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N-Aminoimidazole Derivatives Inhibiting Retroviral Replication via a Yet Unidentified Mode of Action

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Laboratory of Medicinal Chemistry and Laboratory of Virology and Chemotherapy, Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, B-3000 Leuven, Belgium
Cite this: J. Med. Chem. 2003, 46, 8, 1546–1553
Publication Date (Web):March 11, 2003
https://doi.org/10.1021/jm0211117
Copyright © 2003 American Chemical Society

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    Abstract

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    The synthesis of a series of N-aminoimidazoles (NAIMs) with an uncommon spectrum of antiretroviral activity is described. From a group of 60 closely related molecules, we were able to subdivide the molecules in different groups based on their anti-HIV and anti-SIV activity in vitro:  (i) molecules acting on a new, immediate postintegration step, (ii) molecules acting on both postintegration and HIV-1 reverse transcriptase (RT) as NNRTI, and (iii) molecules that mainly act at the HIV-1 RT according to an NNRTI-type mode of action.

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     Laboratory of Medicinal Chemistry.

     Both authors contributed equally.

    *

     To whom correspondence should be addressed. Phone: +32 16 33 73 87. Fax:  +32 16 33 73 40. E-mail:  piet.herdewijn@ rega.kuleuven.ac.be.

    §

     Laboratory of Virology and ChemotherapyIntroduction.

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    Syntheses and NMR data of NAIM derivatives. This material is available free of charge via the Internet at http://pubs.acs.org.

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