1339147-87-3Relevant academic research and scientific papers
Derivatives of Benzimidazol-2-ylquinoline and Benzimidazol-2-ylisoquinoline as Selective A1 Adenosine Receptor Antagonists with Stimulant Activity on Human Colon Motility
Cosimelli, Barbara,Taliani, Sabrina,Greco, Giovanni,Novellino, Ettore,Sala, Annalisa,Severi, Elda,DaSettimo, Federico,LaMotta, Concettina,Pugliesi, Isabella,Antonioli, Luca,Fornai, Matteo,Colucci, Rocchina,Blandizzi, Corrado,Daniele, Simona,Trincavelli, Maria Letizia,Martini, Claudia
, p. 1909 - 1918 (2011)
A number of quinolines and isoquinolines connected in various ways to a substituted benzimidazol-2-yl system were synthesized and evaluated as novel antagonists of adenosine receptors (ARs) by competition experiments using human A1, A2A, and A3 ARs. The new compounds were designed based on derivatives of 2-(benzimidazol-2-yl)quinoxaline, previously reported as potent and selective antagonists of A1 and A3 ARs. Among these, 3-[4-(ethylthio)-1H-benzimidazol-2-yl]isoquinoline 4b exhibited the best combination of potency toward the A1 AR (Ki=1.4nM) and selectivity against the A2A (Ki>10μm), A2B (Ki>10μm), and A3 ARs (Ki>1μM). Functional experiments in circular smooth muscle preparations of isolated human colon showed that 4b behaves as a potent and selective antagonist of the A1 AR in the neuromuscular compartment of this intestinal region. Biological and pharmacological data suggest that 4b is a suitable starting point for the development of novel agents endowed with stimulant properties on colonic activity.
