Bagli, Jehan; Bogri, T.; Palameta, B.; Rakhit, S.; Peseckis, S.; McQuillan, J.; Lee, D. K. H. published the article 《Chemistry and positive inotropic effect of pelrinone and related derivatives. A novel class of 2-methylpyrimidones as inotropic agents》. Keywords: inotropic activity aminomethylpyrimidinone preparation; chronotropic activity aminomethylpyridinone; cardiotonic activity aminomethylpyrimidinone; mol structure cardiotonic activity; crystal structure cyanomethylpyridylmethylaminopyrimidinone salt.They researched the compound: 6-Hydroxy-2-methylpyrimidin-4(3H)-one( cas:1194-22-5 ).Synthetic Route of C5H6N2O2. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:1194-22-5) here.
Novel pyrimidine derivatives (e.g., I; R = cyano, R1 = 3-pyridylmethyl) were synthesized and evaluated for pos. inotropic activity. Thus, (MeS)2C:C(CN)CO2Me cyclocondensed with MeC(:NH)NH2·HCl to give cyano methyl(methythio)dihydropyrimidinone II, which was treated with 3-(aminomethyl)pyridine to give 48% I (R = cyano, R1 = 3-pyridylmethyl). Inotropic and chronotropic effects were determined in vitro in cat papillary muscle and right atrium, resp. Selected compounds were then evaluated in vivo in a dog heart failure model. Changes in ventricular dP/dt, heart rate, and blood pressure were monitored. Several of these agents produced relatively minor changes in heart rate. This class of agents demonstrated a varying degree of vasodilator effects concomitant with increases in ventricular contractility. The most potent analogs, I (R = cyano, R1 = 3-pyridylmethyl; R = Br, R1 = Et, 3-pyridylmethyl), were evaluated orally in conscious dogs with implanted Konisberg pressure transducers, and their effect on left ventricular dP/dt was compared with that of milrinone. Mechanistically, the agents of this novel class appear not to mediate their effect either via β-receptors or inhibition of Na+/K+-ATPase. A major component of their inotropic effect is mediated by the inhibition of cardiac phosphodiesterase (PDE)-Fr. III. This was clearly demonstrated by I. Compound I (R = Br, R1 = 3-pyridylmethyl) was found to be the most potent inhibitor of PDE-Fr. III from among the compounds tested in this assay. The crystal structure of I (R = cyano, 3-pyridylmethyl)·HBF4 is also reported.
As far as I know, this compound(1194-22-5)Synthetic Route of C5H6N2O2 can be applied in many ways, which is helpful for the development of experiments. Therefore many people are doing relevant researches.
Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem