Mode of action of 2‐(diethylamino)‐7‐ethoxychromone on human platelets

Abstract

The in vitro effect of 2-(diethylamino)-7-ethoxychromone (RC39XVIII) on human platelet aggregation induced by several agonists and on thromboxane B2 formation, granule release and intracellular cAMP elevation has been studied. The chromosome-derivative exerts a dose-dependent inhibitory effect on aggregation produced by U46619, arachidonic acid, thrombin, collagen and ADP. RC39XVIII inhibits aggregation, TxB2 formation and granule release in parallel. Moreover the drug potentiates cAMP accumulation induced by iloprost and forskolin. The drug also inhibits soluble cAMP phosphodiesterase in a dose-dependent manner. No effect on adenylate cyclase activity measured in platelet membranes was evident.

Chromone: A Valid Scaffold in Medicinal Chemistry

“…Numerous biological activities have been attributed to simple chromones and their analogues, such as anticoagulants and antiplatelet [143][144][145][146] as well as antidiabetics [147] activities. Their ability to act as inhibitors of carbonic anhydrase [148,149] , NADH:ubiquinonereductase (complex I) [150,151] and calpain [152,153] was also reported.…”

“…The most active compound was 2-(diethylamino)-7-ethoxychromone (13) (Figure 12). 69c, 164 The synthesis and biological evaluation of a series of 2morpholinylchromones as antiplatelet inhibitors has been described. 163a The SAR study performed so far led to the discovery of a series of 7-[(aminoethyl)oxy]-8-methylchromone derivatives as potent inhibitors of ADP-induced platelet aggregation.…”

“…Afterward, several 2-(diethylamino)-7-ethoxychromone derivatives were obtained and tested to check their effect on human blood platelet aggregation. The most active compound was 2-(diethylamino)-7-ethoxychromone ( 13 ) (Figure ). , …”

One-Pot Synthesis of Functionalized Spirobenzofuranones via MCR involving 3-Cyanochromones

“…Derivatives of 4 H -1-benzopyran-4-one, also known as 4 H- chromen-4-ones or chromones, are important natural products possessing wide range of valuable physiological activities . The chromone moiety is also part of pharmacophores of various biologically active molecules , including anticancer agents such as psorospermin and pluramycin A. , Concerning 3-cyano-4-benzopyrones, the introduction of an electron-withdrawing group at the 3-position of the chromone system changes crucially the reactivity of the pyrone ring and provides a broad synthetic potential in organic and medicinal chemistry. As a result, 3-cyano-4-benzopyrones are important intermediates not only in the synthesis of therapeutically useful antiallergic drugs such as amlexanox but also in the synthesis of benzopyranopyridines with antiarthritic activity .…”

One-Pot Five-Component Synthesis of Spirocyclopenta[b]chromene Derivatives and Their Acid-Catalyzed Rearrangement

“…In addition to forming the basic nucleus of an entire class of natural products, i.e., flavones, the chromone moiety is also part of pharmacophores of various biologically active molecules , including anticancer agents such as psorospermin and pluramycin A , (Figure ). Concerning 3-cyano-4-benzopyrones, the introduction of an electron-withdrawing group at the 3-position of the chromone system changes crucially the reactivity of the pyrone ring and provides a broad synthetic potential in organic and in medicinal chemisty.…”