Title of article
Discovery of orally available spirodiketopiperazine-based CCR5 antagonists Original Research Article
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 ,
Issue Information
روزنامه با شماره پیاپی سال 2010
Pages
16
From page
5208
To page
5223
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.
Keywords
CCR5 , Chemokine , Anti HIV
Journal title
Bioorganic and Medicinal Chemistry
Serial Year
2010
Journal title
Bioorganic and Medicinal Chemistry
Record number
1306720
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