Category: isoquinoline

Ojah, Emmanuel Onah published the artcileChemical Compositions, Antioxidant and Anti-diabetic Activities of Root Wood and Root Bark Essential Oils from Pterocarpus soyauxii TAUB., SDS of cas: 151-10-0, the main research area is Pterocarpus root bark essential oil antioxidant antidiabetic agent.

The chem. composition of essential oils (EOs) isolated by hydrodistillation from Pterocarpus soyauxii Taub. root wood and root bark were determined for the first time by GC/MS anal. The EOs gave a percentage yield (weight/weight) of 0.34% and 0.31% for root wood and root bark resp. A total of 60 compounds accounting for 86.1% of the root wood EO composition were identified with monoterpenes (45.4%) and sesquiterpenes (14.7%) as predominant constituents. Root bark EO gave 53 identified constituents which make up about 78.5% of the EO dominated by non-terpenes (23.4%) and alkanes (14.1%). The EOs are good sources of limonene (16.9%), γ-terpinene (9.8%) and p-cymene (6.70%). The anti-diabetic (α-amylase and α-glucosidase models) and antioxidant activities (DPPH and H2O2 models) of EOs were evaluated in comparison with standard drugs. Alpha-amylase inhibition gave IC50 values (mg/mL) of 0.0493 and 0.0471 for root wood and root bark EOs resp., compared to acarbose the standard anti-diabetic drug (0.0401) while α-glucosidase assay gave IC50 values (mg/mL) of 0.0517 and 0.0486 for root wood and root bark EOs resp., compared with acarbose (0.0418). In the DPPH antioxidant assay, root bark EO showed higher activity (0.157 mg/mL) compared to root wood EO (0.159 mg/mL) while Root wood and root bark EOs had IC50 values (mg/mL) of 0.157 and 0.171 resp. using the H2O2 model. Results revealed the presence of chem. constituents in the EOs which could be responsible for activities expressed by the plant.

Journal of Essential Oil-Bearing Plants published new progress about Antidiabetic agents. 151-10-0 belongs to class isoquinoline, name is 1,3-Dimethoxybenzene, and the molecular formula is C8H10O2, SDS of cas: 151-10-0.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Patchipala, Suri Babu published the artcileSynthesis, in-vivo anti-diabetic & anticancer activities and molecular modelling studies of tetrahydrobenzo[d]thiazole tethered nicotinohydrazide derivatives, COA of Formula: C9H10O3, the main research area is tetrahydrobenzothiazole nicotinohydrazide preparation docking antidiabetic anticancer activity.

A series of thirty new thiazole-pyridine derivatives I (R = Ph, pyridin-3-yl, 2,5-difluoro Ph, etc.; R1 = H, cyclopropylmethyl) was synthesized by reaction of 4,4,7,7-tetra-methyl-4,5,6,7-tetrahydrobenzo[d]thiazol-2-amine with 6-chloronicotinate followed by condensing with benzaldehydes RCHO and screened for their anti-diabetic activity by in vivo housing Swiss albino mice. All synthesized compounds resulted in reducing the glucose level when compared with reference standard drug glibenclamide. In specific, Et 6-((4,4,7,7-tetramethyl-4,5,6,7-tetrahydrobenzo[d]thiazol-2-yl)amino)nicotinate exhibited significant activity in terms of fasting blood glucose level reduction In addition, the in-silico binding studies of the potential compounds I (R = 4-fluoro-3-methoxyphenyl, R1 = H; R = 5-fluoro-2-nitrophenyl, R1 = H) with human PPAR-γ protein complexed with Retinoid X Receptor (RXR) alpha Nuclear Receptor showed good interactions when compared to the standard drug Rosiglitazone. The newly synthesized drugs may be potential anti-diabetic drugs with possible specific actions.

Arabian Journal of Chemistry published new progress about Antidiabetic agents. 86-51-1 belongs to class isoquinoline, name is 2,3-Dimethoxybenzaldehyde, and the molecular formula is C9H10O3, COA of Formula: C9H10O3.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Pansuriya, Ketan published the artcileTrimethylsilyl chloride catalyzed synthesis of fluoro substituted tetrahydropyrimidines: Molecular docking and antidiabetic studies, SDS of cas: 598-50-5, the main research area is tetrahydropyrimidine preparation antidiabetic docking; aldehyde ethyl acetoacetate urea Biginelli condensation trimethylsilyl chloride catalyst.

A novel series of tetrahydropyrimidine derivatives I [R1 = H, Me; R2 = H, Me] and II [R3 = NC, COOH, CO2Me, CO2Et] containing azepino indole and aryl substitution was achieved by a multicomponent synthetic approach using Biginelli condensation. Various catalysts were employed in the reactions for yield increment but trimethylsilyl chloride gave the highest yield. Moreover, all synthesized mols. were checked for in vitro antidiabetic potential. In addition, mol. docking of these synthesized mols. was studied using barley alpha-amylase isoenzyme 1 (amy1) (1RPK). The result revealed that compounds I [R1 = R2 = H; R1 = R2 = Me] had a good inhibitory potential.

Chemical Data Collections published new progress about Antidiabetic agents. 598-50-5 belongs to class isoquinoline, name is 1-Methylurea, and the molecular formula is C2H6N2O, SDS of cas: 598-50-5.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Anderson, Niall A. published the artcileDiscovery of an Orally Bioavailable Pan αv Integrin Inhibitor for Idiopathic Pulmonary Fibrosis, Application of 4-Methoxyphenylacetic acid, the main research area is phenylbutyrate derivative preparation oral integrin inhibitor idiopathic pulmonary fibrosis.

The heterodimeric transmembrane αv integrin receptors have recently emerged as potential targets for the treatment of idiopathic pulmonary fibrosis. Herein, we describe how subtle modifications of the central aromatic ring of a series of phenylbutyrate-based antagonists of the vitronectin receptors αvβ3 and αvβ5 significantly change the biol. activities against αvβ6 and αvβ8. This resulted in the discovery of a pan αv antagonist (compound 39, 4-40 nM for the integrin receptors named above) possessing excellent oral pharmacokinetic properties in rats (with a clearance of 7.6 mL/(min kg) and a bioavailability of 97%).

Journal of Medicinal Chemistry published new progress about Antifibrotic agents. 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

Borowska, Ewa published the artcileDegradation of Iodinated Contrast Media in Aquatic Environment by Means of UV, UV/TiO2 Process, and by Activated Sludge, Synthetic Route of 117-96-4, the main research area is activated sludge UV radiation iodinated contrast media aquatic environment; Iodinated contrast media; Membrane bioreactors; Photolysis; UV/TiO2 process.

Iodinated contrast media (ICM), which are used for radiol. visualization of human tissue and cardiovascular system, are poorly biodegradable; hence, new methods of their removal are sought. In this study, the effectiveness of selected X-ray ICM removal by means of UV and UV/TiO2 pretreatment processes from synthetic hospital wastewater was demonstrated. The following compounds were investigated: iodipamide, iohexol, and diatrizoate. The experiments were as follows: (i) estimated susceptibility of the ICM to decay by UV radiation in different aquatic matrixes, (ii) determined an optimal retention time of hospital wastewater in the UV reactor, (iii) determined optimum TiO2 concentration to improve the effectiveness of the UV pretreatment, and (iv) investigated removal of ICM by combination of the photochem. and biol. treatment methods. The quantum yields of selected ICM decay in deionized water (pH = 7.0) were established as 0.006, 0.004, and 0.029 for iohexol, diatrizoate, and iodipamide, resp. Furthermore, the experiments revealed that diatrizoate and iohexol removal in the UV/TiO2 process is more efficient than in UV process alone. For diatrizoate, the removal efficiency equaled to 40 and 30 %, resp., and for iohexol, the efficiency was 38 and 27 %, resp. No significant increase in iodipamide removal in UV and UV/TiO2 processes was observed (29 and 28 %, resp.). However, highest removal efficiency was demonstrated in synthetic hospital wastewater with the combined photochem. and biol. treatment method. The removal of diatrizoate and iohexol increased to at least 90 %, and for iodipamide, to at least 50 %.

Water, Air, & Soil Pollution published new progress about Aquatic environment. 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

Frost, Anna Buus published the artcileThe Pharmacokinetics of the Weakly Protein-Bound Anionic Compound Diatrizoate in Serum and Synovial Fluid of the Horse, SDS of cas: 117-96-4, the main research area is pharmacokinetics protein anionic diatrizoate blood synovium fluid horse.

Purpose: To establish a pharmacokinetic model for the model drug, sodium diatrizoate (DTZ), allowing joint disappearance kinetics to be estimated from serum appearance kinetics following intra-articular administration, and to calculate the relative joint exposure after i.v. and intra-articular DTZ administration (Fiv/IA). Methods: Each of five horses received an aqueous solution of 3.9 mg/kg sodium diatrizoate both i.v. and intra-articularly separated by a one-week wash out period. Serum and synovial samples were collected over 7 h and analyzed for content of model compound using inductively coupled plasma mass spectrometry. Results: Differential equations were used for describing the transport of DTZ between the joint and the central compartment. The three-compartment lag-time model obtained demonstrates that the rate of drug appearance in the systemic circulation equals the rate of disappearance from the joint compartment. Following i.v. and intra-articular administration, an average Fiv/IA of 0.04% (n = 4) was calculated based on the synovial fluid profiles of DTZ. Conclusions: This study implies that aspects of the intra-articular fate of DTZ can be obtained from serum data in case synovial fluid samplings are limited, for various possible reasons. The low Fiv/IA may stimulate future research in the field of intra-articular administration of anti-osteoarthritic drugs.

Pharmaceutical Research published new progress about Articular cartilage. 117-96-4 belongs to class isoquinoline, name is Diatrizoic Acid, and the molecular formula is C11H9I3N2O4, SDS of cas: 117-96-4.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Shafieyan, Yousef published the artcileDiffusion of MRI and CT Contrast Agents in Articular Cartilage under Static Compression, Name: Diatrizoic Acid, the main research area is diffusion MRI CT contrast agent articular cartilage static compression.

Cartilage has a limited capacity for self-repair and focal damage can eventually lead to complete degradation of the tissue. Early diagnosis of degenerative changes in cartilage is therefore essential. Contrast agent-based computed tomog. and magnetic resonance imaging provide promising tools for this purpose. However, the common assumption in clin. applications that contrast agents reach steady-state distributions within the tissue has been of questionable validity. Characterization of nonequilibrium diffusion of contrast agents rather than their equilibrium distributions may therefore be more effective for image-based cartilage assessment. Transport of contrast agent through the extracellular matrix of cartilage can be affected by tissue compression due to matrix structural and compositional changes including reduced pore size and fluid content. We therefore investigate the effects of static compression on diffusion of three common contrast agents: sodium iodide, sodium diatrizoate, and gadolinium diethylenetriamine-pentaacid (Gd-DTPA). Results showed that static compression was associated with significant decreases in diffusivities for sodium iodide and Gd-DTPA, with similar (but not significant) trends for sodium diatrizoate. Mol. mass of contrast agents affected diffusivities as the smallest one tested, sodium iodide, showed higher diffusivity than sodium diatrizoate and Gd-DTPA. Compression-associated cartilage matrix alterations such as glycosaminoglycan and fluid contents were found to correspond with variations in contrast agent diffusivities. Although decreased diffusivity was significantly correlated with increasing glycosaminoglycan content for sodium iodide and Gd-DTPA only, diffusivity significantly increased for all contrast agents by increasing fluid fraction. Because compounds based on iodine and gadolinium are commonly used for computed tomog. and magnetic resonance imaging, present findings can be valuable for more accurate image-based assessment of variations in cartilage composition associated with focal injuries.

Biophysical Journal published new progress about Articular cartilage. 117-96-4 belongs to class isoquinoline, name is Diatrizoic Acid, and the molecular formula is C11H9I3N2O4, Name: Diatrizoic Acid.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Sun, Yu published the artcileInducing secondary metabolite production of Aspergillus sydowii through microbial co-culture with Bacillus subtilis, Formula: C2H6N2O, the main research area is secondary metabolite Aspergillus sydowii microbial coculture Bacillus subtilis; Aspergillus sydowii; Bacillus subtilis; Co-culture; Natural products.

The co-culture strategy which mimics natural ecol. by constructing an artificial microbial community is a useful tool to activate the biosynthetic gene clusters to generate new metabolites. However, the conventional method to study the co-culture is to isolate and purify compounds separated by HPLC, which is inefficient and time-consuming. Furthermore, the overall changes in the metabolite profile cannot be well characterized. A new approach which integrates computational programs, MS-DIAL, MS-FINDER and web-based tools including GNPS and MetaboAnalyst, was developed to analyze and identify the metabolites of the co-culture of Aspergillus sydowii and Bacillus subtilis. A total of 25 newly biosynthesized metabolites were detected only in co-culture. The structures of the newly synthesized metabolites were elucidated, four of which were identified as novel compounds by the new approach. The accuracy of the new approach was confirmed by purification and NMR data anal. of 7 newly biosynthesized metabolites. The bioassay of newly synthesized metabolites showed that four of the compounds exhibited different degrees of PTP1b inhibitory activity, and compound N2 had the strongest inhibition activity with an IC50 value of 7.967 μM. Co-culture led to global changes of the metabolite profile and is an effective way to induce the biosynthesis of novel natural products. The new approach in this study is one of the effective and relatively accurate methods to characterize the changes of metabolite profiles and to identify novel compounds in co-culture systems.

Microbial Cell Factories published new progress about Aspergillus sydowii. 598-50-5 belongs to class isoquinoline, name is 1-Methylurea, and the molecular formula is C2H6N2O, Formula: C2H6N2O.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Febrianto, N. A. published the artcileCocoa-like flavor compound development of rambutan seed fat as the effect of fermentation and roasting, Name: 5-Methyl-2-phenylhex-2-enal, the main research area is rambutan seed fat fermentation roasting pyrazine ketone alc ester.

Rambutan seed waste has become a noteworthy problem in rambutan canning industry that need to be solved. Previous finding showed that rambutan seed could be utilized by extracting the fat that could be utilized as confectionery fat with improved characteristic by fermentation and roasting treatment. The study to evaluate the cocoa-like flavor compounds development as the effect of these process was carried out. The rambutan seed was fermented for 3, 6, and 9 days followed/unfollowed by roasting process at 150°C for 30 min. The browning index of the powder, the Maillard Reaction Products (MRPs) and the volatile flavor compounds of the rambutan seed fat were analyzed. The study found that the fermentation treatment followed by roasting treatment significantly increase the browning index and melanoidin content in powder and fat, resp. Six and 9 days fermentation followed by roasting possessed highest value of browning index (1.4875 and 1.5485 AU, resp.) and melanoidin content (0.318 and 0.295 AU, resp.). The result also showed that fermentation of rambutan seed followed by roasting process could successfully developed desired pyrazine compounds, in which the contribution of the pyrazine content could be as much as 42.69% of total flavor compound of rambutan seed fat.

International Food Research Journal published new progress about Bacillus megaterium. 21834-92-4 belongs to class isoquinoline, name is 5-Methyl-2-phenylhex-2-enal, and the molecular formula is C13H16O, Name: 5-Methyl-2-phenylhex-2-enal.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Joshi, Robin published the artcileEffect of decaffeination conditions on quality parameters of Kangra orthodox black tea, HPLC of Formula: 21834-92-4, the main research area is temperature pressure black tea decaffeination volatile supercritical carbon dioxide.

Effect of extraction temperature and pressure on the removal of caffeine from Kangra orthodox black tea using supercritical carbon dioxide was investigated. Maximum caffeine as well as volatile flavor components was extracted at 35 °C/170 bar using 60 g/min flow rate for 90 min extraction in dynamic mode. Satisfactory decaffeination and quality retention were achieved at extraction at 60 °C/90 bar. The quality of extracts reduced at higher extraction temperature and pressure combinations. Maximum amounts of theaflavins (88.88%), thearubigins (81.18%) and catechins (73.53%) were retained at these extraction conditions. Volatile components in original (caffeinated) and decaffeinated black teas were isolated by simultaneous distillation extraction (SDE), and analyzed by gas chromatog. (GC) and gas chromatog.-mass spectrometry (GC-MS). 2-Hexenal, 3-hexenol, phenylacetaldehyde, cis-linalool oxide, linalool, trans-geraniol, nerolidol, Me salicylate, α- and β-ionones decreased in decaffeinated black teas compared to untreated control. β-ionone (1.77%), trans-linalool oxide (5.36%), linalool (7.84%), trans-geraniol (4.32%) and Me salicylate (1.90%) were retained in satisfactory amount in decaffeination at 60 °C/90 bar. Application of aroma extract dilution anal. revealed 11 odor active compounds with flavor dilution (FD) factor ranging from 8 to 512 and odor quality investigated by GC-FID, GC-MS. Some unknown compounds quant. reduced or disappeared during decaffeination process. Although there was considerable loss of theaflavins and thearubigins as well as volatile flavor components, SFE extraction at 60 °C/90 bar for 90 min appears as the method suitable for selective removal of caffeine from the Kangra orthodox black tea.

Food Research International published new progress about Black tea beverages. 21834-92-4 belongs to class isoquinoline, name is 5-Methyl-2-phenylhex-2-enal, and the molecular formula is C13H16O, HPLC of Formula: 21834-92-4.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem