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Identification of Novel Non-nucleoside Reverse Transcriptase Inhibitors Using Fragment-based Lead Generation

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Abstract

Design, synthesis and anti-HIV activity of a series of 4,6-diaryl-2-aminopyrimidines are reported in this paper. Two of the synthesized compounds proved to be effective in inhibiting HIV-1 replication at micromolar concentrations. However, their selectivity indices are rather weak.

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Authors and Affiliations

  1. Pharmacy Department, Faculty of Technology and Engineering, Kalabhavan, The M.S University of Baroda, Vadodara, 390 001, India

    R. Ramajayam, Rajani Giridhar, M. R. Yadav & Dhaval G. Prajapati

  2. Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, B-3000, Leuven, Belgium

    Erick De Clercq & Christophe Pannecouque

Authors
  1. R. Ramajayam
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  2. Rajani Giridhar
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  3. M. R. Yadav
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  4. Erick De Clercq
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  5. Christophe Pannecouque
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  6. Dhaval G. Prajapati
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Corresponding author

Correspondence to Rajani Giridhar.

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Ramajayam, R., Giridhar, R., Yadav, M.R. et al. Identification of Novel Non-nucleoside Reverse Transcriptase Inhibitors Using Fragment-based Lead Generation. Med Chem Res 14, 475–487 (2005). https://doi.org/10.1007/s00044-006-0151-5

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  • DOI: https://doi.org/10.1007/s00044-006-0151-5

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