Results 191 to 200 of about 6,313 (204)
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Acidic elements in histamine H3 receptor antagonists
Bioorganic & Medicinal Chemistry Letters, 2010Antagonists 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 ...
Kerstin, Sander +7 more
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Keynote review: Histamine H3 receptor antagonists reach out for the clinic
Drug Discovery Today, 2005Antagonists of the histamine H(1) and H(2) receptors have been successful as blockbuster drugs for treating allergic conditions and gastric ulcers, respectively. As such, histamine receptors have made a significant contribution to establishing G-Protein-coupled receptors as the favored drug targets of the industry.
Celanire, S. +4 more
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Journal of Molecular Graphics and Modelling, 2008
Histamine H3 receptors are presynaptic autoreceptors found in both central and peripheral nervous systems of many species. The central effects of these receptors suggest a potential therapeutic role for their antagonists in treatment of several neurological disorders such as epilepsy, schizophrenia, Alzheimer's and Parkinson's diseases.
Siavoush, Dastmalchi +3 more
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Histamine H3 receptors are presynaptic autoreceptors found in both central and peripheral nervous systems of many species. The central effects of these receptors suggest a potential therapeutic role for their antagonists in treatment of several neurological disorders such as epilepsy, schizophrenia, Alzheimer's and Parkinson's diseases.
Siavoush, Dastmalchi +3 more
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Novel human histamine H3 receptor antagonists
Bioorganic & Medicinal Chemistry Letters, 2002AbstractFor Abstract see ChemInform Abstract in Full Text.
Chandra, Shah +8 more
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Medicinal chemistry of histamine H3 receptor antagonists
1998Publisher Summary This chapter discusses medicinal chemistry of histamine H3 receptor antagonists and provides an update on the recent progress being made. Several improved clinical candidates have emerged and are progressing towards human clinical trials.
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Two novel syntheses of the histamine H3 antagonist thioperamide
Tetrahedron, 1995Abstract The previously described route for the synthesis of the histamine H 3 antagonist thioperamide 3 has been improved considerably. Furthermore, two straightforward novel synthetic routes towards 3 are described herein. The last synthetic route (Scheme 3) is preferable as it is very suitable for the production of multigram quantities of ...
Jos H.M. Lange +4 more
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Theophylline derivatives as potential histamine H3-receptor antagonists.
Die Pharmazie, 1998Previous results of histamine H3-receptors investigations allowed to formulate a general structure of H3-receptor antagonists. According to this model a series of compounds were obtained. As heterocycles they contained a theophylline moiety connected with a polar group (amine, ester, amide, and thiourea function) via an alkyl chain linked by a spacer ...
K, Kieć-Kononowicz, M T, Cegła
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Amine-constrained pyridazinone histamine H3 receptor antagonists
Bioorganic & Medicinal Chemistry Letters, 2011Babu G. Sundar +7 more
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Histamine H3- Receptor Agonists and Antagonists
2008Holger Stark, Walter Schunack
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The Evolution of Histamine H3 Antagonists/Inverse Agonists
Current Topics in Medicinal Chemistry, 2011Evan P. Lebois +2 more
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