Discovery and Selection of TMC114, a Next Generation HIV-1 Protease Inhibitor §
✍ Scribed by Surleraux, Dominique L. N. G.; Tahri, Abdellah; Verschueren, Wim G.; Pille, Geert M. E.; de Kock, Herman A.; Jonckers, Tim H. M.; Peeters, Anik; De Meyer, Sandra; Azijn, Hilde; Pauwels, Rudi; de Bethune, Marie-Pierre; King, Nancy M.; Prabu-Jeyabalan, Moses; Schiffer, Celia A.; Wigerinck, Piet B. T. P.
- Book ID
- 121495023
- Publisher
- American Chemical Society
- Year
- 2005
- Tongue
- English
- Weight
- 343 KB
- Volume
- 48
- Category
- Article
- ISSN
- 0022-2623
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Several small, achiral nonpeptide inhibitors of HIV-1 protease with low micromolar activity were identified by mass screening of the Parke-Davis compound library. Two of the compounds, structurally similar, were both found to be competitive and reversible inhibitors [compound 1, 4-hydroxy-3-(3-pheno