Day: December 1, 2022

Jerkovic, I. published the artcileContribution to the characterisation of honey-based Sardinian product abbamele: Volatile aroma composition, honey marker compounds and antioxidant activity, Recommanded Product: 5-Methyl-2-phenylhex-2-enal, the main research area is honey abbamele aroma marker antioxidant.

Sardinian abbamele is a typical product obtained from the honey recuperation from combs (traditional procedure) or by concentration of the honey diluted in water (industrial procedure). Seven abbamele samples were obtained to study the volatiles’ composition, the presence of honey marker compounds and their relationship with the production procedures. The long thermal treatment applied in abbamele production caused very high (1007.0-4405.8 mg/kg) HMF content (HPLC-DAD), while glucose and fructose amounts were quite similar to the honey ones (HPLC-RI). Total antioxidant activity (FRAP assay) of the samples ranged between 13.3 and 71.2 mmol Fe2+/kg, while antiradical activity (DPPH assay) ranged between 3.8 and 23.3 mmol TEAC/kg. Such high antioxidant values were linearly correlated with total phenol amount (1297.8-4469.5 mg GAE/kg) determined by Folin-Ciocalteau method. Thermally derived furan derivatives and terpenes were abundant among the headspace volatiles (HS-SPME), particularly limonene (0.5-76.0%) that probably originated from citrus rinds’ addition during abbamele production GC and GC-MS analyses of USE isolates revealed HMF predominance as well as the honey marker compounds (if/when existing) such as Me syringate (up to 49.2%), marker of Asphodelus microcarpus honey. High isophorone percentage (up to 30.9%) determined by HS-SPME followed by minor percentage of 4-ketoisophorone and norisoprenoids in one sample indicated Arbutus unedo L. honey use in the production HPLC-DAD anal. confirmed the presence of specific honey markers: two samples showed high Me syringate concentrations (150.4-120.1 mg/kg) while homogentisic acid and other specific markers of A. unedo honey were found in one sample. The compared GC-MS and HPLC-DAD data proved to be useful to obtain information about the use of specific honey in the production and to verify citrus addition

Food Chemistry published new progress about Antioxidants. 21834-92-4 belongs to class isoquinoline, name is 5-Methyl-2-phenylhex-2-enal, and the molecular formula is C13H16O, Recommanded Product: 5-Methyl-2-phenylhex-2-enal.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Bhagat, Kavita published the artcileMicrowave-assisted synthesis of 11-substituted-3,3-dimethyl-2,3,4,5,10,11-hexahydrodibenzo[b,e][1,4]diazepin-1-one derivatives catalysed by silica supported fluoroboric acid as potent antioxidant and anxiolytic agents, Recommanded Product: 2,3-Dimethoxybenzaldehyde, the main research area is dimethyl hexahydrodibenzodiazepinone preparation antioxidant anxiolytic activity green chem; phenylenediamine dimedone aldehyde fluoroboric acid catalyst cyclocondensation microwave irradiation.

A novel series of benzodiazepine derivatives I [R = Ph, 4-chlorophenyl, 4-bromophenyl, etc.] as antioxidant and anxiolytic agents were synthesized. All the compounds were obtained in good yield by facile synthesis. To check their antioxidant potential, DPPH (2,2-diphenyl-1-picrylhydrazyl) free radical scavenging assay was performed. Among all the synthetics seven derivatives I [R = 3-methoxyphenyl, 4-nitrophenyl, 3-methyl-2-thienyl, cinnamyl, 1-naphthyl 3,4-dichlorophenyl, 3-bromophenyl] exhibited IC50 values ranging from 76 to 489 nM. These seven compounds were further evaluated to check their binding abilities towards the benzodiazepine binding site on GABAA receptors. Three best-fit ligands I [R = 3-methoxyphenyl, 1-naphthyl, 3,4-dichlorophenyl] were further evaluated for their anxiolytic effect by using three in-vivo mice models i.e. Elevated Plus Maze, Light & Dark box, and Mirror Chamber model. The study revealed that compounds I [R = 3,4-dichlorophenyl, 1-naphthyl] showed the best anxiolytic effect as compared to standard drug diazepam even at an oral dose of 1.0 mg/kg.

Medicinal Chemistry Research published new progress about Antioxidants. 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

Smirnova, Irina published the artcileHollongdione arylidene derivatives induce antiproliferative activity against melanoma and breast cancer through pro-apoptotic and antiangiogenic mechanisms, Application of 2,3-Dimethoxybenzaldehyde, the main research area is melanoma breast cancer hollongdione arylidene derivative antiangiogensis; Antiproliferative activity; Arylidene; CAM assay; Claisen-Schmidt aldol condensation; Cytotoxicity; Dammarane triterpenoids; Dipterocarpol; Hollongdione; NCI-60; rtPCR.

The use of natural compounds as starting point for semisynthetic derivatives has already been proven as a valuable source of active anticancer agents. Hollongdione (4,4,8,14-tetramethyl-18-norpregnan-3,20-dion), obtained by few steps from dammarane type triterpenoid dipterocarpol, was chem. modified at C2 and C21 carbon atoms by the Claisen-Schmidt aldol condensation to give a series of arylidene derivatives The anticancer activity of the obtained compounds was assessed on NCI-60 cancer cell panel, revealing strong antiproliferative effects against a large variety of cancer cells. 2,21-Bis-[3-pyridinyl]-methylidenohollongdione 9 emerged as the most active derivative as indicated by its GI50 values in the micromolar range which, combined with its high selectivity index values, indicated its suitability for deeper biol. investigation. The mechanisms involved in compound 9 antiproliferative activity, were investigated through in vitro (DAPI staining) and ex vivo (CAM assay) tests, which exhibited its apoptotic and antiangiogenic activities. In addition, compound 9 showed an overall inhibition of mitochondrial respiration. rtPCR anal. identified the more intimate activity at pro-survival/pro-apoptotic gene level. Collectively, the hollongdione derivative stand as a promising therapeutic option against melanoma and breast cancer provided that future in vivo anal. will certify its clin. efficacy.

Bioorganic Chemistry published new progress about Angiogenesis. 86-51-1 belongs to class isoquinoline, name is 2,3-Dimethoxybenzaldehyde, and the molecular formula is C9H10O3, Application of 2,3-Dimethoxybenzaldehyde.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Wang, Cong published the artcileDiscovery of chalcone-modified estradiol analogs as antitumour agents that Inhibit tumour angiogenesis and epithelial to mesenchymal transition, Name: 2,3-Dimethoxybenzaldehyde, the main research area is estradiol chalcone analog preparation antitumor antiangiogenic; 2-Methoxyestradiol; Angiogenesis; Antitumour; EMT; Migration.

Angiogenesis plays an essential role in tumorigenesis and tumor progression, and anti-angiogenesis therapies have shown promising antitumor effects in solid tumors. 2-Methoxyestradiol (2ME2), an endogenous metabolite of estradiol, has been regarded as a potential antitumor agent mainly targeting angiogenesis. Here we synthesized a novel series of chalcones based on 2-methoxyestradiol and evaluated their potential activities against tumors. Compound I was demonstrated to have potent antiangiogenic activity. Further studies showed that I suppressed tumor growth in human breast cancer (MCF-7) xenograft models without obvious side effects. Evaluation of the mechanism revealed that I targeted the epithelial to mesenchymal transition (EMT) process in MCF-7 cells and inhibited HUVEC migration and then contributed to hindrance of angiogenesis. Thus, I may be a promising antitumor agent with excellent efficacy and low toxicity.

European Journal of Medicinal Chemistry published new progress about Angiogenesis. 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

Yuan, Xu published the artcileDesign, synthesis and in vitro evaluation of 6-amide-2-aryl benzoxazole/benzimidazole derivatives against tumor cells by inhibiting VEGFR-2 kinase, Computed Properties of 104-01-8, the main research area is amide aryl benzoxazole preparation antitumor antiangiogenesis VEGFR2 tyrosine kinase; benzimidazole amide aryl preparation antitumor antiangiogenesis VEGFR2 tyrosine kinase; Angiogenesis; Antitumor activity; Benzimidazole; Benzoxazole; VEGFR-2.

A library of thirty-seven 6-amide-2-aryl benzoxazoles I (R1 = H, F, Br, Cl and MeO; R2 = F, Br, Cl, Me and MeO; R3 = H and MeO; X = O; X1 = H and Cl; X2 = H, 2-F, 2-Cl, 2-Br and 3-Br; n = 0, 1)/benzimidazoles I (R1 = H, F, Br and MeO; R2 = Cl, Me and MeO; R3 = H and MeO; R3 = Cl, Me and OMe; X = NH; X1 = Cl; X2 = H; n = 0, 1) has been designed and synthesized based on the highly conserved active site of VEGFR-2. Several title compounds I exhibited selective inhibitory activities against VEGFR-2 than EGFR kinases, which also displayed selective anti-proliferation potency against the HUVEC and HepG2 than the A549 and MDA-MB-231 cancer cell lines. The newly synthesized compounds I were evaluated for anti-angiogenesis capability by chick chorioallantoic membrane (CAM) assay. Among them, compounds I (R1 = R3 = H; R2 = OMe; n = 1; X = NH; X1 = Cl; X2 = H) showed the most potent anti-angiogenesis ability (79% inhibition at 10 nM/eggs), the efficient cytotoxic activities (in vitro against the HUVEC and HepG2 cell lines with IC50 values of 1.47 and 2.57 μM, resp.), and excellent VEGFR-2 kinase inhibition (IC50 = 0.051 μM). The mol. docking anal. revealed that compound I (R1 = R3 = H; R2 = OMe; n = 1; X = NH; X1 = Cl; X2 = H) is a Type II inhibitor of VEGFR-2 kinase. These results indicated that the 6-amide-2-arylbenzoxazoles and 6-amide-2-aryl benzimidazoles I are promising inhibitors of VEGFR-2 kinase for the potential treatment of anti-angiogenesis.

European Journal of Medicinal Chemistry published new progress about Angiogenesis. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Computed Properties of 104-01-8.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Vidic, Jasmina Minic published the artcileQuantitative assessment of olfactory receptors activity in immobilized nanosomes: a novel concept for bioelectronic nose, Synthetic Route of 1205-17-0, the main research area is olfactory receptor immobilization nanosome bioelectronic nose.

The authors describe how mammalian olfactory receptors (ORs) could be used as sensing elements of highly specific and sensitive bioelectronic noses. An OR and an appropriate Gα protein were co-expressed in Saccharomyces cerevisiae cells from which membrane nanosomes were prepared, and immobilized on a sensor chip. By Surface Plasmon Resonance, the authors were able to quant. evaluate OR stimulation by an odorant, and G protein activation. The authors demonstrate that ORs in nanosomes discriminate between odorant ligands and unrelated odorants, as in whole cells. This assay also provides the possibility for quant. assessment of the coupling efficiency of the OR with different Gα subunits, without the interference of the cellular transduction pathway. The authors’ findings will be useful to develop a new generation of electronic noses for detection and discrimination of volatile compounds, particularly amenable to micro- and nano-sensor formats.

Lab on a Chip published new progress about Alkyl groups. 1205-17-0 belongs to class isoquinoline, name is 2-Methyl-3-(3,4-methylenedioxyphenyl)propionaldehyde, and the molecular formula is C11H12O3, Synthetic Route of 1205-17-0.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Yang, Jinfei published the artcileMn(II)-Catalysed ortho-alkenylation of aromatic amines and its application in reproductive diseases, Recommanded Product: 4-Methoxy-N-methylaniline, the main research area is manganese catalyst aromatic amine alkenylation reproductive disease.

A Mn(II)-catalyzed ortho-alkenylation of aromatic amines and its application in reproductive diseases were developed. The use of MnCl2 was critical for the ortho-alkenylation of aromatic amines. The general applicability of this procedure was highlighted by the synthesis of 27 vinylanilines, with good regioselectivities. The value of our approach in practical applications was investigated by studying the effects of one of the compounds 3m on 8 wk-old adult male rats with azoospermia as a mammalian model. The results show that a small amount of sperm will gradually be produced in the epididymis and testes by treatment of 8 wk-old adult male rats with azoospermia with 1 mg kg-13m after two weeks, while treatment with 10 mg kg-13m led to obvious sperm production Notably, if we increase the dose to 100 mg kg-1, there will be a lot of sperm production in the epididymis and testes after two weeks of treatment. The results of this study will be of great significance in research on drugs for treating azoospermia and oligospermia diseases.

RSC Advances published new progress about Alkenylation. 5961-59-1 belongs to class isoquinoline, name is 4-Methoxy-N-methylaniline, and the molecular formula is C8H11NO, Recommanded Product: 4-Methoxy-N-methylaniline.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Jia, Xiaofan published the artcileSynthesis of Stilbenes by Rhodium-Catalyzed Aerobic Alkenylation of Arenes via C-H Activation, COA of Formula: C8H10O2, the main research area is stilbene preparation rhodium catalyzed alkenylation vinyl arene.

Arene alkenylation is commonly achieved by late transition metal-mediated C(sp2)-C(sp2) cross-coupling, but this strategy typically requires prefunctionalized substrates (e.g., with halides or pseudohalides) and/or the presence of a directing group on the arene. Transition metal-mediated arene C-H activation and alkenylation offers an alternative method to functionalize arene substrates. Herein, we report a rhodium-catalyzed oxidative arene alkenylation from arenes and styrenes to prepare stilbene and stilbene derivatives The reaction is successful with several functional groups on both the arene and the olefin including fluoride, chloride, trifluoromethyl, ester, nitro, acetate, cyanide, and ether groups. Reactions of monosubstituted arenes are selective for alkenylation at the meta and para positions, generally with approx. 2:1 selectivity, resp. Resveratrol and (E)-1,2,3-trimethoxy-5-(4-methoxystyryl)benzene (DMU-212) are synthesized by this single-step approach in high yield. Comparison with palladium catalysis showed that rhodium catalysis is more selective for meta-functionalization for monosubstituted arenes and that the Rh catalysis has better tolerance of halogen groups.

Journal of the American Chemical Society published new progress about Alkenylation. 151-10-0 belongs to class isoquinoline, name is 1,3-Dimethoxybenzene, and the molecular formula is C8H10O2, COA of Formula: C8H10O2.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Walpen, Nicolas published the artcileApplication of UV absorbance and electron-donating capacity as surrogates for micropollutant abatement during full-scale ozonation of secondary-treated wastewater, Synthetic Route of 117-96-4, the main research area is micropollutant ozonation wastewater treatment UV absorbance electron donating capacity; Electron-donating capacity; Micropollutant abatement; On-line monitoring; Ozonation; UV absorbance.

Ozonation of secondary-treated wastewater for the abatement of micropollutants requires a reliable control of ozone doses. Changes in the UV absorbance of dissolved organic matter (DOM) during ozonation allow to estimate micropollutant abatement online and were therefore identified as feed-back control parameter. In this study, the suitability of the electron-donating capacity (EDC) as an addnl. surrogate parameter which is independent of optical DOM properties was evaluated during full-scale ozonation. For this purpose, a recently developed EDC analyzer was enhanced to enable continuous online EDC and UV absorbance measurements. During a multi-week monitoring campaign at the wastewater treatment plant of Zurich, Switzerland, specific ozone doses were varied from 0.13 to 0.91 mgO3·mgDOC-1 and selected micropollutants with different ozone reactivities were analyzed by LC-MS in conjunction with bromate anal. by IC-MS. In agreement with previous laboratory studies, the relative residual UV absorbance and EDC both decreased exponentially as a function of the specific ozone dose and, in comparison to the residual UV absorbance, residual EDC values showed a more pronounced decrease at low specific ozone doses â‰?.34 mgO3·mgDOC-1. Logistic regression models allowed to estimate relative residual micropollutant concentrations in the ozonation effluent using either the residual UV absorbance or EDC as explanatory variable. Averaging those models along the explanatory variables allowed to estimate target values in relative residual UV absorbances and EDC for specific micropollutant abatement targets. In addition, both parameters allowed to identify conditions with elevated conversions of bromide to bromate. Taken together, these findings show that the integration of relative residual EDC values as a second control parameter can improve existing absorbance-based ozonation control systems to meet micropollutant abatement targets, particularly for treatment systems where low ozone doses are applied.

Water Research published new progress about Absorptivity. 117-96-4 belongs to class isoquinoline, name is Diatrizoic Acid, and the molecular formula is C11H9I3N2O4, Synthetic Route of 117-96-4.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Galmes, Sebastia published the artcileAbsorption, Distribution, Metabolism, and Excretion of the Main Olive Tree Phenols and Polyphenols: A Literature Review, Formula: C9H10O3, the main research area is review olive tree phenol polyphenol absorption metabolism excretion; bioavailability; hydroxytyrosol; metabolic reactions; oleuropein; olive polyphenols; toxicity.

The effects of olive tree (poly)phenols (OPs) are largely dependent upon their bioavailability and metabolization by humans. Absorption, distribution, metabolism, and excretion (ADME) are fundamental for the nutritional efficacy and toxicol. impact of foods containing OPs. This review includes studies on the administration of hydroxytyrosol (HT), oleuropein (Ole), or other OPs and foods, products, or mixtures that contain them. Briefly, data from in vivo studies indicate that OPs are absorbable by intestinal cells. Both absorption and bioavailability depend upon each compound and/or the matrix in which it is contained. OPs metabolism begins in enterocytes and can also continue in the liver. Metabolic phase I mainly consists of the hydrolysis of Ole, which results in an increase in the HT content. Phase II metabolic reactions involve the conjugation of (poly)phenols mainly with glucuronide and sulfate groups. This review offers a complete perspective of the ADME processes of OPs, which could support the future nutritional and/or toxicol. studies in this area.

Journal of Agricultural and Food Chemistry published new progress about Olea europaea. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Formula: C9H10O3.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem