Tag: M.W=150-200

Kavetsou, Eleni published the artcileNovel 3-aryl-5-substituted-coumarin analogues: Synthesis and bioactivity profile, COA of Formula: C9H10O3, the main research area is phenyl methylcoumarin preparation antioxidant antitumor lipoxygenase inhibition SAR docking; acetyloxy-moiety; coumarins; cytotoxicity; lipoxygenase; molecular modeling; oxyprenylated analogues.

Eighteen 3-phenyl-5-substituted-coumarins, among them six were 5-acetyloxy-derivatives, six 5-hydroxy-derivatives and six 5-geranyloxy-derivatives I [R = hydroxy, acetoxy, geranyloxy; R1 = H, MeO, Br; R2 = H, MeO, Br, O2N, etc.] were synthesized, structurally characterized and their antioxidant activity, lipoxygenase inhibitory ability, as well as their cytotoxic activity against human neuroblastoma SK-N-SH and HeLa adenocarcinoma cell lines were evaluated. The compounds I [R = hydroxy, acetoxy, geranyloxy; R1 = H, MeO, Br; R2 = H, MeO, Br, O2N, etc.] were found to be the best cytotoxic agents among all the compounds studied. The bromo-substituted coumarins I [R = acetoxy, R1 = H, R2 = Br; R = acetoxy, R1 = Br, R2 = H] were remarkably active against HeLa cell line showing IC50 1.8 and 6.1μM, resp. Coumarin I [R = geranyloxy, R1 = MeO, R2 = H] presented dual bioactivity, while compound I [R = geranyloxy, R1 = H, R2 = MeO] was the most competent soybean lipoxygenase inhibitor of this series (IC50 10μM). As shown by in-silico docking studies, the studied mols. present allosteric interactions with soybean lipoxygenases.

Drug Development Research published new progress about Antioxidants. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, COA of Formula: C9H10O3.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Li, Qing published the artcileSynthesis of (1,3,4-thiadiazol-2-yl)-acrylamide derivatives as potential antitumor agents against acute leukemia cells, Related Products of isoquinoline, the main research area is thiadiazole acrylamide preparation antitumor leukemia caspase dependent apoptosis; (1,3,4-thiadiazol-2-yl)-acrylamide; Acute leukemia; Antitumor agents; Cell apoptosis; Cytotoxicity.

A lead compound with the (1,3,4-thiadiazol-2-yl)-acrylamide scaffold was discovered to have significant cytotoxicity on several tumor cell lines in an inhouse cell-based screening. A total of 60 derivative compounds were then synthesized and tested in a CCK-8 cell viability assay. Some of them exhibited improved cytotoxic activities. The most potent compounds had IC50 values of 1-5μM on two acute leukemia tumor cell lines, i.e. RS4;11 and HL-60. Flow cytometry anal. of several active compounds and detection of caspase activation indicated that they induced caspase-dependent apoptosis. It was also encouraging to observe that these compounds did not have obvious cytotoxicity on normal cells, i.e. IC50 > 50μM on HEK-293T cells. Although the mol. targets of this class of compound are yet to be revealed, our current results suggest that this class of compound represents a new possibility for developing drug candidates against acute leukemia.

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Related Products of isoquinoline.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Luo, Guolin published the artcileDesign, synthesis and antitumor evaluation of novel 5-methylpyrazolo[1,5-a]pyrimidine derivatives as potential c-Met inhibitors, Product Details of C9H10O3, the main research area is methyl pyrazolopyrimidine preparation antitumor cMet kinase inhibitor docking SAR; Antitumor activity; Molecular docking; Pyrazolo[1,5-a]pyrimidine derivatives; Synthesis; c-Met kinase inhibitor.

A series of novel 5-methylpyrazolo[1,5-a]pyrimidine derivatives I (R = pyrazin-2-yl, 4-chlorophenyl, 2-fluorobenzyl, etc.; R1 = H, Me) were designed, synthesized, and evaluated for their in vitro inhibitory activities against c-Met kinase and antiproliferative activities against the SH-SY5Y, MDA-MB-231, A549, and HepG2 cell lines. Most of the compounds remarkably inhibited c-Met kinase and showed moderate to good cytotoxicity and selectivity toward the four cancer cell lines. Among them, compounds I (R = pyrazin-2-yl, 4-fluorophenyl; R1 = H) were the two most potent selective c-Met inhibitors with half-maximal inhibitory concentration (IC50) values of 5.17 ± 0.48 nM and 5.62 ± 0.78 nM, resp., and suppression abilities comparable with the pos. control cabozantinib. Cell proliferation assay further demonstrated that the two most promising compounds I (R = 3,5,6-trimethylpyrazin-2-yl, pyrazin-2-yl, ; R1 = H) also showed good cytotoxicity and selectivity toward MDA-MB-231 cells, with IC50 values of 26.67 ± 2.56μM and 26.83 ± 2.41μM, resp. Compounds I (R = 4-fluorophenyl, 4-methoxy-3-fluorophenyl; R1 = H) showed cytotoxicity and selectivity toward A549 cells, with IC50 values of 20.20 ± 2.04μM and 21.65 ± 1.58μM, resp. All antiproliferative activities were within the range of those of cabozantinib. Notably, these compounds I presented relatively low hepatotoxicity compared with reference drugs. Moreover, the preliminary structure-activity relationship and docking studies revealed that replacement of a nitrogen-containing heterocycle on the R (block A) group might improve the c-Met kinase inhibitory and antiproliferative effects in MDA-MB-231 cells, whereas displacement by a substituted benzene ring, especially for the p-fluorophenyl or 4-fluoro-3-methoxyphenyl moiety, on the R group enhanced cytotoxicity toward A549 cells. Together, these results suggest that I (R = pyrazin-2-yl, 4-fluorophenyl; R1 = H) are promising compounds and provide a basis for their development as new antitumor agents.

Bioorganic Chemistry published new progress about Antitumor agents. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Product Details of C9H10O3.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Liu, Jun published the artcileNovel 2-Substituted 3-Hydroxy-1,6-dimethylpyridin-4(1H)-ones as Dual-Acting Biofilm Inhibitors of Pseudomonas aeruginosa, Application of 4-Methoxyphenylacetic acid, the main research area is hydroxy dimethylpyridinone synthesis drug design Pseudomonas aeruginosa biofilm inhibitor.

2-Heptyl-3-hydroxy-4(1H)-quinolone (PQS), a compound from P. aeruginosa, functions as both a quorum sensing (QS) regulator and a potent iron chelator to induce expression of pyoverdine and pyochelin which are involved in high-affinity iron transport systems. A potential dual-acting antibiofilm strategy requires mols. designed to interfere with iron uptake and the QS system of P. aeruginosa. A series of 2-substituted 3-hydroxy-1,6-dimethylpyridin-4-ones have been designed, synthesized, and tested as biofilm inhibitors of P. aeruginosa. One compound, N-((1,3,6-trimethyl-4-oxo-1,4-dihydropyridin-2-yl)methyl)hexanamide, I, exhibits 68.67% biofilm inhibitory activity at 20μM. Further mechanistic studies have confirmed that this compound not only inhibits the QS systems of P. aeruginosa but also acts as an iron chelator to compete strongly with pyoverdine, causing iron deficiency in bacteria. The pyoverdine receptor FpvA was revealed as the target of I by the Pvds mutant strain, fpvA-overexpressed strain, and in silico studies.

Journal of Medicinal Chemistry published new progress about Antibiotic resistance (bacterial). 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Application of 4-Methoxyphenylacetic acid.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Saadiq, Muhammad published the artcileSynthesis, Bioactivity Assessment, and Molecular Docking of Non-sulfonamide Benzimidazole-Derived N-Acylhydrazone Scaffolds as Carbonic Anhydrase-II Inhibitors, SDS of cas: 86-51-1, the main research area is benzimidazole acylhydrazone preparation mol docking carbonic anhydrase inhibitor.

This research reports the synthesis of new benzimidazole-derived N-acylhydrazones (NAH), their characterization using various spectroscopic methods, and in vitro evaluation as potent carbonic anhydrase-II inhibitors. Among the target compounds, few showed higher inhibition than the standard acetazolamide (IC50: 18.6 ± 0.43μM). Mol. docking was performed on the most active compounds, which revealed their binding interactions with the active site of the enzyme, thus supporting the exptl. findings.

ACS Omega published new progress about Carbonic anhydrase inhibitors. 86-51-1 belongs to class isoquinoline, name is 2,3-Dimethoxybenzaldehyde, and the molecular formula is C9H10O3, SDS of cas: 86-51-1.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Bao, Ming published the artcileGold-Catalyzed 1,2-Acyloxy Migration/Coupling Cascade of Propargyl Diazoacetates: Synthesis of Isomycin Derivatives, Safety of 4-Methoxyphenylacetic acid, the main research area is propargyl diazoacetate gold catalyst carbocyclization acyloxy migration coupling cascade; isomycin derivative preparation.

An efficient gold(I)-catalyzed carbocyclization reaction for the synthesis of isomycin derivatives from propargyl diazoacetates has been developed. The suggested cyclization pathway delineated the first example of a vinyl gold carbenoid species generated in situ from gold(I)-catalyzed 1,2-acyloxy migration and intercepted by a cross-coupling reaction with the remaining tethered diazo functionality. The use of protic additives was essential to regulating the reaction outcome by fine-tuning the catalytic preference of the gold(I) complex.

Organic Letters published new progress about Cross-coupling reaction. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Safety of 4-Methoxyphenylacetic acid.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Shalaby, Raed published the artcileSAR and molecular mechanism studies of monoamine oxidase inhibition by selected chalcone analogs, Computed Properties of 86-51-1, the main research area is monoamine oxidase chalcone; Monoamine oxidase; chalcone; dopamine; mRNA; reversibility.

The present study describes the synthesis of a series of 22 chalcone analogs. These compounds were evaluated as potential human MAO-A and MAO-B inhibitors. The compounds showed varied selectivity against the two isoforms. The IC50 values were found to be in the micromolar to submicromolar range. The Ki values of compound 16(I) were determined to be 0.047 and 0.020 μM for the inhibition of MAO-A and MAO-B, resp. Dialysis of enzyme-inhibitor mixtures indicated a reversible competitive mode of inhibition. Most of the synthesized chalcone analogs showed a better selectivity toward MAO-B. However, introducing of 2,4,6-trimethoxy substituents on ring B shifted the selectivity toward MAO-A. In addition, we investigated the mol. mechanism of MAO-B inhibition by selected chalcone analogs. Our results revealed that these selected chalcone analogs increased dopamine levels in the rat hepatoma (H4IIE) cells and decreased the relative mRNA expression of the MAO-B enzyme.

Journal of Enzyme Inhibition and Medicinal Chemistry published new progress about Enzyme kinetics. 86-51-1 belongs to class isoquinoline, name is 2,3-Dimethoxybenzaldehyde, and the molecular formula is C9H10O3, Computed Properties of 86-51-1.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Jiang, Liping published the artcileDiscovery and evaluation of chalcone derivatives as novel potential anti-Toxoplasma gondii agents, Recommanded Product: 2,3-Dimethoxybenzaldehyde, the main research area is chalcone diphenyl propanone preparation Toxoplasma gondii antiparasitic SAR; AI-based drug design; Antiparasitic agents; Chalcone derivatives; Structure-activity relationship; Toxoplasma gondii.

Due to numerous side effects of traditional treatments for toxoplasmosis, it is urgent to develop new anti-Toxoplasma agents with high efficiency and low toxicity. In this study, using drug-food-homologous chalcone skeleton as a leading compound, 6 series of chalcone derivatives were designed, synthesized, and almost 1/2 compounds have good anti-Toxoplasma activity in vitro. The quant. structure-activity relationship model of the anti-Toxoplasma activity of the second batch of compounds was established by random forest method (R2 = 0.9407). The Michael receptor in the mol. skeleton of chalcones plays an important role in improving the activity. Among these compounds, four chalcone derivatives exhibited potent anti-T. gondii activity and low cytotoxicity in vitro. Specifically, 1-(4-aminophenyl)-3-(3,4-dichlorophenyl)propan-1-one, (E)-3-(3,4-dichlorophenyl)-1-(4-(isopropylamino)phenyl) prop-2-en-1-one and 1-(3-aminophenyl)-3-(2,3-dimethoxyphenyl)propan-1-one derivatives effectively inhibited the proliferation of Toxoplasma tachyzoites in vivo. Liver and spleen index and biochem. parameters, such as alanine aminotransferase, aspartate aminotransferase and malondialdehyde were significantly decreased by the three chalcone derivatives, suggesting that they have protective effects on the liver of mice infected with Toxoplasma tachyzoites. Overall, this article provides a series of promising compounds for the development of anti-Toxoplasma agents.

European Journal of Medicinal Chemistry published new progress about Parasitic infection. 86-51-1 belongs to class isoquinoline, name is 2,3-Dimethoxybenzaldehyde, and the molecular formula is C9H10O3, Recommanded Product: 2,3-Dimethoxybenzaldehyde.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Mokrov, G. V. published the artcileSynthesis and Cardiotropic Activity of Linear Methoxyphenyltriazaalkanes, Name: 2,3-Dimethoxybenzaldehyde, the main research area is methoxyphenyltriazaalkane preparation antiischemic antiarrhythmic antifibrillatory cardiotropic activity.

A new group of potential pFOX inhibitors among linear methoxyphenyltriazaalkanes RCH2NH(CH2)nNH(CH2)mNHCH2R (R = 2,3-(OCH3)2C6H3, 2,4-(OCH3)2C6H3, 2,5-(OCH3)2C6H3, 2,3,4-(OCH3)3C6H2, 2,4,5-(OCH3)3C6H2, 2,4,6-(OCH3)3C6H2; n = 2, 3; m = 2, 3) were designed and synthesized. Cardiotropic activity in rodent experiments was found for most of the synthesized compounds The most active compound RCH2NH(CH2)nNH(CH2)mNHCH2R (R = 2,3,4-(OCH3)3C6H2; n = 2; m = 2) combined with anti-ischemic, antiarrhythmic, and antifibrillatory activities (1 mg/kg, i.v.) and low toxicity (LD50 = 119 mg/kg, mice, i.p.) was selected for development as a potential cardiotropic drug.

Pharmaceutical Chemistry Journal published new progress about Amines Role: PAC (Pharmacological Activity), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), PREP (Preparation), USES (Uses). 86-51-1 belongs to class isoquinoline, name is 2,3-Dimethoxybenzaldehyde, and the molecular formula is C9H10O3, Name: 2,3-Dimethoxybenzaldehyde.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Kenia, Hasti published the artcileEthyl-4-(dimethylamino)-2-(4-methoxyphenyl) propanote as anxiolytic, anti-inflammatory and anti-bacterial agent, Synthetic Route of 104-01-8, the main research area is ethyl dimethylamino methoxyphenyl propanote preparation anxiolytic antipsychotic antidepressant antiinflammatory; antibacterial ethyl dimethylamino methoxyphenyl propanote preparation.

An improved process for the synthesis of ethyl-4-(dimethylamino)-2-(4-methoxyphenyl)propanote I was carried out by hydrolysis of 2-(4-methoxyphenyl)acetonitrile using sodium hydroxide to obtain 2-(4-methoxyphenyl)acetic acid which was then esterified with ethanol to obtain 2-(4-methoxyphenyl)acetate which on further Mannich reaction with paraformaldehyde and dimethylamine in presence of catalytic amount of tert-Bu ammonium bromide. Compound I was subjected to pharmacol. screening for anxiolytic activity by elevated plus maze test, open field test and motor co-ordination test by Rota rod. Compound I was also screened for in-vivo antipsychotic, in-vivo antidepressant, in-vitro anti-inflammatory activity by protein denaturation method and antibacterial activity by serial dilution method.

World Journal of Pharmacy and Pharmaceutical Sciences published new progress about Anti-inflammatory agents. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Synthetic Route of 104-01-8.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem