Journal of Medicinal Chemistry published new progress about 4760-35-4. 4760-35-4 belongs to imidazoles-derivatives, auxiliary class Chloride,Benzimidazole, name is 2-(Chloromethyl)-1-methyl-1H-benzo[d]imidazole, and the molecular formula is C9H9ClN2, Application In Synthesis of 4760-35-4.
Musser, John H. published the artcileN-[(Arylmethoxy)phenyl] carboxylic acids, hydroxamic acids, tetrazoles, and sulfonyl carboxamides. Potent orally active leukotriene D4 antagonists of novel structure, Application In Synthesis of 4760-35-4, the publication is Journal of Medicinal Chemistry (1990), 33(1), 240-5, database is CAplus and MEDLINE.
Four types of N-[(arylmethoxy)phenyl] title compounds were prepared as leukotriene D4 (I) antagonists. In the hydroxamic acid series, 3-(2-quinolinylmethoxy)benzeneacetohydroxamate II was the most potent inhibitor of I-induced bronchoconstriction with an oral ED50 of 7.9 mg/kg. II also orally inhibited ovalbumin-induced bronchoconstriction in the guinea pig with an ED50 of 3.6 mg/kg. In vitro against I-induced contraction of isolated guinea pig trachea pretreated with indomethacin and L-cysteine, II produced a pKB value of 6.08. In the sulfonyl carboxamide series, N-[(4-methylphenyl)sulfonyl]-3-(2-quinolinylmethoxy)benzamide (III) was the most potent antagonist. III orally inhibited both I– and ovalbumin-induced bronchoconstriction with ED50s of 0.4 and 20.2 mg/kg, resp. In vitro, against I-induced contraction of isolated guinea pig trachea, III produced a pKB value of 7.78. In the carboxylic acid series, which served as intermediates for the above two series, 3-(2-quinolinyl)methoxybenzeneacetic acid IV was the most potent inhibitor of I-induced bronchoconstriction (99%, at 25 mg/kg, intraduodenally); however, the pKB for IV was disappointing (5.79). In the tetrazole series the most potent inhibitor was 2-[[3-(1H-tetrazol-5-ylmethyl)phenoxy]methyl]quinoline (V). The resp. inhibitory ED50s were 3.0 mg/kg vs. I and 17.5 mg/kg vs. ovalbumin. In the isolated guinea pig trachea, V produced a pKB value of 6.70.
Journal of Medicinal Chemistry published new progress about 4760-35-4. 4760-35-4 belongs to imidazoles-derivatives, auxiliary class Chloride,Benzimidazole, name is 2-(Chloromethyl)-1-methyl-1H-benzo[d]imidazole, and the molecular formula is C9H9ClN2, Application In Synthesis of 4760-35-4.
Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem