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Friedelin and 3β-Friedelinol: Pharmacological Activities
The interest in herbal medicine as a source of drug leads is being reinforced, especially for tackling challenging therapeutic areas such as...
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Alternative Synthesis of Cobimetinib
A novel approach for synthesis of Cobimetinib was reported, avoiding usage of a strong base in any of the steps with a chiral substrate. An efficient...
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Synthesis of β-Dihydroagarofuran Derivatives and Preliminary Research on Their Insecticidal Activity
Eighteen new β-dihydroagarofuran derivatives were designed and synthesized using 1β,2β,4α,6α,8β,9α,12-heptahydroxy-β-dihydroagarofuran as starting...
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Synthesis and Various Biological Properties of 3-(4-Benzylpiperizino)-1-(4-Ethoxyphenyl)-1-Alkyl(Aryl)-2-Phenylpropan-1-OL Dihydrochlorides
Aminomethylation of 1-(4-ethoxyphenyl)-2-phenylethanone yielded 3-(4-benzylpiperazin-1-yl)-1-(4-ethoxyphenyl)-2-phenylpropan-1-one. Reduction of this...
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Synthesis and Cytostatic Activity of 14β,15β-Oxazino and 14β,15β-Pyrrolidino Estradiol Derivatives
C-14–C-15 condensed heterocyclic estradiol derivatives were synthesized via rearrangement of 3-benzoyloxy-...
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The antiprotozoal potencies of newly prepared 3-azabicyclo[3.2.2]nonanes
3-Azabicyclo[3.2.2]nonanes are already reported as antiprotozoal agents. Structural variations were performed by attachment of several basic side...
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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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Synthesis and Antibacterial Activity of 2-[2,2-Dimethyl-4(3-Trifluoromethylphenyl)-Tetrahydropyran-4-Yl]Arylamine Oxalates
Interaction of ethylcyano(2,2-dimethyltetrahydro-2 H -puran-4-yl)acetate with 3-trifluoromethylphenylmagnesium bromide yielded cyanoesters,...
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Ionic complex of risedronate with positively charged deoxycholic acid derivative: evaluation of physicochemical properties and enhancement of intestinal absorption in rats
Risedronate is widely used clinically to treat osteoporosis, Paget’s disease, hypercalcemia, bone metastasis, and multiple myeloma. However, its oral...
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Synthesis and evaluation of peptidyl α,β-unsaturated carbonyl derivatives as anti-malarial calpain inhibitors
Malarial calpain is a cysteine protease believed to be a central mediator essential for parasitic activities....
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Synthesis and biological properties of 2-(4-chlorophenyl)-3-morpholin-4-yl-(4-alkoxyphenyl)alkanol hydrochlorides
New 2-(4-chlorophenyl)-3-morpholin-4-yl-1-(4-alkoxyphenyl)propan-1-ones were synthesized via aminomethylation of...
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Reaction of deoxyvasicinone with organolithium compounds
4-Butyl-4-hydroxydeoxypeganine was prepared by lithiation of deoxyvasicinone. Deoxypeganine and 1,2-dihydrodeoxypeganine were produced by reduction...
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Design and synthesis of 3′-fluoropenciclovir analogues as antiviral agents
Based on fluorine switch approach, a series of 3′-fluoropenciclovir analogues with different purine and pyrimidine bases were designed and...
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Synthesis of DAAS derivatives and their enhancement of HL-60 leukemia cell differentiation
DAAS is the diacetoxy acetal derivative of a-santonin and induces HL-60 cell differentiation into granulocytes. In this report, we investigated the...
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Synthesis and biological activity of 5-(4-[2-(Methyl-p-substituted phenylamino)ethoxy]benzyl)thiazolidine-2,4-diones
Thiazolidinedione derivatives are potential antidiabetic drugs that bind and activate peroxisome proliferator activated receptor γ (PPARγ), which is...
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Exploration of essential structure of malloapelta B for the inhibitory activity against TNF induced NF-κB activation
For the exploration of pharmacophoric moiety of malloapelta B ( 1 ) possessing the inhibitory activity of NF-κB activation, structural variation of...
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Synthesis and biological activity of cyclohexylamine derivatives
2-( p -hydroxyphenyl)cyclohexylamides were synthesized from ω-chlorocarboxylic acids using the Ritter reaction. Subsequent reduction under the action...
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Synthesis of diacetoxy acetal derivatives of santonin and their enhancing effects on HL-60 leukemia cell differentiation
Several diacetoxy acetal analogues have been synthesized from santonin and assessed for their ability of inducing or enhancing the differentiation of...
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Insect Pheromones Synthesized by Oxidative Transformations of Natural Monoterpenoids
The literature on oxidative transformations of natural monoterpenoids to synthesize insect pheromones was reviewed.