Author/Authors :
Wallace T. Ashton، نويسنده , , Rosemary M. Sisco، نويسنده , , Yi Tien Yang، نويسنده , , Jane-Ling Lo، نويسنده , , Joel B. Yudkovitz، نويسنده , , Kang Cheng، نويسنده , , Mark T. Goulet، نويسنده ,
Abstract :
The 2-aryltryptamine class of GnRH receptor antagonists has been modified to incorporate carboxamide and acetamide substituents at the indole 5-position. With either a phenol or methanesulfonamide terminus on the N-aralkyl side chain, potent binding affinity to the GnRH receptor was achieved. A functional assay for GnRH antagonism was even more sensitive to structural modification and revealed a strong preference for branched tertiary amides.
