Tag: M.W=150-200

Wang, Yueqi published the artcileA reactive oxygen species-responsive dendrimer with low cytotoxicity for efficient and targeted gene delivery, HPLC of Formula: 1869-45-0, the publication is Chinese Chemical Letters (2020), 31(1), 275-280, database is CAplus.

Nonviral vectors have been attracting more attention for several advantages in gene delivery and the development of nonviral gene carriers with high delivery efficiency and low cytotoxicity has long been a key project. Starburst polyamidoamine dendrimers are a class of synthetic polymers with unique structural and phys. characteristics. However, when they are used as gene carrier, the gene transfection efficiency is not satisfactory. Herein, a novel thioketal-core polyamidoamine dendrimer (i.e., ROS-PAMAM) was synthesized and characterized. Compared to ethylenediamine-core dendrimers or widely used cationic polymers of polyetherimide, ROS-PAMAM showed lower cytotoxicity. Moreover, ROS-PAMAM demonstrated reactive oxygen species responsive characteristics, which can facilitate the release of siRNA in the tumor microenvironment. In vitro gene transfection experiments based on A549 cells confirmed that siRNA/ROS-PAMAM exhibits high gene transfection efficiency. It is concluded that ROS-PAMAM shows great potential as a generalizable vehicle for gene therapy applications.

Chinese Chemical Letters 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 C19H21N3O3S, HPLC of Formula: 1869-45-0.

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

Tong, Wei published the artcilePalladium-Metalated Porous Organic Polymers as Recyclable Catalysts for the Chemoselective Synthesis of Thiazoles from Thiobenzamides and Isonitriles, Related Products of amides-buliding-blocks, the publication is Organic Letters (2018), 20(8), 2494-2498, database is CAplus and MEDLINE.

Two types of thiazole derivatives are synthesized through a multistep cascade sequence with Pd-metalated phosphorus-doped porous organic polymers (POPs) as heterogeneous catalysts. The POPs could be used as both ligands and catalyst supports. No obvious aggregation and loss of any catalytic activity of the catalysts were observed after 10 runs of the reaction. More importantly, imidazo[4,5-d]thiazoles, which are a new class of thiazole derivatives, could be obtained through K₂CO₃-promoted intramol. cyclization of the synthesized polysubstituted thiazoles. Furthermore, the in vitro anticancer activity of these new compounds were tested with MTT assay, and compound I exhibited good antitumor activity toward T-24 and A549 cells with IC₅₀ values of 10.3 ± 0.8 and 11.8 ± 0.5 μM, resp. In addition, the action mechanism of compound I on tumor cells was determined

Organic Letters published new progress about 64559-06-4. 64559-06-4 belongs to amides-buliding-blocks, auxiliary class Amine,Benzene,Amide,Ether, name is 3-Methoxybenzothioamide, and the molecular formula is C11H15NOS, Related Products of amides-buliding-blocks.

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

Ma, Yao published the artcileIdentification of benzofused five-membered sultams, potent dual NOD1/NOD2 antagonists in vitro and in vivo, Related Products of amides-buliding-blocks, the publication is European Journal of Medicinal Chemistry (2020), 112575, database is CAplus and MEDLINE.

Nucleotide-binding oligomerization domain-containing proteins 1 and 2 play important roles in immune system activation. Recently, a shift has occurred due to the emerging knowledge that preventing nucleotide-binding oligomerization domains (NODs) signaling could facilitate the treatment of some cancers, which warrants the search for dual antagonists of NOD1 and NOD2. Herein, we undertook the synthesis and identification of a new class of derivatives of dual NOD1/NOD2 antagonists with novel benzofused five-membered sultams. Compound 14k(I) was finally demonstrated to be the most potent mol. that inhibits both NOD1-and NOD2-stimulated NF-κB and MAPK signaling in vitro and in vivo.

European Journal of Medicinal Chemistry 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, Related Products of amides-buliding-blocks.

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

Graham, Laurine L. published the artcileChemical shift assignments in N,N-disubstituted trifluoroacetamides, Computed Properties of 360-92-9, the publication is Organic Magnetic Resonance (1972), 4(2), 335-42, database is CAplus.

Due to hindered rotation about the central C-N bond in N,N-disubstituted trifluoroacetamides, CF3CONR1R2, two resonance peaks are usually observed for each proton in R1 and R2. Chem. shift assignments are made for the following amides: R1 = R2 = Me; R1 = R2 = Et; R1 = Me, R2 = Me2CH; R1 = Me, R2 = Bu; R1 = Me, R2 = cyclohexyl; R1 = R2 = Me2CH; R1 = Me2CH, R2 = cyclohexyl. Amides, where R1 = R2 = Me2CH and R1 = Me2CH, R2 = cyclohexyl, show an inversion of the relative chem. shift for both the methine and methyl protons of the 2-propyl group as compared with the amide where R1 = Me, R2 = Me2CH. For non-fluorinated amides, aromatic solvents shift the trans alkyl peaks to higher field faster than those cis (to the carbonyl oxygen atom); however, this generalization does not apply to all trifluoroacetamide proton peaks.

Organic Magnetic Resonance 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, Computed Properties of 360-92-9.

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

Gryszkiewicz-Trochimowski, E. published the artcileAmides of carboxylic acids of the heterocyclic series, Application of N,N-Diethylisonicotinamide, the publication is Roczniki Chemii (1931), 193-202;201-2 in French, database is CAplus.

In analogy with the N-diethylamide of 3-pyridinecarboxylic acid coramine, 3 new diethylamides were prepared, viz., of 2-pyridinecarboxylic, of 4-pyridinecarboxylic and of tetramethylpyrrolinecarboxylic acid, resp., and their chem. and physiol. properties were investigated. Picolinyl chloride (I) is prepared according to Meyer, Monatsh. 22, 112(1901), from the acid (II) and SOCl₂. N-Diethylamide of II, prepared from pulverized (I) and dry Et₂NH, almost odorless oil of bitter taste, neutral, m. 26-8°, b₃ 122.5-3°, corrected, d₄^16.2 1.0603, n_α^16.2 1.5209, n_D^16.2 1.5254, n_β^16.2 1.5348. Coramine, m. 21-3°, b₃ 128.5-9°, corrected, n_α16.2 1.5235, n_D^16.2 1.5279, n_β^16.2 1.5391. N-Diethylamide of 4-pyridinecarboxylic acid (isonicotinic acid), prepared similarly to II, is a neutral, viscous oil, m. 22-4°, b₃ 123-3.5°, corrected, d₄^16.2 1.0630, n_α^16.2 1.5225, n_D^16.2 1.5269, n_β^16.2 1.5380. N-Diethylamide of 2,2′,5,5′-tetramethylpyrrolinecarboxylic acid (III), prepared by interaction of dibromotriacetoneamine-HBr (prepared according to Pauly, Ber. 31, 672), and 33% aqueous Et₂NH, m. 33-4°, b₉ 129.5-30°. It tastes bitter and reacts strongly alk. The 3 diethylamides differ in their physiol. action. The 2-isomer has an action on the heart similar to that of coramine, but does not affect the nervous system. The physiol. action of III is entirely different from that of coramine.

Roczniki Chemii 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, Application of N,N-Diethylisonicotinamide.

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

Ivanciuc, Ovidiu published the artcileSupport vector machines prediction of the mechanism of toxic action from hydrophobicity and experimental toxicity against Pimephales promelas and Tetrahymena pyriformis, Application of 2,4-Dichlorobenzamide, the publication is Internet Electronic Journal of Molecular Design (2004), 3(12), 802-821, database is CAplus.

Motivation: The prediction of the mechanism of action (MOA) using structural descriptors has major applications in selecting the appropriate quant. structure-activity relationships (QSAR) model, to identify chems. with similar toxicity mechanism, and in extrapolating toxic effects between different species and exposure regimes. Method: The SVM (support vector machines) algorithm was recently proposed as an efficient and flexible classification method for various bioinformatics and cheminformatics applications. In this study we have investigated the application of SVM for the classification of 337 organic compounds from eight MOA classes (nonpolar narcosis, polar narcosis, ester narcosis, amine narcosis, weak acid respiratory uncoupling, electrophilicity, proelectrophilicity, and nucleophilicity). The MOA classification was based on three indexes, namely: log K_ow, the octanol-water partition coefficient; log 1/IGC₅₀, the 50% inhibitory growth concentration against Tetrahymena pyriformis; log 1/LC₅₀, the 50% lethal concentration against Pimephales promelas. The prediction power of each SVM model was evaluated with a leave – 5/% – out cross – validation procedure. Results: In order to find classification models with good predictive power, we have investigated a large number of SVM models obtained with the dot, polynomial, radial basis function, neural, and anova kernels. The MOA classification performances of SVM models depend strongly on the kernel type and various parameters that control the kernel shape. The discrimination between nonpolar narcotic compounds and the other chems. can be obtained with radial and anova SVM models, with a prediction accuracy of 0.80. The separation of less reactive compounds (polar, ester, and amine narcotics) from more reactive compounds (electrophiles, proelectrophiles, and nucleophiles) is obtained with a slightly higher error (prediction accuracy 0.71, obtained with radial SVM models). Conclusions: SVM models that use as input parameters hydrophobicity and exptl. toxicity against Pimephales promelas and Tetrahymena pyriformis represent an effective MOA classification method for a large diversity of organic compounds This approach can be used to predict the aquatic toxicity mechanism and to select the appropriate QSAR model for new chem. compounds

Internet Electronic Journal of Molecular Design 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, Application of 2,4-Dichlorobenzamide.

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

Jart, A. published the artcileInfrared spectra of carboxylic acid derivatives. IV. Amides and hydrazides, HPLC of Formula: 2447-79-2, the publication is Acta Polytech. Scand., Chem. Met. Ser. (1965), 55 pp., database is CAplus.

cf. CA 63, 14654f. The ir spectra of 91 carboxylic acid amides, 6 thioamides, and 11 sulfonamides, as well as 30 carboxylic acid monohydrazides, and 3 sym. dihydrazides are given. The spectra were recorded by means of a Perkin-Elmer grating spectrophotometer, model 421, within the range 550-4000 cm.^-1 by using the KBr disk technique. Some of the amides and hydrazides prepared have not been described previously in the literature. M.ps. are given for all the compounds considered.

Acta Polytech. Scand., Chem. Met. Ser. 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

Jart, Aage published the artcileInfrared spectra of carboxylic acid derivatives. VI. Equivalent weight determination. Quantitative aspects of the pressed halide disk technique, Computed Properties of 2447-79-2, the publication is Acta Polytechnica Scandinavica, Chemistry Including Metallurgy Series (1974), 118 pp., database is CAplus.

Ir spectroscopic quant. equivalent weight measurements were made using the C:O band and other absorptions exhibited by the KBr pellets of amides and esters as well on the bands exhibited by the KBr pellets of S-benzylthiouronium salts. The sp. absorptions and intensity variations of 19 p-thiocyanatoanilides, 12 p-thiocyanatophenacyl esters, 12 p-thiocyanato-S-benzylthiouronium salts and 21 p-cyano-S-benzylthiouronium salts were examined The p-cyano-S-benzylthiouronium salts were models for the study of internal standards, the relation between band intensity and the nature of the matrix, and to the interchange between the sample and the KBr, RbBr, CsBr, or TlBr matrixes. A quant. method for the determination of the equivalent weight of carboxylic acids in KBr based on lyophilization with HBr (extinction coefficient measured at 2233 cm-1) was also developed.

Acta Polytechnica Scandinavica, Chemistry Including Metallurgy Series 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, Computed Properties of 2447-79-2.

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

Joullie, Madeleine M. published the artcileReactions of amines with esters of polyhalogenated acids, Category: amides-buliding-blocks, the publication is Journal of the American Chemical Society (1955), 6662-3, database is CAplus.

Me₂C:CH₂ passed 1 hr. into 37 g. CF₃CO₂H (I) at 50°, and the mixture allowed to stand overnight, treated with more Me₂C:CH₂ until the heat evolution ceased, and fractionated yielded 75% CF₃CO₂CMe₃ (II), b₆₀ 30°, b₇₆₀ 83°, n_D²⁵ 1.3300. An appropriate ester treated gradually with the appropriate amine, and the mixture allowed to stand overnight and fractionated gave the corresponding amide; the mixtures with II were allowed to stand 4 days before fractionation. In this manner were prepared the following amides of I (m.p. or b.p./mm., % yield, n_D²⁵ given): di-Et, 30°/2, 60, 1.3780; piperidide, 44°/1, 84, 1.4153; morpholide, 47°/1, 87, 1.4177. C₂F₅CO₂H: Bu, 48°/1, 80, 1.3642; morpholide, 59°/1 (m.p. 46-7°), 85, -. C₃F₇CO₂H: Bu, 56°/2, 80, 1.3568; piperidide, 57°/2, 85, 1.3846; pyrrolidide, 65°/2, 76, 1.3755; morpholide, 72°/2, 89, 1.3850; piperidide of CHF₂CO₂H, 66°/3, 85, 1.4500. CClF₂CO₂H piperidide, 98°/10, 90, 1.4520. CHCl₂CO₂H pyrrolidide, 120°/2, 75, 1.5182.

Journal of the American Chemical Society 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, Category: amides-buliding-blocks.

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

Klosa, Josef published the artcileSynthesis of carboxylic acid amides from carboxylic acids and amines by means of polyphosphoric acid, Application In Synthesis of 530-40-5, the publication is Journal fuer Praktische Chemie (Leipzig) (1966), 31(1-2), 41-8, database is CAplus.

4-Amino-1-phenyl-2,3-dimethyl-5-pyrazolone (I) (100 g.) and 62 g. nicotinic acid (II) added with stirring in portions at 100-10° to 300 g. polyphosphoric acid (III) and heated 1.5-2 hrs. at 160-80° gave 135-40 g. 4-(pyridine-3-carboxamido)-2,3-dimethyl-1-phenyl-5-pyrazolone (IV), m. 256-8°. I (100 g.) and 62 g. II treated with 300-400 g. III, heated with occasional stirring to 100-20° and then during 1-2 hrs. to 160-80°, poured into 1-2 l. H₂O, and stirred 1-2 hrs. gave 145 g. IV. Similarly were prepared the following analogs of IV (4-substituent, m.p., and % yield given): pyridine-4-carboxamido, 273-5°, 90; 6-methylpyridine-2-carboxamido, 206-8°, 80; 4-methylpyridine-3-carboxamido, 248-60°, 65; 4-ethylpyridine-3-carboxamido, 240-2°, 70; 2,4-dimethylpyridine-3-carboxamido, 267-9° (MeOH), 75; 2,6-dimethyl-3-pyridinecarboxamido, 264-6° (MeOH), 85; 2-methylpyridine-5-carboxamido, >280° (decomposition), 78; 2-methylpyridine-4-carboxamido, >300° (decomposition), 70; 2,4,6-trimethylpyridine-3-carboxamido, >300° (decomposition with charring), 82; 2,3,4-trimethylpyridine-5-carboxamido, >300° (decomposition with charring), 80; 6-phenylpyridine-5-carboxamido, 270-2° (decomposition), 65; 2-methyl-6-phenylpyridine-3-carboxamido, >290° (decomposition), 65; 4-chloropyridine-2-carboxamido, >265-7° (decomposition), 65; 5-chloropyridine-2-carboxamido, >280° (decomposition), 75; 2-chloropyridine-3-carboxamido, from 260° (decomposition), 70; 3-chloropyridine-4-carboxamido, >300° (decomposition), 85; 4,6-dichloropyridine-2-carboxamido, from 250° (decomposition with browning), 68; 2,3-dichloropyridine-5-carboxamido, from 260° (decomposition and browning), 88; 2,6-dichloropyridine-4-carboxamido, >280°, 85; 2-hydroxypyridine-5-carboxamido, >300°, 65; 2-hydroxy-3-chloropyridine-5-carboxamido, >300° (decomposition), 60; 2-hydroxy-6-chloropyridine-4-carboxamido, from 270° (decomposition), 65; 2-phenylquinoline-4-carboxamido, 245-7°, 90; 2-phenyl-6-methoxyquinoline-4-carboxamido, 282-4°, 75. Similarly were prepared the following compounds (m.p. or b.p. and % yield given): p-ethoxyanilide of II, 170-2°, 60; diethylamide of II, 276-8°/760 mm., 65; piperidide of II, 314-16°/760, 60; diethylamide of isonicotinic acid (V), 26-8°, 68; p-ethoxyanilide of V, 198-290°, 75; 2-methylpyridine-5-carboxanilide (VI), 138-40°, 68; 2-Ph analog of VI, 200-2°, 70.

Journal fuer Praktische Chemie (Leipzig) 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, Application In Synthesis of 530-40-5.

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