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Discovery and SAR of cyclic isothioureas as novel NPY Y1 receptor antagonists |
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| Authors: | Zhong-Yue Sun Zhaoning Zhu Yuanzan Ye Brian McKittrick Michael Czarniecki William Greenlee Deborra Mullins Mario Guzzi |
| Affiliation: | 1. Department of Medicinal Chemistry, Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA;2. Department of Neurobiology, Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA |
| Abstract: | 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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