New organofluorine building blocks: inhibition of the malarial aspartic proteases plasmepsin II and IV by alicyclic alpha,alpha-difluoroketone hydrates.
暂无分享,去创建一个
F. Diederich | W. Schweizer | L. Hardegger | D. Bur | L. Baitsch | Solange Meyer | C. Fäh
[1] M. Bottomley,et al. Structural and Functional Analysis of the Human HDAC4 Catalytic Domain Reveals a Regulatory Structural Zinc-binding Domain* , 2008, Journal of Biological Chemistry.
[2] Jon Cooper,et al. The catalytic mechanism of an aspartic proteinase explored with neutron and X-ray diffraction. , 2008, Journal of the American Chemical Society.
[3] F. Diederich,et al. Exploring the Flap Pocket of the Antimalarial Target Plasmepsin II: The “55 % Rule” Applied to Enzymes , 2008, ChemMedChem.
[4] F. Diederich,et al. Fluorine in Pharmaceuticals: Looking Beyond Intuition , 2007, Science.
[5] Manfred Kansy,et al. Predicting and Tuning Physicochemical Properties in Lead Optimization: Amine Basicities , 2007, ChemMedChem.
[6] M. Schlitzer,et al. Malaria Chemotherapeutics Part I: History of Antimalarial Drug Development, Currently Used Therapeutics, and Drugs in Clinical Development , 2007, ChemMedChem.
[7] Y. Ebizuka,et al. Actinorhodin biosynthesis: structural requirements for post-PKS tailoring intermediates revealed by functional analysis of ActVI-ORF1 reductase. , 2007, Biochemistry.
[8] Bruno Martoglio,et al. Aspartic proteases in drug discovery. , 2007, Current pharmaceutical design.
[9] L. Prade,et al. Achiral, Cheap, and Potent Inhibitors of Plasmepsins I, II, and IV , 2006, ChemMedChem.
[10] F. Diederich,et al. Starving the malaria parasite: inhibitors active against the aspartic proteases plasmepsins I, II, and IV. , 2006, Angewandte Chemie.
[11] L. Prade,et al. X-ray Structure of Plasmepsin II Complexed with a Potent Achiral Inhibitor* , 2005, Journal of Biological Chemistry.
[12] François Diederich,et al. Orthogonal multipolar interactions in structural chemistry and biology. , 2005, Angewandte Chemie.
[13] S. Hay,et al. The global distribution of clinical episodes of Plasmodium falciparum malaria , 2005, Nature.
[14] Jun Liu,et al. The Role of Plasmodium falciparum Food Vacuole Plasmepsins* , 2005, Journal of Biological Chemistry.
[15] J. Dame,et al. Genetic Disruption of the Plasmodium falciparum Digestive Vacuole Plasmepsins Demonstrates Their Functional Redundancy* , 2004, Journal of Biological Chemistry.
[16] C. Tanyeli,et al. Chemoenzymatic synthesis of a '- and a-acetoxylated cyclic ketones , 2004 .
[17] L. Toupet,et al. A difluorosulfide as a Freon-free source of phosphonodifluoromethyl carbanion. , 2003, Organic & biomolecular chemistry.
[18] J. Cooper,et al. The structure of endothiapepsin complexed with the gem-diol inhibitor PD-135,040 at 1.37 A. , 2003, Acta crystallographica. Section D, Biological crystallography.
[19] Jun Liu,et al. Four plasmepsins are active in the Plasmodium falciparum food vacuole, including a protease with an active-site histidine , 2002, Proceedings of the National Academy of Sciences of the United States of America.
[20] T. Steiner. The hydrogen bond in the solid state. , 2002, Angewandte Chemie.
[21] L. Reeves,et al. Difluoroketones as inhibitors of matrix metalloprotease-13. , 2000, Bioorganic & medicinal chemistry letters.
[22] J. Guthrie. Hydration of Carbonyl Compounds, an Analysis in Terms of Multidimensional Marcus Theory , 2000 .
[23] Maria Cristina Burla,et al. SIR97: a new tool for crystal structure determination and refinement , 1999 .
[24] T. Blundell,et al. The three-dimensional structure at 2.4 A resolution of glycosylated proteinase A from the lysosome-like vacuole of Saccharomyces cerevisiae. , 1997, Journal of molecular biology.
[25] R. Chambers,et al. Elemental fluorine. Part 6. Fluorination of cyclic 1,3-diketones and related compounds , 1996 .
[26] R E Cachau,et al. Inhibition and catalytic mechanism of HIV-1 aspartic protease. , 1996, Journal of molecular biology.
[27] Paul R. Gerber,et al. MAB, a generally applicable molecular force field for structure modelling in medicinal chemistry , 1995, J. Comput. Aided Mol. Des..
[28] P. Bernstein,et al. Examination of peptidic α′,β-diamino-α,α-difluoroketones as inhibitors of human leukocyte elastase , 1994 .
[29] Stephen P. Miller,et al. Synthesis and inhibitory activity of difluoroketone substrate analogs of N-myristoyltransferase. , 1994 .
[30] S. Vasavanonda,et al. Pseudo‐symmetrical difluoroketones , 1993, FEBS letters.
[31] Michael H. Gelb,et al. Crystallographic analysis of transition state mimics bound to penicillopepsin: difluorostatine- and difluorostatone-containing peptides. , 1994 .
[32] C. Tarnus,et al. MDL 74147, a novel selective and soluble inhibitor of human renin. Synthesis, structure-activity relationship, species and protease selectivities. , 1992 .
[33] T L Blundell,et al. Direct observation by X‐ray analysis of the tetrahedral “intermediate” of aspartic proteinases , 1992, Protein science : a publication of the Protein Society.
[34] A. Doherty,et al. Design and synthesis of potent, selective, and orally active fluorine-containing renin inhibitors. , 1992, Journal of medicinal chemistry.
[35] S. Ghosh,et al. A chemoenzymatic approach to (R)-tetrahydro-5-oxo-2-(2-hydroxyethyl)furan, a useful chiral synthon: Application to the synthesis of (S)-4-hexanolide, pheromone antipode of . , 1991 .
[36] C. Debouck,et al. Inhibition of human immunodeficiency virus 1 protease in vitro: rational design of substrate analogue inhibitors. , 1989, Proceedings of the National Academy of Sciences of the United States of America.
[37] G. A. Jeffrey. Water structure in organic hydrates , 1969 .
[38] R. Bell,et al. The hydration of acetaldehyde in aqueous solution , 1952 .