID34139325 Banerjee A; Velagaleti R; Patil S; Pawar M; Yadav P; Kadam P; Qadri MM; Chakraborti S; Saini JS; Behera DB; Karanjai K; Iyer PS; Gharat LA; Das S Bioorg Med Chem Lett 2021[Sep]; 47 (ä): 128202 PMID34139325show ga Cathepsin C plays a key role in the activation of several degradative enzymes linked to tissue destruction in chronic inflammatory and autoimmune diseases. Therefore, Cathepsin C inhibitors could potentially be effective therapeutics for the treatment of diseases such as chronic obstructive pulmonary disease (COPD) or acute respiratory distress syndrome (ARDS). In our efforts towards the development of a novel series of Cathepsin C inhibitors, we started working around AZD5248 (1), an alpha-amino acid based scaffold having potential liability of aortic binding. A novel series of amidoacetonitrile based Cathepsin C inhibitors were developed by the application of a conformational restriction strategy on 1. In particular, this work led to the development of a potent and selective Cathepsin C inhibitor 3p, free of aortic binding liability. |*COVID-19 Drug Treatment[MESH] |Acetonitriles/chemistry/pharmacology[MESH] |Amino Acids/chemistry/pharmacology[MESH] |Aorta/*metabolism[MESH] |Biphenyl Compounds/pharmacology[MESH] |COVID-19/complications[MESH] |Cathepsin C/*antagonists & inhibitors[MESH] |Cysteine Proteinase Inhibitors/*chemical synthesis/*pharmacology[MESH] |Humans[MESH] |Models, Molecular[MESH] |Molecular Structure[MESH] |Respiratory Distress Syndrome/*drug therapy/etiology[MESH]Development of potent and selective Cathepsin C inhibitors free of aor(epmc).pdf DeepDyve Pubget Overpricing