Detailed structure–activity relationship of indolecarboxamides as H 4 receptor ligands

…, J Dobler, M Mayer, S Lips, H Arnhof, D Scharn…

文献索引：Engelhardt, Harald; De Esch, Iwan J.P.; Kuhn, Daniel; Smits, Rogier A.; Zuiderveld, Obbe P.; Dobler, Julia; Mayer, Moriz; Lips, Sebastian; Arnhof, Heribert; Scharn, Dirk; Haaksma, Eric E.J.; Leurs, Rob European Journal of Medicinal Chemistry, 2012 , vol. 54, p. 660 - 668

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被引用次数: 14

摘要

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 H4R antagonists was synthesized and a comparison of predicted and measured values demonstrates the robustness of the model (47–55). In addition to ...