کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2010830 | 1066990 | 2011 | 11 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Structure-cardiovascular activity relationships in a group of new 8-alkylamino-1,3-dimethyl-7-(2-hydroxy-3-aminopropyl)-3,7-dihydro-1H-purine-2,6-diones
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موضوعات مرتبط
علوم زیستی و بیوفناوری
بیوشیمی، ژنتیک و زیست شناسی مولکولی
زیست شیمی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Structure-cardiovascular activity relationships in a group of new 8-alkylamino-1,3-dimethyl-7-(2-hydroxy-3-aminopropyl)-3,7-dihydro-1H-purine-2,6-diones Structure-cardiovascular activity relationships in a group of new 8-alkylamino-1,3-dimethyl-7-(2-hydroxy-3-aminopropyl)-3,7-dihydro-1H-purine-2,6-diones](/preview/png/2010830.png)
چکیده انگلیسی
On the basis of our earlier studies in a group of 7,8-disubstituted derivatives of 1,3-dimetyl-3,7-dihydropurine-2,6-dione, a series of new 8-alkylamino-1,3-dimethyl-7-(2-hydroxy-3-aminopropyl)-3,7-dihydropurine-2,6-diones (8-15) were synthesized and tested for their electrocardiographic, antiarrhythmic and hypotensive activity and for α1- and α2-adrenoreceptor affinities. Among the new derivatives, compounds with the 7-[2-hydroxy-3-(4-phenylpiperazine)-propyl] substituent (9-11) displayed prophylactic antiarrhythmic activity in epinephrine-induced arrhythmia. Analogue 10 with the 8-(2-morpholin-4-yl)-ethylamino group was the most active (ED50 = 3.9 mg/kg and TI = 59.8), which may indicate that this substituent is preferably important for the antiarrhythmic effect. Only compound 11 with the 8-(2-diethylamino)-ethylamino group significantly decreased the systolic (20.4-28.1%) and diastolic (23.4-33.2%) pressure, but this effect lasted for only 1-5 min. The pharmacologically active compounds 9-11 with the phenyl-piperazine moiety showed affinity for α1-receptors (Ki = 0.143-0.383 µM), but the other compounds were almost (12-15) or completely (8) inactive at this site. Compounds 9-11 and 13-15 displayed moderate to low affinity for α2-receptors (Ki = 0.36-2.7 µM).
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Pharmacological Reports - Volume 63, Issue 2, MarchâApril 2011, Pages 476-486
Journal: Pharmacological Reports - Volume 63, Issue 2, MarchâApril 2011, Pages 476-486
نویسندگان
Grażyna ChÅoÅ-Rzepa, PaweÅ Å»mudzki, Maciej PawÅowski, MaÅgorzata Zygmunt, Barbara Filipek,