1.
Bioorg Med Chem Lett
; 15(16): 3753-7, 2005 Aug 15.
Article
in English
| MEDLINE
| ID: mdl-16002287
ABSTRACT
Virtual screening studies have identified a series of phenylpyrroles as novel 5-HT7 receptor ligands. The synthesis and the affinity for the 5-HT7 receptor of these phenylpyrroles are described. Some of these compounds exhibited high affinity for the 5-HT7 receptors.
Subject(s)
Pyrroles/classification , Pyrroles/pharmacology , Receptors, Serotonin/drug effects , Animals , Binding, Competitive/drug effects , Drug Evaluation, Preclinical , Humans , Ligands , Molecular Structure , Pyrroles/chemical synthesis , Rats , Structure-Activity Relationship
2.
J Enzyme Inhib Med Chem
; 19(6): 585-93, 2004 Dec.
Article
in English
| MEDLINE
| ID: mdl-15662962
ABSTRACT
Fifteen new thieno[2,3-b ]- and thieno[3,4-b]pyrrolizines were synthesized and tested against two protein kinases, CDK1/cyclin B and GSK-3. Among these compounds, 3-(3-hydroxy-4-methoxyphenyl)-8H-thieno[2,3-b]pyrrolizin-8-one 4g was identified as a moderate inhibitor of these kinases. Its molecular modeling study brought to the fore the pivotal role of the 2-methoxyphenol grouping and the interest in replacing it by bioisosteric moieties in future pharmacomodulations.