Category: 622-40-2

Naidu, Priya S. R. published the artcileNovel Hydrophilic Copolymer-Based Nanoparticle Enhances the Therapeutic Efficiency of Doxorubicin in Cultured MCF-7 Cells, Recommanded Product: 2-Morpholinoethanol, the publication is ACS Omega (2019), 4(17), 17083-17089, database is CAplus and MEDLINE.

Nanoparticle drug delivery applications have predominantly focused on the entrapment and delivery of hydrophobic mols. with poor water solubility However, benefits can also be obtained from nanoparticle-based delivery of hydrophilic therapeutics. This study reports on the development of a p(HEMA-ran-GMA)-based nanoparticle synthesized via a spontaneous water-in-oil inverse nanoemulsion to deliver doxorubicin, a water-soluble chemotherapeutic. High drug loading efficiency and sustained release of doxorubicin from Cy5-functionalized p(HEMA-ran-GMA) nanoparticles enabled effective inhibition of the MCF-7 human breast cancer derived cell line. Direct comparative analyses with a hydrophobic PGMA nanoparticle demonstrated enhanced capabilities of the p(HEMA-ran-GMA)-based nanoparticle in vitro. The results suggest that p(HEMA-ran-GMA)-based nanoparticles, which are better suited for hydrophilic drug loading and delivery, may have the potential for the improved therapeutic effect in vivo by enhanced permeation and retention of the nanoparticles by avoidance of off-site side effects of the chemotherapeutic.

ACS Omega published new progress about 622-40-2. 622-40-2 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Alcohol, name is 2-Morpholinoethanol, and the molecular formula is C6H13NO2, Recommanded Product: 2-Morpholinoethanol.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Sakti, Aditya Wibawa published the artcileRigorous pK_a Estimation of Amine Species Using Density-Functional Tight-Binding-Based Metadynamics Simulations, Quality Control of 622-40-2, the publication is Journal of Chemical Theory and Computation (2018), 14(1), 351-356, database is CAplus and MEDLINE.

Predicting pK_a values for different types of amine species with high accuracy and efficiency is of critical importance for the design of high performance and economical solvents in carbon capture and storage with aqueous amine solutions In this study, we demonstrate that d.-functional tight-binding (DFTB) metadynamics simulations are a promising approach to calculate the free energy difference between the protonated and neutral states of amines in aqueous solution with inexpensive computational cost. The calculated pKa values were in satisfactory agreement with the exptl. values, the mean absolute deviation being only 0.08 pK_a units for 34 amines commonly used in CO₂ scrubbing. Such superior reproducibility and correlation compared to estimations by static quantum mech. calculations highlight the significant effect of dynamical proton transfer processes in explicit solvent mols. for the improvement of the estimation accuracy. Note that the accuracy of the estimated pK_a might be dependent on the adopted systems, due to the limitation of the DFTB parameter.

Journal of Chemical Theory and Computation published new progress about 622-40-2. 622-40-2 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Alcohol, name is 2-Morpholinoethanol, and the molecular formula is C6H13NO2, Quality Control of 622-40-2.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Hoang, Van-Hai published the artcileDiscovery of Conformationally Restricted Human Glutaminyl Cyclase Inhibitors as Potent Anti-Alzheimer’s Agents by Structure-Based Design, Recommanded Product: 2-Morpholinoethanol, the publication is Journal of Medicinal Chemistry (2019), 62(17), 8011-8027, database is CAplus and MEDLINE.

Alzheimer’s disease (AD) is an incurable, progressive neurodegenerative disease whose pathogenesis cannot be defined by one single element but consists of various factors; thus, there is a call for alternative approaches to tackle the multifaceted aspects of AD. Among the potential alternative targets, we aim to focus on glutaminyl cyclase (QC), which reduces the toxic pyroform of β-amyloid in the brains of AD patients. On the basis of a putative active conformation of the prototype inhibitor 1, a series of N-substituted thiourea, urea, and α-substituted amide derivatives were developed. The structure-activity relationship analyses indicated that conformationally restrained inhibitors demonstrated much improved QC inhibition in vitro compared to nonrestricted analogs, and several selected compounds demonstrated desirable therapeutic activity in an AD mouse model. The conformational anal. of a representative inhibitor indicated that the inhibitor appeared to maintain the Z-E conformation at the active site, as it is critical for its potent activity.

Journal of Medicinal Chemistry published new progress about 622-40-2. 622-40-2 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Alcohol, name is 2-Morpholinoethanol, and the molecular formula is C6H13NO2, Recommanded Product: 2-Morpholinoethanol.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Aghekyan, A. A. published the artcileSynthesis and Biological Activity of Arylcyclopentane-1-carboxylic Acids Aminoesters, Related Products of alcohols-buliding-blocks, the publication is Russian Journal of General Chemistry (2019), 89(5), 1051-1054, database is CAplus.

1-Arylcyclopentane-1-carboxylic acids were synthesized by alk. hydrolysis of the corresponding nitriles. Reactions of the acid chlorides with N,N-dialkylaminoalkyl-and hetarylalkylalkanols provided new amino ester derivatives of 1-arylcyclopentane-1-carboxylic acids. Sympatholytic and adrenolytic activity of the obtained amino esters hydrochlorides was studied.

Russian Journal of General Chemistry published new progress about 622-40-2. 622-40-2 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Alcohol, name is 2-Morpholinoethanol, and the molecular formula is C6H13NO2, Related Products of alcohols-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Shirai, Fumiyuki published the artcileDesign and Discovery of an Orally Efficacious Spiroindolinone-Based Tankyrase Inhibitor for the Treatment of Colon Cancer, Safety of 2-Morpholinoethanol, the publication is Journal of Medicinal Chemistry (2020), 63(8), 4183-4204, database is CAplus and MEDLINE.

Tankyrases (TNKS/TNKS2) belong to the poly(ADP-ribose) polymerase family. Inhibition of their enzymic activities attenuates the Wnt/β-catenin signaling, which plays an important role in cancer pathogenesis. We previously reported the discovery of RK-287107, a spiroindoline-based, highly selective, potent tankyrase inhibitor. Herein we describe the optimization process of RK-287107 leading to RK-582, which exhibits a markedly improved robust tumor growth inhibition in a COLO-320DM mouse xenograft model when orally administered. In addition to the dose-dependent elevation and attenuation of the levels of biomarkers AXIN2 and β-catenin, resp., results of the TCF reporter and cell proliferation studies on COLO-320DM are discussed.

Journal of Medicinal Chemistry published new progress about 622-40-2. 622-40-2 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Alcohol, name is 2-Morpholinoethanol, and the molecular formula is C6H8O4, Safety of 2-Morpholinoethanol.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Arustamyan, Zh. S. published the artcileSynthesis and Anticonvulsant Activity of Amino Amides and Amino Esters Based on 1-(2,3-Dihydro-1,4-benzodioxin-6-yl)-cyclopentane-1-carboxylic Acid, Name: 2-Morpholinoethanol, the publication is Russian Journal of Organic Chemistry (2019), 55(6), 796-799, database is CAplus.

Alk. hydrolysis of 1-(2,3-dihydro-1,4-benzodioxin-6-yl)cyclopentane-1-carbonitrile gave the corresponding caroxylic acid which was converted to the carbonyl chloride. The latter reacted with N,N-di-alkylalkane-α,ω-diamines H₂N(CH₂)_nNR¹R² [R¹ = R² = Et, Me; R¹R² = -(CH₂)₅-, -(CH₂)₂O(CH₂)₂-; n = 2, 3] and (dialkylamino)alkanols HOCH(R³)CH₂NR⁴R⁵ [R³ = H, Me; R⁴ = R⁵ = Et, Me; R⁴R⁵ = -(CH₂)₄-, -(CH₂)₂O(CH₂)₂-, -(CH₂)₅-] to afford new amino amides I [R = NH(CH₂)_nNR¹R²] and amino esters I [R = OCH(R³)CH₂NR⁴R⁵] which were isolated as hydrochlorides. Anticonvulsant activity of the synthesized compounds was studied.

Russian Journal of Organic Chemistry published new progress about 622-40-2. 622-40-2 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Alcohol, name is 2-Morpholinoethanol, and the molecular formula is C6H13NO2, Name: 2-Morpholinoethanol.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Goncalves, Leticia C. P. published the artcileBoosting photobioredox catalysis by morpholine electron donors under aerobic conditions, Recommanded Product: 2-Morpholinoethanol, the publication is Catalysis Science & Technology (2019), 9(10), 2682-2688, database is CAplus.

Light-driven reduction of flavins, e.g. FAD or FMN, by sacrificial electron donors emerged as a convenient method to promote biocatalytic transformations. However, flavin activation has been restricted to oxygen-free conditions to prevent enzyme deactivation caused by reactive oxygen species (ROS). Herein, we show that the photoreduction of FMN by morpholines, including 3-(N-morpholino)propanesulfonic acid (MOPS), lessens the deactivation of the enoate reductase XenB from Pseudomonas sp. during the stereoselective asym. enzymic reduction of a model α,β-unsaturated diketone under aerobic conditions, leading to a 91% GC-yield and a stereoselectivity greater than 94%. The kinetic stability of the thermolabile XenB was increased by more than 20-fold in MOPS buffer compared to that in Tris-HCl buffer, and a pronounced pos. effect on the transition midpoint temperature was observed The reactive form of the FMN photocatalyst is stabilized by the formation of a ³[FMN^–̇-MOPS⁺̇] ensemble, which reduces the formation of hydrogen peroxide and other ROS in the presence of oxygen. These results contribute to broaden the application of photobiocatalytic transformations using flavin-dependent reductases.

Catalysis Science & Technology published new progress about 622-40-2. 622-40-2 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Alcohol, name is 2-Morpholinoethanol, and the molecular formula is C6H13NO2, Recommanded Product: 2-Morpholinoethanol.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Cooper, Anna G. published the artcileAlkyl indole-based cannabinoid type 2 receptor tools: Exploration of linker and fluorophore attachment, COA of Formula: C6H13NO2, the publication is European Journal of Medicinal Chemistry (2018), 770-789, database is CAplus and MEDLINE.

Cannabinoid type 2 (CB₂) receptor continues to emerge as a promising drug target for many diseases and conditions. New tools for studying CB₂ receptor are required to further inform how this receptor functions in healthy and diseased states. The alkyl indole scaffold is a well-recognized ligand for cannabinoid receptors, and in this study the indole C5-7 positions were explored for linker and fluorophore attachment. A new high affinity, CB₂ receptor selective inverse agonist was identified (16b, 3-(4-methoxybenzoyl)-1-[(oxan-4-yl)methyl]-7-propoxy-1H-indole) along with a general trend of C5-substituted indoles acting as agonists vs. C7-substituted indoles acting as inverse agonists. The indole C7 position was found to be the most tolerant to linker extension and resulted in a high affinity inverse agonist with a medium length linker (19, Me 5-[[3-(4-methoxybenzoyl)-1-[(oxan-4-yl)methyl]-1H-indol-7-yl]oxy]pentanoate). Although a high affinity fluorescent ligand for CB₂ receptor was not identified in this study, the indole C7 position shows great promise for fluorophore or probe attachment.

European Journal of Medicinal Chemistry published new progress about 622-40-2. 622-40-2 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Alcohol, name is 2-Morpholinoethanol, and the molecular formula is C6H13NO2, COA of Formula: C6H13NO2.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Fan, Lingling published the artcileSynthesis and antifungal activity of imidazo[1,2-b]pyridazine derivatives against phytopathogenic fungi, Safety of 2-Morpholinoethanol, the publication is Bioorganic & Medicinal Chemistry Letters (2020), 30(14), 127139, database is CAplus and MEDLINE.

A series of 3,6-disubstituted imidazo[1,2-b]pyridazine derivatives were synthesized and characterized with spectroscopic analyses. The antifungal activities of these compounds against nine phytopathogenic fungi were evaluated by the mycelium growth rate method. The in vitro antifungal bioassays indicated that most of compounds displayed excellent and broad-spectrum antifungal activities. Especially, compounds 6-chloro-3-phenylimidazo[1,2-b]pyridazine, 6-chloro-3-(2-fluorophenyl)imidazo[1,2-b]pyridazine, 6-chloro-3-(2-chlorophenyl)imidazo[1,2-b]pyridazine, 6-chloro-3-(thiophen-3-yl)imidazo[1,2-b]pyridazine and 6-methoxy-3-phenylimidazo[1,2-b]pyridazine exhibited 1.9-25.5 fold more potent than the com. available fungicide hymexazol against Corn Curvalaria Leaf Spot (CL), Alternaria alternate (AA), Pyricularia oryzae (PO) and Alternaria brassicae (AB) strains. Structure-activity relation anal. showed that the enhanced antifungal activity is significantly affected by the substituents on the benzene ring and pyridazine ring.

Bioorganic & Medicinal Chemistry Letters published new progress about 622-40-2. 622-40-2 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Alcohol, name is 2-Morpholinoethanol, and the molecular formula is C6H13NO2, Safety of 2-Morpholinoethanol.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Lin, Jian published the artcileDiscovery and Optimization of Quinolinone Derivatives as Potent, Selective, and Orally Bioavailable Mutant Isocitrate Dehydrogenase 1 (mIDH1) Inhibitors, HPLC of Formula: 622-40-2, the publication is Journal of Medicinal Chemistry (2019), 62(14), 6575-6596, database is CAplus and MEDLINE.

Mutations at the arginine residue (R132) in isocitrate dehydrogenase 1 (IDH1) are frequently identified in various human cancers. Inhibition of mutant IDH1 (mIDH1) with small mols. has been clin. validated as a promising therapeutic treatment for acute myeloid leukemia and multiple solid tumors. Herein, we report the discovery and optimization of a series of quinolinones to provide potent and orally bioavailable mIDH1 inhibitors with selectivity over wild-type IDH1. The X-ray structure of an early lead 24 in complex with mIDH1-R132H shows that the inhibitor unexpectedly binds to an allosteric site. Efforts to improve the in vitro and in vivo absorption, distribution, metabolism, and excretion (ADME) properties of 24 yielded a preclin. candidate 63. The detailed preclin. ADME and pharmacol. studies of 63 support further development of quinolinone-based mIDH1 inhibitors as therapeutic agents in human trials.

Journal of Medicinal Chemistry published new progress about 622-40-2. 622-40-2 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Alcohol, name is 2-Morpholinoethanol, and the molecular formula is C6H13NO2, HPLC of Formula: 622-40-2.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts