An attempt to chemically state the cross-talk between monomers of COX homodimers by double/hybrid inhibitors mofezolac-spacer-mofezolac and mofezolac-spacer …

MG Perrone, M Miciaccia, P Vitale, S Ferorelli… - European Journal of …, 2021 - Elsevier
Cardiovascular diseases (CVDs) account for over 17 million death globally each year,
including arterial thrombosis. Platelets are key components in the pathogenesis of this …

A further pocket or conformational plasticity by mapping COX-1 catalytic site through modified-mofezolac structure-inhibitory activity relationships and their antiplatelet …

R Solidoro, M Miciaccia, C Bonaccorso… - European Journal of …, 2024 - Elsevier
Cyclooxygenase enzymes have distinct roles in cardiovascular, neurological, and
neurodegenerative disease. They are differently expressed in different type of cancers …

COX-1/COX-2 inhibitors based on the methanone moiety

G Dannhardt, BL Fiebich… - European journal of …, 2002 - Elsevier
This paper focuses on the synthesis and the in vitro testing of dual COX-1/COX-2 inhibitors.
Starting from structures of non-steroidal anti-inflammatory drugs (NSAIDs) the diaryl …

Evaluation of COX-1/COX-2 selectivity and potency of a new class of COX-2 inhibitors

J Gierse, M Nickols, K Leahy, J Warner, Y Zhang… - European journal of …, 2008 - Elsevier
A new class of selective cyclooxygenase-2 (COX-2) inhibitors has been identified by high
throughput screening. Structurally distinct from previously described selective COX-2 …

SC‐560 and mofezolac isosteres as new potent COX‐1 selective inhibitors with antiplatelet effect

M Sisa, L Konečný, V Temml, A Carazo… - Archiv der …, 2023 - Wiley Online Library
Abstract Selective cyclooxygenase (COX)‐1 inhibitors can be employed as potential
cardioprotective drugs. Moreover, COX‐1 plays a key role in inflammatory processes and its …

Synthesis of heteroaromatic analogues of (2-aryl-1-cyclopentenyl-1-alkylidene)-(arylmethyloxy) amine COX-2 inhibitors: effects on the inhibitory activity of the …

A Balsamo, I Coletta, A Guglielmotti, C Landolfi… - European journal of …, 2003 - Elsevier
Several heteroaromatic analogues of (2-aryl-1-cyclopentenyl-1-alkylidene)-(arylmethyloxy)
amine COX-2 inhibitors, in which the cyclopentene moiety was replaced by pyrazole …

Structural approach for COX-2 inhibition.

C Michaux, C Charlier - Mini reviews in medicinal chemistry, 2004 - europepmc.org
The design of selective COX-2 inhibitors is a new approach to obtain potent, anti-
inflammatory drugs but with less side effects. Several families of such inhibitors were …

Synthesis, biological evaluation, and docking studies of novel heterocyclic diaryl compounds as selective COX-2 inhibitors

G Eren, S Ünlü, MT Nuñez, L Labeaga, F Ledo… - Bioorganic & medicinal …, 2010 - Elsevier
Three novel series of diaryl heterocyclic derivatives bearing the 2-oxo-5H-furan, 2-oxo-3H-1,
3-oxazole, and 1H-pyrazole moieties as the central heterocyclic ring were synthesized and …

Selective COX-1 inhibition: A therapeutic target to be reconsidered

MG Perrone, A Scilimati, L Simone… - Current medicinal …, 2010 - ingentaconnect.com
Since cyclooxygenase (COX) isozymes discovery, many papers and reviews have been
published to describe the structural bases of COX inhibition, and to debate on the …

Design, synthesis and biological evaluation of new (E)-and (Z)-1, 2, 3-triaryl-2-propen-1-ones as selective COX-2 inhibitors

S Arfaie, A Zarghi - European journal of medicinal chemistry, 2010 - Elsevier
A group of (E)-and (Z)-1, 2, 3-triaryl-2-propen-1-one derivatives possessing a methylsulfonyl
COX-2 pharmacophore at the para position of the C-1 phenyl ring were synthesized and …