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Design of HIV-1 protease inhibitors active on multidrug-resistant virus. 2005
Dominique L N G Surleraux, and
Herman A de Kock, and
Wim G Verschueren, and
Geert M E Pille, and
Louis J R Maes, and
Anik Peeters, and
Sandrine Vendeville, and
Sandra De Meyer, and
Hilde Azijn, and
Rudi Pauwels, and
Marie-Pierre de Bethune, and
Nancy M King, and
Moses Prabu-Jeyabalan, and
Celia A Schiffer, and
Piet B T P Wigerinck
Tibotec BVBA, Generaal de Wittelaan L 11B 3, B-2800 Mechelen, Belgium.
On the basis of structural data gathered during our ongoing HIV-1 protease inhibitors program, from which our clinical candidate TMC114 9 was selected, we have discovered new series of fused heteroaromatic sulfonamides. The further extension into the P2' region was aimed at identifying new classes of compounds with an improved broad spectrum activity and acceptable pharmacokinetic properties. Several of these compounds display an exceptional broad spectrum activity against a panel of highly cross-resistant mutants. Certain members of these series exhibit favorable pharmacokinetic profiles in rat and dog. Crystal structures and molecular modeling were used to rationalize the broad spectrum profile resulting from the extension into the P2' pocket of the HIV-1 protease.
Related Publications
Dominique L N G Surleraux, and
Herman A de Kock, and
Wim G Verschueren, and
Geert M E Pille, and
Louis J R Maes, and
Anik Peeters, and
Sandrine Vendeville, and
Sandra De Meyer, and
Hilde Azijn, and
Rudi Pauwels, and
Marie-Pierre de Bethune, and
Nancy M King, and
Moses Prabu-Jeyabalan, and
Celia A Schiffer, and
Piet B T P Wigerinck
October 1998,
Drug design and discovery,
Dominique L N G Surleraux, and
Herman A de Kock, and
Wim G Verschueren, and
Geert M E Pille, and
Louis J R Maes, and
Anik Peeters, and
Sandrine Vendeville, and
Sandra De Meyer, and
Hilde Azijn, and
Rudi Pauwels, and
Marie-Pierre de Bethune, and
Nancy M King, and
Moses Prabu-Jeyabalan, and
Celia A Schiffer, and
Piet B T P Wigerinck
April 2018,
ChemMedChem,
Dominique L N G Surleraux, and
Herman A de Kock, and
Wim G Verschueren, and
Geert M E Pille, and
Louis J R Maes, and
Anik Peeters, and
Sandrine Vendeville, and
Sandra De Meyer, and
Hilde Azijn, and
Rudi Pauwels, and
Marie-Pierre de Bethune, and
Nancy M King, and
Moses Prabu-Jeyabalan, and
Celia A Schiffer, and
Piet B T P Wigerinck
January 1998,
The Journal of clinical investigation,
Dominique L N G Surleraux, and
Herman A de Kock, and
Wim G Verschueren, and
Geert M E Pille, and
Louis J R Maes, and
Anik Peeters, and
Sandrine Vendeville, and
Sandra De Meyer, and
Hilde Azijn, and
Rudi Pauwels, and
Marie-Pierre de Bethune, and
Nancy M King, and
Moses Prabu-Jeyabalan, and
Celia A Schiffer, and
Piet B T P Wigerinck
July 2008,
Expert opinion on drug discovery,
Dominique L N G Surleraux, and
Herman A de Kock, and
Wim G Verschueren, and
Geert M E Pille, and
Louis J R Maes, and
Anik Peeters, and
Sandrine Vendeville, and
Sandra De Meyer, and
Hilde Azijn, and
Rudi Pauwels, and
Marie-Pierre de Bethune, and
Nancy M King, and
Moses Prabu-Jeyabalan, and
Celia A Schiffer, and
Piet B T P Wigerinck
May 2003,
Bioorganic & medicinal chemistry letters,
Dominique L N G Surleraux, and
Herman A de Kock, and
Wim G Verschueren, and
Geert M E Pille, and
Louis J R Maes, and
Anik Peeters, and
Sandrine Vendeville, and
Sandra De Meyer, and
Hilde Azijn, and
Rudi Pauwels, and
Marie-Pierre de Bethune, and
Nancy M King, and
Moses Prabu-Jeyabalan, and
Celia A Schiffer, and
Piet B T P Wigerinck
April 2003,
Journal of medicinal chemistry,
Dominique L N G Surleraux, and
Herman A de Kock, and
Wim G Verschueren, and
Geert M E Pille, and
Louis J R Maes, and
Anik Peeters, and
Sandrine Vendeville, and
Sandra De Meyer, and
Hilde Azijn, and
Rudi Pauwels, and
Marie-Pierre de Bethune, and
Nancy M King, and
Moses Prabu-Jeyabalan, and
Celia A Schiffer, and
Piet B T P Wigerinck
May 2013,
Journal of medicinal chemistry,
Dominique L N G Surleraux, and
Herman A de Kock, and
Wim G Verschueren, and
Geert M E Pille, and
Louis J R Maes, and
Anik Peeters, and
Sandrine Vendeville, and
Sandra De Meyer, and
Hilde Azijn, and
Rudi Pauwels, and
Marie-Pierre de Bethune, and
Nancy M King, and
Moses Prabu-Jeyabalan, and
Celia A Schiffer, and
Piet B T P Wigerinck
May 2004,
Clinical infectious diseases : an official publication of the Infectious Diseases Society of America,
Dominique L N G Surleraux, and
Herman A de Kock, and
Wim G Verschueren, and
Geert M E Pille, and
Louis J R Maes, and
Anik Peeters, and
Sandrine Vendeville, and
Sandra De Meyer, and
Hilde Azijn, and
Rudi Pauwels, and
Marie-Pierre de Bethune, and
Nancy M King, and
Moses Prabu-Jeyabalan, and
Celia A Schiffer, and
Piet B T P Wigerinck
November 2003,
Bioorganic & medicinal chemistry letters,
Dominique L N G Surleraux, and
Herman A de Kock, and
Wim G Verschueren, and
Geert M E Pille, and
Louis J R Maes, and
Anik Peeters, and
Sandrine Vendeville, and
Sandra De Meyer, and
Hilde Azijn, and
Rudi Pauwels, and
Marie-Pierre de Bethune, and
Nancy M King, and
Moses Prabu-Jeyabalan, and
Celia A Schiffer, and
Piet B T P Wigerinck
March 1998,
Biochemistry,
