Literature DB >> 20005712

Spirodiketopiperazine-based CCR5 antagonists: Improvement of their pharmacokinetic profiles.

Rena Nishizawa1, Toshihiko Nishiyama, Katsuya Hisaichi, Keisuke Hirai, Hiromu Habashita, Yoshikazu Takaoka, Hideaki Tada, Kenji Sagawa, Shiro Shibayama, Kenji Maeda, Hiroaki Mitsuya, Hisao Nakai, Daikichi Fukushima, Masaaki Toda.   

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. Copyright 2009 Elsevier Ltd. All rights reserved.

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Year:  2009        PMID： 20005712      PMCID： PMC7553643          DOI： 10.1016/j.bmcl.2009.11.018

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  14 in total

Review 1.  Chemokines and disease.

Authors:  C Gerard; B J Rollins
Journal:  Nat Immunol       Date:  2001-02       Impact factor: 25.606

2.  Multicomponent Reactions with Isocyanides.

Authors: 
Journal:  Angew Chem Int Ed Engl       Date:  2000-09-15       Impact factor: 15.336

Review 3.  New therapeutics that modulate chemokine networks.

Authors:  Matthias K Schwarz; Timothy N C Wells
Journal:  Nat Rev Drug Discov       Date:  2002-05       Impact factor: 84.694

4.  Spirodiketopiperazine-based CCR5 antagonists: Lead optimization from biologically active metabolite.

Authors:  Rena Nishizawa; Toshihiko Nishiyama; Katsuya Hisaichi; Naoki Matsunaga; Chiaki Minamoto; Hiromu Habashita; Yoshikazu Takaoka; Masaaki Toda; Shiro Shibayama; Hideaki Tada; Kenji Sagawa; Daikichi Fukushima; Kenji Maeda; Hiroaki Mitsuya
Journal:  Bioorg Med Chem Lett       Date:  2006-11-01       Impact factor: 2.823

Review 5.  A comprehensive listing of bioactivation pathways of organic functional groups.

Authors:  Amit S Kalgutkar; Iain Gardner; R Scott Obach; Christopher L Shaffer; Ernesto Callegari; Kirk R Henne; Abdul E Mutlib; Deepak K Dalvie; Jae S Lee; Yasuhiro Nakai; John P O'Donnell; Jason Boer; Shawn P Harriman
Journal:  Curr Drug Metab       Date:  2005-06       Impact factor: 3.731

6.  Identification of a major co-receptor for primary isolates of HIV-1.

Authors:  H Deng; R Liu; W Ellmeier; S Choe; D Unutmaz; M Burkhart; P Di Marzio; S Marmon; R E Sutton; C M Hill; C B Davis; S C Peiper; T J Schall; D R Littman; N R Landau
Journal:  Nature       Date:  1996-06-20       Impact factor: 49.962

7.  CC CKR5: a RANTES, MIP-1alpha, MIP-1beta receptor as a fusion cofactor for macrophage-tropic HIV-1.

Authors:  G Alkhatib; C Combadiere; C C Broder; Y Feng; P E Kennedy; P M Murphy; E A Berger
Journal:  Science       Date:  1996-06-28       Impact factor: 47.728

Review 8.  Chemokine receptors as HIV-1 coreceptors: roles in viral entry, tropism, and disease.

Authors:  E A Berger; P M Murphy; J M Farber
Journal:  Annu Rev Immunol       Date:  1999       Impact factor: 28.527

9.  Design, synthesis, and biological evaluation of the combinatorial library with a new spirodiketopiperazine scaffold. Discovery of novel potent and selective low-molecular-weight CCR5 antagonists.

Authors:  Hiromu Habashita; Masaya Kokubo; Shin-ichi Hamano; Nobuyuki Hamanaka; Masaaki Toda; Shiro Shibayama; Hideaki Tada; Kenji Sagawa; Daikichi Fukushima; Kenji Maeda; Hiroaki Mitsuya
Journal:  J Med Chem       Date:  2006-07-13       Impact factor: 7.446

10.  Spirodiketopiperazine-based CCR5 inhibitor which preserves CC-chemokine/CCR5 interactions and exerts potent activity against R5 human immunodeficiency virus type 1 in vitro.

Authors:  Kenji Maeda; Hirotomo Nakata; Yasuhiro Koh; Toshikazu Miyakawa; Hiromi Ogata; Yoshikazu Takaoka; Shiro Shibayama; Kenji Sagawa; Daikichi Fukushima; Joseph Moravek; Yoshio Koyanagi; Hiroaki Mitsuya
Journal:  J Virol       Date:  2004-08       Impact factor: 5.103
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  3 in total

1.  Discovery of 4-[4-({(3R)-1-butyl-3-[(R)-cyclohexyl(hydroxy)methyl]-2,5-dioxo-1,4,9-triazaspiro[5.5]undec-9-yl}methyl)phenoxy]benzoic acid hydrochloride: a highly potent orally available CCR5 selective antagonist.

Authors:  Rena Nishizawa; Toshihiko Nishiyama; Katsuya Hisaichi; Chiaki Minamoto; Masayuki Murota; Yoshikazu Takaoka; Hisao Nakai; Hideaki Tada; Kenji Sagawa; Shiro Shibayama; Daikichi Fukushima; Kenji Maeda; Hiroaki Mitsuya
Journal:  Bioorg Med Chem       Date:  2011-05-20       Impact factor: 3.641

2.  Discovery of orally available spirodiketopiperazine-based CCR5 antagonists.

Authors:  Rena Nishizawa; Toshihiko Nishiyama; Katsuya Hisaichi; Keisuke Hirai; Hiromu Habashita; Yoshikazu Takaoka; Hideaki Tada; Kenji Sagawa; Shiro Shibayama; Kenji Maeda; Hiroaki Mitsuya; Hisao Nakai; Daikichi Fukushima; Masaaki Toda
Journal:  Bioorg Med Chem       Date:  2010-05-25       Impact factor: 3.641

3.  Spirodiketopiperazine-based CCR5 antagonist: discovery of an antiretroviral drug candidate.

Authors:  Rena Nishizawa; Toshihiko Nishiyama; Katsuya Hisaichi; Chiaki Minamoto; Naoki Matsunaga; Yoshikazu Takaoka; Hisao Nakai; Stephen Jenkinson; Wieslaw M Kazmierski; Hideaki Tada; Kenji Sagawa; Shiro Shibayama; Daikichi Fukushima; Kenji Maeda; Hiroaki Mitsuya
Journal:  Bioorg Med Chem Lett       Date:  2010-12-28       Impact factor: 2.823
  3 in total

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