Author: Jessica.F

Johnson, Adiv A. published the artcile< Lipid Hydrolase Enzymes: Pragmatic Prolongevity Targets for Improved Human Healthspan?>, Product Details of C29H53NO5, the main research area is lipase lipid hydrolase lifespan aging; aging; healthspan; lifespan; lipase; lipid hydrolase; rejuvenation.

Compelling evidence suggests that lipid metabolism, which plays critical roles in fat storage, cell membrane maintenance, and cell signaling, is intricately linked to aging. Lipid hydrolases are important enzymes that catalyze the hydrolysis of more complex lipids into simpler lipids. Diverse interventions targeting lipid hydrolases can prolong or shorten life in model organisms. For example, the genetic removal of or RNAi knockdown against a phospholipase can reduce lifespan in Caenorhabditis elegans, Drosophila melanogaster, and Mus musculus. The removal of lysosomal acid lipase results in premature death in mice, while its overexpression in nematodes generates lean, long-lived individuals. The overexpression or inhibition of diacylglycerol lipase leads to enhanced or reduced longevity, resp., in both worms and flies. Lifespan can also be extended by knocking down triacylglycerol lipases in yeast, overexpressing fatty acid amide hydrolase in worms, or removing hepatic lipase in a mouse model of coronary disease. Conversely, flies lacking the triacylglycerol lipase Brummer are obese and short lived. Linking sphingolipids and aging, removing the sphingomyelinase inositol phosphosphingolipid phospholipase shortens chronol. lifespan in Saccharomyces cerevisiae, while inhibiting an acid sphingomyelinase in worms or inactivating alk. ceramidase in flies extends lifespan. The clin. potential of manipulating these enzymes is highlighted by the FDA-approved obesity drug orlistat, which is an inhibitor of pancreatic and hepatic lipases that induces weight loss and improves insulin/glucose homeostasis. Addnl. research is warranted to better understand how these lipid hydrolases impact aging and to determine if clin. interventions targeting them are capable of improving human healthspan.

Rejuvenation Research published new progress about Caenorhabditis elegans. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Product Details of C29H53NO5.

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

Abdel-Salam, Omar M. E.; Sleem, Amany A.; Youness, Eman R.; Morsy, Fatma A. published the artcile< Exacerbation of toluene's neuro- and hepato-toxicity by amiodarone or chlorpropamide: involvement of oxidative stress>, Name: 4-Chloro-N-(propylcarbamoyl)benzenesulfonamide, the main research area is amiodarone chlorpropamide neuroprotectant neurotoxicity hepatotoxicity.

Volatile solvent abuse is an important health problem and results in serious injury to the central nervous system. Neuroprotective effects were reported for the sulfonylurea group of drugs and for the anti-arrhythmic agent amiodarone, and these drugs have a K+ channel-blocking effect. The K+ channels are of interest for their ability to modulate brain damage. The aim of this study was to investigate the effect of amiodarone and chlorpropamide on the development of oxidative stress and brain and liver damage induced by toluene injection in rats. Toluene (900 mg/kg) was i.p. (i.p.) administered alone or in combination with amiodarone or chlorpropamide (18 or 36 mg/kg, orally) once a day for 2 consecutive days. The brain and liver content of malondialdehyde (MDA), reduced glutathione (GSH), and nitric oxide (NO), and the activity of paraoxonase-1 (PON-1) were determined In addition, butyrylcholinesterase (BChE) and the concentration of the anti-apoptotic protein (Bcl-2) were determined in brain homogenates. Histopathol. examination of brain and liver sections was also performed. Results showed that compared to controls, toluene resulted in increased oxidative stress in the brain and liver tissues. MDA and NO concentrations were markedly raised along with decreased levels of GSH and PON-1 activity. Toluene also inhibited BChE activity and decreased Bcl-2 level in the brain tissue. The biochem. changes induced by toluene were aggravated by the administration of either amiodarone or chlorpropamide. Rats treated with toluene exhibited dead neurons, perineuronal vacuolations, infiltrative cells, glial cells, and degeneration of some Purkinje cells. In the liver, massive hepatic inflammatory infiltrate, hemorrhage, vacuolar degeneration, apoptosis, and degeneration of hepatocytes were observed The co-administration of either amiodarone or chlorpropamide caused dose-dependent exacerbation of the toluene-induced pathol. changes. These findings suggest the involvement of oxidative stress in the neuro- and hepato-toxicity by toluene and imply a greater toxicity in toluene abusers treated with either amiodarone or chlorpropamide.

Reactive Oxygen Species published new progress about Bcl-2 proteins Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 94-20-2 belongs to class amides-buliding-blocks, and the molecular formula is C10H13ClN2O3S, Name: 4-Chloro-N-(propylcarbamoyl)benzenesulfonamide.

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

Manohar, Smitha; Sharma, J. N.; Shah, B. V.; Wattal, P. K. published the artcile< Process development for bulk separation of trivalent actinides and lanthanides from radioactive high-level liquid waste>, Recommanded Product: 2-Chloro-N,N-diisobutylacetamide, the main research area is actinide lanthanide solvent extraction radioactive liquid waste.

Inhouse R and D studies resulted in the development of processes for the bulk separation of trivalent actinides and lanthanides from radioactive high-level liquid waste. Synthesis of solvents, namely, n-octyl (phenyl)-N,N-di-iso-Bu carbamoyl Me phosphine oxide and diglycolamide-based tetra (2-ethylhexyl) diglycolamide (TEHDGA), at the required purity was carried out, and a suitable process for their resp. use in actual application was developed. Inactive scale engineering runs comprised of simultaneous extraction and stripping operations were carried out to establish the process on an engineering scale, including reuse of the solvent system. The composition of surrogate high-level waste (HLW) used at engineering-scale studies corresponds to 1st-cycle raffinate from reprocessing of long-cooled pressurized D2O reactor fuel with a burnup of 6500 MWd/ton. Since trivalent lanthanides and actinides exhibits similar extraction behavior at higher acidity, Ce and La were only used in making surrogate HLW to represent all the trivalent lanthanides and actinides. Indigenously developed mixer-settlers using a passive system of mixing were used for these runs. Over a period of ∼10 h, ∼ 300 e of surrogate HLW solutions were contacted with solvent. The results of such repeated trials showed near-total removal of Ce and La (>99.8% and 97%, resp.) at aqueous-to-organic ratio of 2.5:1 for a TEHDGA system. As the distribution coefficient values for trivalent actinide (241Am) are significantly higher than those for trivalent lanthanides for both of the solvent systems under consideration, it can be inferred that separation of trivalent actinides along with lanthanides could be feasible using these solvent systems.

Nuclear Science and Engineering published new progress about Actinides Role: REM (Removal or Disposal), PROC (Process). 5326-82-9 belongs to class amides-buliding-blocks, and the molecular formula is C10H20ClNO, Recommanded Product: 2-Chloro-N,N-diisobutylacetamide.

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

Yin, Yaguang; Kong, Xiuqi; Li, Min; Wang, Jingchao; Dai, Xiaoyu; Zhang, Yunyan; Lin, Weiying published the artcile< Development of an esterase fluorescent probe based on naphthalimide-benzothiazole conjugation and its applications for qualitative detection of esterase in orlistat-treated biosamples>, Application of C29H53NO5, the main research area is ESIPT; Esterase fluorescent probe; Fast response; Orlistat-treated cell imaging; Zebrafish imaging.

Esterase is a large hydrolysis family, and widely distributed in many kinds of cells. It is responsible for multiple physiol. and pathol. functions including metabolism, gene expression. While abnormality of esterase is associated with many pathol. activities in obesity, Wolman′s disease, and cancer. Thereby, it is essential to design an effective tool for esterase in situ detection in biol. systems. Herein, a novel fluorescent probe Y-1 for monitoring esterase in living cells was rationally designed. Probe Y-1 was synthesized by the conjugation between an acetylation of 4-hydroxy naphthalimide and benzothiazole group. Benzothiazole moiety is a typical Excited-state intramol. proton transfer (ESIPT) controller. Acetate group was selected as the responsive site and ESIPT initiator. As the acetate group could block the ESIPT effect, the probe emits no fluorescence under the excitation of 455 nm. When binding with esterase, Y-1 shows distinct fluorescence with the peak at 560 nm with short time when ESIPT is on. Y-1 displays high sensitivity (LOD is 0.216 x 10-3 U/mL), fast response (within 5 min), high selectivity and photostability towards esterase. Furthermore, the %RSD (relative standard deviation) of within-day and day-to-day precision was no more than 13.0% and the accuracy ranged from -6.5 to -12.3%. Kinetics performance of Y-1 indicates that esterase has high affinity and hydrolysis to Y-1. For biol. applications, our probe is a time-dependent visualizing esterase in living HepG2 and CoLo205 cells within 15 min. After the treatment of orlistat (1 and 5 μM) for inhibiting the activity of esterase, the bright fluorescence has also been detected using our probe. Furthermore, it has been successful in monitoring the esterase in zebrafish, the data were consistent with cellular phenomena. Therefore, all these findings indicate that the robust probe Y-1 is a useful qual. tool for detecting esterase in biol. systems.

Analytica Chimica Acta 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

Guerra, Walter D.; Lucena-Agell, Daniel; Hortigueela, Rafael; Rossi, Roberto A.; Fernando Diaz, J.; Padron, Jose M.; Barolo, Silvia M. published the artcile< Design, Synthesis, and in vitro Evaluation of Tubulin-Targeting Dibenzothiazines with Antiproliferative Activity as a Novel Heterocycle Building Block>, Application In Synthesis of 6961-82-6, the main research area is dibenzothiazine preparation antiproliferative SAR cell cycle tubulin inhibitor human; Antiproliferation; dibenzothiazines; drug design; sulfonamides; tubulin inhibitors.

A series of free NH and N-substituted dibenzonthiazines I [R1 = H, F, CF3, Ph; R2 = H, 9-F, 7-Ph, etc.; R3 = H, Me, Bn, etc.] with potential anti-tumor activity from N-aryl-benzenesulfonamides was prepared A biol. test of synthesized compounds was performed in vitro measuring their antiproliferative activity against a panel of six human solid tumor cell lines and its tubulin inhibitory activity. Compounds I [R1 = R2 = H; R3 = SO2C6H5, 4-MeC6H4SO2] showed as the best compounds with promising values of activity (overall range of 2-5.4μM).

ChemMedChem published new progress about Antiproliferative agents. 6961-82-6 belongs to class amides-buliding-blocks, and the molecular formula is C6H6ClNO2S, Application In Synthesis of 6961-82-6.

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

Vyas, Vijyesh K.; Knighton, Richard C.; Bhanage, Bhalchandra M.; Wills, Martin published the artcile< Combining Electronic and Steric Effects To Generate Hindered Propargylic Alcohols in High Enantiomeric Excess>, Safety of Chloro[N-[(1R,2R)-1,2-diphenyl-2-[[3-(η6-phenyl)propyl]amino-κN]ethyl]-4-methylbenzenesulfonamidato-κN]ruthenium, the main research area is combining electronic steric effect generate hindered propargylic alc high; asym transfer hydrogenation arylacetylenic ketone Tethered ruthenium catalyst; crystallog arylacetylenic ketone asym transfer hydrogenation.

Tethered ruthenium-TsDPEN complexes have been applied to the catalysis of the asym. transfer hydrogenation of a range of aryl/acetylenic ketones. The introduction of an ortho- substituent to the aryl ring of the substrate results in a reversal of the enantioselectivity, while the introduction of two o-fluoro substituents results in an improvement to the reduction enantioselectivity, as does the replacement of a Ph ring on the alkyne with a trimethylsilyl group. These effects are rationalized as resulting from a change in the steric properties of the aryl ring and the electronic properties of the alkyne which, when matched in the reduction transition state, combine within a “”window”” of substrate/catalyst matching to generate products of high ee.

Organic Letters published new progress about Absolute configuration. 1192620-83-9 belongs to class amides-buliding-blocks, and the molecular formula is C30H31ClN2O2RuS, Safety of 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

Wang, Ying; Sarris, Kathy; Sauer, Daryl R.; Djuric, Stevan W. published the artcile< An expeditious and convenient synthesis of acylsulfonamides utilizing polymer-supported reagents>, Application of C6H6FNO2S, the main research area is acylsulfonamide preparation; acylation sulfonamide carboxylic acid polymer supported reagent.

Acylsulfonamides can be rapidly and conveniently synthesized from a variety of carboxylic acids and sulfonamides utilizing the com. available reagents, PS-DCC and DMAP under mild reaction conditions. DMAP can be efficiently scavenged by utilization of a silica-supported tosic acid cartridge (Si-SCX). In most of the cases studied, products with high purities and yields were obtained without the need for further purification

Tetrahedron Letters published new progress about Acylation. 1524-40-9 belongs to class amides-buliding-blocks, and the molecular formula is C6H6FNO2S, Application of C6H6FNO2S.

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

Zhang, Cong; Sheng, Lei; Yuan, Ming; Hu, Junjie; Meng, Yan; Wu, Yong; Chen, Liang; Yu, Huifan; Li, Shan; Zheng, Guohua; Qiu, Zhenpeng published the artcile< Orlistat delays hepatocarcinogenesis in mice with hepatic co-activation of AKT and c-Met>, Reference of 96829-58-2, the main research area is orlistat AKT cMet hepatic carcinoma antitumor agent; Fatty acid synthase; Hepatocarcinogenesis; Lipogenesis; Orlistat; Proliferation.

Orlistat (Xenical), a US Food and Drug Administration (FDA)-approved anti-obesity drug, shows efficacy against multiple tumor types, including hepatocellular carcinoma (HCC), due to its ability to inhibit fatty acid synthase (FASN) activity. However, whether orlistat affects hepatocellular malignant transformation during hepatocarcinogenesis in vivo is unknown. This study assessed the antisteatotic and antitumorigenic efficacy of orlistat in a rapid HCC FVB/N mouse model established via hydrodynamic transfection of activated forms of AKT and c-Met proto-oncogenes. Human hepatoma cell lines were used for mech. validation in vitro. Hematoxylin and eosin staining, immunohistochem., and immunoblotting were applied for the mechanistic investigation. The results revealed that when orlistat was administered in the early stage of AKT/c-Met-triggered hepatocarcinogenesis, it resulted in the elimination of hepatic tumor burden. Mechanistically, orlistat efficiently elevated PTEN expression and suppressed AKT/SREBP1/FASN signaling both in vivo and in vitro, impairing AKT/c-Met-driven de novo lipogenesis and aberrant proliferation. Altogether, this study demonstrates the antilipogenic and antiproliferative efficacy of orlistat in hepatocarcinogenesis, suggesting that orlistat may be beneficial for the treatment of HCC, especially in NAFLD-related HCCs featuring activated AKT/mTOR cascade and increased lipogenesis in livers.

Toxicology and Applied Pharmacology published new progress about Antitumor agents. 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

Kwon, Yu-Jin; Kwon, Go Eun; Lee, Hye Sun; Choi, Man Ho; Lee, Ji-Won published the artcile< The Effect of Orlistat on Sterol Metabolism in Obese Patients.>, Name: (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate, the main research area is anti-obesity drug; cardiovascular disease; obesity; orlistat; sterol.

Background: Orlistat, a reversible inhibitor of pancreatic and gastric lipase, is known to have anti-obesity and antioxidant properties. Cholesterol intermediates and metabolites have diverse and important functions in cardiovascular disease. Therefore, we aimed to evaluate the effect of orlistat on sterol metabolism in overweight and obese adults after weight loss during the intervention or weight loss at 12 weeks. Methods: A total of 51 (27 in the control group and 24 in the experimental group), patients with a BMI of 27 or greater were randomly assigned in a 1:1 ratio to receive either orlistat (120 mg) three times a day plus phentermine hydrochloride (37.5 mg) once daily or a placebo three times a day plus phentermine hydrochloride (37.5 mg) once daily. The primary study outcome was sterol metabolism. Results: The experimental group exhibited significantly decreased metabolic signatures of serum sterols, free cholesterol, sitosterol, 7α-hydroxycholesterol (7α-OHC), and 7β-OHC at 12 weeks. The experimental group also exhibited significantly decreased metabolic ratios of sitosterol and 7α-OHC to cholesterol at 12 weeks. Regarding changes in sterol signatures from baseline to 6-month follow-up, free cholesterol, plant sterols, and cholesterol precursors tended to decrease with weight loss during the intervention and increase again as the weight was regained in both groups. Conclusion: Orlistat treatment improves oxysterol metabolism in overweight and obese adults. Our findings support that orlistat plays a crucial role in the process of endothelial dysfunction and atherosclerosis via oxysterol modulation.

Frontiers in endocrinology 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

Cheng, Dongping; Yan, Xianhang; Pu, Yueqi; Shen, Jing; Xu, Xiaoliang; Yan, Jizhong published the artcile< 2,3-Dichloro-5,6-dicyano-1,4-benzoquinone (DDQ)-Mediated Tandem Oxidative Annulation for Preparing 2,2-Disubstituted 2,3-Dihydroquinazolin-4(1H)-ones>, Product Details of C7H7BrN2O, the main research area is aminobenzamide diarylpropene DDQ tandem oxidative annulation; dihydroquinazolinone preparation.

An efficient tandem oxidative annulation for the synthesis of 2,2-disubstituted 2,3-dihydroquinazolin-4(1H)-ones via DDQ-mediated dual cross-dehydrogenative-coupling (CDC) reactions is described. This transformation proceeds from easily available o-aminobenzamides and 1,3-diarylpropenes under mild conditions, and the corresponding products are obtained in moderate to excellent yields.

European Journal of Organic Chemistry published new progress about Aryl alkenes Role: RCT (Reactant), RACT (Reactant or Reagent) (1,3-diarylpropenes). 112253-70-0 belongs to class amides-buliding-blocks, and the molecular formula is C7H7BrN2O, Product Details of C7H7BrN2O.

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