In an article, published in an article,authors is Watanabe, Nobuhisa, once mentioned the application of Safety of Thiomorpholine 1,1-dioxide, Name is Thiomorpholine 1,1-dioxide,molecular formula is C4H9NO2S, is a conventional compound. this article was the specific content is as follows. Safety of Thiomorpholine 1,1-dioxide
4-(3-Chloro-4-methoxybenzyl)aminophthalazines: Synthesis and inhibitory activity toward phosphodiesterase 5
We synthesized various 4-(3-chloro-4-methoxybenzyl)aminophthalazines substituted at the 1-and 6-positions and evaluated their inhibitory activity toward phosphodiesterase 5 (PDE5) and their vasorelaxant activity in isolated porcine coronary arteries precontracted with prostaglandin F2alpha (10-5 M). The preferred substituents at the 1-position of the phthalazine were 4- hydroxypiperidino, 4-hydroxymethylpiperidino, 4-(2-hydroxyethyl)piperidino, and 4-oxopiperidino. Among these compounds, [4:(3,chloro-4- methoxybenzyl)amino-1-(4-hydroxy)piperidino]-6-phthalazinecarbonitrile monohydrochloride (13) exhibited potent PDE5 inhibitory activity (IC50 = 0.56 nM) with > 1700-fold high selectivity over other PDE isozymes (PDE 1-4). Compound 13 exhibited the most potent vasorelaxant action (EC50 = 13 nM) in this series of compounds. Compound 13 reduced mean pulmonary arterial pressure by 29.9 ¡À 3.1% when administered intravenously at 30 mug/kg to the chronically hypoxic rats and had an apparent oral bioavailability of about 19.5% in rats and was selected for further biological evaluation.
Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. I hope my blog about is helpful to your research. Safety of Thiomorpholine 1,1-dioxide
Reference£º
Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem