Tag: M.W=150-200

Xu, Liang published the artcileOxidative cyclization of N-alkyl-o-methyl-arenesulfonamides to biologically important saccharin derivatives, Application of 4-Fluoro-2-methylbenzenesulfonamide, the publication is Tetrahedron (2006), 62(33), 7902-7910, database is CAplus.

Various biol. important saccharin skeletons and their N-alkyl derivatives were efficiently prepared by Cr(VI) oxide-catalyzed H₅IO₆ oxidation of N-alkyl-o-methyl-arenesulfonamides in MeCN. N-tert-Bu saccharin skeletons were easily prepared by H₅IO₆-CrO₃ oxidation of N-tert-butyl-o-Me arenesulfonamides in the presence of acetic anhydride. The method that furnished the novel fluoro- and trifluoromethyl-substituted saccharin skeletons was characterized by two steps, a simple work-up procedure, a single purification and good overall yields from substituted toluene derivatives For example, 58 % 2-tert-butyl-6-trifluoromethyl-1,2-benzisothiazol-3-one 1,1-dioxide was obtained from 1-methyl-4-(trifluoromethyl)benzene.

Tetrahedron published new progress about 489-17-8. 489-17-8 belongs to amides-buliding-blocks, auxiliary class Fluoride,Sulfamide,Amine,Benzene, name is 4-Fluoro-2-methylbenzenesulfonamide, and the molecular formula is C17H20ClN3, Application of 4-Fluoro-2-methylbenzenesulfonamide.

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

Sattler, H. J. published the artcileStructure-activity relations in analeptics of nicethamide type. I. Diethylamides of homologs and vinylogs of nicotinic and isonicotinic acids, Computed Properties of 530-40-5, the publication is Arzneimittel-Forschung (1974), 24(5), 743-6, database is CAplus and MEDLINE.

The diethylamides I and II (bond in 3 or 4 position, Z = bond, CH2, CH2CH2, or CH:CH) were prepared and showed respiratory analeptic activities in rabbits. I were prepared in 68-76% yield by reaction of the corresponding pyridinecarboxylic acid with ClCO2Et and Et2NH. II were prepared by reaction of acetylpyridines with MeONa and HCO2Et and subsequently with Et2NH.

Arzneimittel-Forschung published new progress about 530-40-5. 530-40-5 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is N,N-Diethylisonicotinamide, and the molecular formula is C10H14N2O, Computed Properties of 530-40-5.

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

Sattler, Hans J. published the artcileNMR spectroscopy of heterocycles, 2. Ring alkylated and isomeric nicetamide derivatives, COA of Formula: C10H14N2O, the publication is Archiv der Pharmazie (Weinheim, Germany) (1976), 309(3), 222-8, database is CAplus and MEDLINE.

Barriers to amide group rotation (ΔG*) in I (R = H, Me; R1 = H, Me; R2 = H, CONEt2; R3 = H, Me), II, and III (R = H, Me, CONEt2) were determined via 1H NMR spectral data. The ΔG* values ranged from 14.9 to 17.5 kcal/mole.

Archiv der Pharmazie (Weinheim, Germany) published new progress about 530-40-5. 530-40-5 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is N,N-Diethylisonicotinamide, and the molecular formula is C10H14N2O, COA of Formula: C10H14N2O.

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

Anilkumar, Gopinadhan N. published the artcileII. Novel HCV NS5B polymerase inhibitors: discovery of indole C2 acyl sulfonamides, COA of Formula: C7H8FNO2S, the publication is Bioorganic & Medicinal Chemistry Letters (2012), 22(1), 713-717, database is CAplus and MEDLINE.

Development of SAR at the C2 position of indole lead I, a palm site inhibitor of HCV NS5B polymerase (NS5B IC₅₀ = 0.053 μM, replicon EC₅₀ = 4.8 μM), is described. Initial screening identified an acyl sulfonamide moiety as an isostere for the C2 carboxylic acid group. Further SAR investigation resulted in identification of acyl sufonamide analog II (NS5B IC₅₀ = 0.039 μM, replicon EC₅₀ = 0.011 μM) with >100-fold improved replicon activity.

Bioorganic & Medicinal Chemistry Letters published new progress about 489-17-8. 489-17-8 belongs to amides-buliding-blocks, auxiliary class Fluoride,Sulfamide,Amine,Benzene, name is 4-Fluoro-2-methylbenzenesulfonamide, and the molecular formula is C7H8FNO2S, COA of Formula: C7H8FNO2S.

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

Fishwick, Colin W. G. published the artcileAn efficient route to S-N-(9-fluorenylmethyoxycarbonyl)-4′-(1-azi-2,2,2-trifluoroethyl)phenylalanine, Product Details of C6H10F3NO, the publication is Tetrahedron Letters (1994), 35(26), 4611-14, database is CAplus.

An extremely efficient synthesis of optically pure photoactivatable phenylalanine derivative I is described. The key step involves a highly diastereoselective alkylation of chiral glycine equivalent II with benzyl iodide III to give benzylated product IV.

Tetrahedron Letters 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

Rusu, Georgeta published the artcileAntibacterial activity of urotropin salts of the oxazolidine series, Product Details of C7H5Cl2NO, the publication is Revista Medico-Chirurgicala (1988), 92(1), 133-6, database is CAplus.

Six urotropin salts of the oxazolidine series (I; R = Ph, substituted Ph) were prepared and their antimicrobial properties were determined Good activity was evident against Staphylococcus aureus, Bacillus subtilis, and Candida albicans.

Revista Medico-Chirurgicala 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, Product Details of C7H5Cl2NO.

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

Lieber, Charles M. published the artcileKinetic studies of ligand substitution rates for the Ru(NH₃)₅(H₂O)²⁺ ion in Nafion films, Synthetic Route of 530-40-5, the publication is Journal of the American Chemical Society (1986), 108(20), 6103-8, database is CAplus.

Substitution rates were measured for reaction of a number of pyridines with the Nafion-bound Ru(NH₃)₅(H₂O)²⁺ complex. Reaction activities were determined by electrochem. techniques, which also allow for determination of site thermodn. and heterogeneity during the course of the reaction. Diffusion-coefficient effects were investigated by variation in polymer film thickness, and partition coefficients were determined under equilibrium conditions by optical absorbance techniques. The partition-coefficient corrected rate law is 1st order in Nafion-bound [Ru^II] and first order in ligand concentration in the polymer phase. The partition-coefficient corrected bimol. rate constants for a variety of pyridine ligands vary by a factor of 5, which contrasts with the relatively constant substitution rates observed in aqueous solution Also, sterically hindered ligands, such as 2-pyropylpyridine, have surprisingly high substitution rate constants on the Nafion-bound Ru^II ion. These rate data indicate that pronounced mol. reactivity changes can occur upon electrode modification and have implications with respect to the design of chem. modified electrodes for use in electrocatalysis.

Journal of the American Chemical Society published new progress about 530-40-5. 530-40-5 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is N,N-Diethylisonicotinamide, and the molecular formula is C10H14N2O, Synthetic Route of 530-40-5.

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

Sinks, Glendon D. published the artcileCorrelation of Tetrahymena and Pimephales toxicity: evaluation of 100 additional compounds, Recommanded Product: 2,4-Dichlorobenzamide, the publication is Environmental Toxicology and Chemistry (2001), 20(4), 917-921, database is CAplus and MEDLINE.

In the summary/recommendations for the Ecotoxicol. Session of TestSmart-a Humane and Efficient Approach to Screening Information Data Sets (SIDS) Data Workshop, it was recommended that more population growth impairment data using Tetrahymena be generated and compared with available lethality data for the fathead minnow. To comply with this recommendation, 100 addnl. chems. were tested in the ciliate assay. Toxicity values for the 96-h Pimephales promelas mortality assay (log[LC50^-1]) and the 2-d Tetrahymena pyriformis growth assay (log[IGC50^-1]) were compared. Each chem. was a priori assigned a mode of action. The majority of compounds were classified as either narcotics (n = 46) or direct-acting electro(nucleo)philes (n = 43), while 11 chems. were listed as carboxylic acids, diesters, proelectrophiles, or weak acid respiratory uncouplers. Toxicities for narcotics showed an excellent relationship between endpoints with the coefficient of determination (r²) being 0.93. A weaker relationship, r² = 0.78, was observed for the electro(nucleo)philes. The poorer fit for the covalent-reacting electro(nucleo)philes is attributed to differences in protocol, in particular, to test-medium composition and exposure scheme. Those chems. whose potency is mediated by metabolism in fish (diesters and proelectrophiles) as well as the acids exhibited a poor correlation between endpoints, with toxicity in the fish assay being greater than that predicted from the ciliate data. The regression anal. between endpoints, regardless of mode or mechanism of toxic action, yielded the model log(LC50^-1) = 1.12(log[IGC50^-1]) + 0.46, with n = 92, r² = 0.82, s (root of the mean square error) = 0.87, F = 399, and p > F = 0.0001. A result for the present investigation supports earlier findings that, with noted exceptions, there is a strong relationship between toxicity potency as quantified by P. promelas mortality and T. pyriformis growth impairment.

Environmental Toxicology and Chemistry 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 C10H18O, Recommanded Product: 2,4-Dichlorobenzamide.

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

Jack, Thomas published the artcileSynthesis and characterization of photoaffinity probes that target the 5-HT₃ receptor, Application of N,N-Diethyl-2,2,2-trifluoroacetamide, the publication is Chimia (2014), 68(4), 239-242, database is CAplus and MEDLINE.

The 5-HT₃ receptor is one of several ion channels responsible for the transmission of nerve impulses in the peripheral and central nervous systems. Until now, it was difficult to characterize transmembrane receptors with classical structural biol. approaches like x-ray crystallog. The use of photoaffinity probes is an alternative approach to identify regions in the protein where small mols. bind. To this end, the authors present two photoaffinity probes based on granisetron, a well known antagonist of the 5-HT₃ receptor. These new probes show nanomolar binding affinity for the orthosteric binding site. In addition, the authors investigated their reactivity using irradiation experiments

Chimia 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, Application of N,N-Diethyl-2,2,2-trifluoroacetamide.

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

Patil, Prarthana published the artcileReactive oxygen species-degradable polythioketal urethane foam dressings to promote porcine skin wound repair, Safety of 2,2,2-Trifluoro-N-(2-mercaptoethyl)acetamide, the publication is Science Translational Medicine (2022), 14(641), eabm6586, database is CAplus and MEDLINE.

Porous, resorbable biomaterials can serve as temporary scaffolds that support cell infiltration, tissue formation, and remodeling of nonhealing skin wounds. Synthetic biomaterials are less expensive to manufacture than biol. dressings and can achieve a broader range of physiochem. properties, but opportunities remain to tailor these materials for ideal host immune and regenerative responses. Polyesters are a well-established class of synthetic biomaterials; however, acidic degradation products released by their hydrolysis can cause poorly controlled autocatalytic degradation Here, we systemically explored reactive oxygen species (ROS)-degradable polythioketal (PTK) urethane (UR) foams with varied hydrophilicity for skin wound healing. The most hydrophilic PTK-UR variant, with seven ethylene glycol (EG7) repeats flanking each side of a thioketal bond, exhibited the highest ROS reactivity and promoted optimal tissue infiltration, extracellular matrix (ECM) deposition, and reepithelialization in porcine skin wounds. EG7 induced lower foreign body response, greater recruitment of regenerative immune cell populations, and resolution of type 1 inflammation compared to more hydrophobic PTK-UR scaffolds. Porcine wounds treated with EG7 PTK-UR foams had greater ECM production, vascularization, and resolution of proinflammatory immune cells compared to polyester UR foam-based NovoSorb Biodegradable Temporizing Matrix (BTM)-treated wounds and greater early vascular perfusion and similar wound resurfacing relative to clin. gold standard Integra Bilayer Wound Matrix (BWM). In a porcine ischemic flap excisional wound model, EG7 PTK-UR treatment led to higher wound healing scores driven by lower inflammation and higher reepithelialization compared to NovoSorb BTM. PTK-UR foams warrant further investigation as synthetic biomaterials for wound healing applications.

Science Translational Medicine published new progress about 1869-45-0. 1869-45-0 belongs to amides-buliding-blocks, auxiliary class Trifluoromethylated Building Blocks, name is 2,2,2-Trifluoro-N-(2-mercaptoethyl)acetamide, and the molecular formula is C4H6F3NOS, Safety of 2,2,2-Trifluoro-N-(2-mercaptoethyl)acetamide.

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