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Structure-activity relationships of non-imidazole H3 receptor ligands. Part 3: 5-Substituted 3-phenyl-1,2,4-oxadiazoles as potent antagonists

Further SAR studies on novel histamine H3 receptor antagonists are presented. Compound 14bb is a potent antagonist of both the rat cortical and human clone receptors, and is demonstrated to act functionally as an antagonist in an in vivo mouse dipsogenia model.

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Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

Discovery of Oxolane-2-carbonyl chloride

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The parmodulin NRD-21 is an allosteric inhibitor of PAR1 Gq signaling with improved anti-inflammatory activity and stability

Novel analogs of the allosteric, biased PAR1 ligand ML161 (parmodulin 2, PM2) were prepared in order to identify potential anti-thrombotic and anti-inflammatory compounds of the parmodulin class with improved properties. Investigations of structure-activity relationships of the western portion of the 1,3-diaminobenzene scaffold were performed using an intracellular calcium mobilization assay with endothelial cells, and several heterocycles were identified that inhibited PAR1 at sub-micromolar concentrations. The oxazole NRD-21 was profiled in additional detail, and it was confirmed to act as a selective, reversible, negative allosteric modulator of PAR1. In addition to inhibiting human platelet aggregation, it showed superior anti-inflammatory activity to ML161 in a qPCR assay measuring the expression of tissue factor in response to the cytokine TNF-alpha in endothelial cells. Additionally, NRD-21 is much more plasma stable than ML161, and is a promising lead compound for the parmodulin class for anti-thrombotic and anti-inflammatory indications.

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Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

The important role of 52449-98-6

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Indolinyl-thiazole based inhibitors of scavenger receptor-BI (SR-BI)-mediated lipid transport

A potent class of indolinyl-thiazole based inhibitors of cellular lipid uptake mediated by scavenger receptor, class B, type I (SR-BI) was identified via a high-throughput screen of the National Institutes of Health Molecular Libraries Small Molecule Repository (NIH MLSMR) in an assay measuring the uptake of the fluorescent lipid DiI from HDL particles. This class of compounds is represented by ML278 (17-11), a potent (average IC50 = 6 nM) and reversible inhibitor of lipid uptake via SR-BI. ML278 is a plasma-stable, noncytotoxic probe that exhibits moderate metabolic stability, thus displaying improved properties for in vitro and in vivo studies. Strikingly, ML278 and previously described inhibitors of lipid transport share the property of increasing the binding of HDL to SR-BI, rather than blocking it, suggesting there may be similarities in their mechanisms of action.

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Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

New explortion of Oxolane-2-carbonyl chloride

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Process for the Preparation of Alfuzosin Hydrochloride

A process for preparing alfuzosin or a salt thereof comprising: (a) condensing 4-amino-2-chloro-6,7-dimethoxyquinazoline with 3-methylaminopropionitrile in the presence of a polar aprotic solvent selected from the group consisting of diglyme, dimethyl formamide, t-butanol, hexamethylphosphoramide or mixtures thereof to form N-(4-amino-6,7-dimethoxyquinazol-2-yl)-N-methyl-2-cyanoethylamine (b) hydrogenating the N-(4-amino-6,7-dimethoxyquinazol-2-yl)-N-methyl-2-cyanoethylamine using a hydrogenating agent under a pressure of less than 10 kg/cm2 to form N-(4-amino-6,7-dimethoxyquinazol-2-yl)-N-methylpropylenediamine and optionally converting the N-(4-amino-6,7-dimethoxyquinazol-2-yl)-N-methylpropylenediamine to an acid addition salt thereof; and (c) converting tetrahydrofuroic acid to an intermediate form and condensing the intermediate form with the N-(4-amino-6,7-dimethoxyquinazol-2-yl)-N-methylpropylenediamine or with the acid addition salt to yield alfuzosin base, and optionally converting alfuzosin base to a salt of alfuzosin.

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Reference£º
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

The important role of Oxolane-2-carbonyl chloride

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Nonionic radiographic contrast agents

New nonionic radiographic contrast agents having the formula STR1 wherein Y is a single bond, –CH2 CH2 –, –CH2 O–, –OCH2 –, STR2 –CH2 –, –CH2 –CH2 –CH2 –, –O– or STR3 R1, R1 ‘ and R2 are the same or different and are hydrogen, alkyl or hydroxyalkyl. Hydroxyalkyl refers to such alkyl groups having 1 or more hydroxy groups. Preferred hydroxyalkyl groups include: STR4 R3 and R4 are the same or different and are hydrogen, methyl or –CH2 CH2 OH; R5 is hydrogen, alkyl, –CH2 CH2 OH, CH2 OH or OH and R6 is alkyl, –CH2 CH2 OH, CH2 OH, OH or hydrogen and may be the same or different than R5 and m is zero or one, with the proviso that no methylene or methine carbon atom of the heterocyclic ring is attached to both a nitrogen and an oxygen atom with the additional proviso that when Y is a single bond, m is not zero. These new contrast agents are water soluble and have desirable low osmolality and anticoagulant properties.

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Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

Awesome Chemistry Experiments For 52449-98-6

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Alpha substituted carboxylic acids

Alpha substituted carboxylic acids of formula (I):

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Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

Simple exploration of Oxolane-2-carbonyl chloride

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Enolate Claisen Rearrangement of Esters from Furanoid and Pyranoid Glycals

A general method is described for the formation of furanoid and pyranoid glycals.Thus, lithium-ammonia reduction of the corresponding 1-chloro-2,3-O-isopropylidene furanoid and pyranoid carbohydrate derivatives affords the desired glycals in 87-92percent yields.Several examples that reveal the scope of this process are described .The formation of C-glycosides from the glycal esters through application of the ester enolate Claisen rearrangement is explored.The characteristics and stereochemistry of this process in both the acyclic and cyclic series of glycal derivatives are described.

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Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

Brief introduction of 52449-98-6

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Tricyclic diazepine vasopressin antagonists and oxytocin antagonists

Tricyclic diazepines of the formula: STR1 wherein A, B, D, E, F, Y and Z are defined in the specification which compounds have vasopressin and oxytocin antagonist activity.

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Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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Use of selective antagonists of the alpha1B-adrenergic receptor for improvement of sexual dysfunction

Described is the use in the treatment of either male or female sexual dysfunction of selective antagonists of the alpha1B-adrenergic receptor and the pharmaceutical compositions containing them as compounds capable of helping the sexual act avoiding at the same time excessive side effects due to acute hypotension.

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Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

Extended knowledge of Oxolane-2-carbonyl chloride

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Related Products of 52449-98-6. In my other articles, you can also check out more blogs about 52449-98-6

Related Products of 52449-98-6, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Article, and a compound is mentioned, 52449-98-6, Oxolane-2-carbonyl chloride, introducing its new discovery.

Identification of Inhibitors of the Leishmania cdc2-Related Protein Kinase CRK3

New drugs are urgently needed for the treatment of tropical parasitic diseases such as leishmaniasis and human African trypanosomiasis (HAT). This work involved a high-throughput screen of a focussed kinase set of ?3400 compounds to identify potent and parasite-selective inhibitors of an enzymatic Leishmania CRK3-cyclin6 complex. The aim of this study is to provide chemical validation that Leishmania CRK3-CYC6 is a drug target. Eight hit series were identified, of which four were followed up. The optimisation of these series using classical SAR studies afforded low-nanomolar CRK3 inhibitors with significant selectivity over the closely related human cyclin dependent kinase CDK2. Selective at last: [1,2,4]Triazolo[1,5-a]pyridines, aminopyrazoles, and disubstituted ureas were explored as potent and parasite-selective inhibitors of an enzymatic Leishmania CRK3-cyclin6 complex. Optimisation of these series using classical SAR studies afforded low-nanomolar CRK3 inhibitors with significant selectivity over the closely related human cyclin-dependent kinase CDK2.

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Reference£º
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem