Month: October 2022

Wang, Han; Zhao, Yang; Ding, Yi-Xuan; Yu, Chang-Bin; Zhou, Yong-Gui published the artcile< Synthesis of cis β-Hydroxy Ketones by Desymmetrization of 1,3-Cyclopentanediones through Ruthenium-Catalyzed Hydrogen Transfer>, HPLC of Formula: 1192620-83-9, the main research area is beta hydroxy ketone preparation stereoselective; cyclopentanedione transfer hydrogenative desymmetrization ruthenium catalyst.

A facile synthesis of chiral cis β-hydroxy ketones I (R = Me, Et, allyl; R1 = Ph, 4-MeC6H4, 3-FC6H4, etc.) was successfully developed through ruthenium-catalyzed transfer hydrogenative desymmetrization of 1,3-cyclopentanedione. The experiment on gram scale could be performed without loss of reactivity and enantioselectivity.

Asian Journal of Organic Chemistry published new progress about Cycloalkanones Role: RCT (Reactant), RACT (Reactant or Reagent). 1192620-83-9 belongs to class amides-buliding-blocks, and the molecular formula is C30H31ClN2O2RuS, HPLC of Formula: 1192620-83-9.

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

Marounek, M; Volek, Z; Taubner, T; Czauderna, M published the artcile< Metabolic Effects of a Hydrophobic Alginate Derivative and Tetrahydrolipstatin in Rats Fed a Diet Supplemented with Palm Fat and Cholesterol.>, Application of C29H53NO5, the main research area is .

The effects of octadecylamide of alginic acid (amidated alginate) and tetrahydrolipstatin on serum and hepatic cholesterol, and the faecal output of fat and sterols, were investigated in rats. Amidated alginate is a sorbent of lipids, tetrahydrolipstatin is an inhibitor of pancreatic lipase. Rats were fed diets containing cholesterol and palm fat at 10 and 70 g/kg, respectively. Palm fat was provided by coconut meal. Amidated alginate at 40 g/kg diet significantly decreased serum total cholesterol, low-density lipoprotein and hepatic cholesterol, and hepatic lipids and increased the faecal output of fat and coprostanol. Tetrahydrolipstatin at 300 mg/kg diet significantly decreased low-density lipoprotein cholesterol and hepatic lipids and increased the faecal output of fat. The intake of feed was not significantly influenced; however, the weight gains in rats fed amidated alginate were lower than in rats of the control group. Both amidated alginate and tetrahydrolipstatin modified the fatty acid profile in excreta lipids. Concentrations of saturated fatty acids were decreased and those of unsaturated fatty acids increased. Despite different modes of action, amidated alginate and tetrahydrolipstatin were equally efficient in removing the dietary fat from the body.

Folia biologica published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Application of C29H53NO5.

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

Ogita, H.; Isobe, Y.; Takaku, H.; Sekine, R.; Goto, Y.; Misawa, S.; Hayashi, H. published the artcile< Synthesis and structure-activity relationship of diarylamide derivatives as selective inhibitors of the proliferation of human coronary artery smooth muscle cells>, Recommanded Product: 2-Amino-4,5-dimethoxybenzamide, the main research area is diarylamide derivative antiproliferative SAR preparation coronary artery.

A series of diarylamide derivatives were synthesized and evaluated for their inhibitory activities against human coronary artery smooth muscle cells (SMCs) and human coronary artery endothelial cells (ECs). I was superior to the lead compound, tranilast, in terms of the potency of the activity and cell selectivity. A series of diarylamide derivatives were synthesized and evaluated for their inhibitory activities against the proliferation of human coronary artery smooth muscle cells (SMCs) and human coronary artery endothelial cells (ECs).

Bioorganic & Medicinal Chemistry Letters published new progress about Arterial endothelium, coronary artery endothelium. 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, Recommanded Product: 2-Amino-4,5-dimethoxybenzamide.

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

Wasta Esmail, Vian Ahmed; Al-Nimer, Marwan S M; Mohammed, Mohammed Omer published the artcile< Effects of Orlistat or Telmisartan on the Serum Free Fatty Acids in Non-alcoholic Fatty Liver Disease Patients: An Open-Labeled Randomized Controlled Study.>, Name: (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate, the main research area is .

BACKGROUND: One of the important inducers of inflammatory responses and accumulation of fat in hepatocytes is free fatty acids which ultimately lead to the development of non-alcoholic fatty liver disease. Patients with non-alcoholic fatty liver disease have high levels of plasma free fatty acids which are usually associated with type 2 diabetes and components of metabolic syndrome including dyslipidemia. Objective of this research is to investigate the effects of orlistat (a lipase enzyme inhibitor) or telmisartan (an angiotensin receptor blocker) on the serum free fatty acids in non-alcoholic fatty liver disease patients taking into consideration the baseline lipid profile. METHODS: This open-label clinical trial was carried out in the Department of Pharmacology, College of Medicine at the University of Sulaimani in cooperation with Shar Teaching Hospital in Sulaimani city-Kurdistan Region of Iraq. A total number of 74 non-alcoholic fatty liver disease patients were recruited and grouped randomly into group I (n = 25) treated with orlistat (120 mg/day orally) for 12 weeks, group II (n = 24) treated with telmisartan (20 mg/day orally) for 8 weeks, and group III (n = 25) treated with placebo (carboxy- methyl cellulose) once daily. Fasting serum level of free fatty acid and lipid profile including total cholesterol, triglyceride, high-density lipoprotein, and non-high-density lipoproteins were determined. RESULTS: Orlistat and telmisartan significantly reduced the triglyceride-glucose index and free fatty acid levels (P < .001) in patients with non-alcoholic fatty liver diseases. CONCLUSION: Short-term treatment with orlistat or telmisartan produce effective and significant reductions in FFAs in patients with non-alcoholic fatty liver disease compared to placebo. Orlistat effectively reduces the free fatty acid irrespective of the baseline lipid profile. The Turkish journal of gastroenterology : the official journal of Turkish Society of Gastroenterology published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Name: (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

Hodgkinson, Roy; Jurcik, Vaclav; Nedden, Hans; Blackaby, Andrew; Wills, Martin published the artcile< An alternative route to tethered Ru(II) transfer hydrogenation catalysts>, Synthetic Route of 1192620-83-9, the main research area is ruthenium arene tethered preparation transfer hydrogenation catalyst ketone aldehyde.

A new route towards a series of tethered η6-arene/Ru(II) catalysts for use in the transfer and pressure hydrogenation of ketones and aldehydes to alcs. is reported. The route proceeds through the formation of an amide from the diamine precursor, followed by reduction, rather than the direct alkylation of the diamine. This has the advantage that dialkylation of the amine is avoided during the synthesis. Through this new route, both racemic and enantiomerically-pure η6-arene/Ru(II) tethered catalysts can be prepared in high yield.

Tetrahedron Letters published new progress about Alcohols Role: SPN (Synthetic Preparation), PREP (Preparation). 1192620-83-9 belongs to class amides-buliding-blocks, and the molecular formula is C30H31ClN2O2RuS, Synthetic Route of 1192620-83-9.

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

Nguyen, Phuong Thuy Viet; Huynh, Han Ai; Van Truong, Dat; Tran, Thanh-Dao; Vo, Cam-Van Thi published the artcile< Exploring aurone derivatives as potential human pancreatic lipase inhibitors through molecular docking and molecular dynamics simulations>, Application of C29H53NO5, the main research area is aurone pancreatic lipase inhibitor anticancer agent leukemia; aurone; human pancreatic lipase; human pancreatic lipase inhibitors; molecular docking; molecular dynamics simulations.

Inhibition of human pancreatic lipase, a crucial enzyme in dietary fat digestion and absorption, is a potent therapeutic approach for obesity treatment. In this study, human pancreatic lipase inhibitory activity of aurone derivatives was explored by mol. modeling approaches. The target protein was human pancreatic lipase (PDB ID: 1LPB). The 3D structures of 82 published bioactive aurone derivatives were docked successfully into the protein catalytic active site, using AutoDock Vina 1.5.7.rc1. Of them, 62 compounds interacted with the key residues of catalytic trial Ser152-Asp176-His263. The top hit compound (A14), with a docking score of -10.6 kcal·mol-1, was subsequently submitted to mol. dynamics simulations, using GROMACS 2018.01. Mol. dynamics simulation results showed that A14 formed a stable complex with 1LPB protein via hydrogen bonds with important residues in regulating enzyme activity (Ser152 and Phe77). Compound A14 showed high potency for further studies, such as the synthesis, in vitro and in vivo tests for pancreatic lipase inhibitory activity.

Molecules published new progress about Antitumor agents. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Application of C29H53NO5.

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

Czumaj, Aleksandra; Zabielska, Judyta; Pakiet, Alicja; Mika, Adriana; Rostkowska, Olga; Makarewicz, Wojciech; Kobiela, Jaroslaw; Sledzinski, Tomasz; Stelmanska, Ewa published the artcile< In vivo effectiveness of orlistat in the suppression of human colorectal cancer cell proliferation>, Name: (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate, the main research area is colorectal cancer cell proliferation orlistat; Colorectal cancer; fatty acid synthase; orlistat; palmitate.

Background/Aim: Fatty acid synthase (FASN) provides palmitate for cell membrane formation in colorectal cancer (CRC) cells, however, palmitate is also available in the blood of CRC patients. The aim of this study was to examine whether orlistat, a FASN inhibitor, is able to attenuate CRC cell growth despite the availability of extracellular palmitate. Materials and Methods: Palmitate concentrations were measured in serum from CRC patients and healthy controls. HT-29 CRC cells were treated with orlistat and palmitate. Results: Treatment of CRC cells with orlistat caused a dose-dependent inhibition of cell proliferation. In turn, delivery of extracellular palmitate at doses lower than those found in the serum of CRC patients reversed inhibition by orlistat concentrations of up to 10μM. Conclusion: Inhibition of CRC cell proliferation by orlistat is reversed by palmitate which is present at high levels in the serum. Therefore, orlistat may be effective in vivo only at high concentrations

Anticancer Research published new progress about Antiproliferative agents. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Name: (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

Lin, Kai-Huang; Luo, Ci-Wen; Chen, Shih-Pin; Tu, Dom-Gene; Lin, Ming-Shian; Kuan, Yu-Hsiang published the artcile< Inhibitor of α-glucosidase can effectively inhibit therisk of tuberculosis in patients with diabetes: a nestedcase-control study>, Computed Properties of 94-20-2, the main research area is alpha glucosidase inhibitor antituberculosis antidiabetic agent tuberculosis diabetes.

Diabetes mellitus (DM) and tuberculosis (TB) are major public health and economic burdens. DM increases Mycobacterium tuberculosis infection rates and treatment durations. This study evaluated the relationship between five classes of oral DM medications and TB infection risk in DM patients. We used longitudinal records from the Taiwan Longitudinal Health Insurance Research Database. DM patients were identified using the International Classification of Diseases. TB patients were identified. Oral DM medications were divided into five classes: sulfonylureas, biguanides, meglitinides, α-glucosidase inhibitors (AGIs), and thiazolidinediones. Users were classified as nonusers, low-concentration users, and high-concentration users. The incidence rate ratio (IRR) was derived using multivariate Poisson regression to calculate the relative risk of TB infection. DM patients using low- and high-concentration AGIs had significantly lower TB infection risks compared with nonusers. The IRRs of the sulfonylureas and AGI users were (CI 0.693-0.948) and (95% CI 0.651-0.995), resp. The other four classes of medications exhibited no significant effect on TB infection risk in DM patients. Furthermore, DM patients using highconcn. AGIs had a significantly lower TB infection risk compared with those using low-concentration AGIs (IRR 0.918, 95% CI: 0.854-0.987). We noted a dose-response relationship in the effects of DM medications on TB risk. Accordingly, we suggest that DM patients use AGIs to benefit from their protective effect on TB infection risk.

BioMed Research International published new progress about Antidiabetic agents. 94-20-2 belongs to class amides-buliding-blocks, and the molecular formula is C10H13ClN2O3S, Computed Properties of 94-20-2.

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

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