2. Academic Validation
  3. N-aminoimidazole derivatives inhibiting retroviral replication via a yet unidentified mode of action

N-aminoimidazole derivatives inhibiting retroviral replication via a yet unidentified mode of action

  • J Med Chem. 2003 Apr 10;46(8):1546-53. doi: 10.1021/jm0211117.
Irene M Lagoja 1,  Christophe Pannecouque,  Arthur Van Aerschot,  Myriam Witvrouw,  Zeger Debyser,  Jan Balzarini,  Piet Herdewijn,  Erik De Clercq
Affiliations

Affiliation

  • 1 Laboratory of Medicinal Chemistry, Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, Belgium.
PMID: 12672256 DOI: 10.1021/jm0211117
Abstract

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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