Yee, Ying K.; Bernstein, Peter R.; Adams, Edward J.; Brown, Frederick J.; Cronk, Laura A.; Hebbel, Kevin C.; Vacek, Edward P.; Krell, Robert D.; Snyder, David W. published the artcile< A novel series of selective leukotriene antagonists: exploration and optimization of the acidic region in 1,6-disubstituted indoles and indazoles>, Name: Methyl 4-(bromomethyl)-3-fluorobenzoate, the main research area is leukotriene antagonistic MSBAR indole indazole preparation; antiasthmatic indole indazole preparation.
A systematic structure-activity exploration of the carboxylic acid region in a series of indole- or indazole-derived leukotriene antagonists I [e.g., R = Me(CH2)3CHEt, X = CH, N, R1 = CO2H] led to several discoveries. Use of the 3-methoxy-p-tolyl fragment (illustrated in I) for connecting the indole and the acidic site provides the most potent carboxylic acids I (R = CO2H) tetrazoles I (R1 = tetraacyl) and aryl sulfonimides, e.g I (R = PhSO2NHCO). The aryl sulfonimides are 5-500 times more potent (in vitro and/or in vivo) than the corresponding carboxylic acids. The o-tolyl sulfonimides such as I (R = cyclohexylmethyl, X = N, R1 = 2-MeC6H4SO2NHCO) show greater oral potency than the Ph sulfonimides at a given level of in vitro activity. Acidic sulfone derivatives e.g., I [R = cyclopentylmethyl; X = CH, N; R1 = PhSO2CH(CO2Me)]-(Nu = CH(CO2CH3)SO2Ph) mimic the activity of the acidic imides.
Journal of Medicinal Chemistry published new progress about Antiasthmatics. 128577-47-9 belongs to class bromides-buliding-blocks, and the molecular formula is C9H8BrFO2, Name: Methyl 4-(bromomethyl)-3-fluorobenzoate.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary