Day: December 6, 2022

Xia, Meng published the artcileA Core-Shell Cascade of Chloroperoxidase and Gold Nanoclusters for Asymmetric Hydroxylation of Ethylbenzene, Application In Synthesis of 30931-67-0, the publication is ChemCatChem (2022), 14(4), e202101732, database is CAplus.

Direct functionalization of C-H bonds catalyzed by chloroperoxidase (CPO) is featured by using H₂O₂ as both oxygen and electron donor. The catalytic process circumvents expensive electron transporters such as NAD(P)H, making it advantageous for green production of fine chems. with complex structures. In situ generation and collaborative supplement of H₂O₂ is strongly desired for an improved productivity and enzyme stability. The present study describes a novel CPO cascade for asym. hydroxylation of ethylbenzene yielding (R)-1-phenylethanol, in which H₂O₂ is generated by oxidation of monosaccharides catalyzed by gold nanoclusters (AuNCs). A core-shell structure of CPO-AuNCs cascade was prepared by using hollow mesoporous silica microspheres (HMSMs) as the support. AuNCs were immobilized on the external surface of HMSMs while CPOs were encapsulated inside the microspheres. Different monosaccharides were examined for H₂O₂ production as a function of the particle size. It was found that galactose exhibits the highest productivity. The high compatibility of CPO and AuNCs against temperature and pH is advantageous in catalyzing a wide spectrum of reactions for C-H functionalization.

ChemCatChem published new progress about 30931-67-0. 30931-67-0 belongs to thiazole, auxiliary class Salt,Hydrazine,Amine,Benzothiazole, name is Ammonium 2,2′-(hydrazine-1,2-diylidene)bis(3-ethyl-2,3-dihydrobenzo[d]thiazole-6-sulfonate), and the molecular formula is C7H8O3, Application In Synthesis of 30931-67-0.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Yang, Wu published the artcileDiscovery of 4-Aryl-7-Hydroxyindoline-Based P2Y₁ Antagonists as Novel Antiplatelet Agents, Recommanded Product: 5-Chlorothiazolo[5,4-b]pyridin-2-amine, the publication is Journal of Medicinal Chemistry (2014), 57(14), 6150-6164, database is CAplus and MEDLINE.

ADP (ADP)-mediated platelet aggregation is signaled through two distinct G protein-coupled receptors (GPCR) on the platelet surface: P2Y₁₂ and P2Y₁. Blocking P2Y₁₂ receptor is a clin. well-validated strategy for antithrombotic therapy. P2Y₁ antagonists have been shown to have the potential to provide equivalent antithrombotic efficacy as P2Y₁₂ inhibitors with reduced bleeding in preclin. animal models. Th have previously reported the discovery of a potent and orally bioavailable P2Y₁ antagonist, I. This paper describes further optimization of I by introducing 4-aryl groups at the hydroxylindoline in two series. In the neutral series, II was identified with excellent potency and desirable pharmacokinetic (PK) profile. It also demonstrated similar antithrombotic efficacy with less bleeding compared with the known P2Y₁₂ antagonist prasugrel in rabbit efficacy/bleeding models. In the basic series, III (BMS-884775) was discovered with an improved PK and liability profile over I. These results support P2Y₁ antagonism as a promising new antiplatelet target.

Journal of Medicinal Chemistry published new progress about 31784-71-1. 31784-71-1 belongs to thiazole, auxiliary class Other Aromatic Heterocyclic,Chloride,Amine, name is 5-Chlorothiazolo[5,4-b]pyridin-2-amine, and the molecular formula is C9H10O4, Recommanded Product: 5-Chlorothiazolo[5,4-b]pyridin-2-amine.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Ning, Qiqi published the artcileDevelopment of an enhanced visual signal amplification assay for GSH detection with DNA-cleaving DNAzyme as a trigger, Formula: C18H24N6O6S4, the publication is Sensors and Actuators, B: Chemical (2022), 131932, database is CAplus.

Glutathione (GSH) plays a significant role in human health. Considering that dietary intake of GSH is an important way to keep GSH levels in the body, it is particularly essential to quantitate the supplemental content of GSH. In this study, an enhanced visual signal amplification assay for GSH detection in food with DNA-cleaving DNAzyme as a trigger was developed. The trigger contained a Trigger-enzyme strand (Pb²⁺ dependent DNAzyme sequence) and a Trigger-substrate strand. In the absence of GSH, DNAzyme was formed with Pb²⁺ induction and Trigger-substrate strand was cleaved to release the initiator sequence. Initiator sequence could initiate RCA reaction and generate abundant G-quadruplex sequences. After G-quadruplex/hemin DNAzyme was formed in the presence of G-quadruplex sequences, a visual signal could be produced by catalyzing ABTS. In the presence of GSH, Pb²⁺ would combine with GSH and there would not be following visual signal production Thus, GSH could be detected with a “turn-off” strategy and GSH concentration was neg. correlated with color change. Besides, Nb. BbvCI nicking endonuclease was introduced to improve the visual effect. The results could be qual. identified by the naked eye and quant. analyzed by spectrophotometry (Linearity range: 10 nM to 1 μM, LOD: 3.99 nM) with good selectivity and reliability. We also developed a smartphone-based visual anal. method to make the quant. anal. independent on a spectrophotometer (Linearity range: 10 nM to 0.5 μM, LOD: 8.17 nM). We believe that this assay showed a good potential for rapid and sensitive detection of GSH in food.

Sensors and Actuators, B: Chemical published new progress about 30931-67-0. 30931-67-0 belongs to thiazole, auxiliary class Salt,Hydrazine,Amine,Benzothiazole, name is Ammonium 2,2′-(hydrazine-1,2-diylidene)bis(3-ethyl-2,3-dihydrobenzo[d]thiazole-6-sulfonate), and the molecular formula is C18H24N6O6S4, Formula: C18H24N6O6S4.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Klunk, William E. published the artcileUncharged thioflavin-T derivatives bind to amyloid-beta protein with high affinity and readily enter the brain, Application of 2-(4-Aminophenyl)-6-methylbenzothiazole, the publication is Life Sciences (2001), 69(13), 1471-1484, database is CAplus and MEDLINE.

In vivo assessment of the beta-sheet proteins deposited in amyloid plaques (Aβ peptide) or neurofibrillary tangles (tau protein) presents a target for the development of biol. markers for Alzheimer’s disease (AD). In an effort to develop in vivo beta-sheet imaging probes, derivatives of thioflavin-T (ThT) were synthesized and evaluated. These compounds lack the pos. charged quaternary heterocyclic nitrogen of ThT and are therefore uncharged at physiol. pH. They are 600-fold more lipophilic than ThT. These ThT derivatives bind to Aβ(1-40) fibrils with higher affinity (K_i = 20.2 nM) than ThT (K_i = 890 nM). The uncharged ThT derivatives stained both plaques and neurofibrillary tangles in post-mortem AD brain, showing some preference for plaque staining. A carbon-11 labeled compound, [N-methyl-¹¹C]6-Me-BTA-1, was prepared, and its brain entry and clearance were studied in Swiss-Webster mice. This compound entered the brain at levels comparable to commonly used neuroreceptor imaging agents (0.223% ID-kg/g or 7.61% ID/g at 2 min post-injection) and showed good clearance of free and non-specifically bound radioactivity in normal rodent brain tissue (brain clearance t_1/2 = 20 min). The combination of relatively high affinity for amyloid, specificity for staining plaques and neurofibrillary tangles in post-mortem AD brain, and good brain entry and clearance makes [N-methyl-¹¹C]6-Me-BTA-1 a promising candidate as an in vivo positron emission tomog. (PET) beta-sheet imaging agent.

Life Sciences published new progress about 92-36-4. 92-36-4 belongs to thiazole, auxiliary class Organic Pigment, name is 2-(4-Aminophenyl)-6-methylbenzothiazole, and the molecular formula is C14H12N2S, Application of 2-(4-Aminophenyl)-6-methylbenzothiazole.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Ni, Qijian published the artcileOrganocatalytic asymmetric [4+2] cyclization of 2-benzothiazolimines with azlactones: access to chiral benzothiazolopyrimidine derivatives, Computed Properties of 95-24-9, the publication is Chemical Communications (Cambridge, United Kingdom) (2020), 56(21), 3155-3158, database is CAplus and MEDLINE.

An organocatalytic asym. domino Mannich/cyclization reaction between 2-benzothiazolimines I (R = H, 6-OMe, 5-Br, etc.; R¹ = Ph, 4-MeC₆H₄, 2-thienyl, etc.) with azlactones II (R² = Me, Bn, 4-FC₆H₄CH₂, etc.; R³ = Ph, 4-MeC₆H₄, 1-naphthyl, etc.) has been successfully developed. With the bifunctional squaramide catalyst, this formal [4+2] cyclization occurs with good to high yields and excellent stereoselectivities (up to 99% ee, >20 : 1 dr), providing an efficient and mild access to chiral benzothiazolopyrimidines III (R = H, 6-OMe, 5-Br, etc.; R¹ = Ph, 4-MeC₆H₄, 2-thienyl, etc.; R² = Me, Bn, 4-FC₆H₄CH₂, etc.; R³ = Ph, 4-MeC₆H₄, 1-naphthyl, etc.) bearing adjacent tertiary and quaternary stereogenic centers.

Chemical Communications (Cambridge, United Kingdom) published new progress about 95-24-9. 95-24-9 belongs to thiazole, auxiliary class Organic Pigment, name is 6-Chlorobenzothiazol-2-ylamine, and the molecular formula is C7H5ClN2S, Computed Properties of 95-24-9.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Deng, Qihuan published the artcileExtraction optimization of polysaccharides from Gougunao tea and assessment of the antioxidant and hypoglycemic activities of its fractions in vitro, Application In Synthesis of 30931-67-0, the publication is Bioactive Carbohydrates and Dietary Fibre (2021), 100287, database is CAplus.

The extraction optimization, characterization, antioxidant activities and hypoglycemic in vitro of polysaccharides from Gougunao tea (GTP) were investigated in this study. The extraction conditions were optimized as extraction time of 3.2 h, solid-liquid ratio of 1:30 (g/mL) and extraction temperature of 95 °C, reaching a maximum yield of 10.78 0.21%. Three new fractions (GTP40, GTP60 and GTP80) were separated from GTP by gradient concentrations of ethanol. Their weight-average mol. weight, number-average mol. weight and polydispersity index were determined to be 48286-195451 Da, 33946-118948 Da, 1.422-1.643 by the high-performance gel permeation chromatog. (HPGPC). Chem. anal. revealed that they were all composed of arabinose, galactose, ribose, glucose, rhamnose, manose, xylose, glucuronic acid, and galacturonic acid with different molar ratios, as well as a small amount of proteins. What′s remarkable is that the antioxidant and hypoglycemic activities in vitro of them were all in the order of GTP40>GTP60>GTP80 in a concentration-dependent manner. The half inhibition concentrations (IC₅₀) of GTP40 for 2,2-Diphenyl-1-picrylhydrazyl radical, 2,2â€?Azino-bis (3-ethylbenzothiazoline- 6-sulfonic acid) radical, hydroxyl radical were 0.066 mg/mL, 0.255 mg/mL and 3.610 mg/mL, and for a-amylase and a-glucosidase were 1.271 mg/mL and 0.013 mg/mL, resp. It will provide a theor. basis for the further utilization of polysaccharides from Gougunao tea.

Bioactive Carbohydrates and Dietary Fibre published new progress about 30931-67-0. 30931-67-0 belongs to thiazole, auxiliary class Salt,Hydrazine,Amine,Benzothiazole, name is Ammonium 2,2′-(hydrazine-1,2-diylidene)bis(3-ethyl-2,3-dihydrobenzo[d]thiazole-6-sulfonate), and the molecular formula is C18H24N6O6S4, Application In Synthesis of 30931-67-0.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Qiao, Jennifer X. published the artcile4-Benzothiazole-7-hydroxyindolinyl Diaryl Ureas Are Potent P2Y₁ Antagonists with Favorable Pharmacokinetics: Low Clearance and Small Volume of Distribution, Safety of 5-Chlorothiazolo[5,4-b]pyridin-2-amine, the publication is ChemMedChem (2014), 9(10), 2327-2343, database is CAplus and MEDLINE.

Current antithrombotic discovery efforts target compounds that are highly efficacious in thrombus reduction with less bleeding liability than the standard of care. Preclin. data suggest that P2Y₁ antagonists may have lower bleeding liabilities than P2Y₁₂ antagonists while providing similar antithrombotic efficacy. This article describes the continuous SAR efforts in a series of 7-hydroxyindolinyl diaryl ureas. When dosed orally, 4-trifluoromethyl-7-hydroxy-3,3-dimethylindolinyl analog I was highly efficacious in a model of arterial thrombosis in rats with limited bleeding. The chem. labile CF₃ group in I was then transformed to various groups via a novel one-step synthesis, yielding a series of potent P2Y₁ antagonists. Among them, the 4-benzothiazole-substituted indolines had desirable PK properties in rats, specifically, low clearance and small volume of distribution. In addition, compound II had high i.v. exposure and modest bioavailability, giving it the best overall profile.

ChemMedChem published new progress about 31784-71-1. 31784-71-1 belongs to thiazole, auxiliary class Other Aromatic Heterocyclic,Chloride,Amine, name is 5-Chlorothiazolo[5,4-b]pyridin-2-amine, and the molecular formula is C6H4ClN3S, Safety of 5-Chlorothiazolo[5,4-b]pyridin-2-amine.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Chen, Haiqiang published the artcileA novel antioxidant peptide purified from defatted round scad (Decapterus maruadsi) protein hydrolysate extends lifespan in Caenorhabditis elegans, Computed Properties of 30931-67-0, the publication is Journal of Functional Foods (2020), 103907, database is CAplus.

The residue rich in protein (up to 88.78%) obtained from round scad (Decapterus maruadsi) after oil extraction, was hydrolyzed by Alcalase to produce antioxidative peptides. The hydrolyzate was separated by ultrafiltration, Sephadex G-15 and RP-HPLC, and the active fractions were screened by 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2′-azino-bis (3-ethylbenzothiazoline- 6 sulfonic acid) diammonium salt (ABTS), reducing power and oxygen radical absorbance capacity (ORAC). The obtained peptide with the highest antioxidative activity was then analyzed by HPLC and LC-MS/MS and its anti-aging effect was examined using Caenorhabditis elegans (C. elegans) model. The peptide (Ile-Leu-Gly-Ala-Thr-Ile-Asp-Asn-Ser-Lys, 1153.4 Da), identified by LC-MS/MS showed the highest antioxidant activity. C. elegans fed with the selected peptide had longer lifespan, higher survival rate, superoxide dismutase (SOD) and catalase (CAT) activities than the control group (P<0.05), demonstrating the promising anti-aging effects of the antioxidant peptide from defatted round scad.

Journal of Functional Foods published new progress about 30931-67-0. 30931-67-0 belongs to thiazole, auxiliary class Salt,Hydrazine,Amine,Benzothiazole, name is Ammonium 2,2′-(hydrazine-1,2-diylidene)bis(3-ethyl-2,3-dihydrobenzo[d]thiazole-6-sulfonate), and the molecular formula is C18H24N6O6S4, Computed Properties of 30931-67-0.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Qi, Mei-Ling published the artcileValidated liquid chromatography method for assay of tizanidine in drug substance and formulated products, Quality Control of 30536-19-7, the publication is Analytica Chimica Acta (2003), 478(2), 171-177, database is CAplus.

A new isocratic stability indicating HPLC method for determination of tizanidine in drug substance and formulated products is described. Chromatog. separation of tizanidine from the related substances and degraded products was achieved with a Hypersil CN column (150 mm×5.0 mm, 5 μm) using a mobile phase comprising a mixture of an ion-pairing solution of heptanesulfonic acid sodium salt (HAS), methanol and acetonitrile (50:57:18 (volume/volume)) within 10 min. The flow-rate was 1.0 mL/min and detection was made at 227 nm. The method has good selectivity towards tizanidine, related substances and degraded products. Limits of quantitation for tizanidine and its synthetic intermediates were determined, ranging from 0.051 to 0.54 μg/mL. The linearity range was found to be 2-20 μg/mL (r=0.9998, n=5). Mean recovery for tizanidine from the tablets was from 99.5 to 99.8%. Precision of the method was 1.0% (n=9). The method can be used for routine anal. and the quality control of tizanidine drug substance and its formulated products.

Analytica Chimica Acta published new progress about 30536-19-7. 30536-19-7 belongs to thiazole, auxiliary class Other Aromatic Heterocyclic,Chloride,Amine, name is 5-Chlorobenzo[c][1,2,5]thiadiazol-4-amine, and the molecular formula is C6H4ClN3S, Quality Control of 30536-19-7.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Zhao, Mengxin published the artcileA highly selective and sensitive colorimetric assay for specific recognition element-free detection of uranyl ion, Application In Synthesis of 30931-67-0, the publication is Sensors and Actuators, B: Chemical, database is CAplus.

Current strategies for visual detection of uranyl ion (UO²⁺2) often require DNAzymes and organophosphorus receptors as well as various nanomaterials that may affect the selectivity, sensitivity, and accuracy in a complicated environment. Here, we circumvent these drawbacks by introducing a formic acid (FA)-assisted photolysis of UO²⁺2 initiated chromogenic reaction for specific recognition element-free colorimetric detection of UO²⁺2. The colorless 2, 2â€?azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS) is oxidized by the superoxide anion from the photolysis of UO²⁺2 to generate green ABTS radical, which enables the determination of UO²⁺2 at a concentration of 0.5 μM with the naked eye. The present colorimetric assay is able to determine concentrations of UO²⁺2 from 0.1 to 100 μM, with a limit of detection as low as 0.01 μM. Impressively, the specific recognition element-free colorimetric assay possesses excellent selectivity over common inoganic ions with even 50-fold higher concentration than UO²⁺2. In addition to good sensitivity and selectivity, this colorimetric assay is also capable of determining UO²⁺2 in natural water samples with satisfactory recoveries.

Sensors and Actuators, B: Chemical published new progress about 30931-67-0. 30931-67-0 belongs to thiazole, auxiliary class Salt,Hydrazine,Amine,Benzothiazole, name is Ammonium 2,2′-(hydrazine-1,2-diylidene)bis(3-ethyl-2,3-dihydrobenzo[d]thiazole-6-sulfonate), and the molecular formula is C3H12Cl2N2, Application In Synthesis of 30931-67-0.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica