68009-06-3Relevant academic research and scientific papers
Imidazo[1,2-a]quinoxalin-4-amines active as adenosine antagonists, process for their preparation and pharmaceutical compositions thereof
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, (2008/06/13)
PCT No. PCT/IB96/01291 Sec. 371 Date May 12, 1998 Sec. 102(e) Date May 12, 1998 PCT Filed Nov. 22, 1996 PCT Pub. No. WO97/19079 PCT Pub. Date May 29, 1997Imidazo[1,2-a]quinoxalin-4-amines derivatives of formula (I) are described, and salt thereof active as adenosine antagonists and a process for their preparation and pharmaceutical compositions containing them as therapeutically active compounds for psychiatric and neurological disorders of the central nervous system.
Imidazo[1,2-a]quinoxalin-4-amines: A novel class of nonxanthine A1- adenosine receptor antagonists
Ceccarelli, Stefano,D'Alessandro, Alessandra,Prinzivalli, Michela,Zanarella, Sergio
, p. 943 - 955 (2007/10/03)
The syntheses and A1 adenosine receptor affinities of a number of imidazo[1,2-a]quinoxalin-4-amines are reported. Structure-activity relationships within the series and in comparison with other similar tricyclic nonxanthine adenosine antagonists are discussed, leading to a putative common binding mode of these nitrogen-containing heterocycles to A1 adenosine receptors. Secondary amino compounds displayed the best affinities toward A1 receptors, while the tertiary amines were almost devoid of activity, thus suggesting a crucial role for the hydrogen bond-forming 4-NH group. Remarkably higher potencies for 1-methyl and N-cyclopentyl derivatives were also found. 4-Cyclopentylamino-1-methylimidazo[1,2-a]quinoxaline (IRFI 165) is the most potent compound in this series, having K(i)(A1) = 7.9 nM. It is also provided with a good A1 selectivity both versus A(2a) and A3 subtypes and was selected for further pharmacological studies.
Method for treating fungal infection in mammals with imidazo [1,2-a]quinoxalines
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, (2008/06/13)
A method for treating a fungal infection in mammals which comprises administering to said mammals having a fungal infection a therapeutically effective amount of a 4-(substituted phenyl)imidazo[1,2-a]quinoxaline.
1-(2-Phenylureylene)imidazoles
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, (2008/06/13)
A 1-(2-acylaminophenyl)imidazole of formula: STR1 wherein R2 is hydrogen or a radical bonded to the nitrogen by a carbon to nitrogen linkage and selected from the group consisting of aliphatic, cycloaliphatic, phenyl, substituted phenyl, fused bicyclic aryl, and monocyclic aryl substituted aliphatic groups.
1-(2-Acylaminophenyl)imidazoles
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, (2008/06/13)
A 1-(2-acylaminophenyl)imidazole of formula: STR1 wherein R5 is hydrogen or an aliphatic, cycloaliphatic, phenyl, substituted phenyl, fused bicyclic aryl or monocyclic aryl substituted aliphatic group bonded to the carbonyl carbon through a carbon-to-carbon linkage. The compounds are useful as intermediates in the preparation of 4-substituted imidazo[1,2-a]quinoxalines.
