14-Sep-2021 News Top Picks: new discover of 120973-72-0

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Licochalcone A (I), isolated from the roots of Chinese licorice, is the most promising antimalarial compound reported so far. In continuation of our drug discovery program, we isolated two similar chalcones, medicagenin (II) and munchiwarin (III), from Crotalaria medicagenia, which exhibited antimalarial activity against Plasmodium falciparum. A library of 88 chalcones were synthesized and evaluated for their in vitro antimalarial activity. Among these, 67, 68, 74, 77, and 78 exhibited good in vitro antimalarial activity against P. falciparum strains 3D7 and K1 with low cytotoxicity. These chalcones also showed reduction in parasitemia and increased survival time of Swiss mice infected with Plasmodium yoelii (strain N-67). Pharmacokinetic studies indicated that low oral bioavailability due to poor ADME properties. Molecular docking studies revealed the binding orientation of these inhibitors in active sites of falcipain-2 (FP-2) enzyme. Compounds 67, 68, and 78 showed modest inhibitory activity against the major hemoglobin degrading cysteine protease FP-2.

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Benzofuran – Wikipedia,
Benzofuran | C8H3939O – PubChem

Brief introduction of 2-Benzoylbenzofuran-5-carbaldehyde

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In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Recommanded Product: 120973-72-0, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 120973-72-0, name is 2-Benzoylbenzofuran-5-carbaldehyde. In an article,Which mentioned a new discovery about 120973-72-0

A compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein: A0 represents nitrogen or a moiety R¹- , wherein, R¹ represents hydrogen, alkyl or a substituted or unsubstituted aryl group;, R² represents a moiety R³-Y-Z- wherein R³ represents substituted or unsubstituted phenyl, substituted or unsubstituted pyridyl or a substituted or unsubstituted oxazolyl group, and Y represents -(CH2)n-wherein n represents zero or any integer in the range of 1 to 6 and Z represents -CH2-,-CH(OH)- or -CO-;, Raand Rbeach represent hydrogen or Raand Rbtogether represent a bond;, A represents a residue of a benzene ring, the carbon atoms of the residue having in total up to four substituents;, and X represents O or S; a process for preparing such a compound, a pharmaceutical composition containing such a compound and the use of the compound and composition in medicine.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H3933O – PubChem

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In heterogeneous catalysis, the catalyst is in a different phase from the reactants. HPLC of Formula: C16H10O3, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 120973-72-0, name is 2-Benzoylbenzofuran-5-carbaldehyde. In an article,Which mentioned a new discovery about 120973-72-0

The search for Insulin Sensitivity Enhancer (ISE) compounds, for potential use in the treatment of Type II diabetes, has led to the synthesis of compounds that contain a benzofuran spacer between an aryloyl substituent and a 2,4-thiazolidinedione pharmacophore. Sequential combination of haloacetyl aryl substrates with 5-formylsalicylaldehyde gave the desired 2-aryloyl-5-formylbenzofuran intermediates. A related class of compounds, those with a methylene tether between the aromatic moiety and the benzofuran spacer, were also prepared through this strategy.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H3935O – PubChem

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Antileishmanial activities of a library of synthetic chalcone analogues have been examined. Among them, five compounds (11, 14, 16, 17, 22, and 24) exhibited better activity than the marketed drug miltefosine in in vitro studies against the intracellular amastigotes form of Leishmania donovani. Three promising compounds, 16, 17, and 22, were tested in a L. donovani/hamster model. Oral administration of chalcone 16, at a concentration of 100 mg/kg of body weight per day for 5 consecutive days, resulted in >84% parasite inhibition at day 7 post-treatment and it retained the activity until day 28. The molecular and immunological studies revealed that compound 16 has a dual nature to act as a direct parasite killing agent and as a host immunostimulant. Pharmacokinetics and serum albumin binding studies also suggest that compound 16 has the potential to be a candidate for the treatment of the nonhealing form of leishmaniasis.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H3934O – PubChem

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A new chemical access for 3′-acetyl-4′-hydroxychalcones using borontrifluoride-etherate via a regioselective Claisen-Schmidt condensation and its application in the synthesis of chalcone hybrids

A new chemical access has been developed for the synthesis of 3′-acetyl-4′-hydroxychalcones from 1-(5-acetyl-2-hydroxy-phenyl)-ethanone and various substituted benzaldehydes via a regioselective Claisen-Schmidt condensation using borontrifluoride-etherate (BF3¡¤OEt 2) at room temperature, in good to excellent yields within 12-24 h. Application of this methodology has also been demonstrated in the synthesis of chalcone hybrids.

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Benzofuran – Wikipedia,
Benzofuran | C8H3937O – PubChem

Can You Really Do Chemisty Experiments About 2-Benzoylbenzofuran-5-carbaldehyde

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 120973-72-0 is helpful to your research. Reference of 120973-72-0

Reference of 120973-72-0, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 120973-72-0, molcular formula is C16H10O3, introducing its new discovery.

2-Aroylindoles and 2-aroylbenzofurans with N-hydroxyacrylamide substructures as a novel series of rationally designed histone deacetylase inhibitors

Histone deacetylase (HDAC) inhibitors are considered to be drugs for targeted cancer therapy and second-generation HDIs are currently being tested in clinical trials. Here, we report on the synthesis and biological evaluation of a novel HDAC inhibitor scaffold with the hydroxamate Zn2+ complexing headgroup, selected from the 2-aroylindol motif. Inhibition of nuclear extract HDAC and recombinant HDAC 1 as well as induction of histone H3K9+14 hyperacetylation mediated by E-N-hydroxy-(2-aroylindole)acrylamides or E-N-hydroxy-(2-aroylbenzofuran)acrylamides were studied. Moreover, the cytotoxic activity, the effects on the cell cycle, and histone H3S10 phosphorylation of selected compounds were determined. By use of a panel of 24 different human tumor cell lines, mean IC50 values of the most potent analogues 6c and 7b were 0.75 and 0.65 muM, respectively. The novel compounds were shown to be no substrates of the P-glycoprotein drug transporter. Comparable to N1-hydroxy-N8-phenyloctanediamide “2 (SAHA)”, cells in the S phase of the cell cycle are depleted, with partial arrest in G1 and G2/M and finally induction of massive apoptosis.

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Benzofuran – Wikipedia,
Benzofuran | C8H3936O – PubChem

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120973-72-0 2-Benzoylbenzofuran-5-carbaldehyde 2794865, abenzofuran compound, is more and more widely used in various fields.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.120973-72-0,2-Benzoylbenzofuran-5-carbaldehyde,as a common compound, the synthetic route is as follows.

General procedure: To a stirred solution of 1 (100 mg, 0.56 mmol) and 4-(dimethylamino)benzaldehyde (2a) (83 mg, 0.56 mmol) in dry 1,4 dioxane was added gradually BF3¡¤OEt2 (0.142 mL, 1.12 mmol) at room temperature. The whole reaction mixture was stirred for 24 h. The reaction mixture was then diluted with ethyl acetate (100 mL) and washed with water (3 x 25 mL) to decompose the BF3¡¤OEt2 complex. The organic solution obtained after extraction was dried over anhyd. Na2SO4, filtered and the solvent was evaporated under reduced pressure. The crude product was purified by silica gel column chromatography using hexane-ethyl acetate (93:7) as a mobile phase to afford 3a. (140 mg, 80%),, 120973-72-0

120973-72-0 2-Benzoylbenzofuran-5-carbaldehyde 2794865, abenzofuran compound, is more and more widely used in various fields.

Reference£º
Article; Narender; Venkateswarlu; Nayak, B. Vishnu; Sarkar; Tetrahedron Letters; vol. 52; 44; (2011); p. 5794 – 5798;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem