title: Novel 8-heterocyclyl xanthine derivatives in drug development - an update.
abstract: Naturally occurring methyl xanthines, especially caffeine and theophylline, have been widely investigated for their pharmacological 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 pharmacological targets, proving to be a versatile scaffold for the development of lead compounds in multiple therapeutic areas. The introduction of a heterocycle at the 8-position of some xanthine derivatives 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, respectively. 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.
authors.affiliation: Università di Ferrara, Dipartimento di Scienze Farmaceutiche, 44100 Ferrara, Italy +39 0532 455921 ; +39 0532 455953 ; baraldi@unife.it.
authors.forename: Pier G
authors.initials: PG
authors.lastname: Baraldi
authors.forename: Francesca
authors.initials: F
authors.lastname: Fruttarolo
authors.forename: Mojgan A
authors.initials: MA
authors.lastname: Tabrizi
authors.forename: Romeo
authors.initials: R
authors.lastname: Romagnoli
authors.forename: Delia
authors.initials: D
authors.lastname: Preti