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1. Synthesis of new thiophene and benzo[b]thiophene hydrazide derivatives as human NPY Y(5) antagonists.

Author

Galiano S, Erviti O, Pérez S, Moreno A, Juanenea L, Aldana I, and Monge A

Subjects
Animals, Binding Sites, COS Cells, Chlorocebus aethiops, Humans, Molecular Structure, Structure-Activity Relationship, Receptors, Neuropeptide Y antagonists & inhibitors, Thiophenes chemical synthesis, Thiophenes pharmacology
Abstract

Neuropeptide Y is one of the most potent appetite stimulating hormones known. Novel thiophene and benzo[b]thiophene hydrazide derivatives were synthetized and evaluated biologically as NPY Y(1) and Y(5) receptor subtype antagonists. They were found to have nanomolar binding affinities for human NPY Y(5) receptor, obtaining the lead compound, trans-N-4-[N'-(thiophene-2-carbonyl)hydrazinocarbonyl]cyclohexylmethyl-4-bromobenzenesulfonamide, which binds with a 7.70 nM IC(50) to the hY(5) receptor.

Published
2004
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