Author/Authors :
Rena Nishizawa، نويسنده , , Toshihiko Nishiyama، نويسنده , , Katsuya Hisaichi، نويسنده , , Keisuke Hirai، نويسنده , , Hiromu Habashita، نويسنده , , Yoshikazu Takaoka، نويسنده , , Hideaki Tada، نويسنده , , Kenji Sagawa، نويسنده , , Shiro Shibayama، نويسنده , , Kenji Maeda، نويسنده , , Hiroaki Mitsuya، نويسنده , , Hisao Nakai، نويسنده , , Daikichi Fukushima، نويسنده , , Masaaki Toda، نويسنده ,
Abstract :
Using the previously reported novel spirodiketopiperazine scaffold, the design and synthesis of orally available CCR5 antagonists was undertaken. Compounds possessing a carboxylic acid function in the appropriate position showed improved oral exposure (AUC) relative to the initial chemical leads without reduction in the antagonist activity. The optimized compound 40 was found to show potent anti-HIV activity. Full details of structure–activity relationship (SAR) study are presented.
