Spirodiketopiperazine-based CCR5 antagonists: Improvement of their pharmacokinetic profiles.
Spirodiketopiperazine-based CCR5 antagonists, showing improved pharmacokinetic profiles without reduction in antagonist activity, were designed and synthesized. We also demonstrate the anti-HIV activity of a representative compound 12, as measured in a p24 assay.
Nishizawa
Rena
R
Minase Research Institute, Ono Pharmaceutical Co., Ltd, Shimamoto, Mishima, Osaka 618-8585, Japan. r.nishizawa@ono.co.jp
Nishiyama
Toshihiko
T
Hisaichi
Katsuya
K
Hirai
Keisuke
K
Habashita
Hiromu
H
Takaoka
Yoshikazu
Y
Tada
Hideaki
H
Sagawa
Kenji
K
Shibayama
Shiro
S
Maeda
Kenji
K
Mitsuya
Hiroaki
H
Nakai
Hisao
H
Fukushima
Daikichi
D
Toda
Masaaki
M
D000818:Animals; D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics*; D065100:CCR5 Receptor Antagonists; D016655:HIV Core Protein p24 / Q000378:metabolism; D006801:Humans; D008862:Microsomes, Liver / Q000378:metabolism; D010879:Piperazines / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics*; D051381:Rats; D019713:Receptors, CCR5 / Q000378:metabolism
D019380:Anti-HIV Agents; D065100:CCR5 Receptor Antagonists; D016655:HIV Core Protein p24; D010879:Piperazines; D019713:Receptors, CCR5