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  • Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 1.

Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 1.

Bioorganic & medicinal chemistry letters (2004-09-03)
Andrew J Souers, Dariusz Wodka, Ju Gao, Jared C Lewis, Anil Vasudevan, Robert Gentles, Sevan Brodjian, Brian Dayton, Christopher A Ogiela, Dennis Fry, Lisa E Hernandez, Kennan C Marsh, Christine A Collins, Philip R Kym
PMID15341942
ABSTRACT

A high-throughput screen was performed in order to identify chemotypes that are bound by the melanin concentrating hormone receptor-1 (MCHr1). A novel 2-amino-8-alkoxyquinoline compound (1) was identified and subsequently optimized using a parallel and automated procedure for the rapid production of multiple analogs. The structure-activity relationships that emerged from this effort are described, along with selected pharmacokinetic parameters of compound (d)-61 when dosed orally in diet-induced obese mice.