Design of novel CXCR4 antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replication

Renato T. Skerlj,Gary J. Bridger,Ernest J. Mceachern,Curtis Harwig,Christopher Ronald Smith,Alan Kaller,Duane Veale,Helen Yee,Krystyna Skupinska,Rossana Wauthy,Letian Wang,Ian R. Baird,Yongbao Zhu,Kate Burrage,Wen Yang,Michael Sartori,Dana Huskens,Erik De Clercq,Dominique Schols

Design of novel CXCR4 antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replication

2011

Renato T. Skerlj
Gary J. Bridger
Ernest J. Mceachern
Curtis Harwig
Christopher Ronald Smith
Alan Kaller
Duane Veale
Helen Yee
Krystyna Skupinska
Rossana Wauthy
Letian Wang
Ian R. Baird
Yongbao Zhu
Kate Burrage
Wen Yang
Michael Sartori
Dana Huskens
Erik De Clercq
Dominique Schols

A novel series of CXCR4 antagonists were identified based on the substantial redesign of AMD070. These compounds possessed potent anti-HIV-1 activity and showed excellent pharmacokinetics in rat and dog.

Keywords:

Viral replication
Chemokine receptor
CXCR4
Virology
Lentivirus
Biology
tertiary amine
Structure–activity relationship
In vitro
Chemistry
Virus
Pharmacokinetics

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