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Tytuł oryginału: Synthesis and pharmacological activity of new carbonyl derivatives of 1-aryl-2-iminoimidazolidine. P. 2: Synthesis and pharmacological activity of 1,6-diaryl-5,7(1H)dioxo-2,3-dihydroimidazo[1,2-ŕ][1,3,5]triazines.
Autorzy: Matosiuk Dariusz, Fidecka Sylwia, Antkiewicz-Michaluk Lucyna, Lipkowski Janusz, Dybala Izabela, Koziol Anna E.
Źródło: Eur. J. Med. Chem. 2002: 37 (9) s.761-772, il., tab., bibliogr. 12 poz.
Sygnatura GBL: 312,629

Hasła klasyfikacyjne GBL:
  • farmacja

    Typ dokumentu:
  • praca doświadczalna
  • praca opublikowana za granicą
  • tytuł obcojęzyczny

    Wskaźnik treści:
  • zwierzęta
  • myszy

    Streszczenie angielskie: Synthesis and pharmacological activity of 1,6-diaryl-5,7 (1H)dioxo-2,3-dihydroimidazo-[1,2-ŕ][1,3,5]triazines (C) are presented. The title compounds were obtained from 1-aryloimidazolinurea derivatives in cyclization reaction with difunctional carbonyl reagents - phosgene (method I) or carbonyldiimidazole (CDI) (method II). Their molecular structures were confirmed by the X-ray analysis of 1-phenyl-6-(4-chlorophenyl)-5,7(1H)-dioxo-2,3-dihydroimidazo[1,2-ŕ][1,3,5]triazine C2) crystals. Compounds C exhibited significant depressive action on the central nervous system (CNS) of the laboratory animals, correlated with very low acute toxicity (LD50 2000 mg kg**-1 i.p.), and showed antinociceptive activity in behavioural models. Reversion of this effect by small dose of naloxone (5 mg kg**-1) can suggest opioid-like mechanism of antinociception produced by these and other carbonyl derivatives of 1-aryl-2-iminoimidazolidine. Additionally, an effect on the serotonin neurotransmission pathway was also observed. The receptor mechanism of activity for investigated compounds was confirmed only for the opioid ć receptor in binding affinity assay test. Same tests performed for the serotonin 5-HT2 and benzodiazepine BZD receptors showed no affinity for tested compounds. The opioid-like and serotonergic activities are similar to these described earlier for chain carbonyl 1-aryl-2-iminoimidazolidine derivatives containing urea moiety, mainly due to similar chemical structure, although compounds C are not able to adopt any of the higher energy confirmations of urea derivatives...

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