Category: 2447-79-2

Lei, Peng published the artcileDesign, synthesis and fungicidal activity of N-substituted benzoyl-1,2,3,4-tetrahydroquinolyl-1-carboxamide, Product Details of C7H5Cl2NO, the publication is Bioorganic & Medicinal Chemistry Letters (2016), 26(10), 2544-2546, database is CAplus and MEDLINE.

To find a new lead compound with high biol. activity, a series of N-substituted benzoyl-1,2,3,4-tetrahydroquinolyl-1-carboxamide were designed using linking active substructures method. The target compounds were synthesized from substituted benzoic acid by four steps and their structures were confirmed by ¹H NMR, IR spectrum and elemental anal. The in vitro bioassay results indicated that some target compounds exhibited excellent fungicidal activities, and the position of the substituents played an important role in fungicidal activities. Especially, 4-t-Bu-substituted compound , exhibited better fungicidal activities than the com. fungicide flutolanil against two tested fungi Valsa mali and Sclerotinia sclerotiorum, with EC₅₀ values of 3.44 and 2.63 mg/L, resp. And it also displayed good in vivo fungicidal activity against S. sclerotiorum with the EC₅₀ value of 29.52 mg/L.

Bioorganic & Medicinal Chemistry 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, Product Details of C7H5Cl2NO.

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

Cao, Yu-Qing published the artcileOne-pot synthesis of dehydrating reagent and its application in preparation of nitriles from amides, Synthetic Route of 2447-79-2, the publication is Organic Chemistry: An Indian Journal (2013), 9(4), 132-136, database is CAplus.

A new efficient, eco-friendly and economic method for the preparation of imine cation containing composite organic salt as a dehydrating reagent was reported. N,N-dimethylformamide (DMF) was reacted with oxalyl chloride [(COCl)₂], and the resultant imine cation reacted with phenol in the presence of triethylamine (Et₃N) to give the corresponding product in high yield. The use of the composite organic salt as an efficient dehydrating reagent has been demonstrated via the preparation of nitriles from amides.

Organic Chemistry: An Indian Journal 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, Synthetic Route of 2447-79-2.

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

Cao, Yu published the artcileSynthesis and activity on bis-ureas of thiadiazole, Computed Properties of 2447-79-2, the publication is Huaxue Shiji (2012), 34(11), 982-984,998, database is CAplus.

Seven new bis-ureas of thiadiazloe derived from 2-amino-5-mercapto-1,3,4-thiadiazole, 1,3-dibromopropane and acyl azides were synthesized and characterized by the phys. constants, elementary anal., IR, and ¹HNMR. The optimal conditions for preparation of bis-ureas of thiadiazloe were as follows: n(bis-ureas of thiadiazloe): n was 1.0:1.0, and the reaction time was 4 h at 40 °C, The product yield of bis-ureas of thiadiazloe could reach 63.5%. The results of biol. activity tests showed that all samples have activity on plant growth hormone and auxin.

Huaxue Shiji 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

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

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

Klabunde, Thomas published the artcileAcyl Ureas as Human Liver Glycogen Phosphorylase Inhibitors for the Treatment of Type 2 Diabetes, Computed Properties of 2447-79-2, the publication is Journal of Medicinal Chemistry (2005), 48(20), 6178-6193, database is CAplus and MEDLINE.

Using a focused screening approach, acyl ureas have been discovered as a new class of inhibitors of human liver glycogen phosphorylase (hlGPa). The x-ray structure of screening hit 1 (IC₅₀ = 2 μM) in a complex with rabbit muscle glycogen phosphorylase b reveals that 1 binds at the AMP site, the main allosteric effector site of the dimeric enzyme. A first cycle of chem. optimization supported by x-ray structural data yielded derivative 21, which inhibited hlGPa with an IC₅₀ of 23±1 nM, but showed only moderate cellular activity in isolated rat hepatocytes (IC₅₀ = 6.2 μM). Further optimization was guided by (i) a 3D pharmacophore model that was derived from a training set of 24 compounds and revealed the key chem. features for the biol. activity and (ii) the 1.9 Å crystal structure of 21 in complex with hlGPa. A second set of compounds was synthesized and led to 42 with improved cellular activity (hlGPa IC₅₀ = 53±1 nM; hepatocyte IC₅₀ = 380 nM). Administration of 42 to anesthetized Wistar rats caused a significant reduction of the glucagon-induced hyperglycemic peak. These findings are consistent with the inhibition of hepatic glycogenolysis and support the use of acyl ureas for the treatment of type 2 diabetes.

Journal of Medicinal 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 C7H5Cl2NO, Computed Properties of 2447-79-2.

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

Zhang, Zeshuai published the artcileSelective N-Monovinylation of Primary Aromatic Amides Using Calcium Carbide as an Alkyne Source, Application In Synthesis of 2447-79-2, the publication is ChemistrySelect (2022), 7(26), e202201463, database is CAplus.

An efficient method for the selective N-monovinylation of primary aromatic amides using calcium carbide as an alkyne source was described. A series of N-vinylbenzamides (enamides) RC(O)NHCH=CH₂ [R = Ph, 2-MeC₆H₄, 4-ClMeC₆H₄, etc.] were readily synthesized by this strategy. The salient features for this protocol were the use of inexpensive, easy-to-handle solid alkyne source, high chemoselectivity, transition metal catalyst-free, good functional group tolerance, and simple work-up procedures. These reactions was also be extended to the gram-scale level.

ChemistrySelect 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 C27H39ClN2, Application In Synthesis of 2447-79-2.

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

Boschelli, Diane H. published the artcileSynthesis and Src kinase inhibitory activity of a series of 4-phenylamino-3-quinolinecarbonitriles, HPLC of Formula: 2447-79-2, the publication is Journal of Medicinal Chemistry (2001), 44(5), 822-833, database is CAplus and MEDLINE.

Screening of a directed compound library in a yeast-based assay identified 4-[(2,4-dichlorophenyl)amino]-6,7-dimethoxy-3-quinolinecarbonitrile (I) as a Src inhibitor. An enzymic assay established that I was an ATP-competitive inhibitor of the kinase activity of Src. We present here SAR data for I which shows that the aniline group at C-4, the carbonitrile group at C-3, and the alkoxy groups at C-6 and C-7 of the quinoline are crucial for optimal activity. Increasing the size of the C-2 substituent of the aniline at C-4 of I from chloro to bromo to iodo resulted in a corresponding increase in Src inhibition. Furthermore, replacement of the 7-methoxy group of I with various 3-heteroalkylaminopropoxy groups provided increased inhibition of both Src enzymic and cellular activity. Compound II, which contains a 3-morpholinopropoxy group, had an IC₅₀ of 3.8 nM in the Src enzymic assay and an IC₅₀ of 940 nM for the inhibition of Src-dependent cell proliferation.

Journal of Medicinal 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 C7H5Cl2NO, HPLC of Formula: 2447-79-2.

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

He, Haifeng published the artcileSynthesis, antitumor activity and mechanism of action of novel 1,3-thiazole derivatives containing hydrazide-hydrazone and carboxamide moiety, SDS of cas: 2447-79-2, the publication is Bioorganic & Medicinal Chemistry Letters (2016), 26(14), 3263-3270, database is CAplus and MEDLINE.

A series of novel 2,4,5-trisubstituted 1,3-thiazole derivatives containing hydrazide-hydrazine and carboxamide moieties including 46 compounds T were synthesized, and evaluated for their antitumor activity in vitro against a panel of five human cancer cell lines. Eighteen title compounds T displayed higher inhibitory activity than that of 5-Fu against MCF-7, HepG2, BGC-823, Hela, and A549 cell lines. Especially, I, II, and III exhibit best cytotoxic activities with IC₅₀ values of 2.21 μg/mL, 1.67 μg/mL, and 1.11 μg/mL, against MCF-7, BCG-823, and HepG2 cell lines, resp. These results suggested that the combination of 1,3-thiazole, hydrazide-hydrazone, and carboxamide moieties was favorable to cytotoxicity activity. Furthermore, the flow cytometry anal. revealed that compounds I and III could induce apoptosis in HepG2 cells, and it was confirmed III led the induction of cell apoptosis by S cell-cycle arrest.

Bioorganic & Medicinal Chemistry 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

Ma, Liang published the artcileSynthesis, Activity, and Docking Study of Novel Phenylthiazole-Carboxamido Acid Derivatives as FFA2 Agonists, Quality Control of 2447-79-2, the publication is Chemical Biology & Drug Design (2016), 88(1), 26-37, database is CAplus and MEDLINE.

Free fatty acid receptor 2 (FFA2), also known as GPR43, is activated by short-chain fatty acids (SCFAs) that are mainly produced by the gut microbiota through the fermentation of undigested carbohydrates and dietary fibers. FFA2 currently appears to be a potential target in the management of obesity, diabetes, inflammatory diseases, and cancer. In the study, a series of novel phenylthiazole-carboxamido acid derivatives has been synthesized and evaluated as potential orthosteric FFA2 ligands for the study of structure-activity relationships. Compound 6e was found to exhibit the twofold potent agonistic activity in the stable hFFA2-transfected CHO-K1 cells (EC₅₀ = 23.1 μm) as that of pos. control propionate (EC₅₀ = 43.3 μm). We also reported the results of mutagenesis studies based on the crystal structure of hFFA1 bound to TAK-875 at 2.3 Å resolution to identify important residues for orthosteric agonist 6e inducing FFA2 activation.

Chemical Biology & Drug 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, Quality Control of 2447-79-2.

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