86867-14-3Relevant academic research and scientific papers
Stereoselective syntheses of fluorescent non-natural aromatic amino acids based on asymmetric michael additions
Chen, Heru,Zhong, Xianbin,Wei, Jin
, p. 1170 - 1182 (2008/02/05)
Four fluorescent non-natural aromatic amino acids have been synthesized based on a key stereoselective Michael addition reaction. S-1-Phenylethylamine was employed as both the source of amine and the stereoselectivity controller. The overall yields were m
Gastric anti-secretory, anti-ulcer and cytoprotective properties of substituted (E)-4-phenyl- and heteroaryl-4-oxo-2-butenoic acids
Bianchi, Mario,Butti, Alina,Christidis, Yani,Perronnet, Jacques,Barzaghi, Fernando,et al.
, p. 45 - 52 (2007/10/02)
A class of anti-secretory, anti-ulcer and cytoprotective agents, the substituted (E)-4-phenyl and heteroaryl-4-oxo-2-butenoic acids, is described.This chemical structure is not related to those of any known anti-cholinergic drugs, histamine H2-receptor antagonists or prostaglandins.Five compounds, 4-(2-methoxyphenyl)- 15, 4-(4-methoxyphenyl)- 22, 4-(3,4-dimethoxyphenyl)- 32, 4-(3,4,5-trimethoxyphenyl)- 40, and 4-(2-furanyl)-4-oxo-2-butenoic acid 44, have cytoprotective activity at a very low dose (0.6 mg/kg, p.o.) and anti-secretory and anti-ulcer activities at higher doses.One of these compounds, RU 38086 40, has been selected for clinical evaluation.Keywords - anti-ulcer agents / cytoprotective agents / (E)-4-phenyl- and heteroaryl-4-oxo-2-butenoic acids.
Amide derivatives
-
, (2008/06/13)
Amide derivatives of the formula: STR1 wherein either R 1 is aryl or heterocyclic and A 1 is a direct link, or R 1 is aryl or heterocyclic, or hydrogen, or halogeno, hydroxy, amino, guanidino, mercapto, carboxy, carbamoyl, or a substituted derivative thereof, and A 1 is alkylene, alkenylene, cycloalkylene or cycloalkenylene; wherein X is carbonyl or hydroxymethylene or substituted derivatives thereof; wherein A 2 is alkylene, alkenylene or alkylidene; wherein R 2 is hydrogen or alkyl which is unsubstituted or which bears an aryl substituent, or R 2 has the formula --Q 2 --R 20 as defined below; wherein R 3 is hydrogen, alkyl or a carbonyl-containing group; wherein R 4 is hydrogen or alkyl which is unsubstituted or which bears a halogeno, hydroxy, amino, guanidino, carboxy, carbamoyl, mercapto, alkoxy, alkylamino, dialkylamino, cyclic amino, alkylthio, alkanoylamino, alkoxycarbonylamino, alkoxycarbonyl, alkoxycarbonyl, aryl or heterocyclyl substituent;wherein --NR 5 --CR 6 R 16 --Q 1 --R 10 is an amino acid residue, R 5, R 6 and R 16 being defined in claim 1, wherein Q 1 and Q 2, which may be the same or different, each is carbonyl (--CO--) or methylene (--CH 2 --); and wherein R 10 and R 20, which may be the same or different, is hydroxy, amino or a substituted derivative thereof or hydroxyamino or arylthio; or a salt thereof where appropriate; processes for their manufacture and pharmaceutical compositions containing them. The compounds are inhibitors of angiotensin converting enzyme and may be used in the treatment of hypertension.
