Synthesis and preliminary pharmacological assessment of novel 9-alkylamino substituted pyrimidino-[2,1-f]-purines.
Two series of N9-alkylaminomethyl-, alkylpiperazino-, alkylpiperidino-substituted 1,3-dimethyl-(hexahydropyrimidino)- and (tetrahydropyrimidono)-[2,1-f]-purines were prepared and their physicochemical and pharmacological properties were described. The most active in central nervous system tests were the compounds with phenylpiperazinealkyl substituent i.e. 1,3-dimethyl-2,4-dioxo-9-[N1N4-(phenyl)-piperazinopropyl]-1, 3,6,7,8,9- hexahydropyrimidino-[2,1-f] purine 6a and its butyl and isobutyl homologs 9 and 12. The compounds depressed statistically significantly spontaneous locomotor and amphetamine activity and showed sedative, analgetic and hypothermizing properties.
Drabczyńska
A
A
Department of Pharmaceutical Chemistry, Medical Academy, Kraków, Poland.
Pawłowski
M
M
Gorczyca
M
M
Malec
D
D
Modzelewski
J
J
D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects*; D001831:Body Temperature / Q000187:drug effects; D002492:Central Nervous System Depressants / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D004353:Drug Evaluation, Preclinical; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D011687:Purines / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D051381:Rats; D017208:Rats, Wistar
D002492:Central Nervous System Depressants; D011687:Purines