New Substituted 1-(2,3-Dihydrobenzo[1,4]dioxin-2-ylmethyl)piperidin-4-yl Derivatives with α2-Adrenoceptor Antagonist Activity
The emergence of a novel theory concerning the role of noradrenaline in the progression and the treatment of neurodegenerative diseases such as Parkinson's and Alzheimer's diseases has provided a new impetus toward the discovery of novel compounds acting at α2-adrenoceptors. A series of su...
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| Veröffentlicht in: | Journal of medicinal chemistry 2000-10, Vol.43 (20), p.3653-3664 |
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| container_end_page | 3664 |
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| container_issue | 20 |
| container_start_page | 3653 |
| container_title | Journal of medicinal chemistry |
| container_volume | 43 |
| creator | Mayer, Patrice Brunel, Pascale Chaplain, Céline Piedecoq, Christel Calmel, Francis Schambel, Philippe Chopin, Philippe Wurch, Thierry Pauwels, Petrus J Marien, Marc Vidaluc, Jean-Louis Imbert, Thierry |
| description | The emergence of a novel theory concerning the role of noradrenaline in the progression and the treatment of neurodegenerative diseases such as Parkinson's and Alzheimer's diseases has provided a new impetus toward the discovery of novel compounds acting at α2-adrenoceptors. A series of substituted 1-(2,3-dihydrobenzo[1,4]dioxin-2-ylmethyl)piperidin-4-yl derivatives bearing an amide, urea, or imidazolidinone moiety was studied. Some members of this series of compounds proved to be potent α2-adrenoceptor antagonists with good selectivity versus α1-adrenergic and D2-dopamine receptors. Particular emphasis is given to compound 33g which displays potent α2-adrenoceptor binding affinity in vitro and central effects in vivo following oral administration. |
| doi_str_mv | 10.1021/jm991121g |
| format | Article |
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Med. Chem</addtitle><description>The emergence of a novel theory concerning the role of noradrenaline in the progression and the treatment of neurodegenerative diseases such as Parkinson's and Alzheimer's diseases has provided a new impetus toward the discovery of novel compounds acting at α2-adrenoceptors. A series of substituted 1-(2,3-dihydrobenzo[1,4]dioxin-2-ylmethyl)piperidin-4-yl derivatives bearing an amide, urea, or imidazolidinone moiety was studied. Some members of this series of compounds proved to be potent α2-adrenoceptor antagonists with good selectivity versus α1-adrenergic and D2-dopamine receptors. Particular emphasis is given to compound 33g which displays potent α2-adrenoceptor binding affinity in vitro and central effects in vivo following oral administration.</description><subject>Biological and medical sciences</subject><subject>Catecholaminergic system</subject><subject>Medical sciences</subject><subject>Neuropharmacology</subject><subject>Neurotransmitters. 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| ispartof | Journal of medicinal chemistry, 2000-10, Vol.43 (20), p.3653-3664 |
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| language | eng |
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| source | American Chemical Society Journals |
| subjects | Biological and medical sciences Catecholaminergic system Medical sciences Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments |
| title | New Substituted 1-(2,3-Dihydrobenzo[1,4]dioxin-2-ylmethyl)piperidin-4-yl Derivatives with α2-Adrenoceptor Antagonist Activity |
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