Month: November 2022

Antonsen, Simen published the artcileSynthesis of the Enantiomers of Thioridazine, Name: (S)-2-Methylpropane-2-sulfinamide, the main research area is thioridazine preparation enantioselective antibacterial activity.

Herein, an auxiliary-based strategy is used for the total synthesis of both enantiomers (+)-thioridazine and (-)-thioridazine in high optical purity and good overall yield. The strategy can easily be scaled up. Both enantiomers were tested against several bacteria. Comparison of the racemic mixture, (-)-thioridazine and its (+)-antipode revealed that they have the same antimicrobial effects. Thus, the non-toxic enantiomer, (-)-thioridazine, can prove useful in this role and should be investigated further.

SynOpen published new progress about Antibacterial agents. 343338-28-3 belongs to class amides-buliding-blocks, name is (S)-2-Methylpropane-2-sulfinamide, and the molecular formula is C4H11NOS, Name: (S)-2-Methylpropane-2-sulfinamide.

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

Venkatramaiah, T. published the artcileDesign, synthesis and evaluation of chlorothiazide derivatives, Recommanded Product: N-Methylformamide, the main research area is chlorothiazide preparation antibacterial antifungal.

Hydrochlorothiazide and chlorthiazide are high potent diuretics used in treatment of hypertension. In recent research trends shows that chlorthiazide derivatives are used in osteoporosis and also has antimicrobial activity against various bacterial species. In this view a series of chlorthiazide derivatives were designed, synthesized six compounds by condensing chloroacetyl chloride with chlorthiazide by using ethanol as a solvent refluxed at 60° temperature Formed compound is taken as intermediate and further refluxed and condensed with aromatic amines to give substituted chlorthiazide derivatives The substituted chlorthiazide derivatives were screened for antibacterial activity.

Asian Journal of Pharmaceutical Analysis and Medicinal Chemistry published new progress about Antibacterial agents. 123-39-7 belongs to class amides-buliding-blocks, name is N-Methylformamide, and the molecular formula is C2H5NO, Recommanded Product: N-Methylformamide.

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

Durand-Reville, Thomas F. published the artcileDiscovery of an Orally Available Diazabicyclooctane Inhibitor (ETX0282) of Class A, C, and D Serine β-Lactamases, Computed Properties of 343338-28-3, the main research area is multidrug resistance GNB Enterobacterales lactamase inhibitor carbapenem orally bioavailable.

Multidrug resistant Gram-neg. bacterial infections are an increasing public health threat due to rapidly rising resistance toward β-lactam antibiotics. The hydrolytic enzymes called β-lactamases are responsible for a large proportion of the resistance phenotype. β-Lactamase inhibitors (BLIs) can be administered in combination with β-lactam antibiotics to negate the action of the β-lactamases, thereby restoring activity of the β-lactam. Newly developed BLIs offer some advantage over older BLIs in terms of enzymic spectrum but are limited to the i.v. route of administration. Reported here is a novel, orally bioavailable diazabicyclooctane (DBO) β-lactamase inhibitor. This new DBO, ETX1317(I), contains an endocyclic carbon-carbon double bond and a fluoroacetate activating group and exhibits broad spectrum activity against class A, C, and D serine β-lactamases. The ester prodrug of ETX1317, ETX0282(II), is orally bioavailable and, in combination with cefpodoxime proxetil, is currently in development as an oral therapy for multidrug resistant and carbapenem-resistant Enterobacterales infections.

Journal of Medicinal Chemistry published new progress about Antibacterial agents. 343338-28-3 belongs to class amides-buliding-blocks, name is (S)-2-Methylpropane-2-sulfinamide, and the molecular formula is C4H11NOS, Computed Properties of 343338-28-3.

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

Mohammad, Haroon published the artcileDiscovery and characterization of potent thiazoles versus methicillin- and vancomycin-resistant Staphylococcus aureus, COA of Formula: C11H15NS, the main research area is thiazole antibacterial Staphylococcus antibiotic resistance.

Methicillin- and vancomycin-resistant Staphylococcus aureus (MRSA and VRSA) infections are growing global health concerns. Structure-activity relationships of phenylthiazoles as a new antimicrobial class have been addressed. The authors present 10 thiazole derivatives that exhibit strong activity against 18 clin. strains of MRSA and VRSA with acceptable PK profile. Three derivatives revealed an advantage over vancomycin by rapidly eliminating MRSA growth within 6 h, and no derivatives are toxic to HeLa cells at 11 μg/mL.

Journal of Medicinal Chemistry published new progress about Antibacterial agents. 1208077-46-6 belongs to class amides-buliding-blocks, name is 4-Butylthiobenzamide, and the molecular formula is C11H15NS, COA of Formula: C11H15NS.

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

Smirnov, Valeriy I. published the artcileThe effect of the side chain structures on the energy of intermolecular interactions of α-amino acids with some formamides in aqueous solutions at T = 298.15 K, Application In Synthesis of 123-39-7, the main research area is amino acid formamide water intermol interaction dissolution enthalpy temperature.

To evaluate the effect of amino acid side chains on the thermodn. of their interaction with the formamides mols. in aqueous solutions, we expanded the range of amino acids by studying in the present investigation the thermodn. of the dissolution of glutamine in mixed solvents {water + (formamide, N-methylformamide and N,N-dimethylformamide)} at T = 298.15 K and organic solvent mole fractions up to x2 ∼ 0.3. The standard enthalpies of solution (ΔsolH°) and transfer (ΔtrH°) of L-glutamine from water to a mixed solvent as well as the enthalpy coefficients of pairwise interactions (hxy) were calculated The interrelation between enthalpic characteristics of L-glutamine dissolution (transfer) and the composition of water-organic mixtures was determined Using the enthalpic coefficients of pairwise interactions of L-glutamine and five more amino acids (glycine, DL-α-alanine, L-valine, L-methionine, and L-threonine), the enthalpic contributions of the side chains of these amino acids to their interparticle interactions with the mols. of formamides were calculated

Journal of Molecular Liquids published new progress about Electric conductivity. 123-39-7 belongs to class amides-buliding-blocks, name is N-Methylformamide, and the molecular formula is C2H5NO, Application In Synthesis of 123-39-7.

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

Hoejgaard Hansen, Anders published the artcileStructure-Activity Relationship Explorations and Discovery of a Potent Antagonist for the Free Fatty Acid Receptor 2, Safety of (S)-2-Methylpropane-2-sulfinamide, the main research area is structure activity relationship FFA2 antagonist; FFA2; GPCR; GPR43; inflammation; short-chain fatty acids.

Free fatty acid receptor 2 (FFA2) is a sensor for short-chain fatty acids that has been identified as an interesting potential drug target for treatment of metabolic and inflammatory diseases. Although several ligand series are known for the receptor, there is still a need for improved compounds One of the most potent and frequently used antagonists is the amide-substituted phenylbutanoic acid known as CATPB (1). We here report the structure-activity relationship exploration of this compound, leading to the identification of homologues with increased potency. The preferred compound 37 (TUG-1958) was found, besides improved potency, to have high solubility and favorable pharmacokinetic properties.

ChemMedChem published new progress about Condensation reaction. 343338-28-3 belongs to class amides-buliding-blocks, name is (S)-2-Methylpropane-2-sulfinamide, and the molecular formula is C4H11NOS, Safety of (S)-2-Methylpropane-2-sulfinamide.

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

Bottcher, Stephan published the artcileNovel Efficient Routes to Indoxyl Glycosides for Monitoring Glycosidase Activities, SDS of cas: 125328-80-5, the main research area is indoxyl glycoside sialoside lactoside preparation monitoring glycosidase activity.

A new efficient synthesis for broad access to indoxyl glycosides was developed. Indoxylic acid allyl ester linked to a sugar structure served as the key intermediate in this route. Selective ester cleavage and mild decarboxylation led to the corresponding indoxyl glycosides in good yields. This synthesis was applied for preparation of indoxyl glycosides of fucose, sialic acid, and 6′-sialyl lactose.

Organic Letters published new progress about Bond cleavage (ester). 125328-80-5 belongs to class amides-buliding-blocks, name is N-(4-Bromo-3-chloro-2-methylphenyl)acetamide, and the molecular formula is C9H9BrClNO, SDS of cas: 125328-80-5.

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

Gascooke, Jason R. published the artcileThe Case for Methyl Group Precession Accompanying Torsional Motion, COA of Formula: C2H5NO, the main research area is toluene torsional motion mol vibration.

For mols. containing a Me group, high precision fits of rotational line data (microwave spectra) that encompass several torsional states require considerably more constants than are required in comparable rigid mols. Many of these addnl. terms are ‘torsion-rotation interaction’ terms, but their precise phys. meaning is unclear. In this paper, we explore the phys. origins of many of these addnl. terms in the case where the Me group is attached to a planar frame. We show that torsion-vibration coupling, which has been observed in toluene and several substituted toluenes, provides the dominant contribution to a number of the torsion-rotation constants in toluene. It is further demonstrated that this coupling is intimately related to precession of the Me group. A number of the constants required in the high resolution fits of rotational line data are shown to arise as a natural consequence of Me precession. By considering several mols. whose rotational line spectra have been fit to high precision, we demonstrate that the exptl. evidence is consistent with the occurrence of Me group precession. Quantum chem. calculations of the optimized mol. structures at key torsional angles provide further evidence that Me precession occurs. There is both a torsional angle dependent tilt of the Cmethyl-frame bond and of the Me group principal rotation axis relative to the Cmethyl-frame bond.

Australian Journal of Chemistry published new progress about Bond angle, torsional. 123-39-7 belongs to class amides-buliding-blocks, name is N-Methylformamide, and the molecular formula is C2H5NO, COA of Formula: C2H5NO.

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

Yuan, Jin-Wei published the artcileTransition-metal free C3-amidation of quinoxalin-2(1H)-ones using Selectfluor as a mild oxidant, Computed Properties of 123-39-7, the main research area is quinoxalinone amide Selectfluor promoter oxidative amidation; oxoquinoxalinyl amide preparation.

A practical and efficient synthetic route to construct a variety of 3-amidated quinoxalin-2(1H)-ones was developed via transition-metal free direct oxidative amidation of quinoxalin-2(1H)-ones with amidates using Selectfluor reagent as a mild oxidant. This protocol features mild reaction conditions, operational simplicity, broad substrate scope, and good to excellent yields.

Organic & Biomolecular Chemistry published new progress about Amidation (oxidative). 123-39-7 belongs to class amides-buliding-blocks, name is N-Methylformamide, and the molecular formula is C2H5NO, Computed Properties of 123-39-7.

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

Yuan, Jinwei published the artcileHighly efficient copper-catalyzed direct C-H amidation of quinoxalin-2(1H)-ones with amidates under microwave irradiation, SDS of cas: 123-39-7, the main research area is quinoxalinone amidate preparation microwave irradiation; amide quinoxalinone amidation copper catalyst.

A novel and highly efficient copper-catalyzed direct oxidative amidation of quinoxalin-2(1H)-ones with a variety of aromatic and aliphatic amides was described. This methodol. provided a practical approach to various 3-acylamino quinoxalin-2(1H)-ones from readily available starting materials in good to excellent yields.

Organic Chemistry Frontiers published new progress about Amidation (oxidative). 123-39-7 belongs to class amides-buliding-blocks, name is N-Methylformamide, and the molecular formula is C2H5NO, SDS of cas: 123-39-7.

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