Category: amides-buliding-blocks

Xiao, Qing published the artcileIncreased expression of Sonic hedgehog restores diabetic endothelial progenitor cells and improves cardiac repair after acute myocardial infarction in diabetic mice, Application of N-((4-Acetamidophenyl)carbamothioyl)-4-(tert-butyl)benzamide, the publication is International Journal of Molecular Medicine (2019), 44(3), 1091-1105, database is CAplus and MEDLINE.

Investigated whether Shh revitalized diabetic EPCs and consequently improved the deteriorative status of DMI. Apoptosis, cell function, and protein expression were investigated in EPCs in vitro. First, the in vitro results demonstrated that the apoptosis of diabetic EPCs was reduced following treatment with Shh protein for 24 h, under normal or hypoxic conditions. Bmi1, an antiapoptotic protein found in several cells, was reduced in diabetic EPCs under normal or hypoxic conditions, but was upregulated after Shh protein stimulation. When Bmi1-siRNA was administered, the antiapoptotic effect of Shh was significantly reversed. In addition, p53, a Bmi1-targeted gene, was demonstrated to mediate the antiapoptotic effect of the Shh/Bmi1 pathway in diabetic EPCs. The Shh/Bmi1/p53 axis also enhanced the diabetic EPC function. In vivo, Shh-modified diabetic EPCs exhibited increased EPC retention and decreased apoptosis at 3 days post-DMI. At 14 days post-DMI, these cells presented enhanced capillary d., reduced myocardial fibrosis and improved cardiac function. In conclusion, the present results demonstrated that the Shh pathway restored diabetic EPCs through the Shh/Bmi1/p53 axis, suppressed myocardial apoptosis and improved myocardial angiogenesis, thus reducing cardiac fibrosis and finally restoring myocardial repair and cardiac function in DMI. Thus, the Shh pathway may serve as a potential target for autologous cell therapy in diabetic myocardial ischemia.

International Journal of Molecular Medicine published new progress about 380315-80-0. 380315-80-0 belongs to amides-buliding-blocks, auxiliary class Apoptosis,p53, name is N-((4-Acetamidophenyl)carbamothioyl)-4-(tert-butyl)benzamide, and the molecular formula is C13H10O2, Application of N-((4-Acetamidophenyl)carbamothioyl)-4-(tert-butyl)benzamide.

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

Hou, Hongcen published the artcileRhodium-catalyzed direct C-H bond alkynylation of aryl sulfonamides with bromoalkynes, Safety of 4-Fluoro-2-methylbenzenesulfonamide, the publication is Organic & Biomolecular Chemistry (2019), 17(11), 2948-2953, database is CAplus and MEDLINE.

An efficient protocol for the synthesis of ortho-(1-alkynyl)benzenesulfonamides I [R = H, 4-Me, 4-OCF₃, etc.] was developed via rhodium-catalyzed direct ortho-mono-alkynylation of aryl sulfonamides with triisopropylsilyl (TIPS)-substituted bromoalkyne. While triethylsilyl or trimethylsilyl (TES or TMS)-substituted bromoalkyne was also amenable to the alkynylation, affording six membered benzosultams II [R¹ = TMS, TES; R² = H, 6-Me, 6-Et, 6-OMe] via the alkynylation/intramol. cyclization cascade reaction. The present protocol displayed high functional group tolerance and broad substrate scope under an air atm. in good to high yields. Mechanistic studies indicated that the reaction proceeded by a turnover limiting C-H activation step and a plausible mechanism was proposed.

Organic & Biomolecular 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, Safety of 4-Fluoro-2-methylbenzenesulfonamide.

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

Hou, Hongcen published the artcileIridium-Catalyzed ortho-C-H Amidation of Benzenesulfonamides with Sulfonyl Azides, SDS of cas: 489-17-8, the publication is Advanced Synthesis & Catalysis (2019), 361(18), 4393-4398, database is CAplus.

An iridium-catalyzed direct C-H activation/C-N bond formation reaction of benzenesulfonamides RS(O)₂NHR¹ (R = Ph, 2-methyl-4-fluorophenyl, 3-chlorophenyl, etc.) with sulfonyl azides R²C₆H₄S(O)₂N₃ (R² = H, 4-Me, 2-Me, 4-OMe) was developed. The amidation reaction provides a protocol for the synthesis of 2-aminobenzenesulfonamides I (R³ = H, 2-Me-4-F, 3-Cl, 4-Ph, etc.) in good to excellent yields. This strategy features a wide substrate scope, tolerates a broad range of functional groups under external oxidant-free conditions and only releases mol. nitrogen as the sole byproduct. Moreover, the preliminary mechanism was investigated and the proposed reaction pathway was provided.

Advanced Synthesis & Catalysis 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, SDS of cas: 489-17-8.

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

Dai, Hong published the artcileSynthesis and biological activity of 1-{4-[(2-cyanoimino-1,3-thiazolidine-3-yl)methyl]thiazol-2-yl}-3-aroyl ureas, Safety of 2,4-Dichlorobenzamide, the publication is Youji Huaxue (2013), 33(7), 1568-1572, database is CAplus.

In search of novel thiazole derivatives with potent biol. activities, a series of new thiazole compounds I (R = 4-Me, 4-Et, 3-F, 4-F, 2-Cl, 4-Cl, 4-Br, 2,4-Cl₂, 3,4-Cl₂) containing acyl urea moiety were synthesized by the condensation of 2-cyanoimino-3-(2-aminothiazol-4-ylmethyl)thiazolidine with various arylacylisocyanates. The structures of the target compounds were determined by ¹H NMR, MS and elemental anal. The structures of I (R = 4-Me, 2-Cl, 2,4-Cl₂) were further characterized by ¹³C NMR spectra. The bioassay data indicated that some of the title compounds showed fungicidal activities to some extent at the concentration of 50 μg/mL. For example, compound I (R = 4-F)displayed 65.3% inhibition rate against Gibberella zeae, compound I (R = 4-Cl) exhibited 67.3% inhibition rate against Cercospora arachidicola, and compound I (R = 4-Br) showed 56.1% inhibition rate against Physalospora piricola.

Youji Huaxue 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, Safety of 2,4-Dichlorobenzamide.

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

Wang, Yu-Hao published the artcilePhosphine-Catalyzed Annulations Based on [3+3] and [3+2] Trapping of Ketene Intermediates with Thioamides, Formula: C8H9NOS, the publication is Organic Letters (2021), 23(21), 8147-8152, database is CAplus and MEDLINE.

A novel annulation via ketene intermediates, allenyl imide I and alkynoates RC₆H₄CCC(O)OC₆H₄-4-NO₂ (R = H, 4-MeC₆H₄, 2-ClC₆H₄, 3-BrC₆H₄, 4-FC₆H₄, 4-ClC₆H₄) bearing good leaving groups is used for their function in a tandem conjugate addition-elimination reaction (SN2′ type) promoted by nucleophilic phosphine catalysts and developed. By utilizing thioamides as R¹C(S)NH₂ (R¹ = 4-chlorophenyl, thiophen-2-yl, naphthalen-2-yl, etc.) 1S,3N-bis-nucleophiles, [3+3] and [3+2] annulations have been established to allow rapid access to 1,3-thiazin-4-ones II and 5-alkenyl thiazolones III in high yields, resp. Furthermore, the possible reaction mechanisms are proposed on the basis of deuterium labeling experiments and d. functional theory calculations

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 C13H16O2, Formula: C8H9NOS.

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

Hu, Shengquan published the artcileDesign, synthesis and biological evaluation of 4-aryl-5,7-dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-one derivatives as a PI3Kα inhibitor, Quality Control of 1197171-76-8, the publication is Biological & Pharmaceutical Bulletin (2019), 42(6), 1013-1018, database is CAplus and MEDLINE.

A series of 4-aryl-5,7-dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-one derivatives I [R = Ph, 6-amino-3-pyridyl, 2-amino-1,3-benzoxazol-5-yl, etc.] were designed as a phosphoinositide 3-kinase α (PI3Kα) inhibitor by scaffold hopping. The target compounds I were synthesized from di-Et malonate and Et chloroacetate by nucleophilic substitution, ring-closure, chlorination and Suzuki reaction, etc. The biol. activities of compounds I were evaluated with cytotoxic activity in vitro on Uppsala 87 Malignant Glioma (U87MG) and prostate cancer-3 (PC-3) by cell counting kit-8 (CCK-8). The results showed that compound I [R = 6-amino-3-pyridyl] displayed higher inhibition than pos. control PI-103, and high PI3Kα inhibitory activity with IC₅₀ of 113 ± 9nM in same order of magnitude as BEZ235. In addition, the LogK_ow values and mol. docking studies were performed to further investigate drug-like properties of target compounds I and interactions between compound I [R = 6-amino-3-pyridyl] and PI3Kα.

Biological & Pharmaceutical Bulletin 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 C14H20BNO3, Quality Control of 1197171-76-8.

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

Du, Xian published the artcileHydrosulfonylation of Alkenes with Sulfonyl Imines via Ir/Cu Dual Photoredox Catalysis, SDS of cas: 169590-42-5, the publication is Organic Letters (2022), 24(22), 3944-3949, database is CAplus and MEDLINE.

Here utilizing sulfonyl imines as sulfonyl radical precursors for hydrosulfonylation of activated alkenes via visible-light irradiation was reported. By preinstallation of functional groups into the sulfonamides and subsequent hydrosulfonylation, a variety of complex sulfones were synthesized with good efficiency under Ir/Cu dual photoredox catalysis. Addnl., this protocol expands the research in late-stage N-S bond modification in sulfonamides.

Organic Letters published new progress about 169590-42-5. 169590-42-5 belongs to amides-buliding-blocks, auxiliary class Sulfamide,Immunology/Inflammation,COX, name is 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, and the molecular formula is C17H14F3N3O2S, SDS of cas: 169590-42-5.

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

Zhi, Xueli published the artcileNanofilamentous Virus-Based Dynamic Hydrogels with Tunable Internal Structures, Injectability, Self-Healing, and Sugar Responsiveness at Physiological pH, HPLC of Formula: 2024542-05-8, the publication is Langmuir (2018), 34(43), 12914-12923, database is CAplus and MEDLINE.

With expanding applications of hydrogels in diverse fields ranging from biomaterials to sensors, actuators, and soft robotics, there is an urgent need to endow one single gel with multiple physicochem. properties, such as stimuli-responsiveness, injectability, self-healing, and tunable internal structures. However, it is challenging to simultaneously incorporate these highly sought-after properties into one single gel. Herein, a conceptual hydrogel system with all of these properties is presented via combining bioconjugate chem., filamentous viruses, and dynamic covalent bonds. Nanofilamentous bioconjugates with diol affinity were prepared by coupling a tailor-synthesized low-pK_a phenylboronic acid (PBA) derivative to a well-defined green nanofiber the M13 virus with a high aspect ratio (PBA-M13). Dynamic hydrogels with tunable mech. strength were prepared by using multiple diol-containing agents such as poly(vinyl alc.) to crosslink such PBA-M13 via the classic boronic-diol dynamic bonds. The as-prepared hydrogels exhibit excellent injectability and self-healing behaviors as well as easy chem. accessibility of the PBA moieties on the virus backbone inside the gel matrix. Ordered internal structures were imparted into virus-based hydrogels by simple shear-induced alignment of the virus nanofibers. Furthermore, unique hydrogels with chiral internal structures were fabricated through in situ gelation induced by diffusion of diol-containing mols. to fix the chiral liquid crystal phase of the PBA-M13 virus. Sugar responsiveness of this gel leads to a glucose-regulated release behavior of payloads such as insulin. All of these properties have been implemented at physiol. pH, which will facilitate future applications of these hydrogels as biomaterials.

Langmuir published new progress about 2024542-05-8. 2024542-05-8 belongs to amides-buliding-blocks, auxiliary class Boronic acid and ester,Boronic Acids, name is 3-(4-Boronobenzamido)propanoic acid, and the molecular formula is C13H10F2, HPLC of Formula: 2024542-05-8.

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

Zhang, Min published the artcileSynthesis and bioactivities of novel pyrazole amides carrying oxazole moiety, Application In Synthesis of 2447-79-2, the publication is Youji Huaxue (2020), 40(6), 1772-1778, database is CAplus.

In order to find new pyrazole amides with wonderful bioactivities, a series of novel pyrazole amide derivatives were synthesized by introducing substituted oxazole ring into the C-5 position of pyrazole skeleton based on the lead chlorantraniliprole. The aimed compounds were structurally characterized through ¹H NMR, ¹³C NMR and elemental anal. The preliminary bioassay results exhibited that all the title compounds displayed more than 90% insecticidal activities against Mythimna separata (Walker) at 500μg/mL. At the dosage of 100μg/mL, five compounds possessed 90%∼100% insecticidal activities against Mythimna separata (Walker), and three compounds exhibited insecticidal property against Aphis craccivora with 90%∼100%. Addnl., at the dosage of 500μg/mL, two compounds possessed insecticidal activity against Tetranychus cinnabarinus with 80%∼100%.

Youji Huaxue 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 C7H8BBrO3, Application In Synthesis of 2447-79-2.

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

Feng, Yue-Hua published the artcileIncreased apolipoprotein M induced by lack of scavenger receptor BI is not activated via HDL-mediated cholesterol uptake in hepatocytes, Application of [(2-Hexylcyclopentylidene)amino]thiourea, the publication is Lipids in Health and Disease (2018), 200/1-200/8, database is CAplus and MEDLINE.

Background: Scavenger receptor BI (SR-BI) is a classic high-d. lipoprotein (HDL) receptor, which mediates selective lipid uptake from HDL cholesterol esters (HDL-C). Apolipoprotein M (ApoM), as a component of HDL particles, could influence preβ-HDL formation and cholesterol efflux. The aim of this study was to determine whether SR-BI deficiency influenced the expression of ApoM. Methods: Blood samples and liver tissues were collected from SR-BI gene knockout mice, and serum lipid parameters, including total cholesterol (TC), triglyceride (TG), high and low-d. lipoprotein cholesterol (HDL-C and LDL-C) and ApoM were measured. Hepatic ApoM and ApoAI mRNA levels were also determined In addition, BLT-1, an inhibitor of SR-BI, was added to HepG2 cells cultured with cholesterol and HDL, under serum or serum-free conditions. The mRNA and protein expression levels of ApoM were detected by RT-PCR and western blot. Results: We found that increased serum ApoM protein levels corresponded with high hepatic ApoM mRNA levels in both male and female SR-BI-/- mice. Besides, serum TC and HDL-C were also significantly increased. Treatment of HepG2 hepatoma cells with SR-BI specific inhibitor, BLT-1, could up-regulate ApoM expression in serum-containing medium but not in serum-free medium, even in the presence of HDL-C and cholesterol. Conclusions: Results suggested that SR-BI deficiency promoted ApoM expression, but the increased ApoM might be independent from HDL-mediated cholesterol uptake in hepatocytes.

Lipids in Health and Disease 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, Application of [(2-Hexylcyclopentylidene)amino]thiourea.

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