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Updated: Aug 9, 2026

12:37
Pharmacologic Induction of Epidermal Melanin and Protection Against Sunburn in a Humanized Mouse Model
Published on: September 7, 2013
Discovery of melanin-concentrating hormone receptor R1 antagonists using high-throughput synthesis
Jing Su1, Brian A McKittrick, Haiqun Tang
1Department of Chemical Research, Schering-Plough Research Institute K15 2545, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. jing.su@spcorp.com
Bioorganic & Medicinal Chemistry
|February 9, 2005
Abstract:
A structure-activity study on benzylpiperidine 1 was accomplished by utilizing high-throughput synthesis. Three focused libraries were designed and synthesized to quickly develop SAR. Further optimization led to the discovery of compound 2, an MCH receptor R1 antagonist with over 400-fold improvement in biological activity over the original lead.

