Εξειδίκευση τύπου :	Άρθρο σε επιστημονικό περιοδικό
Τίτλος:	2-Oxoamide inhibitors of cytosolic group IVA phospholipase A2with reduced lipophilicity
Δημιουργός/Συγγραφέας:	[EL] Αντωνοπούλου, Γεωργία[EN] Antonopoulou, Georgia Magrioti V. Kokotou M.G. Nikolaou A. Barbayianni E. Mouchlis V.D. Dennis E.A. Kokotos G.
Εκδότης:	Elsevier Ltd
Ημερομηνία:	2016
Γλώσσα:	Αγγλικά
ISSN:	0968-0896
DOI:	10.1016/j.bmc.2016.07.057
Άλλο:	PubMed ID: 27522578
Περίληψη:	Cytosolic GIVA phospholipase A2(GIVA cPLA2) initiates the eicosanoid pathway of inflammation and thus inhibitors of this enzyme constitute novel potential agents for the treatment of inflammatory diseases. Traditionally, GIVA cPLA2inhibitors have suffered systemically from high lipophilicity. We have developed a variety of long chain 2-oxoamides as inhibitors of GIVA PLA2. Among them, AX048 was found to produce a potent analgesic effect. We have now reduced the lipophilicity of AX048 by replacing the long aliphatic chain with a chain containing an ether linked aromatic ring with in vitro inhibitory activities similar to AX048.
Τίτλος πηγής δημοσίευσης:	Bioorganic and Medicinal Chemistry
Τόμος/Κεφάλαιο:	24
Τεύχος:	19
Σελίδες:	4544-4554
Θεματική Κατηγορία:	[EL] Φαρμακευτική χημεία[EN] Pharmaceutical chemistry
Λέξεις-Κλειδιά:	2-Oxoamides GIVA cPLA2 Inhibitors Lipophilicity Phospholipase A2
Αξιολόγηση από ομότιμους (peer reviewed):	Ναι
Κάτοχος πνευματικών δικαιωμάτων:	© 2016 Elsevier Ltd
Όροι και προϋποθέσεις δικαιωμάτων:	All Open Access, Green
Σημειώσεις:	National Institutes of Health, NIH: RO1 20,501-40; National Institute of General Medical Sciences, NIGMS: R01GM020501; European Commission, EC. This research has been co-financed by the European Union (European Regional Development Fund-ERDF) and Greek National Funds through the Operational Program ‘Competitiveness and Entrepreneurship’ of the National Strategic Reference Framework (NSRF)—Research Funding Program: ‘Phospholipases A 2 inhibitors: Developing a drug pipeline for the treatment of inflammatory neurological disorders’ (G.K.) and in part by NIH grant RO1 20,501-40 (E.A.D.).
Εμφανίζεται στις συλλογές:	Ινστιτούτο Χημικής Βιολογίας - Επιστημονικό έργο