1027492-31-4Relevant academic research and scientific papers
Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[N- (substituted) piperazin-1-yl]thiophenes as potent allosteric enhancers of the A1 adenosine receptor
Romagnoli, Romeo,Baraldi, Pier Giovanni,Carrion, Maria Dora,Cara, Carlota Lopez,Cruz-Lopez, Olga,Iaconinoto, Maria Antonietta,Preti, Delia,Shryock, John C.,Moorman, Allan R.,Vincenzi, Fabrizio,Varani, Katia,Borea, Pier Andrea
supporting information; experimental part, p. 5875 - 5879 (2009/09/25)
The synthesis and evaluation of a series of 2-amino-3-(4-chlorobenzoyl)-4- [4-(alkyl/aryl)piperazin-yl]thiophene derivatives as allosteric enhancers of the A1-adenosine receptor are described. The nature of substituents on the phenyl ring tethered to the piperazine seem to exert a fundamental influence on the allosteric enhancer activity, with the 4-chlorophenyl 8f and 4-trifluoromethyl 8j derivatives being the most active compounds in binding (saturation and displacement experiments) and functional cAMP studies.
ALLOSTERIC MODULATORS OF THE A1 ADENOSINE RECEPTOR
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Page/Page column 17, (2008/12/05)
The present invention provides compounds of formula (I) wherein R1, R2, R3, R4 and Q have a meaning as defined herein in the specification. The compounds of formula (I) are allosteric modulators of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A1 adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of pain, in particular, chronic pain such as neuropathic pain; cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke; neurological disease or injury; sleep disorder; epilepsy; and depression.
