New Substituted 1-(2,3-Dihydrobenzo[1,4]dioxin-2-ylmethyl)piperidin-4-yl Derivatives with α 2 -Adrenoceptor Antagonist Activity
2000; American Chemical Society; Volume: 43; Issue: 20 Linguagem: Inglês
10.1021/jm991121g
ISSN1520-4804
AutoresPatrice Mayer, P. Brunel, Céline Chaplain, Christel Piedecoq, Francis Calmel, Philippe Schambel, Philippe Chopin, Thierry Wurch, Petrus J. Pauwels, Marc Marien, Jean‐Louis Vidaluc, Thierry Imbert,
Tópico(s)Pharmacological Receptor Mechanisms and Effects
ResumoThe 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 alpha(2)-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 alpha(2)-adrenoceptor antagonists with good selectivity versus alpha(1)-adrenergic and D(2)-dopamine receptors. Particular emphasis is given to compound 33g which displays potent alpha(2)-adrenoceptor binding affinity in vitro and central effects in vivo following oral administration.
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