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The Magic of Crystal Structure-Based Inhibitor Optimization: Development of a Butyrylcholinesterase Inhibitor with Picomolar Affinity and in Vivo Activity

Journal of medicinal chemistry, 2018-01, Vol.61 (1), p.119-139

2018

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Design, Synthesis, and Evaluation of New Thiadiazole-Based Direct Inhibitors of Enoyl Acyl Carrier Protein Reductase (InhA) for the Treatment of Tuberculosis

Journal of medicinal chemistry, 2015-01, Vol.58 (2), p.613-624

2015

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Development of an in-vivo active reversible butyrylcholinesterase inhibitor

Scientific reports, 2016-12, Vol.6 (1), p.39495-39495, Article 39495

2016

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Crystallographic Study of Peptidoglycan Biosynthesis Enzyme MurD: Domain Movement Revisited

PloS one, 2016-03, Vol.11 (3), p.e0152075-e0152075

2016

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Discovery of Novel 5-Benzylidenerhodanine and 5-Benzylidenethiazolidine-2,4-dione Inhibitors of MurD Ligase

Journal of medicinal chemistry, 2010-09, Vol.53 (18), p.6584-6594

2010

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Comparison of the NMR and the Acid Value Determination Methods for Quality Control of Input Polysorbates

Acta chimica Slovenica, 2019-12, Vol.66 (4), p.934-943

2019

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Protein Formulations Containing Polysorbates: Are Metal Chelators Needed at All?

Antioxidants, 2020-05, Vol.9 (5), p.441

2020

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Structure-Based Design of a New Series of d-Glutamic Acid Based Inhibitors of Bacterial UDP-N-acetylmuramoyl-l-alanine:d-glutamate Ligase (MurD)

Journal of medicinal chemistry, 2011-07, Vol.54 (13), p.4600-4610

2011

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Dual Inhibitor of MurD and MurE Ligases from Escherichia coli and Staphylococcus aureus

ACS medicinal chemistry letters, 2012-08, Vol.3 (8), p.626-630

2012

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MurD enzymes: some recent developments

Biomolecular concepts, 2013-12, Vol.4 (6), p.539-556

2013

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Rational design to biologics development: The polysorbates point of view

International journal of pharmaceutics, 2020-05, Vol.581, p.119285-119285, Article 119285

2020

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New direct inhibitors of InhA with antimycobacterial activity based on a tetrahydropyran scaffold

European journal of medicinal chemistry, 2016-04, Vol.112, p.252-257

2016

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Degradation of polysorbates 20 and 80 catalysed by histidine chloride buffer

European journal of pharmaceutics and biopharmaceutics, 2020-09, Vol.154, p.236-245

2020

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Inhibitors of the peptidoglycan biosynthesis enzymes MurA-F

Bioorganic chemistry, 2014-08, Vol.55, p.2-15

2014

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Structure-based development of nitroxoline derivatives as potential multifunctional anti-Alzheimer agents

Bioorganic & medicinal chemistry, 2015-08, Vol.23 (15), p.4442-4452

2015

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New 5-benzylidenethiazolidin-4-one inhibitors of bacterial MurD ligase: Design, synthesis, crystal structures, and biological evaluation

European journal of medicinal chemistry, 2011-11, Vol.46 (11), p.5512-5523

2011

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Simple and effective preparation of amino sulfonylureas from amino acids: application to the synthesis of amino sulfonylurea-containing peptidomimetics

Tetrahedron letters, 2008-06, Vol.49 (24), p.3943-3945

2008

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Second-generation sulfonamide inhibitors of d-glutamic acid-adding enzyme: Activity optimisation with conformationally rigid analogues of d-glutamic acid

European journal of medicinal chemistry, 2011-07, Vol.46 (7), p.2880-2894

2011

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Synthesis and Biological Evaluation of N-Acylhydrazones as Inhibitors of MurC and MurD Ligases

ChemMedChem, 2008-09, Vol.3 (9), p.1362-1370

2008

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False positives in the early stages of drug discovery

Current medicinal chemistry, 2010-12, Vol.17 (34), p.4231

2010

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MurD enzymes: some recent developments

Biomolecular concepts, 2013-12, Vol.4 (6), p.539

2013

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ChemInform Abstract: Simple and Effective Preparation of Amino Sulfonylureas from Amino Acids: Application to the Synthesis of Amino Sulfonylurea-Containing Peptidomimetics

ChemInform, 2008-09, Vol.39 (39), p.no-no

2008

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Practical Marine Spatial Management of Ecologically or Biologically Significant Marine Areas: Emerging Lessons From Evidence-Based Planning and Implementation in a Developing-World Context

Frontiers in Marine Science, 2022-03, Vol.9

2022

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The Magic of Crystal Structure-Based Inhibitor Optimization: Development of a Butyrylcholinesterase Inhibitor with Picomolar Affinity and in Vivo Activity

Design, Synthesis, and Evaluation of New Thiadiazole-Based Direct Inhibitors of Enoyl Acyl Carrier Protein Reductase (InhA) for the Treatment of Tuberculosis

Development of an in-vivo active reversible butyrylcholinesterase inhibitor

Crystallographic Study of Peptidoglycan Biosynthesis Enzyme MurD: Domain Movement Revisited

Discovery of Novel 5-Benzylidenerhodanine and 5-Benzylidenethiazolidine-2,4-dione Inhibitors of MurD Ligase

Comparison of the NMR and the Acid Value Determination Methods for Quality Control of Input Polysorbates

Protein Formulations Containing Polysorbates: Are Metal Chelators Needed at All?

Structure-Based Design of a New Series of d-Glutamic Acid Based Inhibitors of Bacterial UDP-N-acetylmuramoyl-l-alanine:d-glutamate Ligase (MurD)

Dual Inhibitor of MurD and MurE Ligases from Escherichia coli and Staphylococcus aureus

MurD enzymes: some recent developments

Rational design to biologics development: The polysorbates point of view

New direct inhibitors of InhA with antimycobacterial activity based on a tetrahydropyran scaffold

Degradation of polysorbates 20 and 80 catalysed by histidine chloride buffer

Inhibitors of the peptidoglycan biosynthesis enzymes MurA-F

Structure-based development of nitroxoline derivatives as potential multifunctional anti-Alzheimer agents

New 5-benzylidenethiazolidin-4-one inhibitors of bacterial MurD ligase: Design, synthesis, crystal structures, and biological evaluation

Simple and effective preparation of amino sulfonylureas from amino acids: application to the synthesis of amino sulfonylurea-containing peptidomimetics

Second-generation sulfonamide inhibitors of d-glutamic acid-adding enzyme: Activity optimisation with conformationally rigid analogues of d-glutamic acid

Synthesis and Biological Evaluation of N-Acylhydrazones as Inhibitors of MurC and MurD Ligases

False positives in the early stages of drug discovery

MurD enzymes: some recent developments

ChemInform Abstract: Simple and Effective Preparation of Amino Sulfonylureas from Amino Acids: Application to the Synthesis of Amino Sulfonylurea-Containing Peptidomimetics

Practical Marine Spatial Management of Ecologically or Biologically Significant Marine Areas: Emerging Lessons From Evidence-Based Planning and Implementation in a Developing-World Context

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