Category: amides-buliding-blocks

Parekh, Vimal; Ramsden, James A.; Wills, Martin published the artcile< Asymmetric transfer hydrogenation of quinolines using tethered Ru(II) catalysts>, Recommanded Product: Chloro[N-[(1R,2R)-1,2-diphenyl-2-[[3-(η6-phenyl)propyl]amino-κN]ethyl]-4-methylbenzenesulfonamidato-κN]ruthenium, the main research area is asym transfer hydrogenation quinoline ruthenium catalyst.

The first report of an asym. transfer hydrogenation, in formic acid/triethylamine, of quinolines is described. Using a Ru(II) catalyst containing a 4-carbon tether, products of up to 73% ee were formed, while a Rh(III)-tethered catalyst gave products of up to 94% ee.

Tetrahedron: Asymmetry published new progress about Enantioselective synthesis. 1192620-83-9 belongs to class amides-buliding-blocks, and the molecular formula is C30H31ClN2O2RuS, Recommanded Product: 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

Belenguer, Ana M.; Cruz-Cabeza, Aurora J.; Lampronti, Giulio I.; Sanders, Jeremy K. M. published the artcile< On the prevalence of smooth polymorphs at the nanoscale: implications for pharmaceuticals>, SDS of cas: 94-20-2, the main research area is polymorph D sorbitol chlorpropamide acetonitrile anthranilic acid nanoscale crystallite.

We demonstrate, for four different systems of pharmaceutical relevance, that ball mill grinding leads to different polymorphic transformations depending on the milling conditions. In all four cases, the com. polymorph converts to a different polymorph upon ball-mill neat grinding (NG). This transformation can be reversed by grinding the so obtained polymorph in the presence of small amounts of solvent (LAG), leading back to the com. polymorph. Scherrer particle size determinations reveal that NG conditions almost always lead to smaller particle sizes in the nanometer length scales. Computational studies confirm that polymorphs obtained by the specific ball mill LAG conditions reported correspond to the lowest lattice energy forms. Our study further confirms our earlier conclusions that, at the nanoscale, polymorphs with higher lattice energies can become the thermodynamically stable forms if their surfaces are more stable than those of the polymorphs obtained by LAG. We found, however, one exception to this trend in D-sorbitol. We observe that polymorphs with smoother surfaces (low roughness) are usually the ones observed by NG. This observation points to a link between surface roughness and surface stability.

CrystEngComm published new progress about Cell morphology. 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

Tocco, Graziella; Esposito, Francesca; Caboni, Pierluigi; Laus, Antonio; Beutler, John A.; Wilson, Jennifer A.; Corona, Angela; Le Grice, Stuart F. J.; Tramontano, Enzo published the artcile< Scaffold hopping and optimisation of 3′,4′-dihydroxyphenyl- containing thienopyrimidinones: synthesis of quinazolinone derivatives as novel allosteric inhibitors of HIV-1 reverse transcriptase-associated ribonuclease H>, SDS of cas: 5004-88-6, the main research area is HIV1 virus allosteric inhibitors reverse transcriptase RNase H; Bioisosters; HIV-1 virus; RNase H; RNase H allosteric inhibitors; integrase.

Bioisosteric replacement and scaffold hopping are powerful strategies in drug design useful for rationally modifying a hit compound towards novel lead therapeutic agents. Recently, we reported a series of thienopyrimidinones that compromise dynamics at the p66/p51 HIV-1 reverse transcriptase (RT)-associated RNase H (RNase H) dimer interface, thereby allosterically interrupting catalysis by altering the active site geometry. Although they exhibited good submicromolar activity, the isosteric replacement of the thiophene ring, a potential toxicophore, is warranted. Thus, in this article, the most active 2-(3,4-dihydroxyphenyl)-5,6-dimethylthieno[2,3-d]pyrimidin-4(3H)-one was selected as the hit scaffold and several isosteric substitutions of the thiophene ring were performed. A novel series of highly active RNase H allosteric quinazolinone inhibitors was thus obtained. To determine their target selectivity, they were tested against RT-associated RNA-dependent DNA polymerase (RDDP) and integrase (IN). Interestingly, none of the compounds were particularly active on (RDDP) but many displayed micromolar to submicromolar activity against IN.

Journal of Enzyme Inhibition and Medicinal Chemistry published new progress about Antiviral agents. 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, SDS of cas: 5004-88-6.

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

Kamlar, Martin; Reiberger, Robert; Nigrini, Martin; Cisarova, Ivana; Vesely, Jan published the artcile< Enantioselective PCCP Bronsted acid-catalyzed aminalization of aldehydes>, Synthetic Route of 112253-70-0, the main research area is dihydroquinazolinone preparation enantioselective; aldehyde anthranilamide aminalization pentacarboxycyclopentadiene Bronsted acid catalyst; Brønsted acid; PCCP; aminalization; organocatalysis; pentacarboxycyclopentadiene.

Here an enantioselective aminalization of aldehydes catalyzed by Bronsted acids based on pentacarboxycyclopentadienes (PCCPs) is presented. The cyclization reaction using readily available anthranilamides as building blocks provides access to valuable 2,3-dihydroquinazolinones containing one stereogenic carbon center with good enantioselectivity (ee up to 80%) and excellent yields (up to 97%).

Beilstein Journal of Organic Chemistry published new progress about Aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 112253-70-0 belongs to class amides-buliding-blocks, and the molecular formula is C7H7BrN2O, Synthetic Route of 112253-70-0.

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

Soni, Rina; Cheung, Fung Kei; Clarkson, Guy C.; Martins, Jose E. D.; Graham, Mark A.; Wills, Martin published the artcile< The importance of the N-H bond in Ru/TsDPEN complexes for asymmetric transfer hydrogenation of ketones and imines>, Quality Control of 1192620-83-9, the main research area is nitrogen hydrogen bond ruthenium TsDPEN complex; asym transfer hydrogenation ketone imine crystallog.

Ru(II) complexes of TsDPEN containing two alkyl groups on the nontosylated nitrogen atom are poor catalysts for asym. transfer hydrogenation of ketones and imines; this observation provides direct evidence for the importance of the N-H interaction in the transition state for ketone reduction

Organic & Biomolecular Chemistry published new progress about Crystal structure. 1192620-83-9 belongs to class amides-buliding-blocks, and the molecular formula is C30H31ClN2O2RuS, Quality Control of 1192620-83-9.

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

Gatrone, Ralph C.; Rickert, Paul G.; Horwitz, E. Philip; Smith, Barbara F.; Bartholdi, Catherine S.; Martinez, Aaron M. published the artcile< Analysis of n-octyl(phenyl)-N,N-diisobutylcarbamoylmethylphosphine oxide and TRUEX process solvent by gas and liquid chromatography>, Recommanded Product: 2-Chloro-N,N-diisobutylacetamide, the main research area is fuel reprocessing TRUEX solvent analysis chromatog; GC HPLC TRUEX solvent analysis; CMPO extractant analysis GC HPLC; octylphenyldiisobutylcarbamoylmethylphosphine oxide analysis GC HPLC; gas chromatog solvent analysis; liquid chromatog solvent analysis; phosphine oxide organic derivative analysis chromatog.

Complementary anal. procedures using capillary gas chromatog. (GC) and high-performance liquid chromatog. (HPLC) have been developed for the anal. of the TRUEX process solvents (CMPO-TBP-tetrachloroethylene or normal paraffinic hydrocarbons) and the extractant CMPO. GC analyses are accomplished in 20 min using a 15 m × 0.25 μm I.D. DB-5 capillary column with flame ionization detection. The anal. requires derivatization with diazomethane. HPLC analyses are performed in 10 min using a C18 reversed-phase column and a mobile phase consisting of acetonitrile-water-triethylamine (79:29.5:0.5) with refractive index and UV detection. The methods provide information regarding the presence of acidic and neutral impurities in stock extractant, fresh process solvent, and recovered TRUEX solvent.

Journal of Chromatography published new progress about Capillary gas chromatography. 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

Huo, Peng-Chao; Hu, Qing; Shu, Sheng; Zhou, Qi-Hang; He, Rong-Jing; Hou, Jie; Guan, Xiao-Qing; Tu, Dong-Zhu; Hou, Xu-Dong; Liu, Peng; Zhang, Nan; Liu, Zhi-Guo; Ge, Guang-Bo published the artcile< Design, synthesis and biological evaluation of novel chalcone-like compounds as potent and reversible pancreatic lipase inhibitors>, Product Details of C29H53NO5, the main research area is pancreatic lipase inhibition chalcone antiobesity agent; Anti-obesity agent; Chalcone-like compounds; Inhibition; Pancreatic lipase (PL).

Pancreatic lipase (PL), a crucial enzyme responsible for hydrolysis of dietary lipids, has been validated as a key therapeutic target to prevent and treat obesity-associated metabolic disorders. Herein, we report the design, synthesis and biol. evaluation of a series of chalcone-like compounds as potent and reversible PL inhibitors. Following two rounds of structural modifications at both A and B rings of a chalcone-like skeleton, structure-PL inhibition relationships of the chalcone-like compounds were studied, while the key substituents that would be beneficial for PL inhibition were revealed. Among all tested chalcone-like compounds, compound B13 (a novel chalcone-like compound bearing two long carbon chains) displayed the most potent PL inhibition activity, with an IC50 value of 0.33 μM. Inhibition kinetic analyses demonstrated that B13 could potently inhibit PL-mediated 4-MUO hydrolysis in a mixed inhibition manner, with the Ki value of 0.12 μM. Mol. docking simulations suggested that B13 could tightly bind on PL at both the catalytic site and a non-catalytic site that was located on the surface of PL, which was consistent with the mixed inhibition mode of this agent. In addition, B13 displayed excellent stability in artificial gastrointestinal fluids and good metabolic stability in human liver preparations Collectively, our findings suggested that chalcone-like compounds were good choices for design and development of orally administrated PL inhibitors, while B13 could be served as a promising lead compound to develop novel anti-obesity agents via targeting on PL.

Bioorganic & Medicinal Chemistry published new progress about Antiobesity agents. 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

Subandi; Nurowidah, Anis published the artcile< The Potency of Carica papaya L. seeds powder as antiobesity 'coffee' drinks>, Recommanded Product: (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate, the main research area is antiobesity Carica papaya seed pancreatic lipase inhibitor.

Previous studies have shown that papaya seed contained flavonoids, tannins, and saponins Those compounds are potential as an inhibitor for pancreatic lipase, an enzyme that plays an important role for lipid absorption into the body. The aims of this study are to produce ‘coffee’ powder of papaya seeds for drinks; to test the organoleptic properties and the activity as a pancreatic lipase inhibitor. The seed was made into a powder by washing, sun drying, roasting, and then grinding. An organoleptic test was performed at 50 respondents and one trained respondent. Inhibitor activity for pancreatic lipase was measured relative to anti-obesity drugs of Orlistat (Xenical), using titrimetric method. The results showed that every 1.42 g of papaya seeds powder have an inhibitory activity equivalent to 1 tablet (120 mg) of Orlistat. Most of the respondents like with the texture, color, and flavor of the drinks.

IOP Conference Series: Materials Science and Engineering published new progress about Antiobesity agents. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Recommanded Product: (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