title: Spirodiketopiperazine-based CCR5 antagonists: Improvement of their pharmacokinetic profiles.
abstract: 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.
authors.affiliation: Minase Research Institute, Ono Pharmaceutical Co., Ltd, Shimamoto, Mishima, Osaka 618-8585, Japan. r.nishizawa@ono.co.jp
authors.forename: Rena
authors.initials: R
authors.lastname: Nishizawa
authors.forename: Toshihiko
authors.initials: T
authors.lastname: Nishiyama
authors.forename: Katsuya
authors.initials: K
authors.lastname: Hisaichi
authors.forename: Keisuke
authors.initials: K
authors.lastname: Hirai
authors.forename: Hiromu
authors.initials: H
authors.lastname: Habashita
authors.forename: Yoshikazu
authors.initials: Y
authors.lastname: Takaoka
authors.forename: Hideaki
authors.initials: H
authors.lastname: Tada
authors.forename: Kenji
authors.initials: K
authors.lastname: Sagawa
authors.forename: Shiro
authors.initials: S
authors.lastname: Shibayama
authors.forename: Kenji
authors.initials: K
authors.lastname: Maeda
authors.forename: Hiroaki
authors.initials: H
authors.lastname: Mitsuya
authors.forename: Hisao
authors.initials: H
authors.lastname: Nakai
authors.forename: Daikichi
authors.initials: D
authors.lastname: Fukushima
authors.forename: Masaaki
authors.initials: M
authors.lastname: Toda
mesh_terms: 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
chemical_list: D019380:Anti-HIV Agents; D065100:CCR5 Receptor Antagonists; D016655:HIV Core Protein p24; D010879:Piperazines; D019713:Receptors, CCR5