Category: amides-buliding-blocks

Paul, Alexis published the artcileCombining G-quadruplex targeting motifs on a single peptide nucleic acid scaffold: a hybrid (3 + 1) PNA-DNA bimolecular quadruplex, Application In Synthesis of 186046-83-3, the publication is Chemistry – A European Journal (2008), 14(28), 8682-8689, database is CAplus and MEDLINE.

We describe the 1st G-quadruplex targeting approach that combines intercalation and hybridization strategies by investigating the interaction of a G-rich peptide nucleic acid (PNA) acridone conjugate with a 3-repeat fragment of the human telomere G3 to form a hybrid PNA-DNA quadruplex that mimics the biol. relevant (3 + 1) pure DNA dimeric telomeric quadruplex. Using a combination of UV and fluorescence spectroscopy, CD, and mass spectrometry, we show that PNA can induce the formation of a bimol. hybrid quadruplex even at low salt concentration upon interaction with a single-stranded 3-repeat fragment of telomeric DNA. However, PNA cannot invade a short fragment of B-DNA even if the latter contains a CCC motif complementary to the PNA sequence. These studies could open up new possibilities for the design of a novel generation of quadruplex ligands that target not only the external features of the quadruplex but also its central core constituted by the tetrads themselves.

Chemistry – A European Journal published new progress about 186046-83-3. 186046-83-3 belongs to amides-buliding-blocks, auxiliary class Purine,Carboxylic acid,Amine,Benzene,Amide,Others,PNA,, name is 2-(N-(2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)ethyl)-2-(2-(((benzhydryloxy)carbonyl)amino)-6-oxo-5H-purin-9(6H)-yl)acetamido)acetic acid, and the molecular formula is C40H35N7O8, Application In Synthesis of 186046-83-3.

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

Kim, Jun published the artcileLong-Term Anti-Inflammatory effects of injectable celecoxib nanoparticle hydrogels for achilles tendon regeneration., Recommanded Product: 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, the publication is Acta Biomaterialia (2022), 183-194, database is CAplus and MEDLINE.

The treatment of chronic Achilles tendonitis (AT) often requires prolonged therapy and invasive therapeutic methods such as surgery or therapeutic endoscopy. To prevent the progression of chronic AT, excessive inflammation must be alleviated at an early stage. Corticosteroids or nonsteroidal anti-inflammatory drugs are generally prescribed to control inflammation; however, the high doses and long therapeutic periods required may lead to serious side effects. Herein, a local injectable poly(organophosphazene) (PPZ) – celecoxib (CXB) nanoparticle (PCNP) hydrogel system with long-term anti-inflammatory effects was developed for the treatment of tendonitis. The amphiphilic structure and thermosensitive mech. properties of PPZ means that the hydrophobic CXB can be easily incorporated into the hydrophobic core to form PCNP at 4°C. Following the injection of PCNP into the AT, PCNP hydrogel formed at body temperature and induced long-term local anti-inflammatory effects via sustained release of the PCNP. The therapeutic effects of the injectable PCNP system can alleviate excessive inflammation during the early stages of tissue damage and boost tissue regeneration. This study suggests that PCNP has significant potential as a long-term anti-inflammatory agent through sustained nonsteroidal anti-inflammatory drugs (NSAIDs) delivery and tissue regeneration boosting. In the treatment of Achilles tendinitis, a long-term anti-inflammatory effect is needed to alleviate excessive inflammation and induce regeneration of the damaged Achilles tendon. Injectable poly(organophosphazene)(PPZ)-celecoxib(CXB) nanoparticles (PCNP) generated a long-term, localized-anti-inflammatory effect in the injected region, which successfully induced the expression of anti-inflammatory cytokines and suppressed pro-inflammatory cytokines, while the PCNPs degraded completely. Accordingly, regeneration of the damaged Achilles tendon was achieved through the long-term anti-inflammatory effect induced by a single PCNP injection. The PCNP system therefore has great potential in long-term NSAIDs delivery for various tissue engineering applications.

Acta Biomaterialia 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, Recommanded Product: 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide.

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

Kim, Eun-Young published the artcileBLT2 promotes the invasion and metastasis of aggressive bladder cancer cells through a reactive oxygen species-linked pathway, Formula: C12H23N3S, the publication is Free Radical Biology & Medicine (2010), 49(6), 1072-1081, database is CAplus and MEDLINE.

Aggressive bladder cancer is a major cause of morbidity and mortality. Despite the fact that metastatic disease results in death in the majority of bladder cancer cases, the mol. events regulating the invasive phenotype of aggressive bladder cancer are not well understood. In this study, immunohistochem. examination showed that the leukotriene B₄ receptor BLT2 is overexpressed in advanced malignant bladder cancers (human transitional cell carcinomas) in proportion to advancing stages, with high prognostic significance (p < 0.001). Blockade of BLT2 with the specific antagonist LY255283 or siRNA knockdown significantly suppressed the invasiveness of highly aggressive 253 J-BV bladder cancer cells. Moreover, our results demonstrated that BLT2 mediates invasiveness through a signaling pathway dependent on NAD(P)H oxidase (Nox) 1- and Nox4-induced generation of reactive oxygen species (ROS) and subsequent NF-κB stimulation. Metastasis of 253 J-BV cells in mice was also dramatically suppressed by inhibition of BLT2 or its signaling. These findings suggest that a BLT2-Nox-ROS-NF-κB cascade plays a critical role in bladder cancer invasion and metastasis.

Free Radical Biology & Medicine 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, Formula: C12H23N3S.

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

Moutaoukil, Zakaria published the artcileN-Alkylation of organonitrogen compounds catalyzed by methylene-linked bis-NHC half-sandwich ruthenium complexes, Synthetic Route of 1453-82-3, the publication is Organic & Biomolecular Chemistry (2022), 20(4), 831-839, database is CAplus and MEDLINE.

An efficient ruthenium-catalyzed N-alkylation of amines, amides and sulfonamides was developed employing novel pentamethylcyclopentadienylruthenium(II) complexes bearing the methylene linked bis(NHC) ligand bis(3-methylimidazol-2-ylidene)methane. The acetonitrile complex I was proved to be particularly effective with a broad range of substrates with low catalyst loading (0.1-2.5 mol%) and high functional group tolerance under mild conditions. A total of 52 N-alkylated organonitrogen compounds including biol. relevant scaffolds were synthesized from (hetero)aromatic and aliphatic amines, amides and sulfonamides using alcs. or diols as alkylating agents in up to 99% isolated yield, even on gram-scale reactions. In the case of sulfonamides, it was the first example of N-alkylation employing a transition-metal complex bearing NHC ligands.

Organic & Biomolecular Chemistry 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, Synthetic Route of 1453-82-3.

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

Liu, Fangyao published the artcileAtom transfer radical polymerization as a tool for making poly(N-acryloylglycinamide) with molar mass independent UCST-type transitions in water and electrolytes, Category: amides-buliding-blocks, the publication is Polymer Chemistry (2013), 4(10), 3123-3131, database is CAplus.

Atom transfer radical polymerization (ATRP) of N-acryloylglycinamide has been used as a tool to make poly(NAGA) showing UCST-type phase transitions in water and electrolytes independent of molar mass and end-groups. We hypothesized that similarity in the structure of polymer chain ends with the repeat unit of poly(NAGA) could help in eliminating the effect of molar mass dependence of the cloud point especially in the low molar mass region. The monomer-like end-groups were introduced by choosing an appropriate initiator for ATRP like chloropropionamide (CPA). The catalyst system CuCl/CuCl₂ and tris[2-(dimethylamino)ethyl]-amine (Me₆TREN) as a ligand provided controlled polymerization of NAGA in DMSO at 45° with UCST-type transitions retained in water and electrolytes without being influenced by chain ends/M mass and high concentration of salts like NaCl and Na₂SO₄.

Polymer Chemistry published new progress about 2479-62-1. 2479-62-1 belongs to amides-buliding-blocks, auxiliary class Monomers,Acrylamide Monomers, name is N-(2-Amino-2-oxoethyl)acrylamide, and the molecular formula is C5H8N2O2, Category: amides-buliding-blocks.

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

Liu, Fangyao published the artcileA Non-ionic Thermophilic Hydrogel with Positive Thermosensitivity in Water and Electrolyte Solution, Formula: C5H8N2O2, the publication is Macromolecular Chemistry and Physics (2014), 215(15), 1466-1472, database is CAplus.

The first example of a chem. crosslinked synthetic non-ionic hydrogel showing reversible pos. swelling behavior in pure water as well as electrolyte solution is highlighted. Homopolymeric hydrogels are synthesized from N-acryloylglycinamide with N,N’-methylenbis(acrylamide) as a chem. crosslinker via free radical polymerization in DMSO. The swelling-ratio dependency of the hydrogels upon temperature as well as on the amounts of crosslinker from 1 to 4.8 mol% is studied. With 1 mol% crosslinker, the hydrogel is able to take up over three times water of its weight at 37 °C in pure water and phosphate-buffered saline. All the samples show almost 100% of reversibility for at least 6 d up to 37 °C irresp. of the amount of the crosslinker, making them promising candidates for biomedical applications. The sample with a higher amount of crosslinker, i.e., 4.8 mol% is even stable for over 6 d at 70 °C.

Macromolecular Chemistry and Physics published new progress about 2479-62-1. 2479-62-1 belongs to amides-buliding-blocks, auxiliary class Monomers,Acrylamide Monomers, name is N-(2-Amino-2-oxoethyl)acrylamide, and the molecular formula is C5H8N2O2, Formula: C5H8N2O2.

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

Liu, Fangyao published the artcileControlled radical polymerization of N-acryloylglycinamide and UCST-type phase transition of the polymers, Name: N-(2-Amino-2-oxoethyl)acrylamide, the publication is Journal of Polymer Science, Part A: Polymer Chemistry (2012), 50(23), 4920-4928, database is CAplus.

N-Acryloylglycinamide was polymerized via the reversible addition fragmentation transfer process without sacrificing its key property, the upper critical solution temperature in water. This could be achieved by choosing an appropriate nonionic initiator [2,2′-azobis(4-methoxy-2.4-dimethyl valeronitrile) (V-70)] and nonionic chain-transfer agent (cyanomethyl dodecyl trithiocarbonate). A good molar mass control was accomplished as proved by the linear increase of molar mass with conversion, a chain extension experiment, and low dispersity. The influence of molar mass, polymer end groups, or salt concentration on the cloud point was analyzed by turbidimetry. Polymer end groups exerted a distinct effect on the cloud points, whereas the influence increased with decreasing molar masses. © 2012 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem, 2012.

Journal of Polymer Science, Part A: Polymer Chemistry published new progress about 2479-62-1. 2479-62-1 belongs to amides-buliding-blocks, auxiliary class Monomers,Acrylamide Monomers, name is N-(2-Amino-2-oxoethyl)acrylamide, and the molecular formula is C5H8N2O2, Name: N-(2-Amino-2-oxoethyl)acrylamide.

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

Saniee, Fateme published the artcileGlutamate-urea-based PSMA-targeted PLGA nanoparticles for prostate cancer delivery of docetaxel, Synthetic Route of 2418-95-3, the publication is Pharmaceutical Development and Technology (2021), 26(4), 381-389, database is CAplus and MEDLINE.

Targeted drug delivery is a tool to make treatment more specific, selective, and effective and to prevent unwanted complications. Prostate specific membrane antigen (PSMA) is a useful biomarker in order to monitor and control prostate cancer. Glutamate-Urea-R (Glu-Urea-R) is a PSMA enzyme inhibitor capable of binding to this surface marker of prostate cancer cell in an efficient and special manner. The aim of this project was to develop a docetaxel-loaded nanoparticle of poly (lactic-co-glycolic acid) polyethylene glycol which is cojugated to a urea-based anti-PSMA ligand named glutamate-urea-lysine (glu-urea-lys) for targeted delivery of docetaxel in prostate cancer. The obtained nanoparticles, prepared by nanopptn. method, were spheres with a particle size of around 150 nm and zeta potential of -7.08 mV. Uptake studies on the PC3 (as PSMA neg.) and LNCaP (as PSMA pos.) cells demonstrated that drug uptake was efficient by the PSMA pos. cells. IC₅₀ of targeted NPs on LNCaP cell line compared to non-targeted ones was reduced by more than 70% in three different incubation times of 24, 48, and 72 h. In conclusion, the nanoparticles are expected to specifically transport docetaxel to PSMA-pos. prostate cancer cells and consequently, enhance the antitumor efficacy of docetaxel on these cells.

Pharmaceutical Development and Technology 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, Synthetic Route of 2418-95-3.

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

Bridge, Thomas published the artcileSite-Specific Encoding of Photoactivity in Antibodies Enables Light-Mediated Antibody-Antigen Binding on Live Cells, Quality Control of 2418-95-3, the publication is Angewandte Chemie, International Edition (2019), 58(50), 17986-17993, database is CAplus and MEDLINE.

Antibodies found applications in several fields, including, medicine, diagnostics, and nanotechnol., yet methods to modulate antibody-antigen binding using an external agent remain limited. Here, the authors have developed photoactive antibody fragments by genetic site-specific replacement of single tyrosine residues with photocaged tyrosine, in an antibody fragment, 7D12. A simple and robust assay is adopted to evaluate the light-mediated binding of 7D12 mutants to its target, epidermal growth factor receptor (EGFR), on the surface of cancer cells. Presence of photocaged tyrosine reduces 7D12-EGFR binding affinity by over 20-fold in two out of three 7D12 mutants studied, and binding is restored upon exposure to 365 nm light. Mol. dynamics simulations explain the difference in effect of photocaging on 7D12-EGFR interaction among the mutants. Finally, the authors demonstrate the application of photoactive antibodies in delivering fluorophores to EGFR-pos. live cancer cells in a light-dependent manner.

Angewandte Chemie, International Edition 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, Quality Control of 2418-95-3.

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

Kempf, Dale J. published the artcileDiscovery of Ritonavir, a Potent Inhibitor of HIV Protease with High Oral Bioavailability and Clinical Efficacy, HPLC of Formula: 14294-10-1, the publication is Journal of Medicinal Chemistry (1998), 41(4), 602-617, database is CAplus and MEDLINE.

The structure-activity studies leading to the potent and clin. efficacious HIV protease inhibitor ritonavir are described. Beginning with the moderately potent and orally bioavailable inhibitor A-80987, systematic investigation of peripheral (P3 and P2′) heterocyclic groups designed to decrease the rate of hepatic metabolism provided analogs with improved pharmacokinetic properties after oral dosing in rats. Replacement of pyridyl groups with thiazoles provided increased chem. stability toward oxidation while maintaining sufficient aqueous solubility for oral absorption. Optimization of hydrophobic interactions with the HIV protease active site produced ritonavir, with excellent in vitro potency (EC₅₀ = 0.02 μM) and high and sustained plasma concentrations after oral administration in 4 species. Details of the discovery and preclin. development of ritonavir are described.

Journal of Medicinal Chemistry 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 C5H10N2OS, HPLC of Formula: 14294-10-1.

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