Εξειδίκευση τύπου :	Άρθρο σε επιστημονικό περιοδικό
Τίτλος:	Design and Synthesis of Novel Purine Analogues as Potential IL-1β Inhibitors Targeting Vascular Inflammation
Δημιουργός/Συγγραφέας:	Pournara, Dimitra T Fotopoulou, Theano Paramel, Geena Lindkvist, Madelene Grenegård, Magnus Fransén, Karin [EL] Κουφάκη, Μαρία[EN] Koufaki, Maria
Ημερομηνία:	2026-01
Γλώσσα:	Αγγλικά
ISSN:	1612-1872 1612-1880
DOI:	10.1002/cbdv.202502588
Άλλο:	41504126
Περίληψη:	Proinflammatory cytokine interleukin (IL)-1β is a key mediator of the inflammatory response in atherosclerosis. Targeting IL-1β represents a new approach for the anti-inflammatory therapy of cardiovascular diseases. Based on our previous data demonstrating that cardioprotective 6-piperazinyl purines can effectively inhibit IL-1β release in vascular cells, in this study, we present the synthesis of a next generation of purine analogues bearing either a furoxan moiety as a nitric oxide (NO) donor, or a (methylsulfonyl)thio group, a benzothioamide, or a 5-phenyl-3H-1,2-dithiole-3-thione as putative hydrogen sulfide (H2S) donor moieties. NO and H2S are gaseous signaling molecules that can reduce vascular inflammation. The new purine analogues were evaluated for their anti-inflammatory activity by assessing their inhibitory effect on the secretion of lipopolysaccharide (LPS)-induced IL-1β in human aortic smooth muscle cells (HAoSMCs). Our initial findings revealed that compounds bearing a [methylsulfonyl)thio]propanoyl or [methylsulfonyl)thio]hexanoyl group (compounds MK175 and MK169, respectively) could effectively inhibit LPS-induced IL-1β release in HAoSMCs.
Τίτλος πηγής δημοσίευσης:	Chemistry & biodiversity
Τόμος/Κεφάλαιο:	23
Τεύχος:	1
Θεματική Κατηγορία:	[EL] Χημική Βιολογία[EN] Chemical Biology [EL] Οργανική χημεία[EN] Organic chemistry [EL] Θεραπευτική. Φαρμακολογία[EN] Therapeutics.Pharmacology
Λέξεις-Κλειδιά:	6‐piperazinyl purines IL‐1β inhibitors human aortic smooth muscle cells purines
Χρηματοδότης:	The Knowledge Foundation Örebro University, Faculty of Medicine and Health European Union Greece
Χρηματοδοτικό πρόγραμμα:	HÖG2017 HÖG2019 Synergi2021 OPENSCREEN-GR
Αναγνωριστικό χρηματοδοτικού προγράμματος:	HÖG2017 #20170191 HÖG2019#20190088 Synergi2021#20220083-H-0 OPENSCREEN-GR: (MIS) 5002691
Κάτοχος πνευματικών δικαιωμάτων:	© 2026 The Author(s). Chemistry & Biodiversity published by Wiley‐VHCA AG.
Όροι και προϋποθέσεις δικαιωμάτων:	This is an open access article under the terms of the Creative Commons Attribution-NonCommercial-NoDerivs License, which permits use and distribution in any medium, provided the original work is properly cited, the use is non-commercial and no modifications or adaptations are made.
Ηλεκτρονική διεύθυνση στον εκδότη (link):	https://doi.org/10.1002/cbdv.202502588
Εμφανίζεται στις συλλογές:	Ινστιτούτο Χημικής Βιολογίας - Επιστημονικό έργο