Category: amides-buliding-blocks

Singh, Shashi Kala; Yende, Ashutosh S.; Ponnusamy, Kalaiarasan; Tyagi, Rakesh K. published the artcile< A comprehensive evaluation of anti-diabetic drugs on nuclear receptor PXR platform>, Electric Literature of 94-20-2, the main research area is antidiabetic drug screening PXR; Anti-diabetic drugs; Drug screening; Promoter-reporter; Small molecules; Stable cell line.

Pregnane & Xenobiotic Receptor (PXR), one of the members of nuclear receptor superfamily, acts as a ‘master-regulator’ of drug metabolism and disposition machinery (DMD). Activation of PXR enables detoxification and elimination of toxic xenobiotics/endobiotics, and defends the authors’ body against chem. insults. On the contrary, PXR activation also imposes a serious concern for drug-drug interactions (DDIs). Such DDIs could either decrease the efficacy or lead to accumulation of co-administered drugs at toxic level. Therefore, it is desirable that during drug development process the small drug mols. are screened on PXR-platform prior to their clin. trial and prevent late stage failures. In view of this, the authors have selected a group of anti-diabetic drug mols. to examine if the success and potential failure of small mol. modulators can be pre-assessed and judiciously correlated on PXR platform. For this purpose, the authors have examined the PXR activation potential of the selected anti-diabetic drugs. Subsequent to screening of these anti-diabetic drugs, the authors elaborated the study further with rosiglitazone and pioglitazone (thiazolidinediones, TZDs) which are oral anti-diabetic formulations and have been in controversy owing to their association with cardiotoxicity and bladder cancer resp. The authors’ study revealed that some of the selected anti-diabetic drugs possess PXR activation potential, implying that these can up-regulate the expression of CYP3A4, UGT1A1, MDR1 and thereby can be predicted to inflict undesirable consequences.

Toxicology In Vitro published new progress about Animal cell line (HepXREM). 94-20-2 belongs to class amides-buliding-blocks, and the molecular formula is C10H13ClN2O3S, Electric Literature of 94-20-2.

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

Zhao, Yichao; Bruce, Lachlan David; Jin, Jianwen; Xia, Bo; Chan, Philip Wai Hong published the artcile< Copper catalyzed N-formylation of α-silyl-substituted tertiary N-alkylamines by air>, HPLC of Formula: 6280-57-5, the main research area is dialkylaminomethyl trimethylsilane copper catalyst formylation; dialkyl formylamine preparation.

A site-selective method to prepare N-formyl amines efficiently that relies on the copper(I)-catalyzed oxidation of α-silyl-substituted tertiary N-alkylamines by air at room temperature was described. The oxidative protocol was shown to exhibited excellent functional group tolerance as it was applicable to a wide variety of amine substrates and a number of bioactive mols. and natural products. Moreover, it delinates a ligand- and additive-free amine oxidation process mediated by a low-cost metal salt with oxygen from air taking on the role of both the terminal oxidant and as part of the formylation reagent, which was unprecedented in copper catalysis. It also offered the first synthetic method that can selectively generate α-amino radical species as reactive intermediates from α-silylamines under non-photochem. reaction conditions.

Green Chemistry published new progress about Formamides Role: SPN (Synthetic Preparation), PREP (Preparation) (N,N-dialkyl). 6280-57-5 belongs to class amides-buliding-blocks, and the molecular formula is C17H35NO, HPLC of Formula: 6280-57-5.

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

Pant, Amar D.; Ruhela, R.; Limje, C.; Anil Kumar, S.; Singh, A. K.; Kumar, Suja A.; Sugandhi, S.; Kain, V.; Tomar, B. S. published the artcile< Evaluation of BenzoDODA grafted polymeric resin for rapid and reliable assaying of plutonium in sediment samples>, Category: amides-buliding-blocks, the main research area is plutonium BenzoDODA grafted polymeric resin sediment pollution; Alpha spectrometry; BenzoDODA grafted resin; Extraction chromatography; Plutonium; SPEC; Sediments.

The paper reports a new rapid radioanal. procedure for the determination of plutonium (Pu) in sediments by solid phase extraction chromatog. (SPEC) using Bis-(2-ethylhexyl) carbamoyl methoxy phenoxy-bis-(2-ethylhexyl) grafted resin, abbreviated as Benzodioxodiamide (BenzoDODA) grafted resin. The resin was synthesized and evaluated for its sorption behavior towards Pu in batch and column mode to determine its efficacy for selective recovery of Pu from sediment samples. The anal. procedure was based on the radiochem. separation of samples by acid digestion, followed by preconcentration of actinides by co-precipitation with Fe(OH)3 and finally selective recovery of Pu by SPEC using a column filled with BenzoDODA grafted resin. Pu was then radiometrically assayed by preparing alpha disk sources with electro-deposition followed by alpha spectrometry. The method was further validated with IAEA reference materials. This method gives reliable and reproducible results for the activity concentration of Pu in sediment samples within 24 h.

Journal of Environmental Radioactivity published new progress about Acid digestion. 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

Asano, Toru; Yoshikawa, Tomohiro; Nakamura, Hiroyuki; Uehara, Yoshimasa; Yamamoto, Yoshinori published the artcile< Synthesis and biological evaluation of benzamides and benzamidines: structural requirement of a pyrimidine ring for inhibition of EGFR tyrosine kinase>, HPLC of Formula: 5004-88-6, the main research area is benzamide benzamidine preparation epidermal growth factor receptor tyrosine kinase.

The benzamides I (R = cyclohexyl, 3-BrC6H4, 2-pyridyl, etc.) benzamidines II (R1 = 3-BrC6H4, 3-ClC6H4, 3-MeOC6H4, 3-chloro-4-fluorophenyl), and protected benzamidines (III, same R1) were synthesized as the mimics of 4-anilinoquinazolines, which possess inhibition of epidermal growth factor receptor (EGFR) tyrosine kinase, and were tested for cytotoxicity toward A431 and inhibitory activity toward autophosphorylation by the enzyme assay. High cell growth inhibition was observed in a series of the cyclic benzamides III: the IC50 values are 0.09-0.32 mM. The benzamidines III (R1 = 3-BrC6H4, 3-ClC6H4) exhibited high inhibition of EGFR tyrosine kinase at a 1.0 μM concentration, although the benzamides I and the benzamidines II did not show significant kinase inhibition at a 10 μM concentration

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, HPLC of Formula: 5004-88-6.

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

Zhang, Youcan; Yin, Zhiping; Wu, Xiao-Feng published the artcile< Copper-catalyzed carbonylative synthesis of β-homoprolines from N-fluoro-sulfonamides>, Application In Synthesis of 6961-82-6, the main research area is amino acid homoproline synthesis solvent effect; fluoro sulfonamide carbonylation copper catalyst; carbonylation mechanism intramol cyclization free carbon radical.

A new methodol. for the carbonylative transformation of N-fluoro-sulfonamides into N-sulfonyl-β-homoproline esters has been described. In the presence of a catalytic amount of Cu(OTf)2, a range of β-homoproline derivatives were prepared in moderate to good yield. The reaction proceeds via the intramol. cyclization and intermol. carbonylation of a free carbon radical. Notably, this procedure offers the possibility to build potential functionalized bioactive mols.

Organic Letters published new progress about Amino acids Role: SPN (Synthetic Preparation), PREP (Preparation). 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

Sridhar, S. N. C.; Palawat, Saksham; Paul, Atish T. published the artcile< Design, synthesis, biological evaluation and molecular modelling studies of indole glyoxylamides as a new class of potential pancreatic lipase inhibitors>, Synthetic Route of 96829-58-2, the main research area is indole glyoxylamides pancreas lipase inhibition mol dynamics antiobesity; Indole glyoxylamides; Inhibition kinetics; Molecular dynamics; Orlistat; Pancreatic lipase.

A series of eighteen indole glyoxylamide analogs were synthesized, characterized and evaluated for their pancreatic lipase inhibitory activity. Porcine pancreatic lipase (Type II) was used with 4-nitrophenyl butyrate (as substrate) for the in vitro assay. Compound 8f exhibited competitive inhibition against pancreatic lipase with IC50 value of 4.92 μM, comparable to that of the standard drug, orlistat (IC50 = 0.99 μM). Compounds 7a-i and 8a-i were subjected to mol. docking into the active site of human PL (PDB ID: 1LPB) wherein compound 8f possessed a potential MolDock score of -153.037 kcal/mol. Mol. dynamics simulation of 8f complexed with pancreatic lipase, confirmed the role of aromatic substitution in stabilizing the ligand through hydrophobic interactions (maximum observed RMSD = 3.5 Å).

Bioorganic Chemistry published new progress about Amides Role: BSU (Biological Study, Unclassified), PRP (Properties), SPN (Synthetic Preparation), BIOL (Biological Study), PREP (Preparation) (indole glyoxylamides). 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Synthetic Route of 96829-58-2.

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

Khaibrakhmanova, Diliara; Nikiforova, Alena; Sedov, Igor published the artcile< Binding constants of drug-albumin complexes from DSC measurements>, Application In Synthesis of 94-20-2, the main research area is tolbutamide albumin differential scanning calorimetry.

The DSC technique is applied for quantification of the thermodn. binding constants in protein-ligand systems. For this purpose, the thermograms of protein denaturation are recorded at different ligand concentrations The observed dependence of the temperature shift of denaturation peak on ligand concentration is fitted to the two-state model of denaturation. First and second sequential binding constants of drugs tolbutamide, chloropropamide, phenylbutazone, meloxicam, and ampicillin with bovine serum albumin (BSA) are determined Ampicillin shows weak binding with BSA, while four other drugs bind quite tightly. Phenylbutazone and meloxicam bind to two different sites of BSA mol. with similar affinity, while tolbutamide and chloropropamide have higher affinities to one of the binding sites. We extensively review the available data on albumin binding of these drugs determined using different exptl. methods, which are in strong disagreement with each other. DSC measurements provide reproducible denaturation curves that can be a source of data on the protein-ligand binding including the second binding constant inaccessible to some other methods.

Thermochimica Acta published new progress about Bovine serum albumin Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 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

Šrámková, Petra; Fried, Martin published the artcile< Antiobesity drugs before and after bariatric surgery - how to make the best use of them.>, Formula: C29H53NO5, the main research area is bariatric surgery; liraglutide; multifunctional peptides; naltrexone-bupropion; obesity; preoperative weight reduction; set point; weight gain after bariatric surgery.

Obesity as a chronic, serious, and progressive lifelong disease requires an active approach to treatment. Treatment means necessary adjustment of lifestyle with suitable regular physical activity, including pharmacological or bariatric support. Current pharmacological treatment can be an effective helper in the preparation for the surgical treatment of obesity (bariatric and metabolic operations), and in greater adherence of the patient to the necessary regime changes in life and in preoperative weight reduction. With the lapse of time after surgical treatment, in many cases we indicate the start of pharmacological treatment if the weight increases again. We do not yet know the appropriate types of patients and the exact indications for specific therapeutic modalities – a suitable antiobesity drug or type of bariatric surgery. The best long-term results come from a combination of at least two of these options, along with a lifestyle change. Among modern antiobesity drugs, there are naltrexone-bupropion and liraglutide. Orlistat can be mentioned from older ones.

Casopis lekaru ceskych published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Formula: C29H53NO5.

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

Kim, Seongkyu; Kim, Je-Hein; Seok, Su Hyun; Park, Eun-Seok published the artcile< Anti-obesity effect with reduced adverse effect of the co-administration of mini-tablets containing orlistat and mini-tablets containing xanthan gum: In vitro and in vivo evaluation>, HPLC of Formula: 96829-58-2, the main research area is formulation tablet orlistat xanthan gum obesity; Anti-obesity; Oily leakage; Oily stool; Orlistat; Reduced adverse effect; Xanthan gum.

The purpose of this study was to develop an oral dosage form of orlistat for the treatment of obesity with reduced adverse effects, for example, fatty and oily stool that have been reported to be associated with the mechanism of action of orlistat. Based on the in vitro results obtained in this study, xanthan gum was selected as an oil-entrapping agent. Thus, the co-administration of mini-tablets containing orlistat and mini-tablets containing xanthan gum was proposed as the optimized dosage form for orlistat. The prepared mini-tablets showed an equivalent drug release profile with a similarity factor value, f2, more than 50 to that of com. marketed orlistat immediate-release capsules, Xenical capsules. In addition, the optimized formulation also showed the in vivo anti-obesity effects similar to those of Xenical capsules. In particular, the anal. of feces excreted by Sprague-Dawley rats revealed that the optimized formulation resulted in significantly less oily stool, steatorrhea, than Xenical capsules (P < 0.05). Consequently, the proposed formulation, the co-administration of mini-tablets containing orlistat and mini-tablets containing xanthan gum, may be considered as a promising anti-obesity treatment with reduced adverse effects related to orlistat. International Journal of Pharmaceutics (Amsterdam, Netherlands) published new progress about Antiobesity agents. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, HPLC of Formula: 96829-58-2.

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

Cioccoloni, Giorgia; Aquino, Angelo; Notarnicola, Maria; Caruso, Maria Gabriella; Bonmassar, Enzo; Zonfrillo, Manuela; Caporali, Simona; Faraoni, Isabella; Villiva, Cristina; Fuggetta, Maria Pia; Franzese, Ornella published the artcile< Fatty acid synthase inhibitor orlistat impairs cell growth and down-regulates PD-L1 expression of a human T-cell leukemia line>, Name: (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate, the main research area is orlistat fatty acid synthase programmed death ligand expression leukemia; FASN; PD-L1; leukemia.

Fatty Acid Synthase (FASN) is responsible for the de novo synthesis of fatty acids, which are involved in the preservation of biol. membrane structure, energy storage and assembly of factors involved in signal transduction. FASN plays a critical role in supporting tumor cell growth, thus representing a potential target for anti-cancer therapies. Moreover, this enzyme has been recently associated with increased PD-L1 expression, suggesting a role for fatty acids in the impairment of the immune response in the tumor microenvironment. Orlistat, a tetrahydrolipstatin used for the treatment of obesity, has been reported to reduce FASN activity, while inducing a sensible reduction of the growth potential in different cancer models. We have analyzed the effect of orlistat on different features involved in the tumor cell biol. of the T-ALL Jurkat cell line. In particular, we have observed that orlistat inhibits Jurkat cell growth and induces a perturbation of cell cycle along with a decline of FASN activity and protein levels. Moreover, the drug produces a remarkable impairment of PD-L1 expression. These findings suggest that orlistat interferes with different mechanisms involved in the control of tumor cell growth and can potentially contribute to decrease the tumor-associated immune-pathogenesis.

Journal of Chemotherapy (Abingdon, United Kingdom) published new progress about Antitumor 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