Month: December 2022

Ma, Yao published the artcileIdentification of benzofused five-membered sultams, potent dual NOD1/NOD2 antagonists in vitro and in vivo, Related Products of amides-buliding-blocks, the publication is European Journal of Medicinal Chemistry (2020), 112575, database is CAplus and MEDLINE.

Nucleotide-binding oligomerization domain-containing proteins 1 and 2 play important roles in immune system activation. Recently, a shift has occurred due to the emerging knowledge that preventing nucleotide-binding oligomerization domains (NODs) signaling could facilitate the treatment of some cancers, which warrants the search for dual antagonists of NOD1 and NOD2. Herein, we undertook the synthesis and identification of a new class of derivatives of dual NOD1/NOD2 antagonists with novel benzofused five-membered sultams. Compound 14k(I) was finally demonstrated to be the most potent mol. that inhibits both NOD1-and NOD2-stimulated NF-κB and MAPK signaling in vitro and in vivo.

European Journal of Medicinal 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, Related Products of amides-buliding-blocks.

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

Wu, Ziying published the artcileAssociation between tramadol use and risk of pneumonia in the middle-aged and elderly populations: a propensity-score matched cohort study, SDS of cas: 169590-42-5, the publication is European Journal of Pain (Oxford, United Kingdom) (2022), 26(6), 1245-1255, database is CAplus and MEDLINE.

Tramadol is a widely used weak opioid; however, the evidence for its safety profile in respiratory system needs addnl. information. We aimed to examine whether tramadol use is associated with an increased risk of pneumonia in the general population. We conducted five propensity-score (PS) matched cohort studies in The Health Improvement Network database. Participants aged ≥50-years initiated tramadol were compared with those initiated one of the following analgesics: codeine (n = 144,506), naproxen (n = 113,028), diclofenac (n = 74,297), celecoxib (n = 42,538), or etoricoxib (n = 27,232). The outcome was incident pneumonia. During 6-mo follow-up, 395 pneumonia (5.6/1000 person-years) occurred in the tramadol group and 414 pneumonia (5.9/1000 person-years) occurred in the PS matched codeine group. Compared with codeine group, the risk of pneumonia was lower in the tramadol group (hazard ratio [HR] = 0.63, 95% confidence interval [CI]: 0.49-0.82) during the first 30-day follow-up, but comparable between groups over the entire 6-mo follow-up (HR = 0.95, 95%CI: 0.83-1.09). In addition, the risk of pneumonia was higher in the tramadol group than that in the PS matched naproxen (HR = 1.68, 95%CI: 1.37-2.06), diclofenac (HR = 1.63, 95%CI: 1.31-2.03), celecoxib (HR = 1.64, 95%CI: 1.20-2.24) or etoricoxib (HR = 1.61, 95%CI: 1.04-2.49) group. The present study indicated that tramadol initiators had a lower risk of incident pneumonia than codeine initiators during the short-time follow-up, but had a comparable pneumonia risk compared with codeine initiators and had a higher risk of pneumonia compared with NSAIDs initiators over the entire 6-mo follow-up duration. Confirmation of the present findings and determination of the underlying mechanism will require more studies. Tramadol might not be a safer alternative analgesic to codeine or NSAIDs. Both of health-care providers and patients may need to be on alert for its safety profile in respiratory system in future clin. practice.

European Journal of Pain (Oxford, United Kingdom) 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 C4H11NO, SDS of cas: 169590-42-5.

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

Price, Katilyn J. published the artcileEvaluation of peanut tolerance to mid-season applications of PPO-Inhibitor herbicides mixed with different surfactants, Synthetic Route of 79-07-2, the publication is Crop Protection (2021), 105557, database is CAplus.

Protoporphyrinogen oxidase (PPO) inhibitor herbicides are being increasingly used to control acetolactate synthases (ALS) inhibitor-resistant weeds in peanuts (Arachis hypogaea L.). However, PPO-inhibitor herbicides can injure the crop under certain application conditions, especially under abiotic stress and surfactants may exacerbate this injury. The objectives of this study were to (1) investigate the effect of PPO-inhibitor based treatments on dryland peanut growth and yield when applied at three timings in mid-season, (2) evaluate the interactions of surfactants, chloroacetamide herbicides, and PPO-inhibitors, and (3) assess the level of correlation of normalized difference vegetation index (NDVI) readings to traditional visible injury rating. Field studies were conducted in Henry and Escambia counties in Alabama, U.S. during 2018, and 2019. Up to 55% of visible peanut injury was observed with acifluorfen, lactofen, and carfentrazone-Et treatments. In general, the NDVI readings correlated significantly with traditional visible injury ratings. A tank mixture of chloroacetamide herbicides (pyroxasulfone, S-metolachlor, dimethenamid-P) with lactofen did not lead to more injury or yield loss than lactofen applied alone. Yield losses up 27% were observed with carfentrazone-Et plus a high surfactant oil concentrate (HSOC) at 75 and 90 days after planting (DAP) as compared to the non-treated check (NTC). Overall, treatments with HSOC and/or carfentrazone-Et were more likely to cause significant injury and yield loss than treatments with acifluorfen or lactofen plus nonionic surfactant (NIS). Peanuts are more sensitive to PPO-inhibitor herbicides at 75 DAP. NDVI did provide addnl. plant health information to subjective injury ratings, however, neither of these measurements are reliable predictors of peanut yield loss.

Crop Protection 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, Synthetic Route of 79-07-2.

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

Tong, Wei published the artcilePalladium-Metalated Porous Organic Polymers as Recyclable Catalysts for the Chemoselective Synthesis of Thiazoles from Thiobenzamides and Isonitriles, Related Products of amides-buliding-blocks, the publication is Organic Letters (2018), 20(8), 2494-2498, database is CAplus and MEDLINE.

Two types of thiazole derivatives are synthesized through a multistep cascade sequence with Pd-metalated phosphorus-doped porous organic polymers (POPs) as heterogeneous catalysts. The POPs could be used as both ligands and catalyst supports. No obvious aggregation and loss of any catalytic activity of the catalysts were observed after 10 runs of the reaction. More importantly, imidazo[4,5-d]thiazoles, which are a new class of thiazole derivatives, could be obtained through K₂CO₃-promoted intramol. cyclization of the synthesized polysubstituted thiazoles. Furthermore, the in vitro anticancer activity of these new compounds were tested with MTT assay, and compound I exhibited good antitumor activity toward T-24 and A549 cells with IC₅₀ values of 10.3 ± 0.8 and 11.8 ± 0.5 μM, resp. In addition, the action mechanism of compound I on tumor cells was determined

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 C11H15NOS, Related Products of amides-buliding-blocks.

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

Wang, Xiaoran published the artcileAquaporin 4 differentially modulates osmotic effects on vasopressin neurons in rat supraoptic nucleus, Name: N-(1,3,4-Thiadiazol-2-yl)nicotinamide, the publication is Acta Physiologica (2021), 232(3), e13672, database is CAplus and MEDLINE.

Aim : Glial fibrillary acidic protein (GFAP) molecularly associates with aquaporin 4 (AQP4) in astrocytic plasticity. Here, we further examined how AQP4 modulates osmotic effects on vasopressin (VP) neurons in rat supraoptic nucleus (SON) through interactions with GFAP in astrocytes. Methods : Brain slices from adult male rats were kept under osmotic stimulation. Western blot, co-immunoprecipitation, immunohistochem. and patch-clamp recordings were used for anal. of expressions and interactions between GFAP and AQP4, astrocyte-specific proteins in the SON, as well as their influence on VP neuronal activity. Data were analyzed using SPSS software. Results : Hyposmotic challenge (HOC) of acute SON slices caused an early (within 5 min) and transient increase in the colocalization of AQP4 with GFAP filaments. This effect was prominent at astrocytic processes surrounding VP neuron somata and was accompanied by inhibition of VP neuronal activity. Similar HOC effect was seen in the SON isolated from rats subjected to in vivo HOC, wherein a transiently increased mol. association between GFAP and AQP4 was detected using co-immunoprecipitation The late stage rebound excitation (10 min) of VP neurons in brain slices subjected to HOC and the associated astrocytic GFAP’s ‘return to normal’ were both hampered by 2-(nicotinamide)-1,3,4-thiadiazole, a specific AQP4 channel blocker that itself did not influence VP neuronal activity. Moreover, this agent prevented hyperosmotic stress-evoked excitation of VP neurons and associated reduction in GFAP filaments. Conclusion : These findings indicate that osmotically driven increase in VP neuronal activity requires the activation of AQP4, which determines a retraction of GFAP filaments.

Acta Physiologica published new progress about 51987-99-6. 51987-99-6 belongs to amides-buliding-blocks, auxiliary class Pyridine,Thiadiazole,Amine,Amide,Inhibitor, name is N-(1,3,4-Thiadiazol-2-yl)nicotinamide, and the molecular formula is C5H7F3O3, Name: N-(1,3,4-Thiadiazol-2-yl)nicotinamide.

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

Shi, Xiaoyu published the artcileLabel-retention expansion microscopy, Recommanded Product: H-Lys(Boc)-OH, the publication is Journal of Cell Biology (2021), 220(9), e202105067, database is CAplus and MEDLINE.

Expansion microscopy (ExM) increases the effective resolving power of any microscope by expanding the sample with swellable hydrogel. Since its invention, ExM has been successfully applied to a wide range of cell, tissue, and animal samples. Still, fluorescence signal loss during polymerization and digestion limits mol.-scale imaging using ExM. Here, we report the development of label-retention ExM (LR-ExM) with a set of trifunctional anchors that not only prevent signal loss but also enable high-efficiency labeling using SNAP and CLIP tags. We have demonstrated multicolor LR-ExM for a variety of subcellular structures. Combining LR-ExM with superresoln. stochastic optical reconstruction microscopy (STORM), we have achieved mol. resolution in the visualization of polyhedral lattice of clathrin-coated pits in situ.

Journal of Cell Biology 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 C37H30ClIrOP2, Recommanded Product: H-Lys(Boc)-OH.

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

Wang, Zheng published the artcileFormation of disinfection byproducts from chlorinated soluble microbial products: Effect of carbon sources in wastewater denitrification processes, Formula: C2H4ClNO, the publication is Chemical Engineering Journal (Amsterdam, Netherlands) (2022), 134237, database is CAplus.

Carbon sources are crucial for biol. denitrification in wastewater treatment that significantly affects the production of soluble microbial products (SMPs), thereby affecting the formation of disinfection byproducts (DBPs) during subsequent chlorination. However, the effect of carbon sources on DBPs formation has not been studied. In this work, sodium acetate, sodium lactate, and glucose were used as carbon sources, and denitrifying SMPs derived from different carbon sources were used as DBPs precursors to investigate the formation potential (FP) of 16 carbonaceous DBPs and 19 nitrogenous DBPs. Results showed that the carbonaceous DBPs FP of SMPs derived from acetate, lactate, and glucose were 502.1-584.3, 250.3-288.9, and 374.7-439.1μg/L, resp., and the nitrogenous DBPs FP were 19.1-45.6, 12.8-21.9, and 7.9-9.0μg/L, resp. After chlorination, the genotoxicity of SMPs measured by the SOS/umu test was also evaluated with 364 ng 4-NQO/L for acetate, 212 ng 4-NQO/L for lactate, and 138 ng 4-NQO/L for glucose. Based on XPS, chem. structures of SMPs were characterized, and their relationship with DBPs FP was investigated to explain the mechanism of DBPs formation. Aromatic C and C-O were found to be the major precursor structures to form carbonaceous DBPs, and their lowest proportions in lactate-derived SMPs caused the lowest carbonaceous DBPs FP. Organic nitrogen, including aromatic N, amide/peptide N, and primary amine N, was the precursor of nitrogenous DBPs. The lowest concentration of dissolved organic nitrogen for glucose-derived SMPs caused the lowest nitrogenous DBPs FP and genotoxicity. Glucose may be a better choice among the three carbon sources in terms of reducing genotoxicity.

Chemical Engineering Journal (Amsterdam, Netherlands) 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 C15H19BO2, Formula: C2H4ClNO.

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

Ma, Yuying published the artcileApplication of Dually Activated Michael Acceptor to the Rational Design of Reversible Covalent Inhibitor for Enterovirus 71 3C Protease, Safety of 2-Cyano-N-ethylacetamide, the publication is Journal of Medicinal Chemistry (2019), 62(13), 6146-6162, database is CAplus and MEDLINE.

Targeted covalent inhibitors (TCIs) have attracted growing attention from the pharmaceutical industry in recent decades because they have potential advantages in terms of efficacy, selectivity, and safety. TCIs have recently evolved into a new version with reversibility that can be systematically modulated. This feature may diminish the risk of haptenization and help optimize the drug-target residence time as needed. The enteroviral 3C protease (3C^pro) is a valuable therapeutic target, but the development of 3C^pro inhibitors is far from satisfactory. Therefore, we aimed to apply a reversible TCI approach to the design of novel 3C^pro inhibitors. The introduction of various substituents onto the α-carbon of classical Michael acceptors yielded inhibitors bearing several classes of warheads. Using steady-state kinetics and biomol. mass spectrometry, we confirmed the mode of reversible covalent inhibition and elucidated the mechanism by which the potency and reversibility were affected by electronic and steric factors. This research produced several potent inhibitors with good selectivity and suitable reversibility; moreover, it validated the reversible TCI approach in the field of viral infection, suggesting broader applications in the design of reversible covalent inhibitors for other proteases.

Journal of Medicinal Chemistry published new progress about 15029-36-4. 15029-36-4 belongs to amides-buliding-blocks, auxiliary class Nitrile,Amine,Aliphatic hydrocarbon chain,Amide, name is 2-Cyano-N-ethylacetamide, and the molecular formula is C5H8N2O, Safety of 2-Cyano-N-ethylacetamide.

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

Li, Jianting published the artcileStructural landscape investigations on bendable plastic crystals of isonicotinamide polymorphs, Related Products of amides-buliding-blocks, the publication is Chinese Chemical Letters, database is CAplus.

Three polymorphs (forms I, II and V) of isonicotinamide (INA) were mech. flexible and exhibited 1-dimensional (1D) plasticity. Anisotropic intermol. interactions contribute to the plasticity of single crystals: weak dispersive interactions between slip planes such as 1D columns in forms I and II or 2D layers in form V were stabilized by strong H bonds, allowing the layer or column′s surface to glide smoothly without hindrance. The disparity of intermol. interactions on plastic properties of INA polymorphic crystals was confirmed by energy framework anal., nanoindentation tests and micro-Raman spectroscopy.

Chinese Chemical Letters 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, Related Products of amides-buliding-blocks.

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

Peng, Xiaohua published the artcileA Template-Mediated Click-Click Reaction: PNA-DNA, PNA-PNA (or Peptide) Ligation, and Single Nucleotide Discrimination, Formula: C40H35N7O8, the publication is European Journal of Organic Chemistry (2010), 4194-4197, S4194/1-S4194/19, database is CAplus and MEDLINE.

A highly efficient chem. ligation was developed for quant. conjugation of PNA with DNA (PNA or peptide) by using the copper-catalyzed azide-alkyne cycloaddition reaction. Whereas PNAs with an alkyne at the C-terminus and an azide at the N-terminus have been used, an efficient click-click reaction occurs. The PNA click ligation is sequence specific and capable of single nucleotide discrimination.

European Journal of Organic 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 C40H35N7O8, Formula: C40H35N7O8.

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