Karl-Heinz Budt
Aventis Pharma
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Publication
Featured researches published by Karl-Heinz Budt.
Tetrahedron Letters | 1992
Bernd Stowasser; Karl-Heinz Budt; Li Jian-Qi; Anusch Peyman; Dieter Ruppert
Abstract The snythesis of novel hybrid transition state analogs, a combination of phosphinic acid- and hydroxy-methylene-type inhibitors of HIV protease, is demonstrated. These nonsymmetrical structures, placed in a peripheric C 2 -symmetrical environment, inhibit HIV protease in the lower nanomolar range.
Tetrahedron Letters | 1992
Anusch Peyman; Karl-Heinz Budt; Jörg Spanig; Bernd Stowasser; Dieter Ruppert
Abstract The synthesis of the previously not accessible symmetrical bis(α-aminoalkyl)phosphinic acids is demonstrated. These compounds are valuable central building blocks in the synthesis of HIV protease inhibitors.
Bioorganic & Medicinal Chemistry Letters | 1994
Anusch Peyman; Wilhelm Stahl; Konrad Wagner; Dieter Ruppert; Karl-Heinz Budt
Abstract The use of bis(α-aminoalkyl)phosphinic acids as analogs of the tetrahedral intermediate formed on the path to peptide hydrolysis in combination with a mimic for a structural water, which is found in HIV protease inhibitor complexes, leads to potent inhibitors of HIV-1 protease.
Bioorganic & Medicinal Chemistry | 1995
Karl-Heinz Budt; Anusch Peyman; Jutta Hansen; Jochen Knolle; Christoph Meichsner; Arno Paessens; Dieter Ruppert; Bernd Stowasser
A detailed structure-activity relationship of C2-symmetric diol inhibitors of HIV-1 protease leads to inhibitor 6 (HOE/BAY 793) which is outstanding in the inhibition of the enzyme and in the inhibition of viral replication in HIV infected cell culture (IC50: 0.3 nM; EC50: 3 nM). There are well defined steric requirements for the design of the side chains P1-P3 of the inhibitors. In addition, all three side chains need to be lipophilic. While the enzyme tolerates hydrophilic substituents in some cases, drastic reductions in anti-HIV activity are observed in cell culture, most likely due to insufficient cell penetration.
Bioorganic & Medicinal Chemistry Letters | 1994
Anusch Peyman; Konrad Wagner; Karl-Heinz Budt; Jörg Spanig; Dieter Ruppert; Christoph Meichsner; Arno Paessens
Abstract The inhibition of HIV protease with C2-symmetric phosphinic acid based inhibitors is independent of the dissociation grade of the phosphinic acid. The corresponding amides are not only good inhibitors of HIV protease but also inhibit HIV replication in vitro because of their increased lipophilicity.
FEBS Journal | 1997
Gudrun Lange-Savage; Harald Berchtold; Alexander Liesum; Karl-Heinz Budt; Anusch Peyman; Jochen Knolle; Juraj Sedláček; Milan Fábry; Rolf Hilgenfeld
Archive | 1994
Karl-Heinz Budt; Bernd Stowasser; Anuschirwan Peyman; Jochen Knolle; Irvin Winkler; Hans-Gerd Berscheid
Angewandte Chemie | 1993
Anusch Peyman; Karl-Heinz Budt; Jörg Spanig; Dieter Ruppert
Archive | 1991
Anuschirwan Peyman; Eugen Uhlmann; Karl-Heinz Budt; Jochen Knolle; Irvin Winkler; Matthias Helsberg
Archive | 1995
Anuschirwan Peyman; Wilhelm Stahl; Karl-Heinz Budt; Dieter Ruppert; Henning Schüssler; Konrad Wagner