Month: October 2022

Laha, Joydev K.; Jethava, Krupal P.; Tummalapalli, K. S. Satyanarayana; Sharma, Sheetal published the artcile< Synthesis of mono-N-sulfonylimidazolidines by a 1,3-dipolar cycloaddition strategy, as an alternative to selective N-sulfonylation and their ring cleavage to afford 1,2-diamines>, Synthetic Route of 1524-40-9, the main research area is sulfonyl diamine preparation; monosulfonylimidazolidine preparation ring cleavage; azomethine ylide sulfonylimine dipolar cycloaddition; sulfamidate fused imidazolidine preparation; sulfonylketimine azomethine ylide dipolar cycloaddition.

Mono-N-sulfonylimidazolidines I [R1 = H, 4-Me, 4-MeO, 2-OEt, 2,4,6-Me3; R2 = Ts, SO2CH2Ph, 3-FC6H4SO2; R3 = H, 3-MeO, R4 = H, Me; X = bond, CHR4] were synthesized via 1,3-dipolar cycloaddition between nonstabilized azomethine ylides and N-sulfonylimines. The enhanced reactivity of N-sulfonylimines as dipolarophiles toward azomethine ylides largely eliminated possible Michael addition and favored 1,3-dipolar cycloaddition Sulfamidate fused imidazolidines II [R5 = H, Cl; Y = CH2, CH2CH2] were obtained via 1,3-dipolar cycloaddition between azomethine ylides and N-sulfonylketimine. Nucleophile-dependent ring cleavage of N-sulfonylimidazolidines I produced synthetically useful mono-N-sulfonyl-1,2-diamines III [R6 = H, Me, MeO; R7 = H, Me; R8 = Bn, 3-MeOC6H4CH2]. Ring cleavage accompanied by CH2 extrusion, yielded N-[2-(Benzylamino)-1-(p-tolyl)ethyl]-4-methylbenzenesulfonamide III [R6 = Me; R7 = H; R8 = Bn], occurred on treatment with TBAF, whereas N-{2-[Benzyl(methyl)amino]-1-(4-methoxyphenyl)ethyl}-4-methylbenzenesulfonamide III [R6 = MeO; R7 = Me; R8 = Bn] and N-{2-[(3-Methoxybenzyl)(methyl)amino]-1-phenylethyl}-4-methylbenzenesulfonamide III [R6 = H; R7 = Me; R8 = 3-MeOC6H4CH2] were produced on treatment with LAH.

European Journal of Organic Chemistry published new progress about 1,3-Dipolar cycloaddition reaction. 1524-40-9 belongs to class amides-buliding-blocks, and the molecular formula is C6H6FNO2S, Synthetic Route of 1524-40-9.

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

Bochenska, Maria; Banach, Robert; Zielinska, Anna; Kravtsov, Victor Ch. published the artcile< Lower rim substituted tert-butylcalix[4]arenes (I). The structure and complexing properties in ion-selective PVC membrane electrodes>, Computed Properties of 5326-82-9, the main research area is calixarene lower rim amide substituted preparation; ion selective PVC membrane electrode calixarenamide.

Di- and tetraamide tert-butylcalix[4]arenes were synthesized and described. Their ionophoric properties were studied in liquid membrane ion-selective electrodes. The correlation between the chem. structure (conformation in solution determined by 1H NMR) and potentiometric ion-selectivity and complex formation constant have been studied. The PVC membrane electrodes based on tetraamides I (R = n-Bu2N, morpholino, 1-piperidinyl, CH3(CH2)6MeN) show high sodium selectivity and are stable and long lasting. Disubstituted amides II (R = Et2N, n-Pr2N, i-Pr2N, n-Bu2N, i-Bu2N, morpholino, 1-piperidinyl) are selective for larger and more lipophilic ions, e.g., guanidinium ion. The crystal structure of the diamide II (R = n-Bu2N) was determined by single crystal X-ray anal. Crystals of II (R = n-Bu2N) are triclinic, space group P-1, with: a = 16,669(8), b = 17.795(10), c = 20.984(8) Å, α = 91.08(4)°, γ = 90.73(4)° and Z = 4. Ionophore II (R = n-Bu2N) possesses a distorted cone conformation and is substituted at the proximal phenol rings.

Journal of Inclusion Phenomena and Macrocyclic Chemistry published new progress about Conformation. 5326-82-9 belongs to class amides-buliding-blocks, and the molecular formula is C10H20ClNO, Computed Properties of 5326-82-9.

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

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

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

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

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

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