Month: October 2022

Esmail, Vian Ahmed Wasta; Mohammed, Mohammed Omer; Al-Nimer, Marwan S M published the artcile< Short-term orlistat therapy improves fatty infiltration indices and liver fibrosis scores in patients with non-alcoholic fatty liver disease and metabolic syndrome.>, SDS of cas: 96829-58-2, the main research area is Lipid indices; Liver fibrosis scores; Metabolic syndrome; Non-alcoholic fatty liver disease.

BACKGROUND AND STUDY AIMS: Patients with non-alcoholic fatty liver disease (NAFLD) exhibit features of metabolic syndrome, including a high body mass index, central obesity, high blood pressure, and abnormal lipid profile values. Orlistat, an intestinal lipase enzyme inhibitor, improves insulin resistance. We aimed to investigate the effects of short-term therapy with orlistat on the components of metabolic syndrome associated with NAFLD and explore its effect on liver fibrosis scores. PATIENTS AND METHODS: An open-label placebo-controlled clinical study using orlistat for 12 weeks was carried out on 50 patients with NAFLD. They were divided into a placebo group (Group I) and an orlistat treatment group (120 mg per day, Group II). The diagnosis of NAFLD was made by ultrasonography and laboratory investigations. Anthropometric and blood pressure measurements and hepatic liver enzymes, fasting lipids, and blood glucose levels were determined before and after treatment. Lipid indices including cholesterol (Chol-I), triglyceride (TG-I), triglyceride-glucose (TYG-I), and the scores for lipid fibrosis using the NAFLD fibrosis score (NFS) and Fibrosis-4 score (Fib-4) were also determined. RESULTS: Orlistat significantly improved the anthropometric and metabolic indices (TG-I, TYG-I) and liver enzymes. Orlistat demonstrated a favorable impact on the NAS and Fib-4 scores for liver fibrosis. CONCLUSION: Orlistat improves the components of metabolic syndrome, leading to the improvement of insulin resistance and thereby improves fatty infiltration of the liver. To a lesser extent, orlistat improved the liver fibrosis scores.

Arab journal of gastroenterology : the official publication of the Pan-Arab Association of Gastroenterology published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, SDS of cas: 96829-58-2.

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

Dean, Conor; Rajkumar, Sundaram; Roesner, Stefan; Carson, Nessa; Clarkson, Guy J.; Wills, Martin; Jones, Matthew; Shipman, Michael published the artcile< Readily accessible sp3-rich cyclic hydrazine frameworks exploiting nitrogen fluxionality>, Synthetic Route of 1192620-83-9, the main research area is cyclic hydrazine preparation enantioselective principal moment inertia.

Here, a strategy for the creation of sp3-rich, non-planar heterocyclic scaffolds e.g., I suitable for drug discovery is described that obviates the need to generate multiple stereogenic centers with independent control. Asym. transfer hydrogenation using a tethered Ru-catalyst is used to efficiently produce a range of enantiopure cyclic hydrazine building blocks (up to 99% ee) e.g., I. Iterative C-N functionalization at the two nitrogen atoms of these compounds produces novel hydrazine and hydrazide based chem. libraries e.g., I. Wide chem. diversification is possible through variation in the hydrazine structure, use of different functionalization chemistries and coupling partners, and controlled engagement of each nitrogen of the hydrazine in turn. Principal Moment of Inertia (PMI) anal. of this small hydrazine library reveals excellent shape diversity and three-dimensionality. NMR and crystallog. studies confirm that the frameworks prefer to orient their substituents in three-dimensional space under the control of a single stereogenic center through exploitation of the fluxional behavior of the two nitrogen atoms.

Chemical Science published new progress about Aromatic alcohols 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, Synthetic Route of 1192620-83-9.

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

Yamaguchi, Hachiro; Tsujihara, Kenji published the artcile< Sulfonyl diamide derivatives. II. Amide exchange reaction of sulfonyl diamide>, Application In Synthesis of 25999-04-6, the main research area is exchange amine sulfonyl diamide.

In the amide exchange reaction of sulfonyl diamide with amines, the reaction with primary amines under anhydrous conditions gave monosubstituted products at first and then N,N’-disubstituted products. However, the reaction with primary amines under aqueous conditions and with secondary amines in the absence of water gave only mono substituted products. The first intermediates were N-monosubstituted sulfonyl diamides in the case of primary amines, and N,N’-disubstituted sulfonyl diamides in the case of secondary amines. 1,3-Disubstituted imidodisulfonyl diamide was isolated as an intermediate from the reaction under anhydrous conditions, and 1-monosubstituted imidodisulfonyl diamide was isolated as an intermediate from the reaction under aqueous conditions. The former reacted with anhydrous primary amine to give N,N’-disubstituted sulfonyl diamide. The latter reacted with aqueous primary amine to give N-monosubstituted sulfonyl diamide.

Nippon Kagaku Kaishi 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, Application In Synthesis of 25999-04-6.

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

Liu, Tengfei; Yu, Junming; Ge, Chao; Zhao, Fangyu; Chen, Jing; Miao, Chunxiao; Jin, Wenjiao; Zhou, Qingqing; Geng, Qin; Lin, Hechun; Tian, Hua; Chen, Taoyang; Xie, Haiyang; Cui, Ying; Yao, Ming; Xiao, Xiuying; Li, Jinjun; Li, Hong published the artcile< Sperm associated antigen 4 promotes SREBP1-mediated de novo lipogenesis via interaction with lamin A/C and contributes to tumor progression in hepatocellular carcinoma>, Reference of 96829-58-2, the main research area is Hepatocellular carcinoma; Lamin A/C; Lipogenesis; SPAG4; SREBP1.

Hepatocellular carcinoma (HCC) is a highly malignant tumor and its progression is associated with altered lipid metabolism in precancerous lesions, such as non-alc. fatty liver disease. Here, we identified sperm associated antigen 4 (SPAG4), and explored its oncogenic role in HCC progression. Database anal. and immunohistochem. indicated increased level of SPAG4 in HCC tissues which was of prognostic value. Gain/loss-of-function experiments showed that SPAG4 exerted oncogenic roles in HCC growth both in vitro and in vivo. RNA sequencing revealed activation of a lipogenic state and SREBP1-mediated pathway following SPAG4 overexpression. Mechanistically, the N-terminal region of SPAG4 bound to lamin A/C, which increased SREBP1 expression, nuclear translocation, and transcriptional activity. Treatment with orlistat, a lipid synthesis inhibitor, reversed SPAG4-mediated oncogenic effects, and its efficacy varied with SPAG4 level. The effect of orlistat was further amplified when combined with sorafenib in tumor xenograft mouse models. Our study provides evidence that SPAG4 mediates HCC progression by affecting lipid metabolism Administration of orlistat combined with sorafenib reverses SPAG4-mediated oncogenesis in HCC cells and ectopic xenograft tumors in mice, suggesting that this pathway represents a potential target for HCC treatment.

Cancer Letters (New York, NY, United States) published new progress about 96829-58-2. 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

Moukha-Chafiq, Omar; Reynolds, Robert C. published the artcile< Synthesis and General Biological Activity of a Small Adenosine-5'-(Carboxamide and Sulfanilamide) Library>, Safety of 3-Fluorobenzenesulfonamide, the main research area is preparation screening adenosine carboxamide sulfanilamide library; Adenosine peptide analogs; specific or general biological activities.

A small library of fifty-five adenosine peptide analogs was synthesized, under the Pilot Scale Library (PSL) Program of the NIH Roadmap initiative, from 2′,3′-O-isopropylideneadenosine-5′-carboxylic acid . The coupling of amine or sulfanilamide reactants to the free 5′-carboxylic acid moiety of , in automated solution-phase fashion, led after acid-mediated hydrolysis to target compounds in good yields and high purity. No marked anticancer or antimalarial activity was noted on preliminary cellular testing. Initial screening through the MLPCN program, however, indicates that these analogs may show diverse and interesting biol. activities.

Nucleosides, Nucleotides & Nucleic Acids published new progress about Antimalarials. 1524-40-9 belongs to class amides-buliding-blocks, and the molecular formula is C6H6FNO2S, Safety of 3-Fluorobenzenesulfonamide.

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

Qu, Zhen; Ren, Yuning; Shen, Hongyu; Wang, Huihui; Shi, Lijie; Tong, Deyong published the artcile< Combination Therapy of Metastatic Castration-Recurrent Prostate Cancer: Hyaluronic Acid Decorated, Cabazitaxel-Prodrug and Orlistat Co-Loaded Nano-System.>, Related Products of 96829-58-2, the main research area is cabazitaxel; hyaluronic acid; metastatic castration-recurrent prostate cancer; orlistat; prodrug technology.

PURPOSE: Prostate cancer (PCa) is the second leading cause of cancer-related death among men in developed countries. Cabazitaxel (CBZ) is recommended as one of the most active chemotherapy agents for PCa. This study aimed to develop a hyaluronic acid (HA) decorated, cabazitaxel-prodrug (HA-CBZ) and orlistat (ORL) co-loaded nano-system against the prostate cancer in vitro and in vivo. METHODS: Cabazitaxel-prodrug was firstly synthesized by conjugating HA with CBZ through the formation of ester bonds. HA contained ORL and CBZ prodrug co-loaded lipid-polymer hybrid nanoparticles (ORL/HA-CBZ/LPNs) were constructed and characterized in terms of particle size, zeta potential, drug loading capacity and stability. The antitumor efficiency and systemic toxicity of LPNs were evaluated in vitro and in vivo. RESULTS: The resulting ORL/HA-CBZ/LPNs were 150.9 nm in particle size with narrow distribution and high entrapment efficiency. The minimum combination index of 0.57 was found at a drug ratio of 1:2 (ORL:HA-CBZ, w/w) in the drug co-loaded formulations, indicating the strongest synergism effect. ORL/HA-CBZ/LPNs demonstrated an enhanced in vitro and in vivo antitumor effect compared with single drug loaded LPNs and free drug formulations. CONCLUSION: ORL/HA-CBZ/LPNs showed remarkable synergism cytotoxicity and the best tumor inhibition efficiency in mice with negligible systemic toxicity. ORL/HA-CBZ/LPNs can be highly useful for targeted prostate cancer therapy.

Drug design, development and therapy published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Related Products of 96829-58-2.

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

Krishnamurthy, Vijay M.; Bohall, Brooks R.; Kim, Chu-Young; Moustakas, Demetri T.; Christianson, David W.; Whitesides, George M. published the artcile< Thermodynamic parameters for the association of fluorinated benzenesulfonamides with bovine carbonic anhydrase II>, COA of Formula: C6H6FNO2S, the main research area is thermodn crystal structure fluorinated benzenesulfonamide carbonic anhydrase.

This paper describes a calorimetric study of the association of a series of seven fluorinated benzenesulfonamide ligands (C6HnF5-nSO2NH2) with bovine carbonic anhydrase II (BCA). Quant. structure-activity relationships between the free energy, enthalpy, and entropy of binding and pKa and logP of the ligands allowed the evaluation of the thermodn. parameters in terms of the two independent effects of fluorination on the ligand: its electrostatic potential and its hydrophobicity. The parameters were partitioned to the three different structural interactions between the ligand and BCA: the ZnII cofactor-sulfon-amide bond (≈65% of the free energy of binding), the hydrogen bonds between the ligand and BCA (≈10%), and the contacts between the Ph ring of the ligand and BCA (≈25%). Calorimetry revealed that all of the ligands studied bind in a 1:1 stoichiometry with BCA; this result was confirmed by 19F NMR spectroscopy and X-ray crystallog. (for complexes with human carbonic anhydrase II).

Chemistry – An Asian Journal published new progress about Conformation. 1524-40-9 belongs to class amides-buliding-blocks, and the molecular formula is C6H6FNO2S, COA of Formula: C6H6FNO2S.

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

Wang, Yanwei; Liu, Hongxin; Li, Bin; Wang, Baiquan published the artcile< Rhodium(III)-catalyzed Intermolecular Unactivated Secondary C(sp3)-H Bond Amidation Directed by 3,5-dimethylpyrazole>, Application of C6H6ClNO2S, the main research area is pyrazole carboxamide preparation; sulfonyl urea preparation; alkylamide sulfonamine amidation rhodium catalyst.

A Rh(III)-catalyzed intermol. unactivated secondary C(sp3)-H bond amidation via nitrene insertion directed by 3,5-dimethylpyrazole has been reported. This procedure tolerates a broad substrate scope including chain and cyclic N-alkylamides, e.g., N-(sec-butyl)-3,5-dimethyl-1H-pyrazole-1-carboxamide. Notably, the directing group 3,5-dimethylpyrazole of chain N-alkylamide substrates could be easily removed via cascade intermol. amidation and intramol. cyclization in one-pot affording sulfonylureas such as I by increasing the reaction temperature

Advanced Synthesis & Catalysis published new progress about Amidation (regioselective). 6961-82-6 belongs to class amides-buliding-blocks, and the molecular formula is C6H6ClNO2S, Application of C6H6ClNO2S.

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

Suleiman, Joseph Bagi; Nna, Victor Udo; Othman, Zaidatul Akmal; Zakaria, Zaida; Bakar, Ainul Bahiyah Abu; Mohamed, Mahaneem published the artcile< Orlistat attenuates obesity-induced decline in steroidogenesis and spermatogenesis by up-regulating steroidogenic genes>, Computed Properties of 96829-58-2, the main research area is orlistat spermatogenesis steroidogenesis epididymal malondialdehyde; DNA fragmentation; high-fat diet; obesity; orlistat; spermatogenesis; steroidogenesis.

We explored the possible preventive/therapeutic effects of orlistat (a medication prescribed for weight loss) on obesity-induced steroidogenesis and spermatogenesis decline. Twenty-four adult male Sprague Dawley rats weighing 250-300 g were randomized into four groups (n = 6/group), namely; normal control, high-fat diet, high-fat diet plus orlistat preventive group and high-fat diet plus orlistat treatment group. Orlistat was either concurrently administered with high-fat diet for 12 wk or administered from week 7-12 post- high-fat diet feeding. Obesity increased serum leptin and decreased adiponectin levels, decreased serum and intra-testicular levels of FSH, luteinising hormone and testosterone, sperm count, motility, viability, normal morphol. and epididymal antioxidants, but increased epididymal malondialdehyde level and sperm nDNA fragmentation. Further, the levels of steroidogenic acute regulatory protein protein and enzymic activities of CYP11A1, 3β-hydroxysteroid dehydrogenase and 17β-hydroxysteroid dehydrogenase were also significantly decreased in the testes of the high-fat diet group. Orlistat attenuated impaired spermatogenesis and steroidogenesis decline by up-regulating steroidogenic genes. This may not be unconnected to its significant effect in lowering serum leptin levels, since the hormone is known to dampen fertility potential. Therefore, orlistat may improve fertility potential in overweight/obese men.

Andrology published new progress about Adiponectins Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 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

Marques-Vidal, Pedro published the artcile< Comparison of lifestyle changes and pharmacological treatment on cardiovascular risk factors>, Reference of 96829-58-2, the main research area is cardiovascular disease dyslipidemia diabetes hypertension LDL HDL orlistat glucose; diabetes; hypertension; lipoproteins and hyperlipidaemia; smoking cessation.

Cardiovascular disease is the leading cause of morbidity mortality in Europe and world wide. The major modifiable risk afactors are Obesity, Hypertension, Smoking, Dyslipidemia and Diabetes. In this paper, we will make a overview of the effect of life style changes on CVD rik factors and compare them with the effect of pharmacoogical treatment. Weight loss led to a consistent reduction in BP level, smoking cessation leads to an increase in BP levels. Potassium supplementation in Hypertensive subjects decreases BP levels. Any weight loss decreased low-d. lipoprotein(LDL)-cholesterol but had no effect on triglycerides. Drug induced weight loss led to a slight decrease in lipid levels, Orlistat exerting a stronger effect than other drugs. Weight loss decreased both plasma glucose and HbA1c. The risk factors of diabetes increased in the first 3 years after smoking cessation. A low-carbohydrate diet reduced HbA1c together with SBP and triglyceride levels, while increasing HDL-cholesterol levels in patients with diabetes. Adequately implemented, changes in lIfestyle acheive reductions in cardiovascular risk factors close to those of single-drug therapies.

Heart (London, United Kingdom) published new progress about Blood triglycerides Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 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