Category: amides-buliding-blocks

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

Wang, Xiao-Meng published the artcileSynthesis and antitumor activities evaluation of m-(4-morpholinoquinazolin-2-yl)benzamides in vitro and in vivo, Application of N-Methyl-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzamide, the publication is European Journal of Medicinal Chemistry (2015), 382-395, database is CAplus and MEDLINE.

In the present study, a series of m-(4-morpholinoquinazolin-2-yl)benzamides were designed, synthesized, and characterized. The antiproliferative activities of the synthesized compounds were evaluated against two human cell lines (HCT-116 and MCF-7). Compounds with IC₅₀ values below 4 μM were further evaluated against U-87 MG and A549 cell lines. Among these evaluated compounds, compound I displayed a remarkable antiproliferative effect in vitro. The hoechst staining assay showed that compound I caused morphol. changes. The cell cycle and apoptosis assay further indicated that compound I can arrest HCT-116 cells in G2/M and G0/G1 phase and induce apoptosis. PI3K enzyme assays indicated that compounds I and II selectively inhibit PI3Kα. A Western bolt assay further suggested that compound I can block the PI3K/Akt/mTOR pathway. Moreover, compound I inhibited tumor growth on a mice S180 homograft model. These findings directly identify m-(4-morpholinoquinazolin-2-yl)benzamide derivatives as novel anticancer agents.

European Journal of Medicinal Chemistry published new progress about 1197171-76-8. 1197171-76-8 belongs to amides-buliding-blocks, auxiliary class Boronic acid and ester,Amine,Benzene,Amide,Boronate Esters,Boronic Acids,Boronic acid and ester,, name is N-Methyl-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzamide, and the molecular formula is C18H28B2O4, Application of N-Methyl-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzamide.

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

Ouyang, Jinbo published the artcileCocrystal design of vanillin with amide drugs: Crystal structure determination, solubility enhancement, DFT calculation, Recommanded Product: Isonicotinamide, the publication is Chemical Engineering Research and Design (2022), 170-180, database is CAplus.

Vanillin (VAN) is widely used in medicine, food and optoelectronics, but its low solubility leads to the decrease of bioavailability and increase of application costs. Three APIs-nicotinamide (NIC), isonicotinamide (INM) and isoniazid (INH) were chosen to form cocrystals with VAN, aiming at improving the solubility of VAN and APIs simultaneously. Two cocrystals (VAN-NIC, VAN-INM) were obtained through cocrystn. while VAN reacted with INH to form one novel compound (VAN-INH). The crystal structures were characterized by single-crystal X-ray diffraction (SCXRD), Powder X-ray diffraction (PXRD), Fourier-Transform IR Spectroscopy (FT-IR) and Differential Scanning Calorimetry (DSC). The melting temperatures of VAN-NIC and VAN-INM cocrystals are between this of VAN and APIs. Compared with pure VAN and APIs, the solubility and dissolution rate of VAN-NIC and VAN-INM are significantly increased. The melting temperature of VAN-INH is greater than that of VAN and INH, and the solubility and dissolution rate is not increased significantly. The intermol. energy between VAN and APIs as well as lattice energies of cocrystals/novel compound were computed to elucidate the formation mechanism and stability. The present investigation opens a new pathway for the development of natural product-drug cocrystals to improve solubility and dissolution rate of natural product.

Chemical Engineering Research and Design 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, Recommanded Product: Isonicotinamide.

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

Li, Dan published the artcileSLAMF3 and SLAMF4 are immune checkpoints that constrain macrophage phagocytosis of hematopoietic tumors, HPLC of Formula: 321673-30-7, the publication is Science Immunology (2022), 7(67), eabj5501, database is CAplus and MEDLINE.

The interaction of SIRPα with CD47 represents a major mechanism for preventing macrophage phagocytosis. However, CD47-independent mechanisms are poorly defined. Here, we report a critical role of SLAM family receptors (SFRs), ubiquitously expressed on hematopoietic cells and forming homotypic interactions, in constraining macrophage phagocytosis. We found that SFR deficiency triggered macrophage phagocytosis of hematopoietic cells, leading to severe rejection of donor hematopoietic graft in recipient mice. Specific SFR members, mainly SLAMF3 and SLAMF4, were identified as “don’t eat me” receptors on macrophages. These receptors inhibited “eat me” signals, such as LRP1-mediated activation of mTOR and Syk, through SH2 domain-containing phosphatases. SFRs combined with, but were independent of, CD47 to mitigate macrophage phagocytosis, and the combined deletion of SFRs and CD47 resulted in hematopoietic cytopenia in mice. This SFR-mediated tolerance was compromised in patients with hemophagocytic lymphohistiocytosis, a syndrome characterized by inappropriate phagocytosis toward hematopoietic cells. Loss of SFRs potently elicited macrophage rejection of hematopoietic tumors. Deletion of SFRs also significantly enhanced the phagocytosis of CD19-pos. hematopoietic targets by the macrophages expressing the chimeric CD19 antigen receptor. Therefore, SFR-mediated inhibition of macrophage phagocytosis is critical to hematopoietic homeostasis, and SFRs may represent previously unknown targets for tumor immunotherapy.

Science Immunology published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C12H23N3S, HPLC of Formula: 321673-30-7.

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

Jiang, Biao-Lin published the artcileCobalt(II)/N,N’,N”-Trihydroxyisocyanuric Acid Catalyzed Aerobic Oxidative Esterification and Amidation of Aldehydes, Formula: C10H14N2O, the publication is Asian Journal of Organic Chemistry (2018), 7(5), 977-983, database is CAplus.

A protocol for a Co^II/N,N’,N”-trihydroxyisocyanuric acid (THICA)-catalyzed aerobic oxidative esterification and amidation of aldehydes has been developed. Preliminary insight into the mechanism indicates that such an oxidative C-O/N cross-coupling reaction proceeds by masking the aldehyde in a nucleophilic addition reaction with an alkoxy/amino source, thereby keeping the highly reactive formyl group from undesired oxidation This protocol for the oxidative esterification and amidation of aldehydes proceeds through two different pathways that are characterized by the intrinsic nucleophilicity of the alkanol and amine substrates. The former occurs in the presence of TsOH as a cocatalyst and orthoformates as the alkoxy sources, instead of alkanols, to efficiently afford the transient acetals. In contrast, the coupling of the more nucleophilic amines with aldehydes renders a readily accessible cross-coupling reaction that occurs without any cocatalyst but is limited by the potential inhibition of THICA upon nucleophilic substitution by an amine. Consequently, only sterically hindered amines were tolerated in this catalytic system, whereas further condensation occurred in the presence of primary amines to lead to imines.

Asian Journal of Organic Chemistry 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, Formula: C10H14N2O.

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

Li, Tingting published the artcileMechanically Strong Heterogeneous Catalysts via Immobilization of Powderous Catalysts to Porous Plastic Tablets, HPLC of Formula: 2418-95-3, the publication is Chinese Journal of Chemistry (2021), 39(10), 2673-2678, database is CAplus.

We describe a practical and general protocol for immobilization of heterogeneous catalysts to mech. robust porous ultra-high mol. weight polyethylene tablets using inter-facial Lifshitz-van der Waals Interactions. Diverse types of powderous catalysts, including Cu, Pd/C, Pd/Al₂O₃, Pt/C, and Rh/C have been immobilized successfully. The immobilized catalysts are mechanistically robust towards stirring in solutions, and they worked well in diverse synthetic reactions. The immobilized catalyst tablets are easy to handle and reused. Moreover, the metal leaching of immobilized catalysts was reduced significantly.

Chinese Journal of 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, HPLC of Formula: 2418-95-3.

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

Lai, Huifang published the artcileCopper-promoted direct amidation of isoindolinone scaffolds by sodium persulfate, Formula: C2H4ClNO, the publication is Organic & Biomolecular Chemistry (2021), 19(35), 7621-7626, database is CAplus and MEDLINE.

Isoindolinones are ubiquitous structural motifs in natural products and pharmaceuticals. Establishing an efficient method for structural modification of isoindolinones could significantly facilitate new drug development. Herein, authors describe copper-promoted direct amidation of isoindolinone scaffolds mediated by sodium persulfate. The method exhibits mild reaction conditions and high site-selectivity, and enables the structural modification of the drug indobufen ester with various amides with yields of 49 to 98%. It is also gram-scalable. Addnl., the reaction mechanism appears to involve a radical and a carbocationic pathway.

Organic & Biomolecular Chemistry 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, Formula: C2H4ClNO.

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

Cheng, Chuanjie published the artcileA highly efficient Pd-C catalytic hydrogenation of pyridine nucleus under mild conditions, Recommanded Product: N,N-Diethylisonicotinamide, the publication is Tetrahedron (2009), 65(41), 8538-8541, database is CAplus.

A synergistic Pd-C catalytic hydrogenation of 4-pyridinecarboxamides straightforwardly to 4-piperidinecarboxamide hydrochlorides was developed in the presence of ClCH₂CHCl₂. It provided a novel strategy for highly efficient hydrogenation of pyridine nuclear by using low-cost Pd-C catalyst under mild conditions.

Tetrahedron 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, Recommanded Product: N,N-Diethylisonicotinamide.

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

Zhao, Jinwu published the artcilePotassium iodide and ammonium nitrate catalyzed aerobic oxidative cyclization of ketones with thioureas in ionic liquid: an access to 2-aminothiazoles, SDS of cas: 14294-10-1, the publication is Tetrahedron (2015), 71(4), 539-543, database is CAplus.

An efficient procedure for the synthesis of 2-aminothiazoles via KI/NH₄NO₃-catalyzed oxidative cyclization of ketones and thioureas using mol. oxygen as a green oxidant is reported. Different ketones and thioureas went through the transformation and gave corresponding 2-aminothiazole heterocycles in satisfactory yields. E.g., in presence of KI/NH₄NO₃, H₂SO₄, and mol. oxygen in [Bmim]OTf/H₂O (4:1), oxidative cyclization of PhCOMe and H₂NCSNH₂ gave 95% 2-aminothiazole derivative (I).

Tetrahedron published new progress about 14294-10-1. 14294-10-1 belongs to amides-buliding-blocks, auxiliary class Morpholine,Thiourea,Amine,Amide, name is Morpholine-4-carbothioamide, and the molecular formula is C10H14N2Na4O9, SDS of cas: 14294-10-1.

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

Zhao, Jin-Wu published the artcileGreen synthesis of 1,2,4-thiadizoles from thioamides in water using molecular oxygen as an oxidant, Related Products of amides-buliding-blocks, the publication is Chinese Chemical Letters (2014), 25(11), 1499-1502, database is CAplus.

The authors present here an efficient green process for the synthesis of 1,2,4-thiadiazoles via iodine-catalyzed, oxidative dimerization of thioamides in water using mol. oxygen as a terminal oxidant. Under the optimized reaction conditions, aryl thioamides produced 3,5-diaryl-1,2,4-thiadiazoles in good to excellent yields. Alkyl thioamides and substituted thioureas could also provide corresponding 1,2,4-thiadiazole products.

Chinese Chemical Letters published new progress about 14294-10-1. 14294-10-1 belongs to amides-buliding-blocks, auxiliary class Morpholine,Thiourea,Amine,Amide, name is Morpholine-4-carbothioamide, and the molecular formula is C8H17Br, Related Products of amides-buliding-blocks.

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