1457-86-9Relevant articles and documents
The reaction of tertiary anilines with maleimides under visible light redox catalysis
Ju, Xuhui,Li, Dianjun,Li, Weifei,Yu, Wei,Bian, Fengling
supporting information, p. 3561 - 3567 (2013/02/22)
Tertiary anilines can be prompted to react with N-aryl- and N-benzylmaleimides to form tetrahydroquinoline products under photocatalysis using visible light irradiation, the ruthenium or iridium complexes Ru(bpy) 3Cl2 or Ir(ppy)2(dtbbpy)PF6 as catalyst, and air as terminal oxidant.
Nonpeptide angiotensin II antagonists derived from 4H-1,2,4-triazoles and 3H-imidazo[1,2-b][1,2,4]triazoles
Ashton,Cantone,Chang,Hutchins,Strelitz,MacCoss,Chang,Lotti,Faust,Chen,Bunting,Schorn,Kivlighn,Siegl
, p. 591 - 609 (2007/10/02)
By a variety of synthetic routes, we have synthesized a series of 3,4,5- trisubstituted 4H-1,2,4-triazoles and a related series of 3H-imidazo[1,2- b][1,2,4]triazoles and evaluated them in vitro and in vivo as angiotensin II (AII) antagonists. Principal efforts focused on triazoles bearing an n-alkyl substituent at C3 and a 4-[(2-carboxybenzoyl)amino]benzyl, (2'- carboxybiphenyl-4-yl)methyl, or [2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl side chain at N4. Among numerous variations at C5, benzylthio groups gave the best potency. Particularly noteworthy was 3-n-butyl-5-[(2- carboxybenzyl)thio]-4-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-4H-1,2,4- triazole (71, IC50 1.4 nM), which blocked the AII pressor response in conscious rats at 0.3 mg/kg iv with a duration of action of approximately 6 h, similar to that of DuP 753. Although 71 was active orally only at a 10- fold higher dose level, good oral bioavailability was demonstrated for a monoacidic analogue 62. Most potent among the bicyclic derivatives was 2-n- butyl-5,6-dimethyl-3-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-3H- imidazo[1,2-b][1,2,4]triazole (93, IC50 7.8 nM). The effects of hydrophobic, hydrogen-bonding, and ionic interactions with the AT1 receptor are considered.
Antisecretory oxamic acid esters
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, (2008/06/13)
Variously substituted oxanilic acid esters possessing anti-secretary activity are useful anti-ulcer agents.