Naturally occurring Me xanthines, esp. caffeine and theophylline, have been widely investigated for their pharmacol. properties as cognition enhancers, bronchodilator agents and mild diuretics. The xanthine core (3,7-dihydro-1H-purine-2,6-dione) has been largely manipulated in the search for selective ligands for different pharmacol. targets, proving to be a versatile scaffold for the development of lead compds. in multiple therapeutic areas. The introduction of a heterocycle at the 8-position of some xanthine derivs. demonstrated to be a successful strategy for the identification of potent and selective A1 or A2B adenosine receptors antagonists as potential agents for the treatment of Alzheimer's disease and asthma, resp. Interesting examples of 8-heterocyclyl-xanthines as dipeptidyl peptidase IV inhibitors and liver X receptor agonists have been claimed for their possible therapeutic use in the treatment of Type 2 diabetes and atherosclerosis.

Novel 8-heterocyclyl xanthine derivatives in drug development - An update

BARALDI, Pier Giovanni;FRUTTAROLO, Francesca;AGHAZADEH TABRIZI, Mojgan;ROMAGNOLI, Romeo;PRETI, Delia
2007

Abstract

Naturally occurring Me xanthines, esp. caffeine and theophylline, have been widely investigated for their pharmacol. properties as cognition enhancers, bronchodilator agents and mild diuretics. The xanthine core (3,7-dihydro-1H-purine-2,6-dione) has been largely manipulated in the search for selective ligands for different pharmacol. targets, proving to be a versatile scaffold for the development of lead compds. in multiple therapeutic areas. The introduction of a heterocycle at the 8-position of some xanthine derivs. demonstrated to be a successful strategy for the identification of potent and selective A1 or A2B adenosine receptors antagonists as potential agents for the treatment of Alzheimer's disease and asthma, resp. Interesting examples of 8-heterocyclyl-xanthines as dipeptidyl peptidase IV inhibitors and liver X receptor agonists have been claimed for their possible therapeutic use in the treatment of Type 2 diabetes and atherosclerosis.
2007
Baraldi, Pier Giovanni; Fruttarolo, Francesca; AGHAZADEH TABRIZI, Mojgan; Romagnoli, Romeo; Preti, Delia
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/517679
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