title: Synthesis and preliminary pharmacological screening of novel imidazo[2,1-f]theophylline derivatives.
abstract: The three different kinds of imidazo[2,1-f]theophylline derivatives were synthesized and tested for their CNS activity. A series of alkoxy-alkylamides and amino-alkylamides with basic function, derived from 8-benzyl-6,7-dihydroimidazo[2,1-f]theophylline-7-carboxylic acid showed stimulating influence on CNS as they increased the locomotor activity (compound 8 and 10) or enhanced amphetamine and apomorphine effects in mice (compounds 3, 4 and 9). Compounds 1, 5, 8-10 and 12 had anticonvulsant activity in the pentetrazole test; 12 with anellated imidazol-7-on ring (lactam structure) showed sedative properties and antiserotonin effects.
authors.affiliation: Department of Pharmaceutical Chemistry, Collegium Medicum, Jagiellonian University, Kraków, Poland.
authors.forename: Maciej
authors.initials: M
authors.lastname: Pawłowski
authors.forename: Jacek
authors.initials: J
authors.lastname: Katlabi
authors.forename: Sławomir
authors.initials: S
authors.lastname: Jurczyk
authors.forename: Danuta
authors.initials: D
authors.lastname: Malec
authors.forename: Jerzy
authors.initials: J
authors.lastname: Modzelewski
mesh_terms: D000661:Amphetamine / Q000494:pharmacology; D000818:Animals; D001058:Apomorphine / Q000494:pharmacology; D000697:Central Nervous System Stimulants / Q000138:chemical synthesis* / Q000494:pharmacology; D018491:Dopamine Agonists; D004336:Drug Antagonism; D004353:Drug Evaluation, Preclinical; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D012640:Seizures / Q000188:drug therapy / Q000517:prevention & control; D013329:Structure-Activity Relationship; D013806:Theophylline / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000697:Central Nervous System Stimulants; D018491:Dopamine Agonists; D013806:Theophylline; D000661:Amphetamine; D001058:Apomorphine