Author/Authors :
Andrew J. Souers، نويسنده , , Dariusz Wodka، نويسنده , , Qi-Ju Gao، نويسنده , , Jared C. Lewis، نويسنده , , Anil Vasudevan، نويسنده , , Robert Gentles، نويسنده , , Sevan Brodjian، نويسنده , , Brian Dayton، نويسنده , , Christopher A. Ogiela، نويسنده , , Dennis Fry، نويسنده , , Lisa E. Hernandez، نويسنده , , Kennan C. Marsh، نويسنده , , Christine A. Collins، نويسنده , , Philip R. Kym، نويسنده ,
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.
Keywords :
Melanin concentrating hormone , Obesity.* Corresponding author. Tel.: +1-847-937-5312 , fax: +1-847-938-1674 , e-mail: andrew.souers@abbott.com