Discovery of Potent, Selective, and Orally Bioavailable Alkynylphenoxyacetic Acid CRTH2 (DP2) Receptor Antagonists for the Treatment of Allergic Inflammatory Diseases was written by Crosignani, Stefano;Pretre, Adeline;Jorand-Lebrun, Catherine;Fraboulet, Gaele;Seenisamy, Jeyaprakashnarayanan;Augustine, John Kallikat;Missotten, Marc;Humbert, Yves;Cleva, Christophe;Abla, Nada;Daff, Hamina;Schott, Olivier;Schneider, Manfred;Burgat-Charvillon, Fabienne;Rivron, Delphine;Hamernig, Ingrid;Arrighi, Jean-Francois;Gaudet, Marilene;Zimmerli, Simone C.;Juillard, Pierre;Johnson, Zoe. And the article was included in Journal of Medicinal Chemistry in 2011.Safety of 1-((3-Bromo-4-methylphenyl)sulfonyl)piperidine The following contents are mentioned in the article:
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). This study involved multiple reactions and reactants, such as 1-((3-Bromo-4-methylphenyl)sulfonyl)piperidine (cas: 850429-73-1Safety of 1-((3-Bromo-4-methylphenyl)sulfonyl)piperidine).
1-((3-Bromo-4-methylphenyl)sulfonyl)piperidine (cas: 850429-73-1) belongs to piperidine derivatives. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N–H bond in an axial position, and the other in an equatorial position.Safety of 1-((3-Bromo-4-methylphenyl)sulfonyl)piperidine
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem