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  • Syntheses of tetrahydrothio...
    Tran, Joe A.; Chen, Caroline W.; Tucci, Fabio C.; Jiang, Wanlong; Fleck, Beth A.; Chen, Chen

    Bioorganic & medicinal chemistry, 02/2008, Letnik: 18, Številka: 3
    Journal Article

    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.