103175-85-5Relevant academic research and scientific papers
New potent antagonists of leukotrienes C4 and D4. 1. Synthesis and structure-activity relationships
Nakai,Konno,Kosuge,Sakuyama,Toda,Arai,Obata,Katsube,Miyamoto,Okegawa,Kawasaki
, p. 84 - 91 (2007/10/02)
(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-RS411 (19h) were the most potent and orally active antagonists, respectively. Structure-activity relationships are discussed.
(FUSED) BENZ(THIO)AMIDES AND PHARMACEUTICAL USE
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, (2008/06/13)
A (fused) benz(thio)amide of the formula: (I) wherein B represents (i) a carbocyclic ring of from 4 to 8 members being unreplaced or replaced one, two or three of optional carbon atom(s) by oxygen, nitrogen and/or sulphur atom(s) or (ii) a divalent group of the formula: R1 represents a group of formula: (i) (ii) (iii) (iv) a straight or branched alkyl, alkenyl, or alkynyl of from 1 to 20 carbon atoms, R4 represents (i) when B represents a closed ring, a group of the formula: U(CH2)nCOOR8 (CH2)pCOOR8 or (ii) when B does not represent a ring, a group of formula: (CH2)pCOOR8 or with the proviso that compounds of formula: wherein A' is a vinylene or an ethylene group optionally substituted by straight or branched alkyl groups of from 1 to 4 carbon atom(s); R4' is -(CH2)n-COOR8 - and R1' is (i) a group of the formula: or (ii) a group of the formula: are excluded, wherein A, R2, R3, R5, R6, R7, R8, U, n, m, p, q, R5', and R6' are defined as in the above specification, possessing antagonistic activity on leukotrienes (SRS), inhibitory activity on 5 alpha -reductase, on phospholipase and on aldose reductase and being useful for the prevention and/or treatment of diseases induced by leukotrienes, 5 alpha -reductase, phospholipase and aldose reductase in mammals, especially in human beings
