I.J.P. de Esch

prof. dr.

19972019
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Research Output 1997 2019

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Article
2009

Transforming fragments into candidates: small becomes big in medicinal chemistry

de Kloe, G. E., Bailey, D. S., Leurs, R. & de Esch, I. J. P., 2009, In : Drug Discovery Today. 14, 13-14, p. 630-46

Research output: Contribution to JournalArticleAcademicpeer-review

Use of acetylcholine binding protein in the search for novel alpha7 nicotinic receptor ligands. In silico docking, pharmacological screening, and X-ray analysis

Ulens, C., Akdemir, A., Jongejan, A., van Elk, R., Bertrand, S., Perrakis, A., Leurs, R., Smit, A. B., Sixma, T. K., Bertrand, D. & de Esch, I. J. P., 2009, In : Journal of Medicinal Chemistry. 52, p. 2372-2383 11 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Nicotinic Receptors
Computer Simulation
Acetylcholine
Carrier Proteins
X-Rays
2008

[From gene to drug: recent developments in medicinal chemistry]

de Esch, I. J. P. & Leurs, R., 2008, In : Nederlands Tijdschrift voor Geneeskunde. 152, 51-52, p. 2795-800

Research output: Contribution to JournalArticleAcademicpeer-review

4-benzyl-1H-imidazoles with oxazoline termini as histamine H3 receptor agonists

Wijtmans, M., Celanire, S., Snip, E., Gillard, M. R., Gelens, E., Collart, P. P., Venhuis, B. J., Christophe, B., Hulscher, ST., van der Goot, H., Lebon, F., Timmerman, H., Bakker, R. A., Leurs, R., Lallemand, B. I., Talaga, P. & de Esch, I. J. P., 2008, In : Journal of Medicinal Chemistry. 51, 10, p. 2944-53

Research output: Contribution to JournalArticleAcademicpeer-review

Histamine Agonists
Imidazoles
Therapeutic Human Experimentation
Histamine
Aldehydes
Derivatives
Biomarkers
Malondialdehyde
Ammonium Compounds

Fragment based design of new H4 receptor-ligands with anti-inflammatory properties in vivo

Smits, R. A., Lim, H. D., Hanzer, A., Zuiderveld, O. P., Guaita, E., Adami, M., Coruzzi, G., Leurs, R. & de Esch, I. J. P., 2008, In : Journal of Medicinal Chemistry. 51, 8, p. 2457-67

Research output: Contribution to JournalArticleAcademicpeer-review

Histamine
Anti-Inflammatory Agents
Ligands

Noncompetitive antagonism and inverse agonism as mechanism of action of nonpeptidergic antagonists at primate and rodent CXCR3 chemokine receptors

Verzijl, D., Storelli, S., Scholten, D. J., Bosch, L., Reinhart, T. A., Streblow, D. N., Tensen, C. P., Fitzsimons, C. P., Zaman, G. J., Pease, J. E., de Esch, I. J. P., Smit, M. J. & Leurs, R., 2008, In : The Journal of Pharmacology and Experimental Therapeutics. 325, 2, p. 544-55

Research output: Contribution to JournalArticleAcademicpeer-review

CXCR3 Receptors
Chemokine Receptors
Primates
Rodentia
Anilides

Structure-activity relationships for the inhibition of recombinant human cytochromes P450 by curcumin analogues

Appiah-Opong, R., de Esch, I. J. P., Commandeur, J. N. M., Andarini, M. & Vermeulen, N. P. E., 2008, In : European Journal of Medicinal Chemistry. 43, 8, p. 1621-31

Research output: Contribution to JournalArticleAcademicpeer-review

Towards small-molecule CXCR3 ligands with clinical potential

Wijtmans, M., Verzijl, D., Leurs, R., de Esch, I. J. P. & Smit, M. J., 2008, In : ChemMedChem. 3, 6, p. 861-72

Research output: Contribution to JournalArticleAcademicpeer-review

CXCR3 Receptors
Ligands
Animal Disease Models
Phase II Clinical Trials
Molecules

Van gen tot medicijn: moderne ontwikkelingen in de farmacochemie

de Esch, I. J. P. & Leurs, R., 20 Dec 2008, In : Nederlands Tijdschrift voor Geneeskunde. 152, 51-52, p. 2795-800 6 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Pharmaceutical Chemistry
Crystallography
Biological Science Disciplines
Human Genome
Structure-Activity Relationship
2007
Histamine Receptors
Carrageenan
Histamine
Anti-Inflammatory Agents
Inflammation

Antinociceptive activity of furan-containing congeners of improgan and ranitidine

Hough, L. H., Menge, W. M. P. B., van de Stolpe, A., Nalwalk, J. B., Leurs, R. & de Esch, I. J. P., 2007, In : Bioorganic and Medicinal Chemistry Letters. 17, 20, p. 5715-9

Research output: Contribution to JournalArticleAcademicpeer-review

CC12, a high-affinity ligand for [3H]cimetidine binding, is an improgan antagonist

Hough, L. B., Nalwalk, J. W., Phillips, J. G., Kern, B., Shan, Z., Wentland, M. P., de Esch, I. J. P., Janssen, E., Barr, T. & Stadel, R., Apr 2007, In : Neuropharmacology. 52, 5, p. 1244-55 12 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Cimetidine
Ligands
Analgesia
Analgesics
Pharmacology

CC12, a high-affinity ligand for [3H]cimetidine binding, is an improgan antagonist

Hough, L. H., Nalwalk, J. B., Phillips, J. R., Kern, B., Shan, Z., Wentland, M., de Esch, I. J. P., Janssen, EA., Barr, T. & Stadel, R., 2007, In : Neuropharmacology. 52, 5, p. 1244-55

Research output: Contribution to JournalArticleAcademicpeer-review

Cimetidine
Ligands
Analgesics
Pharmacology
SKF 92374

Chemical insights in the concept of hybrid drugs: the antitumor effect of nitric oxide-donating aspirin involves a quinone methide but not nitric oxide nor aspirin

Hulsman, N., Medema, J. P., van den Bos, C. G., Jongejan, A., Leurs, R., Smit, M. J., de Esch, I. J. P., Richel, D. & Wijtmans, M., 2007, In : Journal of Medicinal Chemistry. 50, 10, p. 2424-31

Research output: Contribution to JournalArticleAcademicpeer-review

Antineoplastic Agents
Aspirin
Nitric Oxide
Research
Pharmaceutical Preparations

Histamine H3 receptor ligands break ground in a remarkable plethora of therapeutic areas

Wijtmans, M., Leurs, R. & de Esch, I. J. P., 2007, In : Expert Opinion on Investigational Drugs. 16, 7, p. 967-85

Research output: Contribution to JournalArticleAcademicpeer-review

Histamine H3 Receptors
Histamine
Ligands
Histamine Receptors
Neurotransmitter Agents

QUASI: a novel method for simultaneous superposition of multiple flexible ligands and virtual screening using partial similarity

Todorov, N. P., Alberts, I. L., de Esch, I. J. P. & Dean, P. M., 2007, In : Journal of Chemical Information and Modeling. 47, 3, p. 1007-20

Research output: Contribution to JournalArticleAcademicpeer-review

Screening
Ligands
flexibility
Dynamic models
utilization

Sex- and histamine-dependent long-term cognitive effects of methamphetamine exposure

Acevedo, S. F., de Esch, I. J. P. & Raber, J., 2007, In : Neuropsychopharmacology. 32, 3, p. 665-72

Research output: Contribution to JournalArticleAcademicpeer-review

Methamphetamine
Histamine
Genetic Models
Hippocampus
Newborn Infant
2006

Antinociceptive activity of chemical congeners of improgan: optimization of side chain length leads to the discovery of a new, potent, non-opioid analgesic

Hough, L. H., de Esch, I. J. P., Janssen, E., Phillips, J. R., Svokos, K., Kern, B., Trachler, J., Abood, M. E., Leurs, R. & Nalwalk, J. B., Sep 2006, In : Neuropharmacology. 51, 3, p. 447-456 10 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Analgesics
Cannabinoids
Cannabinoid Receptor CB1
rimonabant
SKF 92374

Characterization of the histamine H4 receptor binding site. Part 1. Synthesis and pharmacological evaluation of dibenzodiazepine derivatives

Smits, R. A., Lim, H. D., Stegink, B., Bakker, R. A., de Esch, I. J. P. & Leurs, R., 2006, In : Journal of Medicinal Chemistry. 49, 15, p. 4512-6

Research output: Contribution to JournalArticleAcademicpeer-review

Histamine Receptors
Histamine
Binding Sites
Pharmacology

Constitutive activity of H3 autoreceptors modulates histamine synthesis in rat brain through the cAMP/PKA pathway

Moreno-Delgado, D., Torrent, A., Gomez-Ramirez, J., de Esch, I. J. P., Blanco, I. & Ortiz, J., 2006, In : Neuropharmacology. 51, 3, p. 517-23

Research output: Contribution to JournalArticleAcademicpeer-review

Histamine Agonists
Autoreceptors
Histamine
Brain

Discovery of S-(2-guanidylethyl)-isothiourea (VUF 8430) as a potent nonimidazole histamine H4 receptor agonist

Lim, H. D., Smits, R. A., Bakker, R. A., van Dam, C. M. E., de Esch, I. J. P. & Leurs, R., 2006, In : Journal of Medicinal Chemistry. 49, 23, p. 6650-1

Research output: Contribution to JournalArticleAcademicpeer-review

Histamine Agonists
Histamine Receptors
Databases
S-(2-guanidylethyl)isothiourea

Synthesis and pharmacological characterization of novel inverse agonists acting on the viral-encoded chemokine receptor US28

Hulshof, J. W., Vischer, H. F., Verheij, M. H. P., Fratantoni, S. A., Smit, M. J., de Esch, I. J. P. & Leurs, R., 2006, In : Bioorganic and Medicinal Chemistry. 14, 21, p. 7213-30

Research output: Contribution to JournalArticleAcademicpeer-review

2005

Keynote review: histamine H3 receptor antagonists reach out for the clinic

Celanire, S., Wijtmans, M., Talaga, P., Leurs, R. & de Esch, I. J. P., 2005, In : Drug Discovery Today. 10, 23-24, p. 1613-27

Research output: Contribution to JournalArticleAcademicpeer-review

Histamine H3 Antagonists
Histamine Antagonists

N-substituted piperidinyl alkyl imidazoles: discovery of methimepip as a potent and selective histamine H3 receptor agonist

Kitbunnadaj, R., Hashimoto, T., Poli, E., Zuiderveld, O. P., Menozzi, A., Hidaka, R., de Esch, I. J. P., Bakker, R. A., Menge, W. M. P. B., Yamatodani, A., Coruzzi, G., Timmerman, H. & Leurs, R., 2005, In : Journal of Medicinal Chemistry. 48, 6, p. 2100-7

Research output: Contribution to JournalArticleAcademicpeer-review

Histamine Agonists
Imidazoles
Histamine
methimepip

Synthesis and structure-activity relationship of the first nonpeptidergic inverse agonists for the human cytomegalovirus encoded chemokine receptor US28

Hulshof, J. W., Casarosa, P., Menge, W. M. P. B., Kuusisto, L. M. S., van der Goot, H., Smit, M. J., de Esch, I. J. P. & Leurs, R., 6 Oct 2005, In : Journal of Medicinal Chemistry. 48, 20, p. 6461-71 11 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Chemokine Receptors
Structure-Activity Relationship
Cytomegalovirus
Ligands
Virus Diseases

The histamine H3 receptor: from gene cloning to H3 receptor drugs

Leurs, R., Bakker, R. A., Timmerman, H. & de Esch, I. J. P., 2005, In : Nature Reviews Drug Discovery. 4, 2, p. 107-20

Research output: Contribution to JournalArticleAcademicpeer-review

Histamine H3 Receptors
Histamine
Organism Cloning
Pharmaceutical Preparations
Genes

The histamine H4 receptor as a new therapeutic target for inflammation

de Esch, I. J. P., Thurmond, R. L., Jongejan, A. & Leurs, R., 2005, In : Trends in Pharmacological Sciences. 26, 9, p. 462-9

Research output: Contribution to JournalArticleAcademicpeer-review

Histamine Receptors
Data Mining
Human Genome
Mast Cells
Histamine

The role and application of in silico docking in chemical genomics research

Jongejan, A., de Graaf, C., Vermeulen, N. P. E., Leurs, R. & de Esch, I. J. P., 2005, In : Methods in Molecular Biology. 310, p. 63-91

Research output: Contribution to JournalArticleAcademicpeer-review

The role and application of in silico docking in chemical genomics research

Jongejan, A., de Graaf, C., Vermeulen, N. P. E., Leurs, R. & de Esch, I. J. P., 2005, In : Methods in Molecular Biology. 310, p. 63-91

Research output: Contribution to JournalArticleAcademicpeer-review

2001

SLATE: a method for the superposition of flexible ligands

Mills, J. E., de Esch, I. J., Perkins, T. D. & Dean, P. M., Jan 2001, In : Journal of Computer-aided Molecular Design. 15, 1, p. 81-96 16 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Ligands
ligands
Hydrogen bonds
Receptor, Serotonin, 5-HT1D
Histamine H3 Receptors

SLATE: a method for the superposition of flexible ligands

Mills, J. E., de Esch, I. J. P., Perkins, T. D. & Dean, P. M., 2001, In : Journal of Computer-aided Molecular Design. 15, 1, p. 81-96

Research output: Contribution to JournalArticleAcademicpeer-review

1999

Synthesis and histamine H3 receptor activity of 4-(n-alkyl)-1H-imidazoles and 4-(omega-phenylalkyl)-1H-imidazoles

De Esch, I. J., Gaffar, A., Menge, W. M. & Timmerman, H., Dec 1999, In : Bioorganic and Medicinal Chemistry. 7, 12, p. 3003-9 7 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Histamine H3 Receptors
Imidazoles
Chain length
imidazole