Month: December 2022

Kaithwas, Gaurav published the artcileEffect of L. usitatissimum (flaxseed/linseed) fixed oil against distinct phases of inflammation, Product Details of C12H23N3S, the publication is ISRN Inflammation (2013), 735158/1-735158/5, 5 pp., database is CAplus and MEDLINE.

The present investigation summarizes the effect of Linum usitatissimum fixed oil against different phases of acute inflammatory reaction, namely, protein exudation, peritoneal capillary permeability and leukocyte migration. The fixed oil exhibited dose-dependent inhibition of protein exudation vascular permeability, comparable to standard aspirin. The oil also inhibited the leukocyte migration in pleural exudates in a dose-dependent manner. Production of less vasodilatory (PGE3) and chemotactic (LTB5) eicosanoids through EPA (derived from linolenic acid) metabolism could account for the above observations.

ISRN Inflammation 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, Product Details of C12H23N3S.

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

Kappauf, Katrin published the artcileModulation of Transaminase Activity by Encapsulation in Temperature-Sensitive Poly(N-acryloyl glycinamide) Hydrogels, Category: amides-buliding-blocks, the publication is ChemBioChem (2021), 22(24), 3452-3461, database is CAplus and MEDLINE.

Smart hydrogels hold much potential for biocatalysis, not only for the immobilization of enzymes, but also for the control of enzyme activity. We investigated upper critical solution temperature-type poly N-acryloyl glycinamide (pNAGA) hydrogels as a smart matrix for the amine transaminase from Bacillus megaterium (BmTA). Phys. entrapment of BmTA in pNAGA hydrogels results in high immobilization efficiency (>89%) and high activity (97%). The temperature-sensitiveness of pNAGA is preserved upon immobilization of BmTA and shows a gradual deswelling upon temperature reduction While enzyme activity is mainly controlled by temperature, deactivation tended to be higher for immobilized BmTA (=62-68%) than for free BmTA (=44%), suggesting a deactivating effect due to deswelling of the pNAGA gel. Although the deactivation in response to hydrogel deswelling is not yet suitable for controlling enzyme activity sufficiently, it is nevertheless a good starting point for further optimization.

ChemBioChem 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

Paul, Bhaskar published the artcileCobalt Catalyzed N-Methylation of Amides using Methanol, HPLC of Formula: 1453-82-3, the publication is Asian Journal of Organic Chemistry (2022), 11(1), e202100678, database is CAplus.

N-Methylation of amides with methanol is reported in the presence of an in-situ generated cobalt catalyst. With this simple protocol, various amides were methylated in up to 99% yield. Notably, the involvement of active cobalt (I) hydride in this methylation process was revealed by control experiments Deuterium labeling studies were carried out using methanol-d₄, taking benzamide and the possible intermediate N-(hydroxymethyl)benzamide to understand this transformation. Addnl., DFT calculations for the amide-formaldehyde coupling were performed to elucidate the influence of catalyst in this step.

Asian Journal of Organic 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, HPLC of Formula: 1453-82-3.

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

Wancewicz, Edward V. published the artcilePeptide Nucleic Acids conjugated to short basic peptides show improved pharmacokinetics and antisense activity in adipose tissue, Computed Properties of 186046-83-3, the publication is Journal of Medicinal Chemistry (2010), 53(10), 3919-3926, database is CAplus and MEDLINE.

A peptide nucleic acid (PNA) targeting a splice junction of the murine PTEN primary transcript was covalently conjugated to various basic peptides. When systemically administered to healthy mice, the conjugates displayed sequence-specific alteration of PTEN mRNA splicing as well as inhibition of full length PTEN protein expression. Correlating activity with drug concentration in various tissues indicated strong tissue-dependence, with highest levels of activity observed in adipose tissue. While the presence of a peptide carrier was found to be crucial for efficient delivery to tissue, little difference was observed between the various peptides evaluated. A second PNA-conjugate targeting the murine insulin receptor primary transcript showed a similar activity profile, suggesting that short basic peptides can generally be used to effectively deliver peptide nucleic acids to adipose tissue.

Journal of Medicinal Chemistry 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 C13H20BNO3, Computed Properties of 186046-83-3.

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

Asghari, Ali Akbar published the artcileAnti-inflammatory, anti-oxidant and anti-apoptotic effects of olive leaf extract in cardiac tissue of diabetic rats., Synthetic Route of 137862-53-4, the publication is The Journal of pharmacy and pharmacology (2022), 74(7), 961-972, database is MEDLINE.

OBJECTIVES: Inflammatory process and apoptosis are involved in the pathogenesis of cardiac injury and oxidative damage caused by diabetes mellitus. The cardioprotective effects of standardized aqueous ethanolic olive leaf extract (OLE), metformin (as a cardiovascular protective agent) and valsartan (as an angiotensin receptor blocker) in the streptozotocin-induced diabetic rats were evaluated. METHODS: Wistar rats divided into control, diabetic, OLE-treated (100, 200 and 400 mg/kg), metformin (300 mg/kg)-treated, valsartan (30 mg/kg)-treated and metformin/valsartan-treated diabetic groups. Biochemical parameters, including malondialdehyde (MDA) levels, superoxide dismutase (SOD) and catalase (CAT) activates, and the total contents of thiol were measured, and histopathological and gene expression studies were done on cardiac tissues. Fasting blood sugar (FBS) and cardiac injury markers were examined in serum. KEY FINDINGS: FBS; the serum levels of lactate dehydrogenase (LDH), creatine kinase-muscle/brain (CK-MB), aspartate aminotransferase (AST); and heart tissue MDA levels due to diabetes were significantly alleviated by OLE treatment (effect size; ηp2 = 0.934, 0.888, 0.848, 0.888 and 0.879, respectively), and SOD and CAT activity and the thiol content in heart tissue were significantly increased (effect size; ηp2 = 0.770, 0.749 and 0.753, respectively). Interleukin-1β (IL-1β), tumour necrosis factor-α (TNF-α) and the number of infiltrating inflammatory cells were reduced in cardiac tissues of OLE-treated groups compared with the diabetic rats (effect size; ηp2 = 0.969 and 0.949, respectively). OLE up-regulated BCL2 gene expression and down-regulated BAX gene expression in cardiac tissue (effect size; ηp2= 0.490 and 0.522, respectively). CONCLUSION: OLE in a dose-dependent manner ameliorates cardiac damage in diabetic cardiomyopathy, perhaps through attenuating inflammation, oxidative stress and apoptosis.

The Journal of pharmacy and pharmacology published new progress about 137862-53-4. 137862-53-4 belongs to amides-buliding-blocks, auxiliary class GPCR/G Protein,Angiotensin Receptor, name is (S)-2-(N-((2′-(1H-Tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid, and the molecular formula is C24H29N5O3, Synthetic Route of 137862-53-4.

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

Orr, Brian published the artcilePhase I trial combining chemokine-targeting with loco-regional chemoimmunotherapy for recurrent, platinum-sensitive ovarian cancer shows induction of CXCR3 ligands and markers of type 1 immunity, Application of 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, the publication is Clinical Cancer Research (2022), 28(10), 2038-2049, database is CAplus and MEDLINE.

Increased prevalence of cytotoxic T lymphocytes (CTL) in the tumor microenvironment (TME) predicts pos. outcomes in patients with epithelial ovarian cancer (EOC), whereas the regulatory T cells (Treg) predict poor outcomes. Guided by the synergistic activity of TLR3 ligands, IFNα, and COX-2 blockers in selectively enhancing CTL-attractants but suppressing Treg-attractants, we tested a novel i.p. chemoimmunotherapy combination (CITC), to assess its tolerability and TME-modulatory impact in patients with recurrent EOC. Twelve patients were enrolled in phase I portion of the trial NCT02432378, and treated with i.p. cisplatin, i.p. rintatolimod (dsRNA, TLR3 ligand), and oral celecoxib (COX-2 blocker). Patients in cohorts 2, 3, and 4 also received i.p. IFNα at 2, 6, and 18 million units (MU), resp. Primary objectives were to evaluate safety, identify phase 2 recommended dose (P2RD), and characterize changes in the immune TME. Peritoneal resident cells and i.p. wash fluid were profiled via NanoString and Meso Scale Discovery (MSD) multiplex assay, resp. The P2RD of IFNα was 6 MU. Median progression-free survival and overall survival were 8.4 and 30 mo, resp. Longitudinal sampling of the peritoneal cavity via i.p. washes demonstrated local upregulation of IFN-stimulated genes (ISG), including CTL-attracting chemokines (CXCL-9, -10, -11), MHC I/II, perforin, and granzymes. These changes were present 2 days after chemokine modulation and subsided within 1 wk. The chemokine-modulating i.p.-CITC is safe, tolerable, and associated with ISG changes that favor CTL chemoattraction and function. This combination (plus DC vaccine) will be tested in a phase II trial.

Clinical Cancer Research 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, Application of 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide.

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

Choudhury, Shubhranshu Shekhar published the artcileHydrogen bond mediated conversion of benzenenitriles and arylacetonitriles to amides: an “on/in-water” reaction strategy, Application In Synthesis of 1453-82-3, the publication is Green Chemistry (2022), 24(12), 4981-4990, database is CAplus.

Owing to the myriad of applications that amides have, hydration of nitriles has emerged as one of the most preferred atom-efficient synthesis methods. Being kinetically slow, this strategy requires some efficient catalysts. Herein, authors discovered choline hydroxide as an environmentally benign, metal-free and inexpensive catalyst for the hydration of aromatic and heteroaromatic nitriles on/in water with excellent yields. All the reactions proceeded under mild/moderate conditions, facilitated by the hydrogen bonds between the catalyst and the reactant or intermediate. D. functional theory (DFT) studies were used to propose the plausible reaction mechanism, which was further corroborated with kinetics measurements using quant. ¹⁹F NMR spectroscopy, thereby revealing the presence of H-bond mediated catalysis which brought down the activation energy barrier even lower than those in previous reports on using H₂SO₄ or Ru(OH)_x/Al₂O₃ as catalysts. This work offers an “on/in-water” reaction strategy for the efficient hydration of nitriles and will pave the path towards novel routes for the com. synthesis of amides.

Green 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, Application In Synthesis of 1453-82-3.

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

Tapolcsanyi, Pal published the artcileSynthesis of the dibenzo[f,h]phthalazine and dibenzo[f,h]cinnoline skeleton via a Suzuki-Pd-catalyzed intramolecular arylation’ and a Suzuki-Pschorr’ approach, Computed Properties of 146140-95-6, the publication is Tetrahedron (2003), 59(31), 5919-5926, database is CAplus.

Palladium-catalyzed intramol. arylation of 2-benzyl-5-(2-bromophenyl)-4-phenylpyridazin-3(2H)-one yielded hitherto unknown 2-benzyldibenzo[f,h]phthalazin-1(2H)-one. The synthesis of this new tetracyclic pyridazinone from 2-benzyl-5-(2-aminophenyl)-4-phenylpyridazin-3(2H)-one via a Pschorr type reaction was also investigated. Similarly, the construction of 2-methyldibenzo[f,h]cinnolin-3(2H)-one from 2-methyl-5-(2-bromophenyl)-6-phenylpyridazin-3(2H)-one and 2-methyl-5-(2-aminophenyl)-6-phenylpyridazin-3(2H)-one is also reported. Removal of the N-benzyl protective group of 2-benzyl-dibenzo[f,h]phthalazin-1(2H)-one with AlCl₃ yielded unsubstituted dibenzo[f,h]phthalazin-1(2H)-one.

Tetrahedron published new progress about 146140-95-6. 146140-95-6 belongs to amides-buliding-blocks, auxiliary class Boronic acid and ester,Amine,Benzene,Amide,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (2-Pivalamidophenyl)boronic acid, and the molecular formula is C15H10O2, Computed Properties of 146140-95-6.

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

Hostyn, Steven published the artcileSynthesis of the benzo-β-carboline isoneocryptolepine: the missing indoloquinoline isomer in the alkaloid series cryptolepine, neocryptolepine and isocryptolepine, HPLC of Formula: 146140-95-6, the publication is Tetrahedron (2005), 61(6), 1571-1577, database is CAplus.

7H-Indolo[2,3-c]quinoline has been synthesized in two steps via a new approach starting from com. available 3-bromoquinoline and 2-bromoaniline. The new methodol. consists of two consecutive palladium-catalyzed reactions: a selective Buchwald/Hartwig amination followed by an intramol. Heck-type reaction. Alternatively, the same skeleton has also been prepared via the combination of a Suzuki arylation with an intramol. nitrene insertion starting from 4-chloroquinoline and {2-[(2,2-dimethylpropanoyl)amino]phenyl}boronic acid. Selective methylation of 7H-indolo[2,3-c]quinoline yielded 5-methyl-5H-indolo[2,3-c]quinoline (isoneocryptolepine, I) which is an interesting new lead compound in the search for new antiplasmodial drugs.

Tetrahedron published new progress about 146140-95-6. 146140-95-6 belongs to amides-buliding-blocks, auxiliary class Boronic acid and ester,Amine,Benzene,Amide,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (2-Pivalamidophenyl)boronic acid, and the molecular formula is C11H16BNO3, HPLC of Formula: 146140-95-6.

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

Cavallari, Ilaria published the artcileSGLT-2 Inhibitors on Top of Current Pharmacological Treatments for Heart Failure: A Comparative Review on Outcomes and Cost Effectiveness, HPLC of Formula: 137862-53-4, the publication is American Journal of Cardiovascular Drugs (2022), 22(3), 263-270, database is CAplus and MEDLINE.

A review. Heart failure (HF) represents a major global health and economic burden with still unacceptably high morbidity and mortality rates. In recent decades, novel therapeutic opportunities with a significant impact on HF outcomes have been introduced in addition to angiotensin-converting enzyme (ACE) inhibitors, β-blockers, and mineralocorticoid receptor antagonists. These include drugs such as ivabradine, sacubitril-valsartan, and sodium-glucose cotransporter-2 (SGLT-2) inhibitors. The availability of an extremely large pharmacol. armamentarium to face this chronic global disease highlights the importance of assessing cost effectiveness to promote sustainable healthcare. In light of the recent approval of SGLT-2 inhibitors for the treatment of HF with reduced ejection fraction, including in individuals without type 2 diabetes mellitus, the aim of this review was to provide an updated comparative evaluation of the efficacy and cost effectiveness of different pharmacol. treatments for the prevention (stage A) and treatment of asymptomatic (stage B) and symptomatic (stages C-D) left ventricular dysfunction.

American Journal of Cardiovascular Drugs published new progress about 137862-53-4. 137862-53-4 belongs to amides-buliding-blocks, auxiliary class GPCR/G Protein,Angiotensin Receptor, name is (S)-2-(N-((2′-(1H-Tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid, and the molecular formula is C24H29N5O3, HPLC of Formula: 137862-53-4.

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