Synthesis and preliminary pharmacological screening of some 8-substituted methylxanthines.
Methods of synthesis, chemical properties and results of preliminary pharmacological screening for 8-amino substituted derivatives of caffeine (1-3) and 7,8-disubstituted derivatives of 8-aminotheophylline (8-12) have been described. The compounds show weak sedative and antidepressive activity and some of them (2, 10, 12) also small antinociceptive effect.
Drabczyńska
A
A
Department of Pharmaceutical Chemistry, Medical Academy, Kraków, Poland.
Pawłowski
M
M
Gorczyca
M
M
Malec
D
D
Modzelewski
J
J
D000700:Analgesics; D000818:Animals; D000927:Anticonvulsants; D001058:Apomorphine / Q000037:antagonists & inhibitors; D001831:Body Temperature / Q000187:drug effects; D055598:Chemical Phenomena; D002621:Chemistry; D006220:Haloperidol / Q000037:antagonists & inhibitors; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D010879:Piperazines / Q000037:antagonists & inhibitors; D011597:Psychomotor Performance / Q000187:drug effects; D051381:Rats; D011919:Rats, Inbred Strains; D012110:Reserpine / Q000037:antagonists & inhibitors; D014970:Xanthines / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity
D000700:Analgesics; D000927:Anticonvulsants; D010879:Piperazines; D014970:Xanthines; D012110:Reserpine; C050592:3-(2-carboxypiperazin-4-yl)propyl-1-phosphonic acid; D006220:Haloperidol; D001058:Apomorphine