Category: amides-buliding-blocks

Chen, Hui; Li, Peng; Qin, Rongfei; Yan, Hong; Li, Gang; Huang, Haihong published the artcile< DMAP-Catalyzed One-Pot Synthesis of Quinazoline-2,4-diones from 2-Aminobenzamides and Di-tert-butyl Dicarbonate>, Category: amides-buliding-blocks, the main research area is quinazolinedione preparation; aminobenzamide di tert butyl dicarbonate heterocyclization DMAP catalyst.

The one-pot synthesis of quinazoline-2,4-diones was developed in the presence of 4-dimethylaminopyridine (DMAP) by metal-free catalysis. The com. available (Boc)2O acted as a key precursor in the construction of the 2-position carbonyl of quinazolinediones. The p-methoxybenzyl (PMB)-activated heterocyclization could smoothly proceed at room temperature instead of the microwave condition. This strategy is compatible with a variety of substrates with different functional groups. Furthermore, this protocol was utilized to smoothly prepare Zenarestat with a total yield of 70%.

ACS Omega published new progress about Benzamides Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation) (amino). 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, Category: amides-buliding-blocks.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Mannucci, Edoardo; Monami, Matteo; Candido, Riccardo; Pintaudi, Basilio; Targher, Giovanni published the artcile< Effect of insulin secretagogues A meta-analysis of randomized controlled trials>, Application In Synthesis of 94-20-2, the main research area is meta analysis cardiovascular disease mortality insulin secretagogues; Insulin secretagogues; Major cardiovascular events; Metanalysis; Mortality; Type 2 diabetes.

Meta-anal. of insulin secretagogues (sulfonylureas and glinides) on major cardiovascular events and all-cause mortality. A MEDLINE database search was performed to identify all RCTs, up to Jan. 1st, 2020, with duration≥52 wk, in which insulin secretagogues (glibenclamide, gliclazide, glimepiride, glipizide, chlorpropamide, repaglinide, nateglinide) were compared with either placebo or active comparators. The principal endpoints were MACE (restricted for RCT reporting MACEs within their outcomes) and all-cause mortality (irresp. of the inclusion of MACEs among the pre-specified outcomes). Mantel-Haenszel odds ratio (MH-OR) with 95% Confidence Interval (95% CI) was calculated for all the endpoints considered. Fourteen RCTs were included in the anal. for MACEs (919 in insulin secretagogues and 1,087 in control group). Insulin secretagogues were not significantly associated with an increased risk of MACEs in comparison with controls (MH-OR 1.08 [95% CI 0.96, 1.22], p = 0.20). When considering the 48 RCTs fulfilling criteria for inclusion in the anal. on all-cause mortality, insulin secretagogues were associated with a significantly increased risk of all-cause mortality (MH-OR 1.11 [1.00, 1.23], p = 0.04).This meta-anal. suggests that insulin secretagogues are associated with an increased risk of all-cause mortality when compared with placebo or other anti-hyperglycemic drugs.

Nutrition, Metabolism & Cardiovascular Diseases published new progress about Cardiovascular disease. 94-20-2 belongs to class amides-buliding-blocks, and the molecular formula is C10H13ClN2O3S, Application In Synthesis of 94-20-2.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Park, Yea-Jin; Seo, Dong-Wook; Ju, Jae-Yun; Cha, Yun-Yeop; An, Hyo-Jin published the artcile< The antiobesity effects of Buginawa in 3T3-L1 preadipocytes and in a mouse model of high-fat diet-induced obesity>, Electric Literature of 96829-58-2, the main research area is high fat diet obesity antiobesity bugi preadipocytes.

There has been a remarkable interest in finding lipid inhibitors from natural products to replace synthetic compounds, and a variety of oriental medicinal herbs are reported to have biol. activity with regard to lipid inhibition. Buginawa (Bugi) is a novel combined formula that contains twelve medicinal herbs with potential for weight loss induction. We hypothesized that Bugi may have antiobesity effects in 3T3-L1 preadipocytes and in a high-fat diet- (HFD-) induced mouse model. In this study, 3T3-L1 cells were treated with varied concentrations of Bugi (62.5, 125, or 250μg/mL). Bugi treatment inhibited adipocyte differentiation by suppressing adipogenic transcription genes, including peroxisome proliferator-activated receptor γ protein (PPARγ), CCAAT/enhancer-binding protein α (C/EBPα), sterol regulatory element-binding protein 1 (SREBP1), and CCAAT/enhancer-binding protein β (C/EBPβ).Mice were fed a normal diet or an HFD for 11 wk, and Bugi was simultaneously administered at 50 or 100mg/kg. Bugi administration significantly reduced body weight gain and white adipose tissue (WAT) weight and effectively inhibited lipid droplet accumulation in epididymal white adipose tissue (eWAT) and liver tissue. Further, Bugi treatment suppressed mRNA levels of PPARγ, C/EBPα, and SREBP1 in eWAT and liver tissue. Our findings demonstrate that Bugi could be an effective candidate for preventing obesity and relatedmetabolic disorders.

BioMed Research International published new progress about Adipocyte. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Electric Literature of 96829-58-2.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Iyer, Malliga R.; Bhattacharjee, Pinaki; Kundu, Biswajit; Rutland, Nicholas; Wood, Casey M. published the artcile< One-Pot Synthesis of Thio-Augmented Sulfonylureas via a Modified Bunte's Reaction>, Category: amides-buliding-blocks, the main research area is thio sulfonylurea preparation; sulfonylurea one pot Bunte reaction.

Authors report the development of a one-pot Bunte’s reaction-enabled expeditious platform under aqueous conditions for the scalable conversion of sulfonylureas to synthetically versatile thio-sulfonylureas. The reaction was further propagated in the same pot to yield diverse chiral and achiral isothiosulfonyl analogs. The protocol enabled the synthesis of various drug-like mols. and was applied to an enantiomeric synthesis of a cannabinoid receptor antagonist SLV326.

ACS Omega published new progress about One-pot synthesis. 94-20-2 belongs to class amides-buliding-blocks, and the molecular formula is C10H13ClN2O3S, Category: amides-buliding-blocks.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Toigawa, Tomohiro; Peterman, Dean R.; Meeker, David S.; Grimes, Travis S.; Zalupski, Peter R.; Mezyk, Stephen P.; Cook, Andrew R.; Yamashita, Shinichi; Kumagai, Yuta; Matsumura, Tatsuro; Horne, Gregory P. published the artcile< Radiation-induced effects on the extraction properties of hexa-n-octylnitrilo-triacetamide (HONTA) complexes of americium and europium>, Category: amides-buliding-blocks, the main research area is radiation induced extraction hexa octylnitrilo triacetamide complex americium europium.

The candidate An(III)/Ln(III) separation ligand hexa-n-octylnitrilo-triacetamide (HONTA) was irradiated under envisioned SELECT (Solvent Extraction from Liquid waste using Extractants of CHON-type for Transmutation) process conditions (n-dodecane/0.1 M HNO3) using a solvent test loop in conjunction with cobalt-60 gamma irradiation The extent of HONTA radiolysis and complementary degradation product formation was quantified by HPLC-ESI-MS/MS. Further, the impact of HONTA radiolysis on process performance was evaluated by measuring the change in 243Am and 154Eu distribution ratios as a function of absorbed gamma dose. HONTA was found to decay exponentially with increasing dose, affording a dose coefficient of d = (4.48 ± 0.19) x 10-3 kGy-1. Multiple degradation products were detected by HPLC-ESI-MS/MS with dioctylamine being the dominant quantifiable species. Both 243Am and 154Eu distribution ratios exhibited an induction period of ~70 kGy for extraction (0.1 M HNO3) and back-extraction (4.0 M HNO3) conditions, after which both values decreased with absorbed dose. The decrease in distribution ratios was attributed to a combination of the destruction of HONTA and ingrowth of dioctylamine, which is capable of interfering in metal ion complexation. The loss of HONTA with absorbed gamma dose was predominantly attributed to its reaction with the n-dodecane radical cation (R ̇+). These R ̇+ reaction kinetics were measured for HONTA and its 241Am and 154Eu complexes using picosecond pulsed electron radiolysis techniques. All three second-order rate coefficients (k) were essentially diffusion limited in n-dodecane indicating a significant reaction pathway: k(HONTA + R ̇+) = (7.6 ± 0.8) x 109 M-1 s-1, k(Am(HONTA)2 + R ̇+) = (7.1 ± 0.7) x 1010 M-1 s-1, and k(Eu(HONTA)2 + R ̇+) = (9.5 ± 0.5) x 1010 M-1 s-1. HONTA-metal ion complexation afforded an order-of-magnitude increase in rate coefficient Nanosecond time-resolved measurements showed that both direct and indirect HONTA radiolysis yielded the short-lived (<100 ns) HONTA radical cation and a second long-lived (μs) species identified as the HONTA triplet excited state. The latter was confirmed by a series of oxygen quenching picosecond pulsed electron measurements, affording a quenching rate coefficient of k(3[HONTA]* + O2) = 2.2 x 108 M-1 s-1. Overall, both the HONTA radical cation and triplet excited state are important precursors to the suite of measured HONTA degradation products. Physical Chemistry Chemical Physics published new progress about Complexation (metal complexation). 6280-57-5 belongs to class amides-buliding-blocks, and the molecular formula is C17H35NO, Category: amides-buliding-blocks.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Guo, Zhijun; Zhang, Weiguang; Niu, Yanning; Tan, Minyu published the artcile< Solvent extraction and separation of thorium(IV) and uranium(VI) by an ether-amide type tripodand>, Synthetic Route of 5326-82-9, the main research area is solvent thorium uranium ether amide tripodand picrate fuel reprocessing.

1,1,1-Tris(N,N-diisobutylcarbamoyl-methylene-oxymethyl)propane (L) was prepared and characterized by using IR, 1H NMR and pos.-ion FAB mass spectra. The extraction of Th4+ and UO22+ with L was studied as a function of concentration of free extractant in an organic phase and of picrate in an aqueous phase from a picrate-nitrate medium at 293 ± 1 K, in view of nuclear fuel reprocessing. The extractability of L for Th4+ is larger than that for UO22+. Both extraction % of Th4+ and UO22+ decreased with an increase in the concentration of HNO3. The mechanism of extraction of Th4+ with L was proposed. The composition of extracted species of L with Th4+ in the organic phase is ThL(Pic)2(NO3)2. The results of extraction of trace 234Th4+ with L from the picrate-nitrate medium containing UO22- (the initial concentration of UO22+, CUO22+0 = 1.23 × 10-4 mol/dm3 (M)) agreed well with those from the extraction of single component solutions The tripodand is useful in separation of Th4+ and UO22+ from each other in picrate-nitrate media with a relatively high separation factor.

Radiochimica Acta published new progress about Nuclear fuel reprocessing. 5326-82-9 belongs to class amides-buliding-blocks, and the molecular formula is C10H20ClNO, Synthetic Route of 5326-82-9.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Soni, Rina; Collinson, John-Michael; Clarkson, Guy C.; Wills, Martin published the artcile< An Unexpected Directing Effect in the Asymmetric Transfer Hydrogenation of α,α-Disubstituted Ketones>, Name: Chloro[N-[(1R,2R)-1,2-diphenyl-2-[[3-(η6-phenyl)propyl]amino-κN]ethyl]-4-methylbenzenesulfonamidato-κN]ruthenium, the main research area is unexpected directing asym transfer hydrogenation disubstituted ketone crystallog.

α,α-Disubstituted ketones containing an aromatic ring or alkene are reduced in high enantiomeric excess using an asym. transfer hydrogenation catalyst. The sense of reduction indicates that the unsaturated region of the ketone adopts a position adjacent to the Ru-bound η6-arene ring in the reduction transition state.

Organic Letters published new progress about Aryl ketones Role: PEP (Physical, Engineering or Chemical Process), RCT (Reactant), PROC (Process), RACT (Reactant or Reagent). 1192620-83-9 belongs to class amides-buliding-blocks, and the molecular formula is C30H31ClN2O2RuS, Name: Chloro[N-[(1R,2R)-1,2-diphenyl-2-[[3-(η6-phenyl)propyl]amino-κN]ethyl]-4-methylbenzenesulfonamidato-κN]ruthenium.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Chinn, Alex J.; Sedillo, Kassandra; Doyle, Abigail G. published the artcile< Phosphine/Photoredox Catalyzed Anti-Markovnikov Hydroamination of Olefins with Primary Sulfonamides via α-Scission from Phosphoranyl Radicals>, Quality Control of 6961-82-6, the main research area is secondary sulfonamide preparation; primary sulfonamide alkene antiMarkovnikov hydroamination phosphine iridium photocatalyst.

A dual phosphine and photoredox catalytic system that enables direct formation of sulfonamidyl radicals from primary sulfonamides RSO2NH2 (R = 4-tert-butylphenyl, Me, cyclopropyl, thiophen-2-yl, etc.) was reported. Mechanistic investigations support that the N-centered radical is generated via α-scission of the P-N bond of a phosphoranyl radical intermediate, formed by sulfonamide nucleophilic addition to a phosphine radical cation. As compared to the recently well-explored β-scission chem. of phosphoranyl radicals, this strategy is applicable to activation of N-based nucleophiles and is catalytic in phosphine. The application of this activation strategy to an intermol. anti-Markovnikov hydroamination of unactivated olefins (such as cyclohexene, hex-1-ene, styrene, etc.) with primary sulfonamides RSO2NH2 is highlighted. A range of structurally diverse secondary sulfonamides [such as 4-(tert-butyl)-N-hexylbenzenesulfonamide, 4-(tert-butyl)-N-(3-phenylpropyl)benzenesulfonamide, 2-chloro-N-cyclohexylbenzenesulfonamide, etc.] can be prepared in good to excellent yields under mild conditions.

Journal of the American Chemical Society published new progress about Alkenes Role: RCT (Reactant), RACT (Reactant or Reagent). 6961-82-6 belongs to class amides-buliding-blocks, and the molecular formula is C6H6ClNO2S, Quality Control of 6961-82-6.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Khedr, Naglaa F.; Ebeid, Abla M.; Khalil, Rania M. published the artcile< New insights into weight management by orlistat in comparison with cinnamon as a natural lipase inhibitor>, Reference of 96829-58-2, the main research area is obesity orlistat cinnamon weight management; Cinnamon; Dopamine; Dyslipidemia; Glutamate; Obesity; Orlistat.

Background and objectives: Orlistat which is taken by obese patients may present some therapeutic assistance through its inhibition of lipase activity. Otherwise, a natural lipase inhibitor as cinnamon is widely used traditional medicine to decrease cholesterol and body weight The current study aimed to investigate the weight management of orlistat in comparison with cinnamon through different obesity related targets. Methods: Subjects were divided into: Group 1: subjects received cinnamon capsules for 60 days. Results: Both orlistat and cinnamon groups showed a significant reduction in BMI, lipid profile, and lipase activity compared with baseline. Orlistat group showed significant elevation (p < 0.001) in glucagon, insulin-degrading enzyme (IDE) and dopamine level concomitant with the decrease of serum glutamate compared with baseline level of the same group and cinnamon group. However, cinnamon reduced serum insulin level and insulin resistance (IR) compared with baseline level of the same group and orlistat group. Conclusions: Orlistat can be used in weight management not only for its pancreatic lipase inhibition but also, due to its indirect appetite reduction effect through elevated glucagon, IDE and dopamine levels and its inhibitory effect on glutamate neurotransmitter, whereas, cinnamon improves BMI and glycemic targets. Endocrine published new progress about Blood serum. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Reference of 96829-58-2.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Zhou, Wenjing; Zhang, Jing; Yan, Mingkun; Wu, Jin; Lian, Shuo; Sun, Kang; Li, Baiqing; Ma, Jia; Xia, Jun; Lian, Chaoqun published the artcile< Orlistat induces ferroptosis-like cell death of lung cancer cells.>, Recommanded Product: (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate, the main research area is FAF2; ferroptosis; lung cancer; orlistat.

Aberrant de novo lipid synthesis is involved in the progression and treatment resistance of many types of cancers, including lung cancer; however, targeting the lipogenetic pathways for cancer therapy remains an unmet clinical need. In this study, we tested the anticancer activity of orlistat, an FDA-approved anti-obesity drug, in human and mouse cancer cells in vitro and in vivo, and we found that orlistat, as a single agent, inhibited the proliferation and viabilities of lung cancer cells and induced ferroptosis-like cell death in vitro. Mechanistically, we found that orlistat reduced the expression of GPX4, a central ferroptosis regulator, and induced lipid peroxidation. In addition, we systemically analyzed the genome-wide gene expression changes affected by orlistat treatment using RNA-seq and identified FAF2, a molecule regulating the lipid droplet homeostasis, as a novel target of orlistat. Moreover, in a mouse xenograft model, orlistat significantly inhibited tumor growth and reduced the tumor volumes compared with vehicle control (P < 0.05). Our study showed a novel mechanism of the anticancer activity of orlistat and provided the rationale for repurposing this drug for the treatment of lung cancer and other types of cancer. Frontiers of medicine published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Recommanded Product: (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics