Tag: M.W=100-150

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.

Reference:
Thiomorpholine – Wikipedia,
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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

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Thiomorpholine – Wikipedia,
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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

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

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

COA of Formula: C7H8N2O. In 2019 EUR J MED CHEM published article about IN-VITRO; CANCER; QUINOXALINONES; EPIGENETICS; EXPRESSION; PHYSIOLOGY; ROLES in [Cheng, Chunhui; Yun, Fan; He, Jie; Ullah, Sadeeq; Yuan, Qipeng] Beijing Univ Chem Technol, Coll Life Sci & Technol, Minist Educ, Key Lab Biomed Mat Nat Macromol, 15 Beisanhuan East Rd, Beijing 100029, Peoples R China in 2019, Cited 43. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6.

A series of novel 2-aminobenzamide derivatives decorated with thioquinazolinone were designed and synthesized as histone deacetylase (HDAC) inhibitors. These derivatives were evaluated for their anti-proliferative activities against several human cancer cell lines including A375, Hela, A549, HCT116 and SMMC7721. It’s significantly indicated that some inhibitors exhibited potent antiproliferative activities towards all the studied cancer cell lines. Compounds 7a, 4i, 4o, and 4p exhibited higher antiproliferative activities towards three cancer cell lines: A375, A549 and SMMC7721 compared to CS055, MS275, and C1994. Compound 4p showed more than 4000-fold the isoform selectivity for HDACI and more than 250-fold selectivity for HDAC2 compared with HDAC6. The molecular docking analysis reasonably explained the HDAC inhibitory activity and isoform selectivity. In addition, compounds 7a, 4i, 4o, and 4p showed potent inhibitory activities in migration assay and colony formation analysis, and also promoted cell apoptosis. Moreover, compounds 7a, 4i, and 4o inhibited the growth of SMMC7721 cells at S phase of the cell cycle. The immunofluorometric analysis indicated that compounds 7a, 4i, 4o, and 4p could increase the acetylation status of H3K9. Furthermore, in vivo anticancer efficacy of compound 4p was assessed in the A549 xenograft models, and 4p demonstrated potent antitumor activity (TGI = 62.5%). This study provided an effective strategy for further development of tumor-targeting therapy. (C) 2019 Elsevier Masson SAS. All rights reserved.

COA of Formula: C7H8N2O. About 2-Aminobenzamide, If you have any questions, you can contact Cheng, CH; Yun, F; He, J; Ullah, S; Yuan, QP or concate me.

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

An article Sulfur-Promoted Synthesis of 2-Aroylquinazolin-4(3H)-ones by Oxidative Condensation of Anthranilamide and Acetophenones WOS:000475925900008 published article about ONE-POT SYNTHESIS; ELEMENTAL SULFUR; REDOX CONDENSATION; QUINAZOLINE DERIVATIVES; O-AMINOBENZAMIDES; AMINES; KETONES; ACCESS; CYCLIZATION; INHIBITORS in [Thanh Binh Nguyen; Hou, Jing-ya; Retailleau, Pascal] Univ Paris Saclay, Inst Chim Subst Nat, CNRS, UPR 2301,Univ Paris Sud, 1 Ave Terrasse, F-91198 Gif Sur Yvette, France in 2019, Cited 50. Name: 2-Aminobenzamide. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6

A sulfur-promoted three-component reaction of isatoic anhydride, primary aliphatic or aromatic amines, and acetophenones leading to densely substituted 3-substituted 2-aroylquinazolin-4(3H)-ones is reported. The key step involves a cascade reaction of selective oxidation of the methyl group of the acetophenones, followed by a condensation with anthranilamides. The scope of the reaction is applicable to the synthesis of tryptanthrin and various 3-unsubstituted 2-aroylquinazolin-4(3H)-ones.

About 2-Aminobenzamide, If you have any questions, you can contact Nguyen, TB; Hou, JY; Retailleau, P or concate me.. Name: 2-Aminobenzamide

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

In 2020.0 J CHROMATOGR A published article about MASS-SPECTROMETRIC DETECTION; ULTRAVIOLET ABSORBENCY; ELUTION ORDER; MOBILE-PHASE; SFC; CLASSIFICATION; OPTIMIZATION; SEPARATIONS; SOLUBILITY; REVERSAL in [Ovchinnikov, Denis, V; Kosyakov, Dmitry S.; Bogolitsyn, Konstantin G.; Ul’yanovskii, Nikolay, V; Falev, Danil, I] Lomonosov Northern Arctic Fed Univ, Core Facil Ctr Arktika, 17 Severnaya Dvina Embankment, Arkhangelsk 163002, Russia; [Pokrovskiy, Oleg, I] Russian Acad Sci, Kurnakov Inst Gen & Inorgan Chem, 31 Leninskiy Prospekt, Moscow 119991, Russia in 2020.0, Cited 32.0. The Name is 1-Phenylurea. Through research, I have a further understanding and discovery of 64-10-8. HPLC of Formula: C7H8N2O

Four polar stationary phases (ethylene-bridged hybrid silica, cyanopropyl, 2-ethylpyridine, and zwitterionic sulfobetaine) have been characterized in supercritical fluid chromatography (SFC) by linear free energy relationships (LFER) method with an extended set of Abraham’s descriptors. Temperature (25-55 degrees C) and pressure (110-180 bar) effects on analyte retention, separation selectivity and LFER-coefficients of chromatographic systems have been studied using the 89 test compounds of various chemical classes and carbon dioxide – methanol (9:1 v/v) binary solvent as a mobile phase. It was found that for the selected stationary phases temperature and pressure had only moderate effects on selectivity. The retention times of all analytes decrease, as can be expected, if the pressure rises at the isothermal conditions due to the increase of the fluid density and its eluting power. The effect of temperature on retention is complicated and depends both on the chemical class of analyzed compounds and the stationary phase type. Temperature and pressure variations lead to small changes in the LFER-coefficients, and general trends observed do not depend much on the stationary phase type. It may be difficult to interpret the LFER-analysis results because of the evident, more significant chromatographic phenomena. (C) 2019 Elsevier B.V. All rights reserved.

HPLC of Formula: C7H8N2O. About 1-Phenylurea, If you have any questions, you can contact Ovchinnikov, DV; Pokrovskiy, OI; Kosyakov, DS; Bogolitsyn, KG; Ul’yanovskii, NV; Falev, DI or concate me.

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

Application In Synthesis of 2-Aminobenzamide. I found the field of Agriculture; Chemistry; Food Science & Technology very interesting. Saw the article Synthesis, Crystal Structure, and Agricultural Antimicrobial Evaluation of Novel Quinazoline Thioether Derivatives Incorporating the 1,2,4-Triazolo[4,3-a]pyridine Moiety published in 2019, Reprint Addresses Bao, XP (corresponding author), Guizhou Univ, Ctr Res & Dev Fine Chem, State Key Lab Breeding Base Green Pesticide & Agr, Key Lab Green Pesticide & Agr Bioengn,Minist Educ, Guiyang 550025, Guizhou, Peoples R China.. The CAS is 88-68-6. Through research, I have a further understanding and discovery of 2-Aminobenzamide.

A total of 22 quinazoline thioether derivatives incorporating a 1,2,4-triazolo[4,3-a]pyridine moiety were designed, synthesized, and evaluated as antimicrobial agents in agriculture. Among these compounds, the chemical structure of compound 61 was further confirmed via single-crystal X-ray diffraction analysis. The bioassay results revealed that some of the compounds possessed noticeable in vitro antibacterial activities against the tested phytopathogenic bacteria. For example, compounds 6b and 6g had EC50 values as low as 10.0 and 24.7 mu g/mL against Xanthomonas axonopodis pv. citri (Xac), respectively, which were significantly better than that of the commercial agrobactericide bismerthiazol (56.9 mu g/mL). Particularly, compound 6b was also found to be capable of suppressing the pathogenic bacterium Xanthomonas oryzae pv. oryzae (Xoo) approximately 12-fold more potent than control bismerthiazol, in terms of their EC 50 values (7.2 versus 89.8 mu g/mL). Importantly, the most active compound 6b turned out to be one with the highest hydrophilicity and the lowest molecular weight within the series. In vivo bioassays further showed the application prospect of 6b as a promising plant bactericide for controlling Xoo. Additionally, in vitro antifungal activities of these compounds were also evaluated at the concentration of 50 mu g/mL. Overall, the present study demonstrated the potential of 1,2,4-triazolo[4,3-a]pyridine-bearing quinazoline thioether derivatives as efficient agricultural antibacterial agents for crop protection.

About 2-Aminobenzamide, If you have any questions, you can contact Fan, ZJ; Shi, J; Luo, N; Ding, MH; Bao, XP or concate me.. Application In Synthesis of 2-Aminobenzamide

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

Authors Bakibaev, AA; Uhov, A; Malkov, VS; Panshina, SY in WILEY published article about CRYSTAL-STRUCTURE; MODULAR APPROACH; DERIVATIVES; CUCURBITURIL in [Bakibaev, Abdigali A.; Uhov, Artur; Malkov, Victor S.; Panshina, Svetlana Yu.] Natl Res Tomsk State Univ, Dept Chem, Tomsk 634050, Russia; [Panshina, Svetlana Yu.] Natl Res Tomsk Polytech Univ, Dept Chem, Tomsk, Russia in 2020.0, Cited 52.0. Product Details of 64-10-8. The Name is 1-Phenylurea. Through research, I have a further understanding and discovery of 64-10-8

Most of the known methods for the synthesis of heterocyclic compounds have disadvantages, such as a long reaction time and aggressive conditions. We have developed a new, rather simple and efficient method for the synthesis of a number of glycoluryls and hydantoins in water using a etidronic acid (HEDP) as Green catalyst. So, for the first time, the condensation reaction of ureas with 1, 2-dicarbonyl compounds was carried out in the presence of HEDP. Also based on NMR studies, a chemism of these reactions, which is stepwise, is proposed. It has been established that the optimal conditions for the synthesis of glycoluryls and hydantoins using HEDP are: temperature 80 degrees C-90 degrees C, 40-20 minutes, and the ratio of urea and HEDP is 1:1. In all cases, the remaining aqueous filtrate containing HEDP after the reaction can be reused for other cycles synthesis of glycoluril and other compounds, because HEDP is not converted during the reaction.

Product Details of 64-10-8. About 1-Phenylurea, If you have any questions, you can contact Bakibaev, AA; Uhov, A; Malkov, VS; Panshina, SY or concate me.

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