| Literature DB >> 3336036 |
H Nakai1, M Konno, S Kosuge, S Sakuyama, M Toda, Y Arai, T Obata, N Katsube, T Miyamoto, T Okegawa.
Abstract
(p-Amylcinnamoyl)anthranilic acid (3a) had moderate antagonist activities against LTD4-induced smooth muscle contraction on guinea pig ileum and LTC4-induced bronchoconstriction in anesthetized guinea pigs. Modifications were made in the hydrophobic part (cinnamoyl moiety) and the hydrophilic part (anthranilate moiety) of 3a. A series of 8-(benzoylamino)-2-tetrazol-5-yl-1,4-benzodioxans and 8-(benzoylamino)-2-tetrazol-5-yl-4-oxo-4H-1-benzopyrans were revealed to be potent antagonists of leukotrienes C4 and D4. Among both series, ONO-RS-347 (18k) and ONO-RS-411 (19h) were the most potent and orally active antagonists, respectively. Structure-activity relationships are discussed.Entities:
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Year: 1988 PMID： 3336036 DOI： 10.1021/jm00396a013
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446