LeMahieu, Ronald A. published the artcileSubstituted (aryloxy)alkanoic acids as antagonists of slow-reacting substance of anaphylaxis, Related Products of bromides-buliding-blocks, the main research area is aryloxyalkanoic acid preparation leukotriene antagonist activity; slow reacting substance anaphylaxis antagonist preparation; antiasthmatic aryloxyalkanoic acid preparation.
A series of aryloxyalkanoic acids [e.g., I, X = CH2)5, n = 3] containing the 4-acetyl-3-hydroxy-2-propylphenoxy moiety of the standard slow-reacting substances of anaphylaxis (SRS-A) antagonist, FPL-55712, was prepared Thus, dihydroxypropylacetophenone II (R = R1 = H) was successively alkylated by treatment with Br(CH2)3CO2Et and K2CO3 in DMF, followed by Br(CH2)5Br in Me2CO to give II [R = Br(CH2)5, R1 = EtO2C(CH2)3] which was treated with II (R = R1 = H) and K2CO3, and then NaOH in aqueous MeOH to give I [X = (CH2)5, n = 3]. The compounds were evaluated for their ability to antagonize SRS-A-induced contractions of guinea pig ilea and leukotriene E4-induced bronchoconstriction in the guinea pig. The results showed that the compounds were all less potent than FPL-55712 in vitro, yet surprisingly, most were more potent by the inhalation route of administration. Some of the most potent analogs were selected for further pharmacol. evaluation and exhibited selective antagonism of leukotrienes as compared with platelet activating factor or histamine. In comparison to FPL-55712, compounds I [X = (CH2)5 n = 1] and I [X = (CH2)3O(CH2)3, n = 3] were more potent against leukotriene E4 and (40- and 80-fold, resp.), leukotriene D4 (4- and 3-fold, resp.), and leukotriene C4 (27- and 20-fold, resp.) induced bronchoconstriction when tested by inhalation.
Journal of Medicinal Chemistry published new progress about Antiasthmatics. 58929-72-9 belongs to class bromides-buliding-blocks, name is 1-Bromo-3-(3-bromopropoxy)propane, and the molecular formula is C6H12Br2O, Related Products of bromides-buliding-blocks.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary