Month: December 2022

Zhang, Rui-Bo published the artcileDesign, Synthesis, and Molecular Mechanism Studies of N-Phenylisoxazoline-thiadiazolo[3,4-a]pyridazine Hybrids as Protoporphyrinogen IX Oxidase Inhibitors, Synthetic Route of 372136-76-0, the publication is Journal of Agricultural and Food Chemistry (2020), 68(47), 13672-13684, database is CAplus and MEDLINE.

Protoporphyrinogen oxidase (PPO, EC 1.3.3.4) is an important target for green agrochem. discovery. Herein, a novel N-phenylisoxazoline-thiadiazolo[3,4-a]pyridazine herbicidal active scaffold was designed by the scaffold hybridization strategy. Systematic structural optimization enabled the discovery of a series of derivatives with excellent weed control at 9.375-150 g ai/ha by the post-emergent application. Some derivatives exhibited improved Nicotiana tabacum PPO (NtPPO)-inhibitory activity than fluthiacet-Me. Of these, I, with K_i = 21.8 nM, displayed higher weed control than fluthiacet-Me at the rate of 12-75 g ai/ha, and selective to maize at 75 g ai/ha. In planta, I was converted into a bioactive metabolite II (K_i = 4.6 nM), which exhibited 4.6-fold more potency than I in inhibiting the activity of NtPPO. Mol. dynamics simulation explained that II formed stronger π-π interaction with Phe392 than that of I. This work not only provides a promising lead compound for weed control in maize fields but is also helpful to understand the mol. mechanism and basis of the designed hybrids.

Journal of Agricultural and Food Chemistry published new progress about 372136-76-0. 372136-76-0 belongs to amides-buliding-blocks, auxiliary class Sulfamide,Amine,Aliphatic hydrocarbon chain, name is N-Methyl-N-isopropylsulfamoyl amide, and the molecular formula is C38H74Cl2N2O4, Synthetic Route of 372136-76-0.

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

Teng, Fan published the artcileA copper-mediated oxidative N-cyanation reaction, COA of Formula: C15H14N2, the publication is Chemical Communications (Cambridge, United Kingdom) (2014), 50(61), 8412-8415, database is CAplus and MEDLINE.

Copper-promoted N-cyanation of aliphatic sec-amine by CuCN is achieved via oxidative coupling. This procedure employs O₂ as a clean oxidant. Notably, sulfoximines and 1,1,3,3-tetramethylguanidine also worked well in this procedure. Thus, it represents a key progress in the C-N bond formation reaction as well as in the cyanation reaction.

Chemical Communications (Cambridge, United Kingdom) published new progress about 2451-91-4. 2451-91-4 belongs to amides-buliding-blocks, auxiliary class Nitrile,Amine,Benzene, name is N,N-Dibenzylcyanamide, and the molecular formula is C13H9FO2, COA of Formula: C15H14N2.

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

Berger, Or published the artcileSpectral Transition in Bio-Inspired Self-Assembled Peptide Nucleic Acid Photonic Crystals, Quality Control of 186046-83-3, the publication is Advanced Materials (Weinheim, Germany) (2016), 28(11), 2195-2200, database is CAplus and MEDLINE.

Guanine-containing short sequences of peptide nucleic acids (PNAs), synthetic nucleic acid analogs with an amide backbone, can self-assemble into ordered structures with unique optical properties. These observations prompted examination as to whether PNA monomers can also undergo a process of self-association and organization into supramol. assemblies, as it had previously been shown that even a single amino acid can self-assemble into fibrils with well-ordered electron diffraction. The 4 PNA monomers were tested for their ability to self-assemble into ordered structures under a variety of conditions including organic solvents (MeOH, EtOH, DMSO, and hexafluoro-2-propanol) and diverse buffer solutions with a range of pH values and concentrations The monomers were examined with or without the addnl. protecting groups, fluorenylmethyloxycarbonyl (Fmoc) and benzhydryloxycarbonyl (Bhoc), which are conjugated to the building blocks used for solid phase synthesis of PNA oligomers. Assembly into ordered structures was evident solely for N-(N-Fmoc-2-aminoethyl)-N-[(N-6-Bhoc-9-guanyl)acetyl]glycine (Fmoc-G-(Bhoc)-aeg-OH) in H₂O. Aromatic protecting groups are known to promote self-assembly of short peptides. The Fmoc moiety has a significant impact on the assembly of aromatic peptide amphiphiles. The PNA monomers could be considered as amphiphiles with the protecting groups serving as lipophilic moieties and the guanine base as the hydrophilic component.

Advanced Materials (Weinheim, Germany) 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, Quality Control of 186046-83-3.

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

Ozaki, Tomoya published the artcileLate-stage sulfonic acid/sulfonate formation from sulfonamides via sulfonyl pyrroles, Synthetic Route of 169590-42-5, the publication is Tetrahedron (2022), 132830, database is CAplus.

An accessible and low-cost route for transforming primary sulfonamides into the corresponding sulfonic acids/sulfonates RSO₂OH·Et₃N [R = 4-MeC₆H₄, 4-H₂NC₆H₄, 4-O₂NC₆H₄, [4-[2-[(4-ethyl-3-methyl-5-oxo-2H-pyrrole-1-carbonyl)amino]ethyl]phenyl]], R¹SO₂OK [R¹ = Et, 4-MeOC₆H₄, Bn, etc.] via sulfonyl pyrroles R¹SO₂R² [R¹ = Et, t-Bu, Bn, etc.; R² = pyrrol-1-yl] was reported. The reaction was demonstrated with a range of substrates including aryl and alkyl sulfonamides, and in the late-stage functionalization of several sulfonamide-containing drug mols.

Tetrahedron 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, Synthetic Route of 169590-42-5.

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

Teo, Yong-Chua published the artcileEfficient ligand-free, copper-catalyzed N-arylation of sulfonamides, HPLC of Formula: 489-17-8, the publication is Synlett (2011), 837-843, database is CAplus.

An efficient and convenient protocol has been developed for the N-arylation of sulfonamides with differently substituted aryl iodides using ligand-free copper iodide to afford the arylated products in good to excellent yields (up to 91%).

Synlett 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 C25H47NO8, HPLC of Formula: 489-17-8.

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

Teo, Yong-Chua published the artcileEfficient Manganese/Copper Bimetallic Catalyst for N-Arylation of Amides and Sulfonamides Under Mild Conditions in Water, Formula: C7H8FNO2S, the publication is European Journal of Organic Chemistry (2013), 2013(3), 515-524, database is CAplus.

An efficient and mild method using a bimetallic MnF₂/CuI catalyst at 60 °C in water was developed for the N-arylation of amides and sulfonamides with aryl halides. A variety of functionalized amides and sulfonamides were coupled with different substituted aryl halides to afford the corresponding N-arylated products in good to excellent yields (up to 97 %).

European Journal of Organic 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 C5H5N3S, Formula: C7H8FNO2S.

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

Sasaki, Fumiyuki published the artcileThe leukotriene receptors as therapeutic targets of inflammatory diseases, Recommanded Product: [(2-Hexylcyclopentylidene)amino]thiourea, the publication is International Immunology (2019), 31(9), 607-615, database is CAplus and MEDLINE.

A review. Leukotrienes (LTs) are inflammatory mediators derived from arachidonic acid. LTs include the di-hydroxy acid LT (LTB₄) and the cysteinyl LTs (CysLTs; LTC₄, LTD₄ and LTE₄), all of which are involved in both acute and chronic inflammation. We and other groups identified a high-affinity LTB₄ receptor, BLT1; the LTC₄ and LTD₄ receptors, CysLT1 and CysLT2; and the LTE₄ receptor, GPR99. Pharmacol. studies have shown that BLT1 signaling stimulates degranulation, chemotaxis and phagocytosis of neutrophils, whereas CysLT1 and CysLT2 signaling induces airway inflammation by increasing vascular permeability and the contraction of bronchial smooth muscle. Recently, we and other groups suggested that the LTB₄-BLT1 axis and the cysteinyl LTs-CysLT1/2 axis are involved in chronic inflammatory diseases including asthma, atopic dermatitis, psoriasis, atherosclerosis, arthritis, obesity, cancer and age-related macular degeneration using animal models for disease and gene knockout mice. This review describes the classical and novel functions of LTs and their receptors in several inflammatory diseases and discusses the potential clin. applications of antagonists for LT receptors and inhibitors of LT biosynthesis.

International 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, Recommanded Product: [(2-Hexylcyclopentylidene)amino]thiourea.

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

Saeki, Kazuko published the artcileIdentification, signaling, and functions of LTB₄ receptors, Formula: C12H23N3S, the publication is Seminars in Immunology (2017), 30-36, database is CAplus and MEDLINE.

Leukotriene B₄ (LTB₄), a lipid mediator produced from arachidonic acid, is a chemoattractant for inflammatory leukocytes. We identified two receptors for LTB₄, the high-affinity receptor BLT1 and the low-affinity receptor BLT2. BLT1 is expressed in various subsets of leukocytes, and analyses of BLT1-deficient mice revealed that the LTB₄/BLT1 axis enhances leukocyte recruitment to infected sites, and is involved in the elimination of pathogens. Hyperactivation of the LTB₄/BLT1 axis induces acute and chronic inflammation, resulting in various inflammatory diseases. BLT2 was originally identified as a low-affinity receptor for LTB₄, and we later identified 12(S)-hydroxy-5Z,8E,10E-heptadecatrienoic acid (12-HHT) as a high-affinity ligand for BLT2. BLT2 is highly expressed in epithelial cells in various tissues including intestine and skin. Large quantities of 12-HHT are produced by activated platelets during skin injury, and activation of BLT2 on epidermal keratinocytes accelerates skin wound healing by enhancing cell migration. BLT2 signaling also enhances cell-cell junctions, protectes against transepidermal water loss, and preventes entry of environmental substances into the body.

Seminars in 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, Formula: C12H23N3S.

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

Bi, Xiaobao published the artcileImmobilization and Intracellular Delivery of Circular Proteins by Modifying a Genetically Incorporated Unnatural Amino Acid, Formula: C11H22N2O4, the publication is Bioconjugate Chemistry (2018), 29(7), 2170-2175, database is CAplus and MEDLINE.

Backbone-cyclic proteins are of great scientific and therapeutic interest owing to their higher stability over their linear counterparts. Modification of such cyclic proteins at a selected site would further enhance their versatility. Here we report a chemoenzymic strategy to engineer site-selectively modified cyclic proteins by combining butelase-mediated macrocyclization with the genetic code expansion methodol. Using this strategy, we prepared a cyclic protein which was modified with biotin or a cell-penetrating peptide at a genetically incorporated noncanonical amino acid, making the cyclization-stabilized protein further amenable for site-specific immobilization and intracellular delivery. Our results point to a new avenue to engineering novel cyclic proteins with improved physicochem. and pharmacol. properties for potential applications in biotechnol. and medicine.

Bioconjugate 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, Formula: C11H22N2O4.

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

Liu, Shanshan published the artcileProtective effect of sacubitril/valsartan in patients with acute myocardial infarction: a meta-analysis, HPLC of Formula: 137862-53-4, the publication is Experimental and Therapeutic Medicine (2022), 23(6), 406, database is CAplus and MEDLINE.

Meta-anal. of the effects and safety of sacubitril/valsartan in patients with acute myocardial infarction (AMI), a total of four databases, including PubMed, Cochrane Library, Embase and Web of Science, and the ClinicalTrials.gov website were searched. Using a combination of medical subject headings and entry terms, the final search was performed in July 2021. A manual search of cross-references from the original articles was also conducted. The meta-anal. was subsequently performed with Revman 5.3 software and a total of four studies comprising 586 patients were included. The results disclosed a significant reduction in major adverse cardiovascular and cerebrovascular events (MACCEs) [odds ratio (OR), 0.47; 95% confidence interval (CI), 0.30-0.73; P = 0.0007], readmission (OR, 0.45; 95% CI, 0.29-0.71; P = 0.0006), incidence of acute heart failure (AHF) (OR, 0.45; 95% CI, 0.28-0.71; P = 0.0007) and N-terminal pro B-type natriuretic peptide [standardized mean difference (SMD), -0.88; 95% CI, -1.55-(-0.21); P = 0.01] in the sacubitril/valsartan group compared with that in the control group, and a random effects model was used to pool these data. No significant differences were identified in the incidence of hypotension (OR, 2.91; 95% CI, 0.55-15.51; P = 0.21), adverse events (OR, 2.19; 95% CI, 0.42-11.37; P = 0.35), left ventricular ejection fraction (mean difference, 1.96; 95% CI, -0.84-4.76; P = 0.17) or soluble suppression of tumorigenesis-2 (SMD, -0.45; 95% CI, -1.62-0.71; P = 0.45) according to the random effects model. In conclusion, the present meta-anal. revealed that sacubitril/valsartan was able to effectively reduce the incidence of MACCEs, readmission and AHF in patients with AMI after revascularization without any obvious adverse events.

Experimental and Therapeutic Medicine 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