Crosignani, Stefano published the artcileDiscovery of Potent, Selective, and Orally Bioavailable Alkynylphenoxyacetic Acid CRTH2 (DP2) Receptor Antagonists for the Treatment of Allergic Inflammatory Diseases, Name: 4-((3-Bromo-4-methylphenyl)sulfonyl)morpholine, the publication is Journal of Medicinal Chemistry (2011), 54(20), 7299-7317, database is CAplus and MEDLINE.
New phenoxyacetic acid antagonists of CRTH2 are described. Following the discovery of a hit compound, I, by a focused screening, high protein binding was identified as its main weakness. Optimization aimed at reducing serum protein binding led to the identification of several compounds that showed not only excellent affinities for the receptor (41 compounds with Ki < 10 nM) but also excellent potencies in a human whole blood assay (IC50 < 100 nM; PGD2-induced eosinophil shape change). Addnl. optimization of the pharmacokinetic characteristics led to the identification of several compounds suitable for in vivo testing. Of these, II (R1 = n-Pr, R2 = Me; R1 = n-Pr, R2 = F) were tested in two different pharmacol. models (acute FITC-mediated contact hypersensitivity and ovalbumin-induced eosinophilia models) and found to be active after oral dosing (10 and 30 mg/kg).
Journal of Medicinal Chemistry published new progress about 850429-74-2. 850429-74-2 belongs to bromides-buliding-blocks, auxiliary class Morpholine,Bromide,Sulfamide,Benzene, name is 4-((3-Bromo-4-methylphenyl)sulfonyl)morpholine, and the molecular formula is C11H14BrNO3S, Name: 4-((3-Bromo-4-methylphenyl)sulfonyl)morpholine.
Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary