Month: December 2022

(2S)-2-Amino-4-(butylsulfonimidoyl)butanoic acid (BD136012) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 4381-25-3 and 1621962-30-8.

A fundamental problem in oncol. is that anticancer chemotherapeutics kill both cancer and healthy cells in the surrounding tissues. Resveratrol is a natural antioxidant with intriguing and opposing biol. properties: it reduces viability of some cancer cells but not of non-transformed ones (in equimolar concentrations). Therefore, we examined resveratrol in human non-transformed primary astrocytes and astrocytoma. Resveratrol reduced reactive oxygen species in astrocytes, but not in astrocytoma. Such cell-type dependent response is particularly evident with analyses at the single cell level showing clear population difference in high and low glutathione levels. Due to resveratrol¡äs poor aqueous solubility that limits its use in clinics, we incorporated it into stimulus-responsive micelles assembled from miktoarm polymers. This could be an attractive chemotherapeutic delivery strategy in nano-oncol. As a proof of principle, we show that these formulations containing resveratrol markedly decrease astrocytoma viability, particularly in combination with temozolomide, a first line chemotherapeutic for astrocytoma.

Human astrocytes and astrocytoma respond differently to resveratrol. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/50578-18-2.html, 145026-07-9

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1. The impurity of diuretic hydrochlorothiazide 04, also be a medical intermediate.
2. It’s mainly used for the detection of drug impurities, the synthesis of hydrochlorothiazide and the screening of medical structural fragments.
3. Presents a weak alkaline,refrigeration.

. Recommended Products is: 5250-72-6 and 22503-72-6.

The following compounds were studied in adult rats: chlorothiazide (K30), 6-chloro-7-sulfamoyl-3,4-dihydro-1,2,4-benzothiadiazine 1,1-dioxide (K32), 6-chloro-7-sulfamoyl-3,4-dihydro-3-trichloromethyl-1,2,4-benzothiadiazine 1,1-dioxide (K33), 6-chloro-7-sulfamoyl-3,4-dihydro-3- methyl-1,2,4-benzothiadiazine 1,1-dioxide (K34), 6-amino-7-sulfamoyl-3,4-dihydro-1,2,4-benzothiadiazine 1,1-dioxide (K35), benzo-1,2,4,9,8,6-dithiadiazine 1,1,9,9-tetroxide (K36), 7-sulfamoyl-3,4-dihydro-1,2,4-benzothiadiazine 1,1-dioxide (K37), 5,6-dichloro-7-sulfamoyl-3,4-dihydro-1,2,4-benzothiadiazine 1,1-dioxide (K38), and 7-sulfamoyl-3-trichloromethyl-3,4-dihydro-1,2,4-benzothiadiazine 1,1-dioxide (K39). K37 and K38 with only a H at C-6 had a weak diuretic action at a dose of 4 mg./kg. A dose of 2 mg. of K30/kg. produced a larger output of Cl than 4 mg./kg. K36 was ineffective over the dose range of 0.54 mg./kg. Cl excretion showed a marked decline with K36. The dihydrochlorothiazide compounds proved to be more potent than K30. With respect to their effect on water diuresis, the order of potency was as follows: K38 > K32 > K34 > K33 > K30; for Cl excretion it was K32 > K34 > K38 > K33 > K30. K38 was most effective for water diuresis while K32 and K34 would be the compounds of choice for increasing the Cl output. The activity of some of these compounds was compared with that of urea. Albuminuria, feebleness, and anorexia were observed in animals given 2-3 g. of K30/kg. All of the test animals survived.

The diuretic action of dihydrochlorothiazide derivatives. Recommended basis is hydrochlorothiazide 20. Products is: https://www.ambeed.com/products/742-20-1.html, 432499-63-3

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

(S-Methylsulfonimidoyl)benzene (BD302898) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 83730-53-4 and 1621962-30-8.

The design and synthesis of a redox-active thianthrenium-containing sulfoximination reagent was reported. Photo-catalyzed acetoxysulfoximination of styrene with various functional groups was described. Preliminary mechanistic studies indicated that the sulfoximination reagent I received a single electron transfer (SET) from the photo-excited Ir(ppy)3 catalyst to produce a sulfoximidoyl radical as a key intermediate in this transformation.

Photo-catalyzed acetoxysulfoximination of styrene with sulfoximidoyl thianthrenium salt. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/50578-18-2.html, 145026-07-9

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

(2S)-2-Amino-4-(butylsulfonimidoyl)butanoic acid (BD136012) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 4381-25-3 and 1621962-30-8.

The integration of diagnostic and therapeutic functions in a nanoplatform has been a rapidly emerging method in the management of cancer. The application of imaging technol. paves the way to track the pharmacokinetics of the nanoplatforms, to guide the treatment, and to monitor the therapeutic processes and outcomes. Herein, we reported a novel type of monodisperses mesoporous silica-coated superparamagnetic iron oxide-based multifunctional nanoplatform (DOX@MMSN-SS-PEI-cit) for the diagnosis and treatment of cancer. The fabrication process included the surface modification of monodisperses mesoporous silica nanoparticle (MMSN) with branched polyethyleneimine (PEI) via disulfide bonds and the further coupling of citraconic anhydride to PEI. Typically, the hydrolysis of amide bonds in the tumor microenvironment (TME) could lead to a neg.-to-pos. charge reversion, which can enhance the endosomal escape of the resulting nanoplatform. The rapid release of doxorubicin hydrochloride (DOX) directly killed the cancer cells. Due to the superparamagnetic iron oxide-based high-resolution T2-weighted MR imaging contrast agents, this novel multifunctional nanoplatform successfully realized MR imaging, targeted drug delivery and controlled release in one system, and achieved significant improvement in tumor diagnosis and therapy. In summary, the therapeutic nanoplatform is a promising option in precise cancer treatment.

A novel intratumoral pH/redox-dual-responsive nanoplatform for cancer MR imaging and therapy. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/50578-18-2.html, 145026-07-9

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1. Trivial name: delta-Cadinene.
2. It’s mainly derived from flue-cured tobacco, burley tobacco and flavoured tobacco, it has a strong aroma and a good fixing effect, suitable for perfume, cosmetics, can also be used in wine, cigarettes, and toothpaste.
. Recommended Products is: 29350-73-0 and 51905-84-1.

The present study aims at comparing the chem. composition of seven varieties of Persea americana leaves essential oils and at evaluating some of its activities such as antibacterial activity, antioxidant activity and acute toxicity. The results showed strong variations in the volatile compounds present in some of the studied oils from these varieties. Estragol was the major component of Ettinger (30.04%) and Fuerte (36.74%) leaf essential oils and is absent from four varieties. Regarding the EO of Hass, Bacon and Maluma Hass, the 2-(8Z,11Z)-8,11-heptadecadienyl-furan was the main volatile compound (67,37%, 43.61% and 59.9% resp.) while Caryophyllene was the main substance in the leaf EO of Reed (36.61%) and Zutano (17.68%) varieties. Concerning the acute toxicity test of these essential oils, the results obtained showed that the LD (LD50) is higher than 2000 mg/kg for EO of Maluma Hass, Reed and Ettinger varieties, whereas it is greater than 300 mg/kg for those of Zutano, Bacon, Hass and Fuerte. The study of antioxidant and antibacterial activities revealed promising values against gram-pos. bacteria (Staphylococcus epidermidis, Staphylococcus aureus) and an encouraging antioxidant power. Based on these results, it appears that avocado leaf essential oils are in fact a potential source of bioactive phytochems. for medical and cosmetic use, and could also be considered as the first report on Persea americana grown in Morocco.

Seven Persea americana varieties essential oils comparison: Chemical composition, toxicity, antibacterial, and antioxidant activities. Recommended basis is Cadinene. Products is: https://www.ambeed.com/products/189165-77-3.html, 51905-84-1

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1. The impurity of diuretic hydrochlorothiazide 04, also be a medical intermediate.
2. It’s mainly used for the detection of drug impurities, the synthesis of hydrochlorothiazide and the screening of medical structural fragments.
3. Presents a weak alkaline,refrigeration.

. Recommended Products is: 5250-72-6 and 22503-72-6.

A new selective, sensitive and Rapid Reverse phase-UPLC method was developed and validated to determine the known potential impurities present in Telmisartan (TL) and Hydrochlorothiazide (HC) in fixed dose combination drug product. The quantification was carried out by using Acquity UPLC, HSS T3 (100 ¡Á 2.1) mm, 1.8¦Ì column, with a flow rate of 0.5mL/min at 225 nm. The mobile phase consists of 0.1% ortho phosphoric acid pH adjusted to 2.6 with diluted sodium hydroxide as Mobile phase A and acetonitrile as Mobile phase B. Separation of the impurities was achieved within 10.0 min of run time. Typical retention times of TL and HC were found to be about 5.4 and 2.0 min resp. The product was subjected to various degradation conditions and validated in terms of linearity, precision, accuracy, LOD, LOQ and robustness in accordance with ICH guidelines. The known impurities quantified in this study were HC imp-1 to 4 for Hydrochlorothiazide and TL imp-1 to 6 for Telmisartan. Recovery was established for all the impurities with resp. to LOQ to 150%. The data supports that the newly developed method is capable to determine all the potential impurities of TL and HC.

Method development and validation for the determination of potential impurities present in telmisartan and hydrochlorothiazide in fixed dose combination drug product by using reverse phase – ultra performance liquid chromatography coupled with diode-array detector. Recommended basis is hydrochlorothiazide 20. Products is: https://www.ambeed.com/products/742-20-1.html, 432499-63-3

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1-Bromo-4-(S-methylsulfonimidoyl)benzene (BD336512) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 4381-25-3 and 83730-53-4.

An efficient kinetic resolution of sulfoximines with enals was realized using chiral N-heterocyclic carbene (NHC) catalysts. The stereoselective amidation proceeds without addnl. acyl transfer agent. Both enantiomers of the sulfoximines can be obtained with excellent ee values (up to 99% ee and -97% ee, resp.). Performing the catalysis on a gram scale allowed using the recovered sulfoximine (+)-MeO2CC6H4SMe(O)(:NH) in an asym. synthesis of FXa inhibitor (+)-F.

Organocatalytic Kinetic Resolution of Sulfoximines. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/1621962-30-8.html, 50578-18-2

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1-Bromo-4-(S-methylsulfonimidoyl)benzene (BD336512) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 4381-25-3 and 83730-53-4.

The synthesis of 1,2-benzothiazine derivatives through rhodium-catalyzed C-H activation/cyclization of S-aryl sulfoximines with iodonium ylides was developed for the first time. In this report, C-H and N-H bond functionalization was realized towards a series of tricyclic and tetracyclic sulfoximine derivatives with moderate to excellent yields under simple reaction conditions.

Rhodium-catalyzed C-H activation/cyclization of aryl sulfoximines with iodonium ylides towards polycyclic 1,2-benzothiazines. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/1621962-30-8.html, 50578-18-2

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

(2S)-2-Amino-4-(butylsulfonimidoyl)butanoic acid (BD136012) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 4381-25-3 and 1621962-30-8.

The recently identified Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) is the cause of the COVID-19 pandemic. How this novel beta-coronavirus virus, and coronaviruses more generally, alter cellular metabolism to support massive production of ?30 kB viral genomes and subgenomic viral RNAs remains largely unknown. To gain insights, transcriptional and metabolomic analyses are performed 8 h after SARS-CoV-2 infection, an early timepoint where the viral lifecycle is completed but prior to overt effects on host cell growth or survival. Here, we show that SARS-CoV-2 remodels host folate and one-carbon metabolism at the post-transcriptional level to support de novo purine synthesis, bypassing viral shutoff of host translation. Intracellular glucose and folate are depleted in SARS-CoV-2-infected cells, and viral replication is exquisitely sensitive to inhibitors of folate and one-carbon metabolism, notably methotrexate. Host metabolism targeted therapy could add to the armamentarium against future coronavirus outbreaks.

SARS-CoV-2 hijacks folate and one-carbon metabolism for viral replication. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/50578-18-2.html, 145026-07-9

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1-Bromo-4-(S-methylsulfonimidoyl)benzene (BD336512) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 4381-25-3 and 83730-53-4.

The asym. synthesis and chem. modification of p-bromophenyl Me sulfoximine is described. Starting from p-bromophenyl menthyl sulfinate, enantiopure 4-bromophenyl Me sulfoximine can be obtained in a short reaction sequence involving a well-established substitution reaction followed by stereospecific imination with O-mesitylenesulfonylhydroxylamine (MSH). Palladium-catalyzed Buchwald/Hartwig, Suzuki, and Stille coupling reactions allow a broad variation of the sulfoximine aryl group, which is otherwise difficult to achieve. The incorporation of a p-morpholino-substituted derivative into a pseudo-tripeptide, e.g., I. demonstrated the applicability of the sulfoximine derivatives

Synthesis and palladium-catalyzed coupling reactions of enantiopure p-bromophenyl methyl sulfoximine. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/1621962-30-8.html, 50578-18-2

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem