Month: October 2022

Permatasari, Happy Kurnia; Firani, Novi Khila; Prijadi, Bambang; Irnandi, Dicky Faizal; Riawan, Wibi; Yusuf, Muhammad; Amar, Nasim; Chandra, Liani Amelia; Yusuf, Vincentius Mario; Subali, Anita Dominique; Nurkolis, Fahrul published the artcile< Kombucha drink enriched with sea grapes (Caulerpa racemosa) as potential functional beverage to contrast obesity: An in vivo and in vitro approach.>, Application In Synthesis of 96829-58-2, the main research area is Caulerpa racemosa; Dyslipidemia; Kombucha; Nutraceuticals; Obesity.

BACKGROUND AND AIMS: Obesity is currently a global issue and is a major cause of the metabolic disorder, including dyslipidemia. However, currently approved treatments have various limitations including serious side effects, numerous contraindications, and lack of acceptance. Caulerpa racemosa, also referred as Sea grapes, is a seaweed known for its various benefits. C. racemosa extract has the potential to improve lipid profile and role as an anti-obese agent. In order to maximize its health benefits, C. racemosa was made using kombucha drink as a carrier medium. This study aims to assess the effect of Sea grapes kombucha drink on lipase activity in vitro and lipid profile in vivo. METHODS: A lipase inhibition test was carried out by incubating Sea grapes kombucha drink compared with orlistat as the control in porcine pancreatic lipase and p-nitrophenyl butyrate in reaction buffer. A total of four groups were made, each containing 10 male swiss webster albino mice; group A received standard dry pellet diet as control, group B received cholesterol and fat-enriched diets (CFED), group C and D received CFED and 150 and 300 mg/kgBW of kombucha drink from Sea grapes respectively for 4 weeks. RESULTS: Sea grapes kombucha drink improved lipid profiles in the way of reducing total cholesterol, triglyceride, LDL, and increasing HDL levels compared to CFED and normal groups. The effect was more robust following the incrementing dose of the Sea grapes excluding total cholesterol. The lipase inhibitory activity of Sea grapes kombucha drink was similar to orlistat at a dose of 250 μg/mL, otherwise, orlistat was superior in the lower doses. CONCLUSIONS: Sea grapes kombucha drink treatment also induced weight loss and increased level of liver SOD. Kombucha drink from C. racemosa has good potential as a functional beverage with anti-obese and lipid improving activity.

Clinical nutrition ESPEN published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Application In Synthesis of 96829-58-2.

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

Othman, Zaidatul Akmal; Zakaria, Zaida; Suleiman, Joseph Bagi; Ghazali, Wan Syaheedah Wan; Mohamed, Mahaneem published the artcile< Anti-atherogenic effects of orlistat on obesity-induced vascular oxidative stress rat model>, Computed Properties of 96829-58-2, the main research area is orlistat antiatherogenic antioxidant glutathione peroxidase obesity oxidative stress; anti-inflammatory; antioxidant; atherosclerosis; obesity; orlistat.

Obesity is typically linked to oxidative stress and inflammation, which lead to vascular damage and initiate the progression of atherosclerosis. The aim of this study was to determine the anti-atherosclerotic effect of orlistat on obesity-induced vascular oxidative stress in obese male rats. Twenty-four male Sprague-Dawley rats were categorized into two groups: normal (Normal group, n = 6) and high-fat diet (HFD group, n = 12). After six weeks, obese rats in the HFD group were administered either with distilled water (OB group) or orlistat 10 mg/kg/day (OB/OR group) for another six weeks. The OB group had a significant increase in lipid profiles (total cholesterol (TC), triglyceride (TG), low-d. lipoprotein (LDL)) and decrease in high-d. lipoprotein (HDL) level compared to the Normal group. The aortic antioxidants enzymes activities (superoxide dismutase (SOD), glutathione peroxidase (GPx), glutathione reductase (GR), glutathione S-transferase (GST), and catalase (CAT)) as well as total glutathione (GSH) and total antioxidant capacity (TAC) of the OB group were significantly decreased compared to the Normal group. Furthermore, pro-inflammatory atherosclerotic markers (tumor necrosis factor-alpha (TNF-a), vascular cell adhesion mol.-1 (VCAM-1), and intercellular cell adhesion mol.-1 (ICAM-1)) expressions were increased significantly, and anti-inflammatory marker (interleukin-10 (IL-10)) was decreased significantly in the OB group compared to the Normal group. Treatment with orlistat significantly improved lipid profile, increased antioxidant enzymes and expression of anti-inflammatory markers, and decreased the expression of the pro-inflammatory marker compared to the OB group. These findings may suggest the therapeutic effect of orlistat in attenuating the progression of the atherosclerotic stage in obesity.

Antioxidants published new progress about Anti-inflammatory agents. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Computed Properties of 96829-58-2.

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

Zhang, Wei; Yang, Darun; Wang, Wengui; Wang, Shoufeng; Zhao, Huaiqing published the artcile< Iridium(III)-Catalyzed Directed ortho-C(sp2)-H Amidation of Arenes with Sulfonamides>, Product Details of C6H6FNO2S, the main research area is sulfonamido aryl ketoxime ether regioselective preparation; iridium catalyst regioselective amidation aryl ketoxime methyl ether sulfonamide; directed amidation aryl ketoxime methyl ether sulfonamide iridium catalyst.

In the presence of [Cp*IrCl2]2 and AgNTf2, aryl ketoxime O-Me ethers underwent directed regioselective amidation with sulfonamides mediated by AgOAc in CH2Cl2 at 60° to give ortho-(sulfonylamino)aryl ketoxime O-Me ethers.

European Journal of Organic Chemistry published new progress about Amination catalysts (regioselective). 1524-40-9 belongs to class amides-buliding-blocks, and the molecular formula is C6H6FNO2S, Product Details of C6H6FNO2S.

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

Satibi, Satibi; Fudholi, Achmad; Amrullah, Hafizh; Itsnayain, Aya Shaufia published the artcile< The impact of training on the storage of high alert drugs: a quasi experimental study>, SDS of cas: 94-20-2, the main research area is training impact high alert drug storage.

A medication error can cause severe injury for the patient, even mortality, and that can be prevented. Preventing medication error is done by upgrading the drugs administrators knowledge at the Community Health Center in handling the high alert drugs. One of the possibility is by training. This research is conducted to understand the influence of training toward the suitability of high alert drugs storage. This research constitutes quasi-exptl. design with pre and post-anal. approach along with by using a control group as a comparison. The population of research consists of all of community health center drugs administrators in Ogan Komering Ilir Regency and Mataram City. The sample of research are the drugs administrators, Human Resources, who work at the Community health center of Ogan Komering Ilir and Mataram city were chosen to use non-probability sample. The intervention was conducted toward the drugs administrators with the material that has been standardized by the Ministry of Health of the Republic of Indonesia. The instrument is in the form of List of Visit that has been validated to assess the suitability of high alert drugs storage at Community health center by using SPSS-23 with Wilcoxon Signed Rank and Mann-Whitney U tests. The result of the research shows that the majority of the Intervention group of Community health center (83,33%) the storage of high alert drugs is appropriate with the standard after training. The percentage difference of the appropriate high alert drugs storage test between intervention group and control group after the training (p<0,05). International Journal of Research in Pharmaceutical Sciences (Madurai, India) published new progress about Chemists. 94-20-2 belongs to class amides-buliding-blocks, and the molecular formula is C10H13ClN2O3S, SDS of cas: 94-20-2.

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

Simons, R. Thomas; Scott, Georgia E.; Kanegusuku, Anastasia Gant; Roizen, Jennifer L. published the artcile< Photochemically Mediated Nickel-Catalyzed Synthesis of N-(Hetero)aryl Sulfamides>, Name: Morpholine-4-sulfonamide, the main research area is photocatalyst nickel heteroaryl sulfamide arylbromide arylation.

A general method for the N-arylation of sulfamides with aryl bromides is described. The protocol leverages a dual-catalytic system, with [Ir(ppy)2(dtbbpy)]PF6 as a photosensitizer, NiBr2•glyme as a precatalyst, and DBU as a base, and proceeds at room temperature under visible light irradiation Using these tactics, aryl boronic esters and aryl chlorides can be carried through the reaction untouched. The developed reactions efficiently engage simple bromoarenes and primary sulfamides in between 66% and quant. yields. For more challenging substrates, such as secondary sulfamides, reaction efficiency is documented. Thereby, these methods complement known Buchwald-Hartwig coupling methods for N-arylation of sulfamides. A general method for the N-arylation of sulfamides with aryl bromides is described. The protocol leverages a dual-catalytic system of Ni and a photoexcitable Ir complex and proceeds at room temperature under visible light irradiation Using these tactics, aryl boronic esters and aryl chlorides can be carried through the reaction untouched. Thereby, this method complements known Buchwald-Hartwig coupling methods for N-arylation of sulfamides.

Journal of Organic Chemistry published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 25999-04-6 belongs to class amides-buliding-blocks, and the molecular formula is C4H10N2O3S, Name: Morpholine-4-sulfonamide.

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

Liu, Jingying; Werner, Ulrich; Funke, Mario; Besenius, Melissa; Saaby, Lasse; Fanoe, Mathias; Mu, Huiling; Mullertz, Anette published the artcile< SEDDS for intestinal absorption of insulin: Application of Caco-2 and Caco-2/HT29 co-culture monolayers and intra-jejunal instillation in rats>, Name: (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate, the main research area is insulin emulsion intestine; Caco-2 monolayers; Caco-2/HT29-MTX co-culture monolayers; Insulin; Intestinal barrier; Intra-jejunal administration; Monoacyl phosphatidylcholine; Self-emulsifying drug delivery systems.

To face the challenges of oral delivery of peptide and protein (P/P) drugs, self-emulsifying drug delivery systems (SEDDSs) containing monoacyl phosphatidylcholine (MAPC), Labrasol (LAB) and medium-chain (MC) monoglycerides as permeation enhancers (PEs) were evaluated for their effect on intestinal absorption of insulin. In this study, insulin was complexed with phosphatidylcholine (SPC) to form an insulin-SPC complex (ins-SPC) with increased lipophilicity. The following three SEDDSs: MCT(MAPC) (MC triglycerides and MAPC included), MCT(RH40) (MC triglycerides and Kolliphor RH40 included) and LCT(MAPC) (long-chain triglycerides and MAPC included) were loading with ins-SPC (4% or 8% weight/weight of SPC). Three SEDDSs generated emulsions with droplet sizes between 50 and 470 nm and with zeta potentials between -5 to -25 mV in a simulated intestinal medium. Mucus-secreting Caco-2/HT29-MTX-E12 co-culture and Caco-2 monolayers were used as in vitro cell transport models to investigate insulin permeability. In comparison to insulin HBSS solution, MCT(MAPC) significantly increased the insulin permeability across co-culture and Caco-2 monolayers (2.0-2.5 × 10-7 cm/s). In an intra-jejunal (i.j.) instillation model in rats, MCT(RH40) significantly decreased the rat blood glucose after 0.5 h by 17.0 ± 2.5% and for MCT(MAPC), it was 23.6 ± 10.6%. Furthermore, a lipase inhibitor orlistat was incorporated into MCT(MAPC) to evaluate the effect of lipid digestion on insulin absorption. Results indicated that the incorporation of orlistat did not significantly alter the in vivo insulin absorption. Overall, the SEDDS MCT(MAPC) composed of natural PEs (MAPC and MC glycerides) and synthetic PE (LAB) significantly increased the intestinal absorption of insulin upon i.j. instillation. Although it is not possible to conclude if a single PE is dominating the intestinal absorption of insulin, MCT(MAPC) seems to have the potential for oral insulin delivery.

International Journal of Pharmaceutics (Amsterdam, Netherlands) published new progress about Antidiabetic 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

Ma, Yao; Li, Xueyuan; Pei, Yameng; Ye, Jingjia; Wei, Xiduan; Yang, Jingshu; Si, Guangxu; Tian, Jingyuan; Dong, Yi; Liu, Gang published the artcile< Identification of benzofused five-membered sultams, potent dual NOD1/NOD2 antagonists in vitro and in vivo>, HPLC of Formula: 6961-82-6, the main research area is nucleotide binding oligomerization domains NOD1 NOD2 antagonist NFkappaB MAPK; Dual NOD1/NOD2 antagonist; Five-membered sultams; MAPK signaling; NF-κB signaling.

Nucleotide-binding oligomerization domain-containing proteins 1 and 2 play important roles in immune system activation. Recently, a shift has occurred due to the emerging knowledge that preventing nucleotide-binding oligomerization domains (NODs) signaling could facilitate the treatment of some cancers, which warrants the search for dual antagonists of NOD1 and NOD2. Herein, we undertook the synthesis and identification of a new class of derivatives of dual NOD1/NOD2 antagonists with novel benzofused five-membered sultams. Compound 14k(I) was finally demonstrated to be the most potent mol. that inhibits both NOD1-and NOD2-stimulated NF-κB and MAPK signaling in vitro and in vivo.

European Journal of Medicinal Chemistry published new progress about Caspase recruitment domain-containing protein 15 Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (inhibitor). 6961-82-6 belongs to class amides-buliding-blocks, and the molecular formula is C6H6ClNO2S, HPLC of Formula: 6961-82-6.

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

Moss, Steven J.; Bobardt, Michael; Leyssen, Pieter; Coates, Nigel; Chatterji, Udayan; Xie, Dejian; Foster, Teresa; Liu, Jinlun; Nur-e-Alam, Mohammad; Suthar, Dipen; Chen, Yongsheng; Warneck, Tony; Zhang, Ming-Qiang; Neyts, Johan; Gallay, Philippe; Wilkinson, Barrie; Gregory, Matthew A. published the artcile< Sangamides, a new class of cyclophilin-inhibiting host-targeted antivirals for treatment of HCV infection>, Category: amides-buliding-blocks, the main research area is sangamide cyclophilin inhibitor HCV antiviral.

Sangamides are amide derivatives of sanglifehrin A, a cyclophilin-binding polyketide natural product which is structurally distinct from cyclosporine A. Cyclosporine A is the starting point for the synthesis of cyclophilin inhibitors such as alisporivir, currently in development for the treatment of HCV infection. We report here initial results of the optimization program which led to identification of the sangamides, compounds that exhibit significantly improved potential for the treatment of chronic HCV infection.

MedChemComm published new progress about Antiviral agents. 5326-82-9 belongs to class amides-buliding-blocks, and the molecular formula is C10H20ClNO, Category: amides-buliding-blocks.

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

Zhang, Yi-Ming; Wang, Dong-Chao; Xie, Ming-Sheng; Qu, Gui-Rong; Guo, Hai-Ming published the artcile< Asymmetric Transfer Hydrogenation of rac-α-(Purin-9-yl)cyclopentones via Dynamic Kinetic Resolution for the Construction of Carbocyclic Nucleosides>, Category: amides-buliding-blocks, the main research area is asym transfer hydrogenation dynamic kinetic resolution purinylcyclopentone; crystal structure hydrogenation kinetic resolution purinylcyclopentone purinylcyclopentanol carbocyclic nucleoside.

An asym. transfer hydrogenation via dynamic kinetic resolution of a broad range of rac-α-(purin-9-yl)cyclopentones was first developed. A series of cis-β-(purin-9-yl)cyclopentanols were obtained with up to 97% yield, >20/1 dr, and >99% ee. This also provides an efficient synthetic route to a variety of chiral carbocyclic nucleosides.

Organic Letters published new progress about Carbocyclic nucleosides Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 1192620-83-9 belongs to class amides-buliding-blocks, and the molecular formula is C30H31ClN2O2RuS, Category: amides-buliding-blocks.

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

Vyas, Vijyesh K.; Bhanage, Bhalchandra M. published the artcile< Kinetic Resolution Driven Diastereo- and Enantioselective Synthesis of cis-β-Heteroaryl Amino Cycloalkanols by Ruthenium-Catalyzed Asymmetric Transfer Hydrogenation>, Reference of 1192620-83-9, the main research area is azolyl cycloalkanol diastereoselective enantioselective preparation; tethered ruthenium catalyst asym transfer hydrogenation azolyl ketone; dynamic kinetic resolution azolyl ketone tethered ruthenium catalyst; phenyltriazolyl bromoindanol crystal structure absolute configuration.

In the presence of a tethered Ru-TsDPEN complex, ketones with α-nitrogen heterocycle substituents such as I underwent diastereoselective and enantioselective dynamic kinetic resolution and transfer hydrogenation reactions with triethylamine and formic acid in dichloromethane for 6 h at 27° to yield cis-azolyl cycloalkanols such as II. Using the method, a nonracemic antileishmanial agent and a nonracemic ionic liquid were prepared The structure and absolute configuration of a (phenyltriazolyl)bromoindanol were determined by X-ray crystallog.

Organic Letters published new progress about Azoles Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation) (β-hydroxycycloalkyl, β-ketocycloalkyl). 1192620-83-9 belongs to class amides-buliding-blocks, and the molecular formula is C30H31ClN2O2RuS, Reference of 1192620-83-9.

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