Author/Authors :
Thomas H. Marsilje، نويسنده , , Jonathan B Roses، نويسنده , , Emily F Calderwood، نويسنده , , Stephen G Stroud، نويسنده , , Nancy E Forsyth، نويسنده , , Christopher Blackburn، نويسنده , , David L Yowe، نويسنده , , Wenyan Miao، نويسنده , , Stacey V Drabic، نويسنده , , Marie D Bohane، نويسنده , , J Scott Daniels، نويسنده , , Ping Li، نويسنده , , Lijun Wu، نويسنده , , Michael A. Patane، نويسنده , , Christopher F. Claiborne، نويسنده ,
Abstract :
A novel series of imidazole-based small molecule antagonists of the melanocortin 4 receptor (MC4-R) is reported. Members of this series have been identified, which exhibit sub-micromolar binding affinity for the MC4-R, functional potency <100 nM, and good oral exposure in rat. Antagonists of the MC4-R are potentially useful in the therapeutic treatment of involuntary weight loss due to advanced age or disease (e.g. cancer or AIDS), an area of large, unmet medical need.
Keywords :
USA.Tel.: +1-858-332-4604 , CA 92121 , e-mail: tmarsilje@gnf.org , MC4-R , Melanocortin receptor , Antagonist.* Corresponding author at present address: Department of MedicinalChemistry , Genomics Institute of the Novartis Research Foundation(GNF) , 10675 John Jay Hopkins Dr. , San Diego , fax: +1-858-812-1648
