کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
9769304 | 1501251 | 2005 | 8 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Antinociceptive activity of new imidazolidine carbonyl derivatives.
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Antinociceptive activity of new imidazolidine carbonyl derivatives. Antinociceptive activity of new imidazolidine carbonyl derivatives.](/preview/png/9769304.png)
چکیده انگلیسی
Synthesis and pharmacological activity of 8-aryl-3,4-dioxo-2H,8H-6,7-dihydroimidazo[2,1-c] [1,2,4]triazines (A) are presented. The title compounds were obtained from 1-aryl-2-hydrazinoimidazolines (1) by cyclization reaction with ethyl oxalate (2). They were tested for pharmacological activity in behavioral animal tests (A1, A3, A5, A6, A8, A9). With relatively low acute toxicity (LD50 in range from 1100 to over 2000 mg kg-1, intraperitoneally, i.p.), some of them exhibited significant antinociceptive activity as the result of the 'writhing' test indicated. Especially strong antinociception for compound A8 and significant for A6 was observed in doses of 12.5-200 mg (0.00625-0.1 LD50) and 37.5-150 mg (0.025-0.1 LD50), respectively. Reversion of the antinociception for A1 and A8 produced in the 'writhing' test by 5 mg kg-1 dose of naloxon can suggest an opioid-like mechanism of their analgesic activity. Additionally, compound A9 reduced number of the “head twitch” episodes after 5-hydroxytryptophan (5-HTP) administration with no antinociceptive effect at all and compound A3 showed significant protection in the pentylentetrazol-induced seizure model. Differences observed in the activity spectrum between A8 and A9 derivatives can be explained on the base of difference in the amido-imido tautomeric equilibrium observed between these two compounds.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Medicinal Chemistry - Volume 40, Issue 2, February 2005, Pages 127-134
Journal: European Journal of Medicinal Chemistry - Volume 40, Issue 2, February 2005, Pages 127-134
نویسندگان
Krzysztof Sztanke, Sylwia Fidecka, Ewa KÄdzierska, Zbigniew Karczmarzyk, Kalevi Pihlaja, Dariusz Matosiuk,