Stelmach, John E. published the artcileDesign and synthesis of potent, orally bioavailable dihydroquinazolinone inhibitors of p38 MAP kinase, HPLC of Formula: 74896-66-5, the main research area is phenyl piperidinyl piperazino dichlorophenylquinazolinone preparation p38 MAP kinase inhibitor; chlorophenylquinazolinone piperidinyl piperazino preparation p38 MAP kinase inhibition pharmokinetic; piperidinylchlorofluorophenylquinazolinone tertbutyl preparation inhibitor p38 MAP kinase TNF; dichlorophenylquinazolinone preparation p38 MAP kinase inhibitor; quinazolinone dichlorophenyl preparation p38 MAP kinase inhibitor; human TNF alpha production inhibition chlorofluorophenylquinazolinone.
The development of potent, orally bioavailable (in rat) and selective dihydroquinazolinone inhibitors I (R = CO2Me, R1 = H, Br, 2-FC6H4, etc.; R = OMe, R1 = 2-Cl-4-FC6H3, 2,4-F2C6H3, 2-ClC6H4), II (R1 = 2-Cl-4-FC6H3, 2,4-F2C6H3, 2-ClC6H4, X = none, O, NH, CH2, CO, Y = CH, N) and III (R2 = Me, Et, CHMe2, etc.) of p38α MAP kinase is described. For example, III (R2 = CMe3) was prepared via the Still coupling of I (R = OSO2CF3, R1 = 2-Cl-4-FC6H3) with 1-tert-butyl-4-(trimethylstannyl)-1,2,3,6-tetrahydropyridine. These analogs are hybrids of a pyridinylimidazole p38α inhibitor reported by Merck Research Laboratories and VX-745. Optimization of the C-5 Ph and the C-7 piperidinyl substituents led to the identification of III (R2 = CMe3) which gave excellent suppression of TNF-α production in LPS-stimulated whole blood (IC50=10 nM) and good oral exposure in rats (F=68%, AUCn PO=0.58 μM h).
Bioorganic & Medicinal Chemistry Letters published new progress about Homo sapiens. 74896-66-5 belongs to class bromides-buliding-blocks, name is Methyl 3,5-dibromo-4-methylbenzoate, and the molecular formula is C9H8Br2O2, HPLC of Formula: 74896-66-5.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary