Title of article :
Syntheses of tetrahydrothiophenes and tetrahydrofurans and studies of their derivatives as melanocortin-4 receptor ligands
Author/Authors :
Joe A. Tran، نويسنده , , Caroline W. Chen، نويسنده , , Fabio C. Tucci، نويسنده , , Wanlong Jiang، نويسنده , , Beth A. Fleck، نويسنده , , Chen Chen، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2008
Abstract :
Piperazinebenzylamine derivatives from trans-4-(4-chlorophenyl)tetrahydrothiophene-3-carboxylic acid 6 and its S-oxide 7 and sulfone 8, and the tetrahydrofuran 9 and its two regioisomers 11 and 13 were synthesized and studied for their binding affinities at the human melanocortin-4 receptor. These five-membered ring constrained compounds possessed similar or lower potency compared to the acyclic analogs.
Keywords :
Stereoisomer , Piperazinebenzylamine , Binding affinity , Synthesis , Tetrahydrothiophene , Tetrahydrofuran , melanocortin-4 receptor , Cyclization , Heterocycle
Journal title :
Bioorganic & Medicinal Chemistry Letters
Journal title :
Bioorganic & Medicinal Chemistry Letters
