129378-52-5Relevant articles and documents
From histamine to imidazolylalkyl-sulfonamides: The design of a novel series of histamine H3-receptor antagonists
Tozer, Matthew J.,Harper, Elaine A.,Kalindjian, S. Barret,Pether, Michael J.,Shankley, Nigel P.,Watt, Gillian F.
, p. 1825 - 1830 (1999)
Histamine was converted to a selective histamine H3-receptor antagonist by capping the primary amine with 2-naphthalenesulfonyl chloride. Higher receptor affinity and lower variability in the data from the various bioassays were achieved with the 2-naphthalensulfonamides of histamine homologues.
Fluorinated imidazoles as 19F probes for biomimetic studies of heme a3 - Cub site in cytochrome c oxidase
Collman, James P.,Boulatov, Roman,Sunderland, Christopher J.,Zhong, Min
, p. 189 - 197 (2000)
A series of 4,5-imidazole carboxylic acids bearing fluorinated substituents is synthesized from simple commercially available fluorinated substrates utilizing several different approaches to modify the imidazole core. These imidazole derivatives are speci
Homologs of Histamine as Histamine H3 Receptor Antagonists: A New Potent and Selective H3 Antagonist, 4(5)-(5-Aminopentyl)-1H-imidazole
Vollinga, Roeland C.,Menge, Wiro M. P. B.,Leurs, Rob,Timmerman, Hendrik
, p. 266 - 271 (1995)
The influence of alkyl chain length variation on the histamine H3 receptor activity of histamine homologs 1 was investigated.A series of 4(5)-(ω-aminoalkyl)-1H-imidazoles 1 was prepared with an alkyl chain length varying from one methylene group to 10 methylene groups.Besides the H3 activity, the affinities of these compounds for the H1 and H2 receptors were determined.The ethylene chain of histamine is optimal for agonistic activity on all three histamine receptor subtypes.For the H3 receptor, elongation of the alkyl chain from three methylene groups on leads to compounds with antagonistic properties. 4(5)-(5-Aminopentyl)-1H-imidazole (impentamine, 1e) is the most potent and selective H3 antagonist from this series of 4(5)-(ω-aminoalkyl)-1H-imidazoles 1, with a pA2 value of 8.4 (on guinea pig jejunum).A specific antagonistic binding site for this compound is proposed.
Full functionalization of the imidazole scaffold by selective metalation and sulfoxide/magnesium exchange
Samann, Christoph,Coya, Estibaliz,Knochel, Paul
supporting information, p. 1430 - 1434 (2014/03/21)
A simple, flexible, and straightforward method for the functionalization of all the positions of the imidazole heterocycle through regioselective arylations, allylations, acylations, and additions to aldehydes is disclosed. Starting from the readily avail
Novel structural analogs of glyphosate based on azoles. 1. Synthesis of 1H-imidazoles containing carboxyl and phosphoryl groups in the ring
Pavlenko,Oos,Yagupolskii,Van Almsick,Willms
scheme or table, p. 36 - 44 (2012/01/03)
A general method has been developed for the synthesis of 1H-imidazoles containing a phosphoryl group in positions 2 or 4(5) based on lithium intermediates. The possibility of further functionalization of the ring using electrophiles has also been demonstrated.
HETEROCYCLODIAZEPINE CANNABINOID RECEPTOR MODULATORS FOR TREATMENT OF DISEASE
-
Page/Page column 28, (2009/04/24)
The present invention relates to compounds and methods useful as modulators of CB2 for the treatment or prevention of disease states including, but not limited to pain, autoimmune disease, malabsorption syndrome, pulmonary disease, osteoporosis, muscle spasm in cancer, neuromuscular disorder, and atherosclerosis progression.
4-(2-Methyl-5,6,7,8-tetrahydro-quinolin-7-ylmethyl)-1,3-dihydro-imidazole-2-thione as specific alpha2B agonist and methods of using the same
-
, (2008/06/13)
The compound of the formula wherein the * indicates an asymmetric carbon, is specific to alpha2B adrenergic receptors in preference over alpha2A and alpha2C adrenergic receptors, and as such has no or only minimal cardivascular and/or sedatory activity. The compound is useful as medicament in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors.
Imidiazoles having reduced side effects
-
, (2008/06/13)
Methods and compounds for the treatment of conditions including pain, particularly chronic pain, glaucoma or elevated intraocular pressure with reduced cardiovascular or sedative side effects. Also included are methods of making and using such compounds.
4-(substituted cycloalkylmethyl) imidazole-2-thiones, 4-(substituted cycloalkenylmethyl) imidazole-2-thiones, 4-(substituted cycloalkylmethyl) imidazol-2-ones and 4-(substituted cycloalkenylmethyl) imidazol-2-ones and related compounds
-
, (2008/06/13)
Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardivascular and/or sedatory activity. These compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors. Compounds of Formula 1 where X is O also have the advantageous property that they have no or only minimal cardivascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardivascular and/or sedatory activity.
Compounds and method of treatment having agonist-like activity selective at alpha 2B or 2B/2C adrenergic receptors
-
, (2008/06/13)
Methods and compounds for the treatment of conditions including pain, particularly chronic pain, glaucoma or elevated intraocular pressure with reduced cardiovascular or sedative side effects. Also included are methods of making and using such compounds.
