Results 171 to 180 of about 3,102 (198)

Design of histamine H3-receptor agonists and antagonists

European Journal of Drug Metabolism and Pharmacokinetics, 1994
The development of highly potent and selective ligands for the characterization of histamine H3-receptors is reviewed. In the field of agonists stereoselectively methylated derivatives of the natural ligand are found to have the desired pharmacodynamic properties. Pharmacokinetic properties could be improved by forming bioreversible azomethine prodrugs
W, Schunack, H, Stark
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Synthesis of Potent Non-imidazole Histamine H3-Receptor Antagonists

Archiv der Pharmazie, 1998
Histamine has been converted into a non-imidazole H3-receptor histamine antagonist by addition of a 4-phenylbutyl group at the N alpha-position followed by removal of the imidazole ring. The resulting compound, N-ethyl-N-(4-phenylbutyl)amine, remarkably has a Ki = 1.3 microM as an H3 antagonist.
C R, Ganellin, F, Leurquin, A, Piripitsi, J M, Arrang, M, Garbarg, X, Ligneau, W, Schunack, J C, Schwartz   +7 more
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Dual serotonin transporter inhibitor/histamine H3 antagonists: Development of rigidified H3 pharmacophores

Bioorganic & Medicinal Chemistry Letters, 2007
A series of tetrahydroisoquinolines acting as dual serotonin transporter inhibitor/histamine H(3) antagonists is described. The introduction of polar aromatic spacers as part of the histamine H(3) pharmacophore was explored. A convergent synthesis of the final products allowing late stage introduction of the aromatic side chain was developed.
John M, Keith, Ann J, Barbier, Sandy J, Wilson, Kirstin, Miller, Jamin D, Boggs, Ian C, Fraser, Curt, Mazur, Timothy W, Lovenberg, Nicholas I, Carruthers   +8 more
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Design of Potent Non-Thiourea H3-Receptor Histamine Antagonists

Journal of Medicinal Chemistry, 1995
Starting from thioperamide, the first potent and selective H3-receptor histamine antagonist, analogues have been synthesized and tested in vitro on rat cerebral cortex to explore structure-activity relationships. The aim has been to design potent compounds which do not possess the thiourea group of thioperamide and which may have improved brain ...
C R, Ganellin, S K, Hosseini, Y S, Khalaf, W, Tertiuk, J M, Arrang, M, Garbarg, X, Ligneau, J C, Schwartz   +7 more
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Synthesis and SAR of novel histamine H3 receptor antagonists

Bioorganic & Medicinal Chemistry Letters, 2006
The synthesis and biological evaluation of novel tetrahydroisoquinoline, tetrahydroquinoline, and tetrahydroazepine antagonists of the human and rat H(3) receptors are described. The substitution around these rings as well as the nature of the substituent on nitrogen is explored.
Cynthia D, Jesudason, Lisa S, Beavers, Jeffrey W, Cramer, Joelle, Dill, Don R, Finley, Craig W, Lindsley, F Craig, Stevens, Robert A, Gadski, Samuel W, Oldham, R Todd, Pickard, Christopher S, Siedem, Dana K, Sindelar, Ajay, Singh, Brian M, Watson, Philip A, Hipskind   +14 more
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Acylated and alkylated histamine derivatives as new histamine H3-receptor antagonists

European Journal of Medicinal Chemistry, 1994
New histamine H3-receptor antagonists were prepared and investigated for their ability to increase synthesis and release of histamine mediated by inhibition of presynaptically located H3-receptors. Acyl derivatives of histamine methylated at different positions show poor activity at H3-receptors, whereas Nα-alkyl and particularly Nα-acyl derivatives of
H Stark, R Lipp, JM Arrang, M Garbarg, JC Schwartz, W Schunack   +5 more
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Non-imidazole histamine H3 ligands. Part III. New 4-n-propylpiperazines as non-imidazole histamine H3-antagonists

European Journal of Medicinal Chemistry, 2005
In search for a new lead of non-imidazole histamine H3-receptor antagonists, a series of 1[(2-thiazolopyridine)-4-n-propyl]piperazines, the analogous 1-[(2-oxazolopyridine)-4-npropyl]piperazines, 1-[(2-benzothiazole)-4-n-propyl]piperazine and 1-[(2-benzooxazole)4-n-propyl]piperazine were prepared and in vitro tested as H3-receptor antagonists (the ...
Krzysztof, Walczyński, Obbe P, Zuiderveld, Henk, Timmerman   +2 more
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Discovery of substituted benzyl tetrazoles as histamine H3 receptor antagonists

Bioorganic & Medicinal Chemistry Letters, 2010
A series of potent and subtype selective H3 receptor antagonists containing a novel tetrazole core and diamine motif is reported. A one-pot multi-component Ugi reaction was utilised to rapidly develop the structure-activity relationships (SAR) of these compounds. Optimisation for liver microsome stability (t(1/2)>60 min), minimal CYP inhibition (IC(50)>
Adam J, Davenport, Christopher C, Stimson, Massimo, Corsi, Darshan, Vaidya, Edward, Glenn, Timothy D, Jones, Sarah, Bailey, Mark J, Gemkow, Ulrike, Fritz, David J, Hallett   +9 more
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Subclasses of histamine H3 antagonist binding sites in rat brain

Brain Research, 1994
Histamine H3 antagonists have been reported to discriminate subclasses of histamine H3 agonist binding in rat cortical membranes. This phenomenon was investigated by autoradiography of cryostat sections of rat forebrain labelled with [3H]N alpha-methylhistamine ([3H]NAMH, 4 nM). Displacement curves with thioperamide detected a single site in cortex and
Cumming, P, Gjedde, A
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Discovery of novel steroidal histamine H3 receptor antagonists/inverse agonists

Bioorganic & Medicinal Chemistry Letters, 2017
Emerging from an HTS campaign, novel steroid-based histamine H3 receptor antagonists were identified and characterized. Structural moieties of the hit compounds were combined to improve binding affinities which resulted in compound 4 as lead molecule.
Istvan, Ledneczki, Pál, Tapolcsányi, Eszter, Gábor, János, Éles, István, Greiner, Éva, Schmidt, Zsolt, Némethy, Rita Soukupné, Kedves, Ottilia, Balázs, Viktor, Román, György, Lévay, Sándor, Mahó   +11 more
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