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10.1080/14756366.2018.1457657 http://scihub22266oqcxt.onion/10.1080/14756366.2018.1457657 C6009894!6009894!29651867     free     free     free Deprecated: Implicit conversion from float 211.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 211.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 211.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 211.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 211.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 245.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 245.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 245.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 245.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 245.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 245.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 278.79999999999995 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\29651867.jpg): Failed to open stream: No such file or directory in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 117       J+Enzyme+Inhib+Med+Chem 2018 ; 33 (1): 755-67 Nephropedia Template TP {{tp|p=29651867|t=2018. Molecular modelling insights into a physiologically favourable approach to eicosanoid biosynthesis inhibition through novel thieno 2,3-b pyridine derivatives |pdf=|usr=}}{{29651867}} gab.com Text Molecular modelling insights into a physiologically favourable approach to eicosanoid biosynthesis inhibition through novel thieno 2,3-b pyridine derivatives JO: J Enzyme Inhib Med Chem http://www.kidney.de/pget.php?&tw=1&pmid=29651867 #FOAvip In this research, we exploited derivatives of thieno[2,3-b]pyridine as dual inhibitors of the key enzymes in eicosanoid biosynthesis, cyclooxygenase (COX, subtypes 1 and 2) and 5-lipoxygensase (5-LOX). Testing these compounds in a rat paw oedema model revealed potency higher than ibuprofen. The most active compounds 7a, 7b, 8b, and 8c were screened against COX-1/2 and 5-LOX enzymes. Compound 7a was the most powerful inhibitor of 5-LOX with IC50?=?0.15?µM, while its p-chloro analogue 7b was more active against COX-2 (IC50?=?7.5?µM). The less desirable target COX-1 was inhibited more potently by 8c with IC50?=?7.7?µM. Surflex docking programme predicted that the more stable anti- conformer of compound (7a) formed a favourable complex with the active site of 5-LOX but not COX-1. This is in contrast to the binding mode of 8c, which resembles the syn-conformer of series 7 and binds favourably to COX-1. Twit Text FOAVip Molecular modelling insights into a physiologically favourable approach to eicosanoid biosynthesis inhibition through novel thieno 2,3-b pyridine derivatives ????J Enzyme Inhib Med Chem http://www.kidney.de/pget.php?&tw=1&pmid=29651867 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=29651867 #FOAvip English Wikipedia <ref>{{Cite pmid|29651867}}</ref> Molecular modelling insights into a physiologically favourable approach to eicosanoid biosynthesis inhibition through novel thieno 2,3-b pyridine derivatives #MMPMID29651867 Mohamed MS; Mansour YE; Amin HK; El-Araby ME J Enzyme Inhib Med Chem 2018[]; 33 (1): 755-67 PMID29651867show ga In this research, we exploited derivatives of thieno[2,3-b]pyridine as dual inhibitors of the key enzymes in eicosanoid biosynthesis, cyclooxygenase (COX, subtypes 1 and 2) and 5-lipoxygensase (5-LOX). Testing these compounds in a rat paw oedema model revealed potency higher than ibuprofen. The most active compounds 7a, 7b, 8b, and 8c were screened against COX-1/2 and 5-LOX enzymes. Compound 7a was the most powerful inhibitor of 5-LOX with IC50?=?0.15?µM, while its p-chloro analogue 7b was more active against COX-2 (IC50?=?7.5?µM). The less desirable target COX-1 was inhibited more potently by 8c with IC50?=?7.7?µM. Surflex docking programme predicted that the more stable anti- conformer of compound (7a) formed a favourable complex with the active site of 5-LOX but not COX-1. This is in contrast to the binding mode of 8c, which resembles the syn-conformer of series 7 and binds favourably to COX-1. äMolecular modelling insights into a physiologically favourable approac(epmc).pdf DeepDyve Pubget Overpricing