Detailed structure-activity relationship of indolecarboxamides as H(4) receptor ligands

H. Engelhardt, I.J.P. de Esch, D. Kuhn, R.A. Smits, O.P. Zuiderveld, J. Dobler, M. Mayer, S. Lips, H. Arnhof, D. Scharn, E.E. Haaksma, R. Leurs

Research output: Contribution to JournalArticleAcademicpeer-review

Abstract

A series of 76 derivatives of the indolecarboxamide 1 were synthesized, which allows a detailed SAR investigation of this well known scaffold. The data enable the definition of a predictive QSAR model which identifies several compounds with an activity comparable to 1. A selection of these new H
Original languageEnglish
Pages (from-to)660-668
JournalEuropean Journal of Medicinal Chemistry
Volume54
DOIs
Publication statusPublished - 2012

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Quantitative Structure-Activity Relationship
Structure-Activity Relationship
Scaffolds
Ligands
Derivatives

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Engelhardt, H. ; de Esch, I.J.P. ; Kuhn, D. ; Smits, R.A. ; Zuiderveld, O.P. ; Dobler, J. ; Mayer, M. ; Lips, S. ; Arnhof, H. ; Scharn, D. ; Haaksma, E.E. ; Leurs, R. / Detailed structure-activity relationship of indolecarboxamides as H(4) receptor ligands. In: European Journal of Medicinal Chemistry. 2012 ; Vol. 54. pp. 660-668.
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abstract = "A series of 76 derivatives of the indolecarboxamide 1 were synthesized, which allows a detailed SAR investigation of this well known scaffold. The data enable the definition of a predictive QSAR model which identifies several compounds with an activity comparable to 1. A selection of these new H",
author = "H. Engelhardt and {de Esch}, I.J.P. and D. Kuhn and R.A. Smits and O.P. Zuiderveld and J. Dobler and M. Mayer and S. Lips and H. Arnhof and D. Scharn and E.E. Haaksma and R. Leurs",
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Engelhardt, H, de Esch, IJP, Kuhn, D, Smits, RA, Zuiderveld, OP, Dobler, J, Mayer, M, Lips, S, Arnhof, H, Scharn, D, Haaksma, EE & Leurs, R 2012, 'Detailed structure-activity relationship of indolecarboxamides as H(4) receptor ligands' European Journal of Medicinal Chemistry, vol. 54, pp. 660-668. https://doi.org/10.1016/j.ejmech.2012.06.016

Detailed structure-activity relationship of indolecarboxamides as H(4) receptor ligands. / Engelhardt, H.; de Esch, I.J.P.; Kuhn, D.; Smits, R.A.; Zuiderveld, O.P.; Dobler, J.; Mayer, M.; Lips, S.; Arnhof, H.; Scharn, D.; Haaksma, E.E.; Leurs, R.

In: European Journal of Medicinal Chemistry, Vol. 54, 2012, p. 660-668.

Research output: Contribution to JournalArticleAcademicpeer-review

TY - JOUR

T1 - Detailed structure-activity relationship of indolecarboxamides as H(4) receptor ligands

AU - Engelhardt, H.

AU - de Esch, I.J.P.

AU - Kuhn, D.

AU - Smits, R.A.

AU - Zuiderveld, O.P.

AU - Dobler, J.

AU - Mayer, M.

AU - Lips, S.

AU - Arnhof, H.

AU - Scharn, D.

AU - Haaksma, E.E.

AU - Leurs, R.

PY - 2012

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N2 - A series of 76 derivatives of the indolecarboxamide 1 were synthesized, which allows a detailed SAR investigation of this well known scaffold. The data enable the definition of a predictive QSAR model which identifies several compounds with an activity comparable to 1. A selection of these new H

AB - A series of 76 derivatives of the indolecarboxamide 1 were synthesized, which allows a detailed SAR investigation of this well known scaffold. The data enable the definition of a predictive QSAR model which identifies several compounds with an activity comparable to 1. A selection of these new H

U2 - 10.1016/j.ejmech.2012.06.016

DO - 10.1016/j.ejmech.2012.06.016

M3 - Article

VL - 54

SP - 660

EP - 668

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

SN - 0223-5234

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