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Pharmacokinetics of YJC-10592, a novel chemokine receptor 2 (CCR-2) antagonist, in rats
YJC-10592, a novel chemokine receptor 2 (CCR-2) antagonist, was developed for treating asthma and atopic dermatitis. We studied the pharmacokinetic...
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Search for new potential anticonvulsants with anxiolytic and antidepressant properties among derivatives of 4,4-diphenylpyrrolidin-2-one
BackgroundThe aim of this study was to synthesize a series of new N -Mannich bases derived from 4,4-diphenylpyrrolidin-2-one having differently...
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Modified Coumarins. 36. Synthesis of Linear and Angular Dihydropyranocoumarincarboxylic Acids
The syntheses of linear and angular dihydropyranocoumarincarboxylic acids, modified structural derivatives of dihydroxanthyletin and dihydroseselin,...
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Design and synthesis of 2,3-dihydro- and 5-chloro-2,3-dihydro-naphtho-[1,2-b]furan-2-carboxylic acid N-(substitutedphenyl)amide analogs and their biological activities as inhibitors of NF-κB activity and anticancer agents
A series of 2,3-dihydro- and 5-chloro-2,3-dihydro-naphtho-[1,2- b ]furan-2-carboxylic acid N -(substitutedphenyl)amide analogs ( 1a–k and 2a–i ) were...
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Differences in extracellular glutamate levels in striatum of rats with high and low exploratory activity
BackgroundMajor inter-individual differences exist in vulnerability to anxiety and affective disorders, and the underlying neurobiology could help in...
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Biological Activity of Adamantane-Containing Mono- and Polycyclic Pyrimidine Derivatives* (A Review)
Biological test results for a series of adamantane-containing pyrimidines, purines, and their derivatives that were synthesized and studied in 1999 –...
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A new pyrrolidine derivative from the rhizome of Coptis chinensis
A new pyrrolidine derivative, 3-hydroxy-1-(4-hydroxyphenethyl)pyrrolidine-2,5-dione ( 1 ), was isolated from the CHCl 3 extract of the rhizome of Coptis...
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Hypoglycemic Potential of Benzimidazole Derivatives
Benzimidazole derivatives exhibiting hypoglycemic and antidiabetic properties were reviewed. Activities of compounds from 22 classes of substituted...
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Modified Coumarins. 34. Synthesis and Transformations of Angular α-Pyronoflavanones
Syntheses of angular α -pyronoflavanones were described. Their reactions with nucleophiles were studied.
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Synthesis and Cytotoxic Activity of Aza-Michael Reaction Products from Ethyl Sorbate and Heterocyclic Amines
The solvent-free reaction of ethyl sorbate and several heterocyclic amines at room temperature was shown to give aza-Michael 1,4-addition products....
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Dimethyldichlorosilane – an Effective Reagent for One-Step Synthesis of \( \boldsymbol{\upalpha} \)-Amino Acid Amides
A preparative method for a one-step synthesis of amino acid amides was developed using dimethyldichlorosilane. This method produces amides with...
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Synthesis and Antitumor Activity of a Novel Series of Helicid-Pyrrolidone Derivatives
This paper reports the synthesis of a new series of helicid–pyrrolidone derivatives ( 4a–4d , 5a–5d , and 6a–6d ), which were tested for antitumor...
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First Spin-Labeled α-Tocopherol and Trolox Succinyl Derivatives
Spin-labeled α-tocopherol succinyl derivatives were synthesized by the reaction of α-tocopherol succinate with...
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Asymmetric synthesis of H1 receptor antagonist (R,R)-clemastine
The first asymmetric synthesis of ( R , R )-clemastine ( 1 ) has been accomplished by the coupling of ( R )-tertiary alcohol 2 and ( R )-chloroethylpyrrolidine ...
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Amination Products of Inula britannica Lactones and Their Antitumor Activity
The reactions with amines of the sesquiterpene lactones britanin and inuchinenolide C isolated from Inula britannica were studied. Migration of the...
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Tricyclic Quinazoline Alkaloids: Isolation, Synthesis, Chemical Modification, and Biological Activity
Results of the last 15–20 years on the isolation, synthesis, chemical modification, and biological activity of natural tricyclic quinazolines and...
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Synthesis and antiprotozoal activities of new 3-azabicyclo[3.2.2]nonanes
Some antimalarial agents in use typically bear basic side chains as ligands. Such ligands were attached to the amino substituent of a bridgehead atom...
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Synthesis and Physicochemical and Biological Properties of 8-Amino-Substituted 7-(2-Aryl-2-Oxoethyl)Xanthines
Asimple laboratory method for preparing 8-amino-substituted 7-(2-aryl-2-oxoethyl)xanthines by reacting the corresponding 8-bromo derivatives with...
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Boehmerine, a New Amide Alkaloid from Piper boehmeriaefolium var. tonkinense, and its Antidepressant Activity
The antidepressant potential of boehmerine, a new amide alkaloid first isolated from Piper boehmeriaefolium (Miq.) C. DC. var. tonkinense, was...