N6-Cycloalkyl-2-substituted adenosine derivatives as selective, high affinity adenosine A1 receptor agonists

A1adenosine receptor agonists and their potential therapeutic applications

“…Thus, a partial agonist may elicit a maximal response only in tissues in which there is some receptor reserve, wherein submaximal receptor occupancy leads to a maximal functional effect. To further differentiate between A 1 -mediated effects in the adipocytes and the CNS, in theory one could design partial antilipolytic agents with polar functionalities to diminish CNS penetration, thus minimizing CNS side effects [68] . In general, most of the A 1 -AdoR agonists contain a ribose moiety which makes these agonists hydrophilic, and therefore, high penetration of CNS through BBB should be limited through passive transport.…”

Synthesis and Applications of Azolylpurine and Azolylpurine Nucleoside Derivatives

“…[87] In 2008, 2-(1,2,3-triazol-1-yl) derivatives of 5Ј-O-[N-(salicyl)sulfamoyl]adenosine (Sal-AMS) 209 ( Figure 4) were tested as inhibitors of aryl acid adenylating enzymes involved in siderophore biosynthesis by Mycobacterium tuberculosis. [88] Siderophores are essential in terms of obtaining iron for the pathogens to contribute to infection inside organisms.…”

1,2,3-Triazoles as leaving groups: SNAr reactions of 2,6-bistriazolylpurines with O- and C-nucleophiles

“…Azolylpurine derivatives are important due to their potential as drug candidates. They can be used as agonists and antagonists of adenosine receptors [58,[64][65][66] and against Mycobacterium tuberculosis [60]. They also show useful fluorescent properties [11,[67][68][69] and can be used as metal ion sensors [70].…”