| Literature DB >> 12192147 |
Axel Reinhard Stoit1, Jos Hubertus Maria Lange, Arnold Peter den Hartog, Eric Ronken, Koos Tipker, Herman Heinrich van Stuivenberg, Jessica Adriana Rigtje Dijksman, Henri Cornelis Wals, Chris Gerrit Kruse.
Abstract
The design, synthesis and biological activities of potent pyrazole-based tricyclic CB1 receptor antagonists (2) are described. The key synthetic step involves the ring closure of the lithiated alpha, gamma-keto ester adduct (4). The optimal nitroderivative (28) in this series exhibits a high CB1 receptor affinity (pKi=7.2) as well as very potent antagonistic activity (pA2=8.8) in vitro. The regioselectivity of the pyrazole ring closure is shown to depend strongly on the aromatic substitution pattern of the applied arylhydrazine.Entities:
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Year: 2002 PMID： 12192147 DOI： 10.1248/cpb.50.1109
Source DB: PubMed Journal: Chem Pharm Bull (Tokyo) ISSN： 0009-2363 Impact factor: 1.645