Tag: 200-300

On September 1, 2022, Han, Yu; Hu, Li-Xin; Liu, Ting; Liu, Jing; Wang, Yu-Qing; Zhao, Jia-Hui; Liu, You-Sheng; Zhao, Jian-Liang; Ying, Guang-Guo published an article.Application of 144-80-9 The title of the article was Non-target, suspect and target screening of chemicals of emerging concern in landfill leachates and groundwater in Guangzhou, South China. And the article contained the following:

Landfill sites have been regarded as a significant source of chems. of emerging concern (CECs) in groundwater. However, our understanding about the compositions of CECs in landfill leachate and adjacent groundwater is still very limited. Here we investigated the CECs in landfill leachates and groundwater of Guangzhou in South China by target, suspect and non-target anal. using high-resolution mass spectrometry (HRMS). A variety of CECs (n = 242), including pharmaceuticals (n = 64), pharmaceutical intermediates (n = 18), personal care products (n = 9), food additives (n = 18), industrial chems. (n = 82, e.g., flame retardants, plasticizers, antioxidants and catalysts), pesticides (n = 26), transformation products (n = 8) and other organic compounds (n = 17) were (tentatively) identified by non-target and suspect screening. 142 CECs were quantitated with target anal., and among them 37, 24 and 27 CECs were detected resp. in the raw leachate (272-1780μg/L), treated leachate (0.25-0.81μg/L) and groundwater (0.10-53.7μg/L). The CECs in the raw leachates were efficiently removed with the removal efficiencies greater than 88.7%. Acesulfame, bisphenol F and ketoprofen were the most abundant compounds in both treated leachate and groundwater. The CECs in groundwater was found most likely to be originated from the landfill sites. Our results highlight the importance of non-target screening in identifying CECs, and reveal the contamination risk of groundwater by landfill leachate. The experimental process involved the reaction of N-((4-Aminophenyl)sulfonyl)acetamide(cas: 144-80-9).Application of 144-80-9

The Article related to chem target screening landfill leachates groundwater guangzhou south china, chemicals of emerging concern, groundwater, high-resolution mass spectrometry, landfill leachate, non-target analysis and other aspects.Application of 144-80-9

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Gogoi, Bhaskarjyoti; Gogoi, Dhrubajyoti; Gogoi, Neelutpal; Mahanta, Saurov; Buragohain, Alak K. published an article in 2022, the title of the article was Network pharmacology based high throughput screening for identification of multi targeted anti-diabetic compound from traditionally used plants.Category: amides-buliding-blocks And the article contains the following content:

The incurable Type 2 diabetes mellitus (T2DM) has now been considered a pandemic with only supportive care in existence. Due to the adverse effects of available anti-diabetic drugs, there arises a great urgency to develop new drug mols. One of the alternatives that can be considered for the treatment of T2DM are natural compounds from traditionally used herbal medicine. The present study undertakes, an integrated multidisciplinary concept of Network Pharmacol. to evaluate the efficacy of potent anti-diabetic compound from traditionally used anti-diabetic plants of north east India and followed by DFT anal. In the course of the study, 22 plant species were selected on the basis of their use in traditional medicine for the treatment of T2DM by various ethnic groups of the north eastern region of India. Initially, a library of 1053 compounds derived from these plants was generated. This was followed by network preparation between compounds and targets based on the docking result. The compounds having the best network property were considered for DFT anal. We have identified that auraptene, a monoterpene coumarin for its activity in the management of Type 2 diabetes mellitus and deciphered its unexplored probable mechanisms. Mol. dynamics simulation of the ligand-protein complexes also reveals the stable binding of auraptene with the target proteins namely, Protein Kinase C θ, Glucocorticoid receptor, 11-β hydroxysteroid dehydrogenase 1 and Aldose Reductase, all of which form uniform interactions throughout the MD simulation trajectory. Therefore, this finding could provide new insights for the development of a new anti-diabetic drug. The experimental process involved the reaction of N-(2-Hydroxy-2-(4-methoxyphenyl)ethyl)cinnamamide(cas: 456-12-2).Category: amides-buliding-blocks

The Article related to traditional plant antidiabetic compound high throughput screening network pharmacol, type 2 diabetes mellitus, insulin resistance, natural products, network pharmacology, traditional knowledge and other aspects.Category: amides-buliding-blocks

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On February 5, 2021, Nanda, Tanmayee; Biswal, Pragati; Pati, Bedadyuti Vedvyas; Banjare, Shyam Kumar; Ravikumar, Ponneri Chandrababu published an article.Formula: C13H12N2O The title of the article was Palladium-Catalyzed C-C Bond Activation of Cyclopropenone: Modular Access to Trisubstituted α,β-Unsaturated Esters and Amides. And the article contained the following:

Strain-driven palladium/N-heterocyclic carbene-catalyzed C-C bond activation of diphenylcyclopropenone (DPC) was explored for one-step access to trisubstituted α,β-unsaturated esters and amides. The designed transformation worked under mild conditions providing exclusively a single stereoisomer. Mechanistic studies support the oxidative addition of the C-C bond of cyclopropenone to in-situ-generated Pd(0) intermediate. Vinylic hydrogen in the product was proved that it is coming from phenol/aniline through deuterium-labeling studies. Late-stage functionalization of bioactive mols. such as procaine, estrone, and hymecromone demonstrated the robustness of this protocol. The experimental process involved the reaction of 1,3-Diphenylurea(cas: 102-07-8).Formula: C13H12N2O

The Article related to trisubstituted unsaturated ester preparation, phenol cyclopropenone bond activation palladium catalyst, amide trisubstituted unsaturated preparation, amine cyclopropenone bond activation palladium catalyst and other aspects.Formula: C13H12N2O

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Xu, Shibo; Takamatsu, Kazutaka; Hirano, Koji; Miura, Masahiro published an article in 2018, the title of the article was Nickel-Catalyzed Stereospecific C-H Coupling of Benzamides with Epoxides.Name: 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione And the article contains the following content:

A Ni(OAc)2-catalyzed C-H coupling of 8-aminoquinoline-derived benzamides with epoxides has been developed. The reaction proceeds with concomitant removal of the 8-aminoquinoline auxiliary to form the corresponding 3,4-dihydroisocoumarins directly. Addnl., the nickel catalysis is stereospecific, and the cis- and trans-epoxides are converted into the corresponding cis- and trans-dihydroisocoumarins with retention of configuration, which is complementary to previously reported palladium catalysis. Moreover, while still preliminary, the Csp3-H functionalization is also achieved in the presence of modified NiCl2 catalysts. The experimental process involved the reaction of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione(cas: 5455-98-1).Name: 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione

The Article related to aminoquinoline benzamide epoxide nickel stereospecific coupling catalyst microwave irradiation, dihydroisocoumarin stereoselective preparation, c−h coupling, epoxides, lactones, nickel, stereospecificity and other aspects.Name: 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On November 1, 2017, Kumar, Prashant; Takayesu, Allen; Abbasi, Usama; Kalathottukaren, Manu Thomas; Abbina, Srinivas; Kizhakkedathu, Jayachandran N.; Straus, Suzana K. published an article.Category: amides-buliding-blocks The title of the article was Antimicrobial peptide-polymer conjugates with high activity: Influence of polymer molecular weight and peptide sequence on antimicrobial activity, proteolysis, and biocompatibility. And the article contained the following:

We report the synthesis, characterization, activity, and biocompatibility of a novel series of antimicrobial peptide-polymer conjugates. Using parent peptide aurein 2.2, we designed a peptide array (∼100 peptides) with single and multiple W and R mutations and identified antimicrobial peptides (AMPs) with potent activity against Staphylococcus aureus (S. aureus). These novel AMPs were conjugated to hyperbranched polyglycerols (HPGs) of different mol. weights and number of peptides to improve their antimicrobial activity and toxicity. The cell and blood compatibility studies of these conjugates demonstrated better properties than those of the AMP alone. However, conjugates showed lower antimicrobial activity in comparison to that of peptides, as determined from minimal inhibition concentrations (MICs) against S. aureus, but considerably better than that of the available polymer-AMP conjugates in the literature. In addition to measuring MICs and characterizing the biocompatibility, CD spectroscopy was used to investigate the interaction of the novel conjugates with model bacterial biomembranes. Moreover, the novel conjugates were exposed to trypsin to evaluate their stability. It was found that the conjugates resist proteolysis in comparison with unprotected peptides. The peptide conjugates were active in serum and whole blood. Overall, the results show that combining a highly active AMP and low-mol.-weight HPG yields bioconjugates with excellent biocompatibility, MICs below 100 μg/mL, and proteolytic stability, which could potentially improve its utility for in vivo applications. The experimental process involved the reaction of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione(cas: 5455-98-1).Category: amides-buliding-blocks

The Article related to antimicrobial peptide polymer conjugate proteolysis biocompatibility, hyperbranched polyglycerol, antimicrobial peptide−polymer conjugates, aurein peptides, biocompatibility, bioconjugation, proteolysis and other aspects.Category: amides-buliding-blocks

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Kakeya, Nobuharu; Yata, Noboru; Kamada, Akira; Aoki, Masaru published an article in 1970, the title of the article was Biological activities of drugs. IX. Structure-activity relation of sulfonamide carbonic anhydrase inhibitors. 4.Application In Synthesis of 3-Nitro-4-chlorobenzenesulfonamide And the article contains the following content:

Hansch-Fujita’s equation has been applied to an anal. of the natriuretic activity of sulfonamide carbonic anhydrase inhibitors using π and πc as hydrophobic parameters, and σ, ΔpKa, Δppm and Δfr as electronic parameters. Sixteen benzenesulfonamide derivatives were satisfactorily applied to the structure-activity anal. of heterocyclic sulfonamides. It was concluded that a strong natriuretic activity was observed for sulfonamides which had an optimal hydrophobicity and low electronegativity at the sulfamoyl group or a strong inhibitory activity against carbonic anhydrase. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Application In Synthesis of 3-Nitro-4-chlorobenzenesulfonamide

The Article related to structure activity sulfonamides antienzymic, activity structure sulfonamides antienzymic, sulfonamides antienzymic structure activity, antienzymic sulfonamides structure activity, carbonic anhydrase inhibitor structure and other aspects.Application In Synthesis of 3-Nitro-4-chlorobenzenesulfonamide

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On January 22, 2015, Bottegoni, Giovanni; De Simone, Alessio; Ruda, Gian Filippo; Cavalli, Andrea; Bandiera, Tiziano; Piomelli, Daniele published a patent.Product Details of 5455-98-1 The title of the patent was Preparation of phenyl carbamates as inhibitors of the fatty acid amide hydrolase (FAAH) enzyme and modulators of the D3 dopamine receptor (D3DR). And the patent contained the following:

Disclosed are compounds I [Ar = aromatic or heteroaromatic single or fused ring comprising heteroatoms selected from N, O and S; R1, R2 = independently H, halo, alkyl, etc.; X = N or CH; Y = -CH2(CH2)nCH2- or -CH2CH:CHCH2- (wherein Y is optionally substituted by B) ; n = 0-3; B = F, OH, CH2OH, etc.; R3 = aromatic or heteroaromatic ring, benzyl, benzoyl (optionally substituted by R5), etc.; R5 = OH, NH2, CN, etc.; R4 = H, halo, alkyl, etc.; or R3 and R4, together with the Ph ring to which they are connected, may form 9H-carbazole ring; or pharmaceutically acceptable salts thereof]. For example, compound II was prepared by following general procedure: to a solution of Boc2O (1.4 equiv) in acetonitrile were added DMAP (1 equiv)/acetonitrile and an amine (1 equiv)/acetonitrile, the resulting mixture was stirred at room temperature for 10 min, treated with an alc. derivative (1.2-1.4 equiv) at room temperature for 22 h, concentrated in vacuo, dissolved in Et acetate, washed with saturated aqueous NaHCO3, dried over Na2SO4, concentrated, and purified. The exemplified compound II exhibited IC50 of 4.4 nM for human FAAH and EC50 of 14.0 nM for D3DR. Compounds I are claimed useful for the treatment of nicotine use disorders, substance abuse addiction, eating diorders, etc. The experimental process involved the reaction of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione(cas: 5455-98-1).Product Details of 5455-98-1

The Article related to fatty acid amide hydrolase faah inhibitor phenyl carbamate preparation, d3 dopamine receptor d3dr modulator phenyl carbamate preparation, nicotine eating disorder substance abuse addiction treatment phenyl carbamate and other aspects.Product Details of 5455-98-1

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On April 25, 2018, Gur, Zehra Tugce; Caliskan, Burcu; Garscha, UIrike; Olgac, Abdurrahman; Schubert, Ulrich S.; Gerstmeier, Jana; Werz, Oliver; Banoglu, Erden published an article.Formula: C6H5ClN2O4S The title of the article was Identification of multi-target inhibitors of leukotriene and prostaglandin E2 biosynthesis by structural tuning of the FLAP inhibitor BRP-7. And the article contained the following:

Leukotrienes (LTs) and prostaglandin (PG)E2 are enzymically produced from arachidonic acid and represent highly bioactive lipid mediators with pro-inflammatory functions. Here, the authors report on novel multi-target inhibitors that potently and dually interfere with 5-lipoxygenase-activating protein (FLAP) and microsomal prostaglandin E2 synthase (mPGES)-1 in LT and PGE2 biosynthesis, based on the previously identified selective FLAP inhibitor BRP-7 (8, IC50 = 0.31 μM). C -substitution of the benzimidazole ring of BRP-7 by carboxylic acid and its bioisosteres provided compounds, exemplified by 57 (5-{1-[(2-chlorophenyl)methyl]-2-{1-[4-(2-methylpropyl)phenyl]ethyl}-1H-benzimidazol-5-yl}-2,3-dihydro-1,3,4-oxadiazole-2-thione) that potently suppress LT formation (IC50 = 0.05 μM) by targeting FLAP along with inhibition of mPGES-1 (IC50 = 0.42 μM). Besides FLAP, also 5-lipoxygenase (5-LO) and LTC4 synthase activities were inhibited by 57, albeit with lower potency (IC50 = 0.6 and 6.2 μM) than FLAP. Docking studies and mol. dynamic simulations with FLAP, mPGES-1 and 5-LO provide valuable insights into potential binding interactions of the inhibitors with their targets. Together, these novel benzimidazole derivatives may possess potential as leads for development of effective anti-inflammatory drugs with multi-target properties for dually inhibiting LT and PGE2 production The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Formula: C6H5ClN2O4S

The Article related to multitarget inhibitor leukotriene prostaglandin e2 flap brp7 analog preparation, 5-lipoxygenase, 5-lipoxygenase-activating protein, benzimidazole, inflammation, leukotriene, microsomal prostaglandin e(2) synthase-1 and other aspects.Formula: C6H5ClN2O4S

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Wang, Yixiao; Li, Jinhua; Ji, Ling; Chen, Lingxin published an article in 2022, the title of the article was Simultaneous Determination of Sulfonamides Antibiotics in Environmental Water and Seafood Samples Using Ultrasonic-Assisted Dispersive Liquid-Liquid Microextraction Coupled with High Performance Liquid Chromatography.Safety of N-((4-Aminophenyl)sulfonyl)acetamide And the article contains the following content:

The residues and abuse of antibiotics have seriously endangered ecol. balance and human health; meanwhile, antibiotics determination is very difficult because of their low levels and multiple categories in complicated matrixes. Appropriate sample pretreatment is usually imperative to enrich (ultra)trace antibiotics and eliminate matrix interference prior to chromatog. anal. Dispersive liquid-liquid microextraction (DLLME) has become an ideal pretreatment technique owing to its simplicity, effectiveness, low-consumption, etc. In this work, an ultrasonic-assisted DLLME (UA-DLLME) was developed for the simultaneous extraction of seven sulfonamides (SAs) antibiotics in environmental water and seafood samples coupled with HPLC-DAD determination Several parameters affecting UA-DLLME efficiency were systematically optimized, and consequently the SAs were separated and detected within 14.5 min. The obtained limits of detection (LODs) and limits of quantification (LOQs) ranged from 0.7-7.8 μg/L and 2.4-26.0 μg/L for three water samples (seawater, aquaculture wastewater and lake water) and two seafood samples (pomfrets and shrimps). High recoveries (80.0-116.0%) with low relative standard deviations (0.1-8.1%) were achieved for all the tested samples at three spiked levels. Notably, sulfadimethoxine was found at 24.49 μg/L in one seawater sample. The facile, robust and benign DLLME-HPLC method demonstrated promising perspectives for multiresidue anal. of antibiotics. The experimental process involved the reaction of N-((4-Aminophenyl)sulfonyl)acetamide(cas: 144-80-9).Safety of N-((4-Aminophenyl)sulfonyl)acetamide

The Article related to seafood sulfonamide antibiotic determination uadllme high performance liquid chromatog, dispersive liquid-liquid microextraction, environmental water, seafood samples, sulfonamides antibiotics, ultrasonic-assisted and other aspects.Safety of N-((4-Aminophenyl)sulfonyl)acetamide

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On March 31, 2021, Gouda, Moustafa A.; Barnawi, Ibrahim O. published an article.Related Products of 144-80-9 The title of the article was Synthesis and cytotoxic activity of some new pyrazolo[1,5-a]pyrimidine derivatives. And the article contained the following:

A series of arylazopyrazolones II [R = amino, hydroxy, acetamido, etc] was synthesized through treatment of the 3-aminopyrazolin-5-one with the appropriate diazonium salts, followed by cyclization of the resulted arylazopyrazolones II [R = hydroxy, (4,6-dimethylpyrimidin-2-yl)amino] and I [R = (4,6-dimethylpyrimidin-2-yl)amino] with acetylacetone in boiling acetic acid. Using doxorubicin as the reference drug, the in-vitro cytotoxic activity of the synthetic arylazopyrazoles II [R = amino, hydroxy, acetamido, etc] and I [R = amino, thiazol-2-ylamino, (4,6-dimethylpyrimidin-2-yl)amino] was evaluated on four human cell lines. The results revealed that compounds II [R = amino, hydroxy, acetamido, etc] revealed good cytotoxic activity toward HepG2, HCT-116, MCF-7, and PC3 cell lines, within IC50 5.89±0.4-19.23±1.6; 7.15±0.6-23.15±1.8; 4.93±0.4-24.35±1.9; and 9.14±0.8-32.09±2.0μg/mL. The derivatives II [R = amino, acetamido, guanidino] displayed accurate anticancer activity toward all most cancers cell lines, even as compounds I [R = thiazol-2-ylamino] exhibited moderate activities, while the pyrazolopyrimidine I [R = amino] has lower anticancer activity. The experimental process involved the reaction of N-((4-Aminophenyl)sulfonyl)acetamide(cas: 144-80-9).Related Products of 144-80-9

The Article related to aryl diazonium chloride aminopyraxolone coupling reaction, oxo aminopyrzolyl sulfonylphenyl hydrazine preparation acetyl acetone heterocyclization, dimethyl oxo dihydropyrazolopyrimidinyl diazenylbenzenesulfonamide preparation antitumor sar and other aspects.Related Products of 144-80-9

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics