Syntheses of tetrahydrothiophenes and tetrahydrofurans and studies of their derivatives as melanocortin-4 receptor ligands

JA Tran, CW Chen, FC Tucci, W Jiang, BA Fleck…

文献索引：Tran, Joe A.; Chen, Caroline W.; Tucci, Fabio C.; Jiang, Wanlong; Fleck, Beth A.; Chen, Chen Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 3 p. 1124 - 1130

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被引用次数: 10

摘要

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.