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2-Oxoamide inhibitors of cytosolic group IVA phospholipase A2with reduced lipophilicity

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2-Oxoamide inhibitors of cytosolic group IVA phospholipase A2with reduced lipophilicity
Nikolaou A.
Kokotos G.
Αντωνοπούλου, Γεωργία
Magrioti V.
Mouchlis V.D.
Kokotou M.G.
Dennis E.A.
Barbayianni E.
Άρθρο σε επιστημονικό περιοδικό
2016
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.
Φαρμακευτική χημεία (EL)
Pharmaceutical chemistry (EN)
GIVA cPLA2 (EN)
Inhibitors (EN)
Phospholipase A2 (EN)
2-Oxoamides (EN)
Lipophilicity (EN)
English
Elsevier Ltd
Bioorganic and Medicinal Chemistry
© 2016 Elsevier Ltd
© 2016 Elsevier Ltd (EN)
Εθνικό Ίδρυμα Ερευνών (ΕΙΕ)
Ήλιος - Αποθετήριο Εθνικού Ιδρύματος Ερευνών



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