Synthesis and Analgesic Activity of Some Side-Chain Modified Anpirtoline Derivatives
| Autor: | Jan Proška, Stanislav Radl, Petr Hezký, Lucie Hejnova, Ivan Krejci |
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| Rok vydání: | 2000 |
| Předmět: |
Male
Models Molecular Pyrrolidines Pyridines Stereochemistry Pharmaceutical Science Mice Inbred Strains Ring (chemistry) Binding Competitive Pyrrolidine Mice chemistry.chemical_compound Acetic acid Piperidines Drug Discovery Side chain Animals Moiety Pain Measurement Octane Analgesics Molecular Structure Brain Rats Piperazine chemistry Receptors Serotonin Piperidine Protein Binding |
| Zdroj: | ResearcherID |
| ISSN: | 1521-4184 0365-6233 |
| Popis: | New derivatives of anpirtoline and deazaanpirtoline modified in the side chain have been synthesized. The series includes compounds 3 with side-chains containing piperidine or pyrrolidine rings, compounds 4 containing 8-azabicyclo[3.2.1]octane moiety, and compounds 5 having piperazine ring in their side-chains. Their receptor binding profiles (5-HT1A, 5-HT1B) and analgesic activity (hot plate, acetic acid induced writhing) have been studied. Optimized structures (PM3-MOPAC, Alchemy 2000, Tripos Inc.) of the synthesized compounds 3-5 were compared with that of anpirtoline. |
| Databáze: | OpenAIRE |
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