56427-50-0Relevant articles and documents
Non-prostanoid thromboxane A2 receptor antagonists with a dibenzoxepin ring system. 1
Ohshima,Takami,Sato,Obase,Miki,Ishii,Karasawa,Kubo
, p. 3394 - 3402 (2007/10/02)
A series of 11-[[2-[(arylsulfonyl)amino]ethyl]thio]-6,11- dihydrodibenz[b,e]oxepin-2-carboxylic acids and related derivatives were synthesized. The compounds were tested for their antagonizing effects on guinea pig platelet TXA2/PGH2 receptors. Structure-activity relationships are discussed. (±)-11-[[2-[(Styrylsulfonyl)amino]ethyl]thio]-6,11- dihydrodibenz[b,e]oxepin-2-carboxylic acid (41) and (±)-11-[[2- [(phenylsulfonyl)amino]ethyl]thio]-6,11-dihydrodibenz[b,e]thiepin-2- carboxylic acid (4af) were the most promising compounds with K(i) values of 6.5 ± 0.29 and 3.7 ± 0.31 nM, respectively, for the TXA2/PGH2 receptor. These compounds also significantly inhibited U-46619-induced guinea pig platelet aggregation ex vivo (10 mg/kg po). Compound 41 was resolved into its optically active form. The (-)-isomer was 60-fold more potent than the (+)- isomer in the TXA2/PGH2 receptor binding assay. Some compounds tested in this study showed both TXA2/PGH2 receptor antagonizing and TXA2 synthase inhibitory effects.
6,11-dihydrodibenz[b,e]oxepin-acetic acids and derivatives
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, (2008/06/13)
6,11-Dihydrodibenz[b,e]oxepin-acetic acids and derivatives having the general formula STR1 are prepared by multi-step sequences. X is C=O, CHCl, CHBr, CH2 or CHOR4 ; Y is alkyl or alkoxy of 1 to 4 carbon atoms, halogen or trifluoromethyl; n is 0, 1, 2 or 3; Z is COOR5, CH2 OR5, CONR25 or CONHOR5 ; and R1 -R5 are hydrogen or alkyl of 1 to 4 carbon atoms. These compounds and the physiologically tolerable salts thereof are useful as antiinflammatory and analgesic agents.
