Wynik wyszukiwania w bazie Polska Bibliografia Lekarska GBL

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Tytuł oryginału: Synthesis and pharmacological activity of new carbonyl derivatives of 1-aryl-2-iminoimidazolidine. P. 3: Synthesis and pharmacological activity of 1-aryl-5,6(1H)dioxo-2,3-dihydroimidazol[1,2-a]imidazoles.
Autorzy: Matosiuk Dariusz, Fidecka Sylwia, Antkiewicz-Michaluk Lucyna, Dybala Izabela, Kozioł Anna E.
Źródło: Eur. J. Med. Chem. 2002: 37 (10) s.845-853, il., tab., bibliogr. 20 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-aryl-5,6(1 H)dioxo-2,3-dihydroimidazo[1,2-a]imidazoles (D) are presented. The title compounds were obtained from 1-aryl-2-iminoimidazolidines (1) by cyclization reaction with oxalic acid derivatives-ethyl ester (2) or chloride (3). They were tested for pharmacological activity in animal and binding assay tests. With moderate acute toxicity (LD50 ~ 200 mg kg**-1, i.p.), they exhibited significant and serotonergic activities as results of the `writhing' and the `hot plate' tests indicated, and reduced number of `head twitch' episodes after 5-HTP (5-hydroxytryptophan) administration. Reversion of the antinociception produced in the `writhing' test by small dose of naloxon (5 mg kg**-1) can suggest an opioid-like mechanism of their analgesic activity. The probable receptor inhibition mechanism of their analgesic and serotonergic activity was confirmed in the binding assay tests (by radioligand displacement) toward the opioid ć and serotonin 5-HT2 receptors. Additionally, they exhibited affinity toward the benzodiazepine (BZD) receptor as well, although in behavioral tests compounds did not produce any clear depressive effect on the central nervous system (CNS) of mice. Simple chemical structure of the title compounds, in comparison to other carbonyl derivatives of 1-aryl-2-iminoimidazolidine presented in this series of papers, underline very important role both of a hydrophobic moiety (aromatic ring) and polar groups (hydrogen-bond acceptors) in the serotonin receptor interaction. The coexistence of opioid-like, serotonergic and BZD receptor inhibition activity can be very interesting and can lead to creation of the novel group of antidepressants.

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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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    Tytuł oryginału: Synteza oraz ocena aktywności w ośrodkowym układzie nerwowym nowych karbonylowych pochodnych imidazoliny : rozprawa habilitacyjna
    Autorzy: Matosiuk Dariusz; Akademia Medyczna Katedra i Zakład Syntezy i Technologii Chemicznej Środków Leczniczych w Lublinie
    Źródło: - Lublin, AM 2002, 147, [68] s. : il., tab., bibliogr. 174 poz., 24 cm. - Zawiera przedruki 6 prac współautorskich
    Sygnatura GBL: 735,649

    Hasła klasyfikacyjne GBL:
  • toksykologia
  • farmacja
  • neurologia

    Typ dokumentu:
  • praca doświadczalna
  • rozprawa habilitacyjna

    Wskaźnik treści:
  • zwierzęta
  • myszy
  • szczury

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