Category: amides-buliding-blocks

Gan, Guohong published the artcileSCASP: A Simple and Robust SDS-Aided Sample Preparation Method for Proteomic Research, Computed Properties of 79-07-2, the publication is Molecular & Cellular Proteomics (2021), 100051, database is CAplus and MEDLINE.

SDS is widely used in sample preparation for proteomic research. However, SDS is incompatible with LC and electrospray ionization. SDS depletion is therefore required ahead of LC-MS anal. Most of current SDS removal strategies are time consuming, laborious, and have low reproducibility. Here, we describe a method, SDS-cyclodextrin (CD)-assisted sample preparation, by which CD can bind to SDS and form CD-SDS complexes in solutions, allowing for direct tryptic digestion. We demonstrate that SDS-CD-assisted sample preparation is a simple, fast, and robust SDS-based sample preparation method for proteomics application.

Molecular & Cellular Proteomics published new progress about 79-07-2. 79-07-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Aliphatic hydrocarbon chain,Amide,Inhibitor, name is 2-Chloroacetamide, and the molecular formula is C2H4ClNO, Computed Properties of 79-07-2.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Dermenci, Alpay published the artcileRh-catalyzed decarbonylation of conjugated ynones via carbon-alkyne bond activation: reaction scope and mechanistic exploration via DFT calculations, Name: N-Methoxy-N-methylisonicotinamide, the publication is Chemical Science (2015), 6(5), 3201-3210, database is CAplus and MEDLINE.

Detailed development of a catalytic decarbonylation of conjugated monoynones to synthesize disubstituted alkynes was described. The reaction scope and limitation has been thoroughly investigated, and a broad range of functional groups including heterocycles were compatible under the catalytic conditions. Mechanistic exploration via DFT calculations has also been executed. Through the computational study, a proposed catalytic mechanism has been carefully evaluated. These efforts are expected to serve as an important exploratory study for developing catalytic alkyne-transfer reactions via carbon-alkyne bond activation.

Chemical Science published new progress about 100377-32-0. 100377-32-0 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is N-Methoxy-N-methylisonicotinamide, and the molecular formula is C8H10N2O2, Name: N-Methoxy-N-methylisonicotinamide.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Mueller, Martin published the artcileImpact of co-administered stabilizers on the biopharmaceutical performance of regorafenib amorphous solid dispersions, Quality Control of 1019206-88-2, the publication is European Journal of Pharmaceutics and Biopharmaceutics (2021), 189-199, database is CAplus and MEDLINE.

Poor solubility of drug candidates is a well-known and thoroughly studied challenge in the development of oral dosage forms. One important approach to tackle this challenge is the formulation as an amorphous solid dispersion (ASD). To reach the desired biopharmaceutical improvement a high supersaturation has to be reached quickly and then be conserved long enough for absorption to take place. In the presented study, various formulations of regorafenib have been produced and characterized in biorelevant in-vitro experiments Povidone-based formulations, which are equivalent to the marketed product Stivarga, showed a fast drug release but limited stability and robustness after that. In contrast, HPMCAS-based formulations exhibited excellent stability of the supersaturated solution, but unacceptably slow drug release. The attempt to combine the desired attributes of both formulations by producing a ternary ASD failed. Only co-administration of HPMCAS as an external stabilizer to the rapidly releasing Povidone-based ASDs led to the desired dissolution profile and high robustness. This optimized formulation was tested in a pharmacokinetic animal model using Wistar rats. Despite the promising in-vitro results, the new formulation did not perform better in the animal model. No differences in AUC could be detected when compared to the conventional (marketed) formulation. These data represent to first in-vivo study of the new concept of external stabilization of ASDs. Subsequent in-vitro studies revealed that temporary exposure of the ASD to gastric medium had a significant and long-lasting effect on the dissolution performance and externally administered stabilizer could not prevent this sufficiently. By applying the co-administered HPMCAS as an enteric coating onto Stivarga tablets, a new bi-functional approach was realized. This approach achieved the desired tailoring of the dissolution profile and high robustness against gastric medium as well as against seeding.

European Journal of Pharmaceutics and Biopharmaceutics published new progress about 1019206-88-2. 1019206-88-2 belongs to amides-buliding-blocks, auxiliary class Protein Tyrosine Kinase/RTK,VEGFR, name is 4-(4-(3-(4-chloro-3-(trifluoromethyl)phenyl)ureido)-3-fluorophenoxy)-N-methylpicolinamide hydrate, and the molecular formula is C21H17ClF4N4O4, Quality Control of 1019206-88-2.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Lawrence, Elliot J. published the artcile3-Aryl-3-(trifluoromethyl)diazirines as Versatile Photoactivated “Linker” Molecules for the Improved Covalent Modification of Graphitic and Carbon Nanotube Surfaces, Product Details of C6H10F3NO, the publication is Chemistry of Materials (2011), 23(16), 3740-3751, database is CAplus.

3-Aryl-3-(trifluoromethyl)diazirines are shown to be synthetically useful photoactivated carbene precursors that can be used as mol. “tethers” to facilitate the improved covalent surface modification of graphitic carbon and carbon nanotubes with a potentially large variety of chem. species. Proof-of-concept is demonstrated by the synthesis, as well as spectroscopic and electrochem. characterization, followed by photoactivated attachment of the organometallic diazirine derivative, 3-[3-(trifluoromethyl)diazirin-3-yl]phenyl ferrocene monocarboxylate, to the surface of vitreous carbon, and also to two different morphologies of multiwalled carbon nanotubes (“bamboo-like” and “hollow-tube”, denoted as b-MWCNTs and h-MWCNTs, resp.). The latter differ only in the relative amounts of “edge-plane-like” defect sites (at the termini of the nanotubes) and “basal-plane-like” pristine sidewall regions. The facile covalent coupling of the ferrocenyl “probe” moiety to the diazirine “linker” was confirmed by UV-vis, ¹H and ¹⁹F NMR spectroscopy, and cyclic voltammetry (CV). Upon exposure to UV irradiation in the presence of graphitic materials, the resulting covalent surface attachment of the ferrocenyl groups via the diazirine “linker” was characterized by Raman and XPS and by CV experiments performed in nonaqueous electrolyte. The surface coverage of 3-[3-(trifluoromethyl)diazirin-3-yl]phenyl ferrocene monocarboxylate, analyzed from both CV and XPS experiments was found to be 7%-11% of that estimated for a complete monolayer, and was 20-fold greater than that achieved in control experiments that employed conventional covalent modification strategies to form esters between ferrocene methanol and surface carboxylate groups on the graphitic materials. The surface loading of ferrocene groups on the b-MWCNTs was found to be only ca. 60%-70% that achieved on h-MWCNTs, reflecting the ability of the functionalized carbene intermediate formed upon photolysis of the parent diazirine to insert into C=C bonds in the otherwise relatively inert sidewalls of the nanotubes. This was further confirmed by Raman spectroscopic characterization, which revealed that the h-MWCNTs experienced significantly more sidewall functionalization than the b-MWCNTs, yet still retained good electronic conduction in electrochem. experiments The relative chem. stability of 3-aryl-3-(trifluoromethyl)diazirines, the ease with which they can be potentially be coupled to a large range of different organic, inorganic, and biol. species, and the enhanced surface loading that can be achieved as a result of the reactive carbene intermediate formed during their photolysis, render diazirines highly versatile and potent “linker” mols. for the development of chem. modified materials.

Chemistry of Materials published new progress about 360-92-9. 360-92-9 belongs to amides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Amine,Aliphatic hydrocarbon chain,Amide, name is N,N-Diethyl-2,2,2-trifluoroacetamide, and the molecular formula is C6H10F3NO, Product Details of C6H10F3NO.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Apgar, James M. published the artcileIbrexafungerp: An orally active β-1,3-glucan synthesis inhibitor, Name: Isonicotinamide, the publication is Bioorganic & Medicinal Chemistry Letters (2021), 127661, database is CAplus and MEDLINE.

We previously reported medicinal chem. efforts that identified MK-5204 (I), an orally efficacious β-1,3-glucan synthesis inhibitor derived from the natural product enfumafungin. Further extensive optimization of the C2 triazole substituent identified 4-pyridyl as the preferred replacement for the carboxamide of MK-5204, leading to improvements in antifungal activity in the presence of serum, and increased oral exposure. Reoptimizing the aminoether at C3 in the presence of this newly discovered C2 substituent, confirmed that the (R) t-Bu, Me aminoether of MK-5204 provided the best balance of these two key parameters, culminating in the discovery of ibrexafungerp (II), which is currently in phase III clin. trials. Ibrexafungerp displayed significantly improved oral efficacy in murine infection models, making it a superior candidate for clin. development as an oral treatment for Candida and Aspergillus infections.

Bioorganic & Medicinal Chemistry Letters published new progress about 1453-82-3. 1453-82-3 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is Isonicotinamide, and the molecular formula is C6H6N2O, Name: Isonicotinamide.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Wall, Brendan J. published the artcileImportance of Hydrogen Bonding: Structure-Activity Relationships of Ruthenium(III) Complexes with Pyridine-Based Ligands for Alzheimer′s Disease Therapy, Formula: C6H6N2O, the publication is Journal of Medicinal Chemistry (2021), 64(14), 10124-10138, database is CAplus and MEDLINE.

Alzheimer′s disease (AD) is the most common form of dementia, where one of the pathol. hallmarks of AD is extracellular protein deposits, the primary component of which is the peptide amyloid-β (Aβ). Recently, the soluble form of Aβ has been recognized as the primary neurotoxic species, making it an important target for therapeutic development. Metal-based drugs are promising candidates to target Aβ, as the interactions with the peptide can be tuned by ligand design. In the current study, 11 ruthenium complexes containing pyridine-based ligands were prepared, where the functional groups at the para position on the coordinated pyridine ligand were varied to determine structure-activity relationships. Overall, the complexes with terminal primary amines had the greatest impact on modulating the aggregation of Aβ and diminishing its cytotoxicity. These results identify the importance of specific intermol. interactions and are critical in the advancement of metal-based drugs for AD therapy.

Journal of Medicinal Chemistry published new progress about 1453-82-3. 1453-82-3 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is Isonicotinamide, and the molecular formula is C13H10F2, Formula: C6H6N2O.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Pierens, Raymond K. published the artcileThe dipole moments, molar Kerr constants, and solution-state conformation of some substituted benzamides, HPLC of Formula: 2447-79-2, the publication is Journal of the Chemical Society, Perkin Transactions 2: Physical Organic Chemistry (1972-1999) (1980), 235-8, database is CAplus.

The dipole moments and molar Kerr constants were determined for 24 substituted benzamides in dioxane, and discussed in relation to preferred solution conformations. The results indicate that for a given ring substituent the dihedral angle between the planar amide group and the benzene ring is similar for both the 3- and 4-substituted benzamides but less than that for the 2-substituted isomer. For the 3-substituted benzamides both cis and trans conformers contribute to the observed dipole moment and molar Kerr constant whereas for the 2-substituted species only that conformer contributes which has the amide C:O bond remote from the ortho substituent.

Journal of the Chemical Society, Perkin Transactions 2: Physical Organic Chemistry (1972-1999) published new progress about 2447-79-2. 2447-79-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Benzene,Amide, name is 2,4-Dichlorobenzamide, and the molecular formula is C7H5Cl2NO, HPLC of Formula: 2447-79-2.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Kario, Kazuomi published the artcileAngiotensin receptor-neprilysin inhibitors for hypertension-hemodynamic effects and relevance to hypertensive heart disease, Formula: C24H29N5O3, the publication is Hypertension Research (2022), 45(7), 1097-1110, database is CAplus and MEDLINE.

A review. Angiotensin receptor-neprilysin inhibitors have multiple beneficial effects on the cardiovascular system. The angiotensin receptor-neprilysin inhibitor sacubitril/valsartan has been shown to effectively reduce ambulatory 24-h blood pressure in patients with hypertension, and improvements in many aspects of hemodynamic function have also been reported. Overall hemodynamic effects on arterial stiffness and nocturnal blood pressure play an important role in the pathogenesis of hypertensive heart disease. Therefore, these could represent mechanistic targets underlying the effects of angiotensin receptor-neprilysin inhibitors on the continuum of cardiovascular disease from hypertension to heart failure. Other potential mechanisms include reductions in circulating volume and sympathetic activity, both of which contribute to the protection against target organ damage and pos. changes in cardiac biomarkers seen during angiotensin receptor-neprilysin inhibitor therapy. The mechanisms of action and beneficial effects of angiotensin receptor-neprilysin inhibitors are complementary to those of a number of other treatment options for hypertension, suggesting the possibility of additive or even synergistic benefits. Based on available data, there are a number of patient groups who will benefit from antihypertensive treatment with an angiotensin receptor-neprilysin inhibitor, including those with salt-sensitive hypertension, structural hypertension, resistant hypertension, and hypertension in the presence of heart failure. Overall, angiotensin receptor-neprilysin inhibitors regulate blood pressure and pulse pressure via multiple mechanisms and provide cardiovascular protection. This provides an option for effective intervention early in the vicious cycle of elevated blood pressure and central pressures with progression toward heart failure that should help to address the growing worldwide heart failure epidemic.

Hypertension Research published new progress about 137862-53-4. 137862-53-4 belongs to amides-buliding-blocks, auxiliary class GPCR/G Protein,Angiotensin Receptor, name is (S)-2-(N-((2′-(1H-Tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid, and the molecular formula is C24H29N5O3, Formula: C24H29N5O3.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Sanz Sharley, Daniel D. published the artcileA selective hydration of nitriles catalyzed by a Pd(OAc)₂-based system in water, SDS of cas: 2447-79-2, the publication is Tetrahedron Letters (2017), 58(43), 4090-4093, database is CAplus.

In situ formation of a [Pd(OAc)₂bipy] (bipy = 2,2′-bipyridyl) complex in water selectively catalyzes the hydration of a wide range of organonitriles at 70°. Catalyst loadings of 5 mol% afford primary amide products RC(O)NH₂ (R = Et, n-Pr, C₆H₅, etc.) in excellent yields in the absence of hydration-promoting additives such as oximes and hydroxylamines.

Tetrahedron Letters published new progress about 2447-79-2. 2447-79-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Benzene,Amide, name is 2,4-Dichlorobenzamide, and the molecular formula is C7H5Cl2NO, SDS of cas: 2447-79-2.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Dunkelmann, Daniel L. published the artcileEngineered triply orthogonal pyrrolysyl-tRNA synthetase/tRNA pairs enable the genetic encoding of three distinct non-canonical amino acids, Synthetic Route of 2418-95-3, the publication is Nature Chemistry (2020), 12(6), 535-544, database is CAplus and MEDLINE.

Expanding and reprogramming the genetic code of cells for the incorporation of multiple distinct non-canonical amino acids (ncAAs), and the encoded biosynthesis of non-canonical biopolymers, requires the discovery of multiple orthogonal aminoacyl-tRNA synthetase/tRNA pairs. These pairs must be orthogonal to both the host synthetases and tRNAs and to each other. Pyrrolysyl-tRNA synthetase (PylRS)/^PyltRNA pairs are the most widely used system for genetic code expansion. Here, we reveal that the sequences of ΔNPylRS/^ΔNPyltRNA pairs (which lack N-terminal domains) form two distinct classes. We show that the measured specificities of the ΔNPylRSs and ^ΔNPyltRNAs correlate with sequence-based clustering, and most ΔNPylRSs preferentially function with ^ΔNPyltRNAs from their class. We then identify 18 mutually orthogonal pairs from the 88 ΔNPylRS/^ΔNPyltRNA combinations tested. Moreover, we generate a set of 12 triply orthogonal pairs, each composed of three new PylRS/^PyltRNA pairs. Finally, we diverge the ncAA specificity and decoding properties of each pair, within a triply orthogonal set, and direct the incorporation of three distinct non-canonical amino acids into a single polypeptide.

Nature Chemistry published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C11H22N2O4, Synthetic Route of 2418-95-3.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics