New xanthine derivatives with potent and long lasting anti-bronchoconstrictive activity
Twenty eight new derivatives of 8-aminoalkyl substituted xanthine have been synthesized.They all have demonstrated a potent anti-bronchoconstrictive effect in the guinea pig and some of them have a very long duration of action (>48 h).Among them, one compound: 1-methyl 3-isobutyl 8-(4-benzhydryl piperazino ethyl)xanthine (57) (S 9795) has been selected for clinical trials in asthmatic patients because of its long duration of action, its lack of CNS stimulating effects and its inhibiting action on mast cell degranulation and phosphodiesterase activity.Keywords - 8-aminoalkyl substituted xanthines / benzhydryl piperazine / piperidine / ethylenediamine / anti-bronchoconstrictors / phosphodiesterase inhibitors / asthma
Regnier, Gilbert L.,Guillonneau, Claude G.,Duhault, Jacques L.,Tisserand, Francoise P.,Saint-Romas, Guy,Holstorp, Sophie M.
p. 243 - 250
(2007/10/02)
Xanthine compounds
New xanthine compounds of the formula: STR1 in which: R1 is hydrogen or alkyl from C1 to C5 inclusive; R2 is a hydrocarbon radical up to C6 having optionally a double bond, phenyl or benzyl; R3/
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(2008/06/13)
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