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- W2056554868 abstract "Abstract 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 A 1 , A 2A , and A 3 ARs. The new compounds were designed based on derivatives of 2‐(benzimidazol‐2‐yl)quinoxaline, previously reported as potent and selective antagonists of A 1 and A 3 ARs. Among these, 3‐[4‐(ethylthio)‐1 H ‐benzimidazol‐2‐yl]isoquinoline 4 b exhibited the best combination of potency toward the A 1 AR ( K i =1.4 n M ) and selectivity against the A 2A ( K i >10 μ m), A 2B ( K i >10 μ m) , and A 3 ARs ( K i >1 μ M ). Functional experiments in circular smooth muscle preparations of isolated human colon showed that 4 b behaves as a potent and selective antagonist of the A 1 AR in the neuromuscular compartment of this intestinal region. Biological and pharmacological data suggest that 4 b is a suitable starting point for the development of novel agents endowed with stimulant properties on colonic activity." @default.
- W2056554868 created "2016-06-24" @default.
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- W2056554868 date "2011-07-27" @default.
- W2056554868 modified "2023-10-12" @default.
- W2056554868 title "Derivatives of Benzimidazol-2-ylquinoline and Benzimidazol-2-ylisoquinoline as Selective A1 Adenosine Receptor Antagonists with Stimulant Activity on Human Colon Motility" @default.
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- W2056554868 doi "https://doi.org/10.1002/cmdc.201100284" @default.
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