Synthesis and preliminary pharmacological screening of novel imidazo[2,1-f]theophylline derivatives.
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.
Pawłowski
Maciej
M
Department of Pharmaceutical Chemistry, Collegium Medicum, Jagiellonian University, Kraków, Poland.
Katlabi
Jacek
J
Jurczyk
Sławomir
S
Malec
Danuta
D
Modzelewski
Jerzy
J
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
D000697:Central Nervous System Stimulants; D018491:Dopamine Agonists; D013806:Theophylline; D000661:Amphetamine; D001058:Apomorphine