دورية أكاديمية
Investigation on the antiplatelet activity of pyrrolo[3,2-c]-pyridine-containing compounds
| العنوان: | Investigation on the antiplatelet activity of pyrrolo[3,2-c]-pyridine-containing compounds |
|---|---|
| المؤلفون: | Voskressensky L.G., Carotti A., Borisova T.N., Kulikova L.N., Varlamov A.V., Altomare C., De Candia M. |
| المصدر: | Journal of Pharmacy and Pharmacology |
| بيانات النشر: | Pharmaceutical Press |
| سنة النشر: | 2020 |
| المجموعة: | NORA (National aggregator of open repositories of Russian universities) / Национальный агрегатор открытых репозиториев российских университетов |
| مصطلحات موضوعية: | 1 (4,5,7 trimethyl 4,5,6,7 tetrahydro 1h pyrrolo[3,2 c]pyridin 2 yl)ethanone, 2 (2 chlorobenzyl) 8 methoxy 2,3,4,5 tetrahydro 1h pyrido[4,3 b]indole oxalic acid, 2 benzylaminomethyl 4,5,6,7 tetrahydro 1h pyrrolo[3,2 c]pyridine, 2 ethyl 2,3,4,5 tetrahydro 1h pyrido[4,3 b]indole, 2 [(4,5,7 trimethyl 4,5,6,7 tetrahydro 1h pyrrolo[3,2 c]pyridin 2 yl)methylene]malononitrile, 2,2,2 trifluoro 1 (4,5,7 trimethyl 4,5,6,7 tetrahydro 1h pyrrolo[3,2 c]pyridin 2 yl)ethanol, 2,2,2 trifluoro 1 (4,5,7 trimethyl 4,5,6,7 tetrahydro 1h pyrrolo[3,2 c]pyridin 2 yl)ethanone, 2,3,4,5 tetrahydro 1h pyrido[4,3 b]indole derivative, 4,5,6,7 tetrahydro 1h pyrrolo[3,2 c]pyridine derivative, 4,5,7 trimethyl 4,5,6,7 tetrahydro 1h pyrrolo[3,2 c]pyridine 2 carbaldehyde oxime, 4,5,7 trimethyl 4,5,6,7 tetrahydro 1h pyrrolo[3,2 c]pyridine 2 carbonitrile, 5 acetyl 1 vinyl 4,5,6,7 tetrahydro 1h pyrrolo[3,2 c]pyridine derivative, 5 benzyl 4,5,6,7 tetrahydro 1h pyrrolo[3,2 c]pyridine, acetylsalicylic acid, adenosine diphosphate, adrenalin, n benzyl n [(4,5,7 trimethyl 4,5,6,7 tetrahydro 1h pyrrolo[3,2 c]pyridin 2 yl)methyl]amine monooxalic acid, n [(4,5,7 trimethyl 4,5,6,7 tetrahydro 1h pyrrolo[3,2 c]pyridin 2 yl)methyl]propane 1,3 diamine monooxalic acid, pyrrolo[3,2 c]pyridine derivative, thromboxane A2, ticlopidine, unclassified drug, adrenalin release, adult, article, calculation, comparative study, controlled study, dose response, drug potency |
| الوصف: | A series of 4,5,6,7-tetrahydro-1H-pyrrolo[3,2-c]pyridines (THPPs), mostly C(2)-substituted derivatives, and some 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles (THPIs) were synthesized and tested in-vitro for their ability to inhibit aggregation of human platelet-rich plasma (PRP) induced by adenosine 5′-diphosphate (ADP) and adrenaline (epinephrine). 5-Benzyl THPP (3), 2-(benzylamino)methyl THPP (5f) and 2-ethyl THPI (6) moderately and dose-dependently inhibited platelet aggregation induced by adrenaline and, to a lesser extent, by ADP. These compounds inhibited the second phase of the PRP aggregation triggered by adrenaline, which largely depends upon thromboxane A2 production and ADP release. In the adrenaline-stimulated aggregation, the THPI derivative 6 was found to be nearly equipotent with aspirin, their IC50 values (concentration effecting 50% inhibition of aggregation) being 90 and 60 μM, respectively. A relation between activity and calculated octanol-water partition coefficient suggested that a log P value around 2.5 should be the optimal lipophilicity value for the activity of THPP-containing compounds. |
| نوع الوثيقة: | article in journal/newspaper |
| اللغة: | English |
| العلاقة: | https://doi.org/10.1211/002235702676Test; https://openrepository.ru/article?id=259077Test |
| الإتاحة: | https://doi.org/10.1211/002235702676Test https://openrepository.ru/article?id=259077Test |
| حقوق: | open access |
| رقم الانضمام: | edsbas.F7836D8 |
| قاعدة البيانات: | BASE |
| الوصف غير متاح. |