Ren, Feng published the artcileDiscovery of novel 1,2,4-thiadiazole derivatives as potent, orally active agonists of sphingosine 1-phosphate receptor subtype 1 (S1P1), Application of 2-(3-Chloro-4-isopropoxyphenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane, the publication is Journal of Medicinal Chemistry (2012), 55(9), 4286-4296, database is CAplus and MEDLINE.
A novel series of 1,2,4-thiadiazole compounds was discovered as selective S1P1 agonists. The extensive structure-activity relationship studies for these analogs were reported. Among them, I was identified to show high in vitro potency with reasonable free unbound fraction in plasma (Fu > 0.5%), good brain penetration (BBR > 0.5), and desirable pharmacokinetic properties in mouse and rat. Oral administration of 1 mg/kg I resulted in significant peripheral lymphocytes reduction at 4 h after dose and rapid lymphocytes recovery at 24 h. Compound I showed a transient lymphopenia profile in the repeated dose study in mouse. In addition, I also demonstrated efficacy comparable to that of FTY720 (II) in the mouse EAE model of MS.
Journal of Medicinal Chemistry published new progress about 1260023-79-7. 1260023-79-7 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Ether,Boronate Esters,Boronic Acids,Boronic acid and ester,, name is 2-(3-Chloro-4-isopropoxyphenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane, and the molecular formula is C15H22BClO3, Application of 2-(3-Chloro-4-isopropoxyphenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane.
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