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10.1080/14756366.2018.1457657 http://scihub22266oqcxt.onion/10.1080/14756366.2018.1457657 C6009894!6009894 !29651867     free     free     free Warning: file_get_contents(https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&id=29651867 &cmd=llinks): Failed to open stream: HTTP request failed! 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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 IC(50)?=?0.15?然, while its p-chloro analogue 7b was more active against COX-2 (IC(50)?=?7.5?然). The less desirable target COX-1 was inhibited more potently by 8c with IC(50)?=?7.7?然. 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[Dec]; 33 (1 ): 755-767 PMID29651867 show 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 IC(50)?=?0.15?然, while its p-chloro analogue 7b was more active against COX-2 (IC(50)?=?7.5?然). The less desirable target COX-1 was inhibited more potently by 8c with IC(50)?=?7.7?然. 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. |Animals [MESH] |Anti-Inflammatory Agents, Non-Steroidal/chemical synthesis/chemistry/*pharmacology [MESH] |Arachidonate 5-Lipoxygenase/metabolism [MESH] |Cyclooxygenase Inhibitors/chemical synthesis/chemistry/*pharmacology [MESH] |Dose-Response Relationship, Drug [MESH] |Edema/*drug therapy [MESH] |Eicosanoids/*antagonists & inhibitors/biosynthesis/chemistry [MESH] |Lipoxygenase Inhibitors/chemical synthesis/chemistry/*pharmacology [MESH] |Male [MESH] |Models, Molecular [MESH] |Molecular Structure [MESH] |Prostaglandin-Endoperoxide Synthases/metabolism [MESH] |Pyridines/chemical synthesis/chemistry/*pharmacology [MESH] |Rats [MESH] |Rats, Sprague-Dawley [MESH]Molecular modelling insights into a physiologically favourable approac(epmc).pdf DeepDyve Pubget Overpricing