Discovery and SAR of cyclic isothioureas as novel NPY Y1 receptor antagonists

A class of novel 2-aminobenzothiazoles have been identified as NPY Y1 antagonists. Various N-heterocyclic substituted aminophenethyl-2-aminobenzothiazole analogs were synthesized to explore the SAR. Isothiourea analogs and ligands with high potency (Ki 30 nM) have been identified.

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