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pubmed-article:20138762pubmed:abstractTextAntagonists of the human histamine H(3) receptor (hH(3)R) often contain a second basic moiety, which is well known to boost affinity on this histamine receptor subtype. Here, we prepared compounds with acidic moieties of different pK(a) values to figure out that the hH(3)R tolerates these functionalities when added to a common pharmacophore blueprint. Depending on the acidic, electronic and steric features the designed ligands showed hH(3)R affinities in the nanomolar concentration range. Additionally, selected ligands were tested but failed as dual acting hH(3)R/hPPAR (human peroxisome proliferator-activated receptor) ligands.lld:pubmed
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pubmed-article:20138762pubmed:copyrightInfoCopyright 2010 Elsevier Ltd. All rights reserved.lld:pubmed
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pubmed-article:20138762pubmed:year2010lld:pubmed
pubmed-article:20138762pubmed:articleTitleAcidic elements in histamine H(3) receptor antagonists.lld:pubmed
pubmed-article:20138762pubmed:affiliationJohann Wolfgang Goethe University, Institute of Pharmaceutical Chemistry, ZAFES/LiFF/CMP, Max-von-Laue-Str. 9, 60438 Frankfurt/Main, Germany.lld:pubmed
pubmed-article:20138762pubmed:publicationTypeJournal Articlelld:pubmed
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