Heterocyclic Building Blocks-Thiomorpholine

Product Details of 64-10-8. In 2020.0 DIABETES CARE published article about TYPE-2 DIABETES-MELLITUS; ADD-ON THERAPY; SGLT2 INHIBITORS; TOLERABILITY; METFORMIN in [Jabbour, Serge A.] Thomas Jefferson Univ, Philadelphia, PA 19107 USA; [Frias, Juan P.] Natl Res Inst, Los Angeles, CA USA; [Ahmed, Azazuddin] Apex Med Res, Chicago, IL USA; [Hardy, Elise] AstraZeneca, Gaithersburg, MD USA; [Choi, Jasmine] Statum Res, Irvine, CA USA; [Sjostrom, C. David] AstraZeneca, Gothenburg, Sweden; [Guja, Cristian] Carol Davila Univ Med & Pharm, Bucharest, Romania in 2020.0, Cited 17.0. The Name is 1-Phenylurea. Through research, I have a further understanding and discovery of 64-10-8.

OBJECTIVE In patients with type 2 diabetes uncontrolled with metformin, exenatide once weekly (QW) plus dapagliflozin produced greater reductions in glycemic parameters (glycated hemoglobin [HbA(1c)], fasting plasma glucose [FPG], and 2-h postprandial glucose [2-h PPG]), weight, and systolic blood pressure (SBP) than exenatide QW or dapagliflozin alone after 28 weeks of treatment in DURATION-8. Following a 24-week extension period, improvements were sustained at 52 weeks. In this study, we investigated efficacy and safety at 104 weeks after randomization. RESEARCH DESIGN AND METHODS DURATION-8 was a 104-week, multicenter, double-blind, randomized, active-controlled, phase 3 trial. In total, 695 adults (aged >= 18 years) with type 2 diabetes and inadequate glycemic control (HbA(1c)8.0-12.0% [64-108 mmol/mol]) despite stable metformin monotherapy (>= 1,500 mg/day) were randomly assigned (1:1:1) to receive exenatide 2 mg QW plus once-daily dapagliflozin 10 mg, exenatide QW plus placebo, or dapagliflozin plus placebo. All 104-week evaluations were exploratory. RESULTS At week 104, 431 (62.0%) patients completed treatment. The adjusted least squares mean change (SE) from baseline to week 104 in HbA(1c)was greater with exenatide QW plus dapagliflozin (-1.70% [0.11]) versus exenatide QW plus placebo (-1.29% [0.12];P= 0.007) and dapagliflozin plus placebo (-1.06% [0.12];P< 0.001). Clinically relevant changes in FPG, 2-h PPG, weight, and SBP were also observed with exenatide QW plus dapagliflozin. There were no unexpected safety findings, and exenatide QW plus dapagliflozin was well tolerated, with no episodes of major hypoglycemia. CONCLUSIONS In this exploratory analysis, among those individuals who completed the trial without rescue therapy, there was clinically relevant efficacy over 2 years with exenatide QW plus dapagliflozin, with no unexpected safety findings. Product Details of 64-10-8. About 1-Phenylurea, If you have any questions, you can contact Jabbour, SA; Frias, JP; Ahmed, A; Hardy, E; Choi, J; Sjostrom, CD; Guja, C or concate me.

Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

An article Triplet Excitons Quenching By Doublet Centers in a Nanoreactor with an External Magnetic Field WOS:000647943800009 published article about ELECTRON-SPIN POLARIZATION; PAIRS; MAGNETOCONDUCTANCE; RECOMBINATION; ANNIHILATION; RESONANCE; STATES in [Kucherenko, M. G.; Penkov, S. A.] Orenburg State Univ, Orenburg 460018, Russia in 2021.0, Cited 41.0. The Name is Benzophenone. Through research, I have a further understanding and discovery of 119-61-9. Name: Benzophenone

The process of spin-selective quenching of a triplet (T) exciton by a fixed spin doublet (D) center in an organic semiconductor nanoparticle (anthracene, tetracene, MEH-PPV) was studied. Random walks of the T-exciton in a spherical nanovolume of a crystal or polymer globule were modeled based on the solution of the Neumann boundary diffusion condition. Time dependences of the spin-nonselective quenching rate of T-excitations were calculated for different values of geometric and diffusion parameters. Taking into account the spin dynamics of T-D-pair reagents allowed calculating magnetic field effects of T-D-quenching rate, which showed a strong influence of the nanoparticles size and initial position of the T-exciton and doublet sink on the absolute value of the effect. The obtained radial dependences of the magnetic field modulation of the quenching efficiency can be approximated by a superposition of two exponents.

Name: Benzophenone. About Benzophenone, If you have any questions, you can contact Kucherenko, MG; Penkov, SA or concate me.

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Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

An article Phosphomolybdic Acid (PMA)-catalyzed One-pot Synthesis of 2,3-Dihydroquinazolines WOS:000474370100005 published article about SOLVENT-FREE; CATALYST; EFFICIENT; 2,3-DIHYDRO-4(1H)-QUINAZOLINONES; QUINAZOLINONES; FACILE in [Chen, Chuanhuan; Xuejiao, A.; Li, Xia; Huang, Guoli; Liu, Bo] Yunnan Normal Univ, Sch Chem & Chem Engn, Kunming 650500, Yunnan, Peoples R China in 2019, Cited 34. Computed Properties of C7H8N2O. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6

We have developed a new method for the synthesis of 2,3-dihydroquinazolin-4(1H)-ones in good to excellent yields via phosphomolybdic acid (PMA)-catalyzed cyclocondensation of 2-aminobenzamides with aldehydes or ketones in N,N-dimethylformamide (DMF) at room temperature. The present method proves to be efficient in terms of short reaction time, high yield, simple workup and easy purification.

Computed Properties of C7H8N2O. About 2-Aminobenzamide, If you have any questions, you can contact Chen, CH; Xuejiao, A; Li, X; Huang, GL; Liu, B or concate me.

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Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

Authors Liao, JN; Dong, JP; Xu, JQ; Wang, W; Wu, YJ; Hou, YX; Guo, HC in AMER CHEMICAL SOC published article about in [Liao, Jianning; Dong, Jipan; Xu, Jiaqing; Hou, Yuxia; Guo, Hongchao] China Agr Univ, Dept Chem, Beijing 100193, Peoples R China; [Wang, Wei; Wu, Yongjun] Zhengzhou Univ, Coll Publ Hlth, Zhengzhou 450001, Peoples R China in 2021.0, Cited 59.0. Recommanded Product: 3-Nitrobenzaldehyde. The Name is 3-Nitrobenzaldehyde. Through research, I have a further understanding and discovery of 99-61-6

A phosphine-catalyzed [3 + 2] annulation of Morita-Baylis-Hillman (MBH) carbonates with 3-methyl-4-nitro-5-styrylisoxazoles has been developed to afford various multifunctional isoxazoles in moderate to good yields with moderate to excellent diastereoselectivities. With a spirocyclic chiral phosphine as the catalyst, up to 89% ee was obtained.

Recommanded Product: 3-Nitrobenzaldehyde. About 3-Nitrobenzaldehyde, If you have any questions, you can contact Liao, JN; Dong, JP; Xu, JQ; Wang, W; Wu, YJ; Hou, YX; Guo, HC or concate me.

Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

Authors Dato, FM; Neudorfl, JM; Gutschow, M; Goldfuss, B; Pietsch, M in ACADEMIC PRESS INC ELSEVIER SCIENCE published article about ACID-AMIDE HYDROLASE; MONOGLYCERIDE LIPASE; ENDOCANNABINOID SYSTEM; ACCURATE DOCKING; MAGL; DERIVATIVES; ANALOGS; GLIDE; IDENTIFICATION; PREDICTION in [Dato, Florian M.; Pietsch, Markus] Univ Cologne, Med Fac, Ctr Pharmacol, Inst Pharmacol 2, Gleueler Str 24, D-50931 Cologne, Germany; [Dato, Florian M.; Neudoerfl, Jorg-Martin; Goldfuss, Bernd] Univ Cologne, Inst Organ Chem, Dept Chem, Greinstr 4, D-50939 Cologne, Germany; [Guetschow, Michael] Univ Bonn, Pharmaceut Inst, Pharmaceut Chem 1, Immenburg 4, D-53121 Bonn, Germany in 2020, Cited 60. Name: 2-Aminobenzamide. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6

The serine hydrolase monoacylglycerol lipase (MAGL) is involved in a plethora of pathological conditions, in particular pain and inflammation, various types of cancer, metabolic, neurological and cardiovascular disorders, and is therefore a promising target for drug development. Although a large number of irreversible-acting MAGL inhibitors have been discovered over the past years, there are only few compounds known so far which inhibit the enzyme in a reversible manner. Therefore, much effort is put into the development of novel chemical entities showing reversible inhibitory behavior, which is thought to cause less undesired side effects. To explore a wide range of chemical structures as MAGL binders, we have applied a virtual screening approach by docking small molecules into the crystal structure of human MAGL (hMAGL) and envisaged a library of 45 selected compounds which were then synthesized. Biochemical investigations included the determination of the inhibitory potency on hMAGL and two related hydrolases, i.e. human fatty acid amide hydrolase (hFAAH) and murine cholesterol esterase (mCEase). The most promising candidates from theses analyses, i.e. three w-quinazolinonylalkyl aryl ureas bearing alkyl spacers of three to five methylene groups, exhibited IC50 values of 20-41 mu M and reversible, detergent-insensitive behavior towards hMAGL. Among these compounds, the inhibitor 1-(3,5-bis(tri-fluoromethyl)phenyl)-3-(4-(4-oxo-3,4 dihydroquinazolin-2-yl)butyl)urea (96) was selected for further kinetic characterization, yielding a dissociation constant K-i = 15.4 mu M and a mixed-type inhibition with a pronounced competitive component (alpha = 8.94). This mode of inhibition was further supported by a docking experiment, which suggested that the inhibitor occupies the substrate binding pocket of hMAGL.

About 2-Aminobenzamide, If you have any questions, you can contact Dato, FM; Neudorfl, JM; Gutschow, M; Goldfuss, B; Pietsch, M or concate me.. Name: 2-Aminobenzamide

Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

Velardo, A; Landi, A; Borrelli, R; Peluso, A in [Velardo, Amalia; Landi, Alessandro; Peluso, Andrea] Univ Salerno, Dipartimento Chim & Biol Adolfo Zambelli, I-84084 Fisciano, SA, Italy; [Borrelli, Raffaele] Univ Torino, Dept Agr Forestry & Food Sci, I-10195 Grugliasco, Italy; [Velardo, Amalia] Univ Torino, Dept Chem, I-10125 Turin, Italy published Reliable Predictions of Benzophenone Singlet-Triplet Transition Rates: A Second-Order Cumulant Approach in 2021.0, Cited 64.0. Category: thiomorpholine. The Name is Benzophenone. Through research, I have a further understanding and discovery of 119-61-9.

Fermi golden rule and second-order cumulant expansion of the time-dependent density matrix have been used to compute from first principles the rate of intersystem crossing in benzophenone, using minimum-energy geometries and normal modes of vibrations computed at the TDDFT/CAM-B3LYP level. Both approaches yield reliable values of the S-1 decay rate, the latter being almost in quantitative agreement with the results of time-dependent spectroscopic measurements (0.154 ps(-1) observed vs 0.25 ps(-1) predicted). The Fermi golden rule slightly overestimates the decay rate of S-1 state (k(d) = 0.45 ps(-1)) but provides better insights into the chemico-physical parameters, which govern the transition from a thermally equilibrated population of S-1, showing that the indirect mechanism is much faster than the direct one because of the vanishingly small Franck-Condon weighted density of states at Delta E of transition.

Category: thiomorpholine. About Benzophenone, If you have any questions, you can contact Velardo, A; Landi, A; Borrelli, R; Peluso, A or concate me.

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Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

An article Evaluation of a series of phenyl-type stationary phases in supercritical fluid chromatography with the linear solvation energy relationship model and its application to the separation of phenolic compounds WOS:000518869100030 published article about LIQUID-CHROMATOGRAPHY; CLASSIFICATION; PURIFICATION; SELECTIVITY; RETENTION; SYSTEM; SFC in [Jiang, Dasen; Ke, Yanxiong; Cai, Jianfeng; Zhang, Huanhuan; Fu, Qing; Jin, Yu; Liang, Xinmiao] East China Univ Sci & Technol, Engn Res Ctr Pharmaceut Proc Chem, Sch Pharm, Minist Educ, Shanghai 200237, Peoples R China; [Liang, Xinmiao] Chinese Acad Sci, Dalian Inst Chem Phys, Key Lab Separat Sci Analyt Chem, Key Lab Nat Med, Dalian 116023, Liaoning, Peoples R China in 2020.0, Cited 29.0. Application In Synthesis of 1-Phenylurea. The Name is 1-Phenylurea. Through research, I have a further understanding and discovery of 64-10-8

In recent years, supercritical fluid chromatography (SFC) has become a powerful tool in modern analytical chemistry, and the diversity of stationary phases in SFC promotes phenyl-type phases to confront with a significant resurgence of interest. In this paper, a series of phenyl-type stationary phases with different substituted benzenes involving N-propylbenzamide (PB), 4-fluoro-N-propylbenzamide (PB-F), and 4-ethyl-N-propylbenzamide (PB-ET) were synthesized. Retention mechanism of these phases in SFC was investigated using a linear solvation energy relationship (LSER) model. The phenyl-type stationary phases with all positive parameters can provide all types of interaction, typically involving hydrogen bonding, dipole-dipole and dispersive interactions. The different benzene’s substituents of the stationary phases mainly affected their hydrogen bonding and dipole-dipole interactions, which could be reflected by the angle between the solvation vectors to some extent. The k-k plot showed that the selectivity difference of phenyl-type stationary phases was closely related to the type of solute. Thus, based on twenty-five natural phenolic compounds, two systems with high orthogonality (63.49%) were constructed using three columns, namely phenyl column (PHE) x PB-F and PB x PB-F. Finally, after investigating the influence of chromatographic conditions, ten flavonoids could be separated by using PB, PB-F and PHE columns in SFC. (C) 2019 Published by Elsevier B.V.

About 1-Phenylurea, If you have any questions, you can contact Jiang, DS; Ke, YX; Cai, JF; Zhang, HH; Fu, Q; Jin, Y; Liang, XM or concate me.. Application In Synthesis of 1-Phenylurea

Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

An article Dual Kit/Aur Inhibitors as Chemosensitizing Agents for the Treatment of Melanoma: Design, Synthesis, Docking Studies and Functional Investigation WOS:000474505900054 published article about AURORA KINASE; MEK INHIBITION; DRUG DESIGN; MECHANISMS; RESISTANCE; BRAF; KIT; IDENTIFICATION; VEMURAFENIB; SIMULATION in [Quattrini, Luca; Coviello, Vito; Sartini, Stefania; La Motta, Concettina] Univ Pisa, Dipartimento Farm, Via Bonanno 6, I-56126 Pisa, Italy; [Di Desidero, Teresa; Orlandi, Paola; Bocci, Guido] Univ Pisa, Dipartimento Med Clin & Sperimentale, Via Roma 55, I-56126 Pisa, Italy; [Ke, Yi-Yu; Liu, Kai-Lun; Hsieh, Hsing-Pang] Natl Hlth Res Inst, Inst Biotechnol & Pharmaceut Res, 35 Keyan Rd, Zhunan Town 350, Miaoli County, Taiwan in 2019.0, Cited 46.0. Product Details of 64-10-8. The Name is 1-Phenylurea. Through research, I have a further understanding and discovery of 64-10-8

Melanoma is the most serious form of skin cancer but its medication is still far from being safe and thoroughly effective. The search of novel therapeutic approaches represents therefore a health emergency to push through eagerly. In this study, we describe a novel class of dual c-Kit/Aur inhibitors, characterized by a 1,2,4-triazole core and developed by a structure-based optimization of a previously developed hit, and report the evidence of their significance as drug candidates for the treatment of melanoma. Compound 6a, merging the best inhibitory profile against the target kinases, showed anti-proliferative efficacy against the human melanoma cell lines A2058, expressing the BRAFV600D mutation, and WM266-4, expressing BRAF V600E. Significantly, it displayed also a highly synergistic profile when tested in combination with vemurafenib, thus proving its efficacy not only per se but even in a combination therapy, which is nowadays acknowledged as the cornerstone approach of the forthcoming tumour management.

Product Details of 64-10-8. About 1-Phenylurea, If you have any questions, you can contact Quattrini, L; Coviello, V; Sartini, S; Di Desidero, T; Orlandi, P; Ke, YY; Liu, KL; Hsieh, HP; Bocci, G; La Motta, C or concate me.

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Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

An article Palladium Catalyzed Cross-Dehydrogenative Coupling/Annulation Reaction: A Practical and Efficient Approach to Hydroxyisoindolo[1,2-b]quinazolinone WOS:000471298500007 published article about C-H; NATURAL-PRODUCTS; ACYLATION; QUINAZOLINONES; ALDEHYDES; QUINAZOLIN-4(3H)-ONES; ANILIDES; BONDS in [Dabiri, Minoo; Lehi, Noushin Farajinia; Movahed, Siyavash Kazemi; Khavasi, Hamid Reza] Shahid Beheshti Univ, Fac Chem & Petr Sci, Dist 1,Daneshjou Blvd, Tehran 1983969411, Tehran Province, Iran in 2019, Cited 38. Safety of 2-Aminobenzamide. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6

The palladium-catalyzed cross-dehydrogenative coupling (CDC) followed by an intramolecular cyclization between arylquinazolinones and aldehydes has been described. This viable transformation provides a variety of novel substituted hydroxyisoindolo[1,2-b]quinazolinone compounds in moderate to good yields. Additionally, the reaction is performed with toluene in place of benzaldehyde by using an excess amount of tert-butyl hydroperoxide (TBHP) as the oxidant in good yield.

Safety of 2-Aminobenzamide. About 2-Aminobenzamide, If you have any questions, you can contact Dabiri, M; Lehi, NF; Movahed, SK; Khavasi, HR or concate me.

Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

An article Anthranilamide-based Short Peptides Self-Assembled Hydrogels as Antibacterial Agents WOS:000512142100008 published article about NANOFIBERS; ARCHITECTURE; TRANSITION; NANOTUBES; GELATORS; NETWORKS; DESIGN; WATER in [Aldilla, Vina R.; Chen, Renxun; Black, David StC; Thordarson, Pall; Kumar, Naresh] Sch Chem, UNSW Sydney NSW, Sydney, NSW 2052, Australia; [Martin, Adam D.] Macquarie Univ, Fac Med & Hlth Sci, Dementia Res Ctr, Sydney, NSW 2109, Australia; [Marjo, Christopher E.; Rich, Anne M.] UNSW Sydney, Mark Wainwright Analyt Ctr, Sydney, NSW 2052, Australia in 2020, Cited 79. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6. Name: 2-Aminobenzamide

In this study, we describe the synthesis and molecular properties of anthranilamide-based short peptides which were synthesised via ring opening of isatoic anhydride in excellent yields. These short peptides were incorporated as low molecular weight gelators (LMWG), bola amphiphile, and C-3-symmetric molecules to form hydrogels in low concentrations (0.07-0.30% (w/v)). The critical gel concentration (CGC), viscoelastic properties, secondary structure, and fibre morphology of these short peptides were influenced by the aromaticity of the capping group or by the presence of electronegative substituent (namely fluoro) and hydrophobic substituent (such as methyl) in the short peptides. In addition, the hydrogels showed antibacterial activity against S. aureus 38 and moderate toxicity against HEK cells in vitro.

About 2-Aminobenzamide, If you have any questions, you can contact Aldilla, VR; Chen, RX; Martin, AD; Marjo, CE; Rich, AM; Black, DS; Thordarson, P; Kumar, N or concate me.. Name: 2-Aminobenzamide

Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem