52824-62-1Relevant academic research and scientific papers
Allosteric modulation of the adenosine A1 receptor. Synthesis and biological evaluation of novel 2-amino-3-benzoylthiophenes as allosteric enhancers of agonist binding
Van Der Klein, Pieter A. M.,Kourounakis, Angeliki P.,IJzerman, Ad P.
, p. 3629 - 3635 (2007/10/03)
Novel allosteric enhancers of agonist binding to the rat adenosine A1 receptor are described. The lead compound for the new series was PD 81,723 ((2-amino-4,5-dimethyl-3-thienyl)[3-(trifluoromethyl)phenyl]methanone), a compound previously reported by Bruns and co-workers (Mol. Pharmacol. 1990, 38, 950-958). The 4,5-dimethyl group and the benzoyl moiety were targets for further modifications, leading to series of 4,5-dialkyl (12a-g), of tetrahydrobenzo (12h-u), and of tetrahydropyridine (13a-g) derivatives. A number of compounds, in particular 12b, 12e, 12j, 12n, and 12u, proved superior to PD 81,723. Their EC50 values for enhancing the binding of the adenosine A1 receptor agonist N6-cyclopentyladenosine to the receptor were lower, and/or their antagonistic activity on the adenosine A1 receptor was shown to be diminished.
Synthesis and pharmacological evaluation of 2,3 dihydro 1H thieno[2,3 e][1,4]diazepines
Tinney,Sanchez,Nogas
, p. 624 - 630 (2007/10/05)
A series of 2,3 dihydro 1H thieno[2,3 e][1,4]diazepines was synthesized and evaluated for CNS activity. A new antianxiety screen for benzodiazepine like drugs was used along with the standard anticonvulsant test. Structure activity relationships are discussed. One compound, 1,3,6,7,8,9 hexahydro 5 phenyl 2H [1]benzothieno[2,3 e][1,4]diazepin 2 one monosulfate (CI 718), is undergoing clinical studies in man.
