40300-80-9Relevant academic research and scientific papers
POLYCYCLIC COMPOUND AND AN ORGANIC ELECTROLUMINESCENCE DEVICE COMPRISING THE POLYCYCLIC COMPOUND OR THE COMPOSITION
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Page/Page column 327-328, (2020/11/03)
Specific polycyclic compounds, a material for an organic electroluminescence device comprising said specific polycyclic compound, an organic electroluminescence device comprising said specific polycyclic compound, an electronic equipment comprising said organic electroluminescence device, a process for preparing said polycyclic compounds, and the use of said polycyclic compounds in an organic electroluminescence. (Formula I) (I)
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
experimental part, p. 1909 - 1918 (2012/07/03)
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.
Congo red analogues as potential anti-prion agents
Villa, Stefania,Cignarella, Giorgio,Barlocco, Daniela,Gervasoni, Marco,Carcassola, Gabriella,Giannino, Laura,Mantegazza, Paolo
, p. 929 - 937 (2007/10/03)
'Transmissible Spongiform Encephalopathies' (TSE) are a group of degenerative, progressive and fatal disorders of CNS which affect both humans and animals, characterised by a long incubation time. The pathogenetic mechanism in TSE is the conversion of normal prion protein (PrPsen) to an altered protease resistant isoform (PrPres) that accumulates in amyloid deposits into the brain; therefore, PrPres is the primary target for therapeutic strategies. The discovery that the sulphonated azo dye Congo red (CR) is able to inhibit the replications of TSE agents and the accumulation of PrPres in animals and in scrapie infected mouse neuroblastoma cells induced us to designe molecules structurally related to CR (1a-f, 2f,g). The compounds were tested in vitro to evaluate their interaction with 263K PrPres. Six of the tested compounds were found to interact with PrPres molecules and to over-stabilise the PrPres aggregates, as CR does. However, none of them induced the reversion of PrP res to PrPsen.
Benzimidazolone-, benzoxazolone-, or benzothiazolone derivatives as ion channel modulating agents
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, (2008/06/13)
The present invention relates to ion channel modulating agents. More particularly, the present invention relates to a particular class of chemical compounds that has proven useful as modulators of SKCa, IKCa and BKCa channels. In further aspects, the present invention relates to the use of these SK/IK/BK channel modulating agents for the manufacture of medicaments, and pharmaceutical compositions comprising the SK/IK/BK channel modulating agents. The SK/IK/BK channel modulating agents of the invention are useful for the treatment or alleviation of diseases and conditions associated with the SK/IK/BK channels.
