Bioorganic and Medicinal Chemistry, volume 21, issue 24, pages 7884-7889

A CD4 mimic as an HIV entry inhibitor: pharmacokinetics.

Chie Hashimoto 1
Tetsuo Narumi 1
HIroyuki Otsuki 2
Yuki Hirota 1
Hiroshi Arai 1
Kazuhisa Yoshimura 3, 4
Shigeyoshi Harada 3, 4
Nami Ohashi 1
Wataru Nomura 1
Tomoyuki Miura 2
Tatsuhiko Igarashi 2
Shuzo Matsushita 5
H Tamamura 1
3
 
AIDS Research Center, National Institute of Infectious Diseases, Shinjuku-ku, Tokyo 162-8640, Japan
4
 
Center for AIDS Research, Kumamoto University, Kumamoto 860-0811, Japan
5
 
Center for AIDS Research, Kumamoto University, Kumamoto 860-0811, Japan.
Publication typeJournal Article
Publication date2013-12-01
Quartile SCImago
Q2
Quartile WOS
Q1
Impact factor3.5
ISSN09680896, 14643391
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Abstract
To date, several small molecules of CD4 mimics, which can suppress competitively the interaction between an HIV-1 envelope glycoprotein gp120 and a cellular surface protein CD4, have been reported as viral entry inhibitors. A lead compound 2 (YYA-021) with relatively high potency and low cytotoxicity has been identified previously by SAR studies. In the present study, the pharmacokinetics of the intravenous administration of compound 2 in rats and rhesus macaques is reported. The half-lives of compound 2 in blood in rats and rhesus macaques suggest that compound 2 shows wide tissue distribution and relatively high distribution volumes. A few hours after the injection, both plasma concentrations of compound 2 maintained micromolar levels, indicating it might have promise for intravenous administration when used combinatorially with anti-gp120 monoclonal antibodies.

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GOST |
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GOST Copy
Hashimoto C. et al. A CD4 mimic as an HIV entry inhibitor: pharmacokinetics. // Bioorganic and Medicinal Chemistry. 2013. Vol. 21. No. 24. pp. 7884-7889.
GOST all authors (up to 50) Copy
Hashimoto C., Narumi T., Otsuki H., Hirota Y., Arai H., Yoshimura K., Harada S., Ohashi N., Nomura W., Miura T., Igarashi T., Matsushita S., Tamamura H. A CD4 mimic as an HIV entry inhibitor: pharmacokinetics. // Bioorganic and Medicinal Chemistry. 2013. Vol. 21. No. 24. pp. 7884-7889.
RIS |
Cite this
RIS Copy
TY - JOUR
DO - 10.1016/j.bmc.2013.10.005
UR - https://doi.org/10.1016/j.bmc.2013.10.005
TI - A CD4 mimic as an HIV entry inhibitor: pharmacokinetics.
T2 - Bioorganic and Medicinal Chemistry
AU - Hashimoto, Chie
AU - Narumi, Tetsuo
AU - Otsuki, HIroyuki
AU - Hirota, Yuki
AU - Arai, Hiroshi
AU - Yoshimura, Kazuhisa
AU - Harada, Shigeyoshi
AU - Ohashi, Nami
AU - Nomura, Wataru
AU - Miura, Tomoyuki
AU - Igarashi, Tatsuhiko
AU - Matsushita, Shuzo
AU - Tamamura, H
PY - 2013
DA - 2013/12/01 00:00:00
PB - Elsevier
SP - 7884-7889
IS - 24
VL - 21
SN - 0968-0896
SN - 1464-3391
ER -
BibTex |
Cite this
BibTex Copy
@article{2013_Hashimoto,
author = {Chie Hashimoto and Tetsuo Narumi and HIroyuki Otsuki and Yuki Hirota and Hiroshi Arai and Kazuhisa Yoshimura and Shigeyoshi Harada and Nami Ohashi and Wataru Nomura and Tomoyuki Miura and Tatsuhiko Igarashi and Shuzo Matsushita and H Tamamura},
title = {A CD4 mimic as an HIV entry inhibitor: pharmacokinetics.},
journal = {Bioorganic and Medicinal Chemistry},
year = {2013},
volume = {21},
publisher = {Elsevier},
month = {dec},
url = {https://doi.org/10.1016/j.bmc.2013.10.005},
number = {24},
pages = {7884--7889},
doi = {10.1016/j.bmc.2013.10.005}
}
MLA
Cite this
MLA Copy
Hashimoto, Chie, et al. “A CD4 mimic as an HIV entry inhibitor: pharmacokinetics..” Bioorganic and Medicinal Chemistry, vol. 21, no. 24, Dec. 2013, pp. 7884-7889. https://doi.org/10.1016/j.bmc.2013.10.005.
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