Category: amides-buliding-blocks

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 August 31, 2015, Subbulakshmi, Karanth N.; Narayana, Badiadka; Yathirajan, Hemmige S.; Akkurt, Mehmet; Celik, Oemer; Ersanli, Cem Cueneyt; Glidewell, Christopher published an article.Category: amides-buliding-blocks The title of the article was Dihydrooxazolones and dihydroimidazolones derived from acylglycines: syntheses, molecular structures and supramolecular assembly. And the article contained the following:

Syntheses and structures are described for some alkylidene-substituted dihydrooxazolones and dihydroimidazoles derived from simple acylglycines. A second, triclinic, polymorph of 4-benzylidene-2-(4-methylphenyl)-1,3-oxazol-5(4H)-one, C17H13NO2, (I), has been identified and the structure of 2-methyl-4-[(thiophen-2-yl)methylidene]-1,3-oxazol-5(4H)-one, C9H7NO2S, (II), has been rerefined taking into account the orientational disorder of the thienyl group in each of the two independent mols. The reactions of phenylhydrazine with 2-phenyl-4-[(thiophen-2-yl)methylidene]-1,3-oxazol-5(4H)-one or 2-(4-methylphenyl)-4-[(thiophen-2-yl)methylidene]-1,3-oxazol-5(4H)-one yield, resp., 3-anilino-2-phenyl-5-[(thiophen-2-yl)methylidene]-3,5-dihydro-4H-imidazol-4-one, C10H15N3OS, (III), and 3-anilino-2-(4-methylphenyl)-5-[(thiophen-2-yl)methylidene]-3,5-dihydro-4H-imidazol-4-one, C21H17N3OS, (IV), which both exhibit orientational disorder in their thienyl groups. The reactions of 2-phenyl-4-[(thiophen-2-yl)methylidene]-1,3-oxazol-5(4H)-one with hydrazine hydrate or with water yield, resp., N-[3-hydrazinyl-3-oxo-1-(thiophen-2-yl)prop-1-en-2-yl]benzamide and 2-(benzoylamino)-3-(thiophen-2-yl)prop-2-enoic acid, which in turn react, resp., with thiophene-2-carbaldehyde to form 2-phenyl-5-[(thiophen-2-yl)methylidene]-3-{[(E)-(thiophen-2-yl)methylidene]amino}-3,5-dihydro-4H-imidazol-4-one, C19H13N3OS2, (V), which exhibits orientational disorder in only one of its thienyl groups, and with methanol to give Me (2Z)-2-(benzoylamino)-3-(thiophen-2-yl)prop-2-enoate, C15H13NO3S, (VI). There are no direction-specific intermol. interactions in the crystal structure of the triclinic polymorph of (I), but the mols. of (II) are linked by two independent C-H···O hydrogen bonds to form C 2 2(14) chains. Compounds (III) and (IV) both form centrosym. R 2 2(10) dimers built from N-H···O hydrogen bonds, while compound (V) forms a centrosym. R 2 2(10) dimer built from C-H···O hydrogen bonds. In the structure of compound (VI), a combination of N-H···O and C-H···π(arene) hydrogen bonds links the mols. into sheets. Comparisons are made with some similar compounds The experimental process involved the reaction of 2-(4-Methylbenzamido)acetic acid(cas: 27115-50-0).Category: amides-buliding-blocks

The Article related to dihydrooxazolone dihydroimidazolone acylglycine mol structure supramol assembly, erlenmeyer azlactones, crystal structure, hydrogen bonding, imidazolones, orientational disorder, oxazolones, supramolecular assembly and other aspects.Category: amides-buliding-blocks

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

On August 16, 2022, Liang, Chao; Zhang, Shan; Robinson, David; Ploeg, Matthew Vander; Wilson, Rebecca; Nah, Jiemin; Taylor, Dale; Beh, Sheryl; Lim, Radiance; Sun, Lei; Muoio, Deborah M.; Stroud, David A.; Ho, Lena published an article.Product Details of 79-07-2 The title of the article was Mitochondrial microproteins link metabolic cues to respiratory chain biogenesis. And the article contained the following:

Electron transport chain (ETC) biogenesis is tightly coupled to energy levels and availability of ETC subunits. Complex III (CIII), controlling ubiquinol:ubiquinone ratio in ETC, is an attractive node for modulating ETC levels during metabolic stress. Here, we report the discovery of mammalian Co-ordinator of mitochondrial CYTB (COM) complexes that regulate the stepwise CIII biogenesis in response to nutrient and nuclear-encoded ETC subunit availability. The COMA complex, consisting of UQCC1/2 and membrane anchor C16ORF91, facilitates translation of CIII enzymic core subunit CYTB. Subsequently, microproteins SMIM4 and BRAWNIN together with COMA subunits form the COMB complex to stabilize nascent CYTB. Finally, UQCC3-containing COMC facilitates CYTB hemylation and association with downstream CIII subunits. Furthermore, when nuclear CIII subunits are limiting, COMB is required to chaperone nascent CYTB to prevent OXPHOS collapse. Our studies highlight CYTB synthesis as a key regulatory node of ETC biogenesis and uncover the roles of microproteins in maintaining mitochondrial homeostasis. The experimental process involved the reaction of 2-Chloroacetamide(cas: 79-07-2).Product Details of 79-07-2

The Article related to respiratory chain biogenesis mitochondrial microprotein homeostasis, cp: metabolism, cytb, seps, smim4, uqcc1, uqcc2, complex iii, electron transport chain, microproteins, nuclear-mitochondrial coordination, smorfs and other aspects.Product Details of 79-07-2

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 June 20, 2022, Wang, Zheng; Liao, Yufeng; Li, Xiuwen; Shuang, Chendong; Pan, Yang; Li, Yan; Li, Aimin published an article.Recommanded Product: 2-Chloroacetamide The title of the article was Effect of ammonia on acute toxicity and disinfection byproducts formation during chlorination of secondary wastewater effluents. And the article contained the following:

Ammonia nitrogen (NH3-N) significantly affects the occurrence of disinfection byproducts (DBPs) and residual chlorine in chlorinated wastewater, thereby affecting the acute toxicity to aquatic organisms. In this paper, the formation of thirty-five halogenated DBPs and the changes in acute toxicity of luminescent bacteria and zebrafish embryos were evaluated after chlorination of seven secondary wastewater effluents with different NH3-N concentrations Results showed that NH3-N significantly reduced the formation of most DBPs by 82-100%. The acute toxicity was enhanced after chlorination and increased linearly with increasing NH3-N concentration for luminescent bacteria (r = 0.986, p < 0.05) and zebrafish embryos (r = 0.972, p < 0.05) due to the coexistence of DBPs and monochloramine. According to the toxicity classification system of wastewater, the fitting results indicated that the toxicity level was acceptable for chlorinated wastewater with NH3-N concentration below 1.00 mg-N/L. DBPs might be the main toxicant to luminescent bacteria in the wastewater with low NH3-N concentrations (0.06-0.31 mg-N/L), which accounted for 68-97% of the toxicity contribution. By contrast, monochloramine contributed over 80% to the toxicity of luminescent bacteria and zebrafish embryos in the wastewater with high NH3-N concentrations (2.66-7.17 mg-N/L). Compared to chlorination, chlorine dioxide and UV disinfection unaffected by NH3-N could reduce acute toxicity by nearly 100%, primarily due to the lack of residual disinfectant. In view of the high toxicity caused by chlorination, chlorination-dechlorination or chlorine dioxide and UV disinfection are highly recommended for the treatment of wastewater with high NH3-N concentration The experimental process involved the reaction of 2-Chloroacetamide(cas: 79-07-2).Recommanded Product: 2-Chloroacetamide

The Article related to ammonia acute toxicity disinfection byproduct secondary wastewater effluent chlorination, alternative disinfection process, ammonia-containing wastewater, dechlorination, residual chlorine, toxicity contribution and other aspects.Recommanded Product: 2-Chloroacetamide

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

On November 1, 2020, Qian, Yunkun; Hu, Yue; Chen, Yanan; An, Dong; Westerhoff, Paul; Hanigan, David; Chu, Wenhai published an article.SDS of cas: 79-07-2 The title of the article was Haloacetonitriles and haloacetamides precursors in filter backwash and sedimentation sludge water during drinking water treatment. And the article contained the following:

Haloacetonitriles (HANs) and haloacetamides (HAMs) are nitrogenous disinfection byproducts that are present in filter backwash water (FBW) and sedimentation sludge water (SSW). In many cases FBW and SSW are recycled to the head of drinking water treatment plants. HAN and HAM concentrations in FBW and SSW, without addnl. oxidants, ranged from 6.8 to 11.6 nM and 2.9 to 3.6 nM of three HANs and four HAMs, resp. Upon oxidant addition to FBW and SSW under formation potential conditions, concentrations for six HANs and six HAMs ranged from 92.2 to 190.4 nM and 42.2 to 95.5 nM, resp. Therefore, at common FBW and SSW recycle rates (2 to 10% of treated water flows), the precursor levels in these recycle waters should not be ignored because they are comparable to levels present in finished water. Brominated HAN and chlorinated HAM were the dominant species in FBW and SSW, resp. The lowest mol. weight ultrafiltration fraction (< 3 kDa) contributed the most to HAN and HAM formations. The hydrophilic (HPI) organic fraction contributed the greatest to HAN precursors in sand-FBW and SSW and were the most reactive HAM precursors in both sand- or carbon-FBWs. Fluorescence revealed that aromatic protein-like compounds were dominant HAN and HAM precursors. Therefore, strategies that remove low mol. weight hydrophilic organic matter and aromatic protein-like compounds will minimize HAN and HAM formations in recycled FBW and SSW. The experimental process involved the reaction of 2-Chloroacetamide(cas: 79-07-2).SDS of cas: 79-07-2

The Article related to haloacetonitrile haloacetamide filter backwash sedimentation sludge water, drinking water treatment, filter backwash water, haloacetamides, disinfection byproducts, haloacetonitriles, sedimentation sludge water and other aspects.SDS of cas: 79-07-2

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

On April 3, 2018, Lamie, Phoebe F.; Philoppes, John N.; Rarova, Lucie published an article.Application In Synthesis of 2-(4-Methylbenzamido)acetic acid The title of the article was Design, synthesis, and biological evaluation of novel 1,2-diaryl-4-substituted-benzylidene-5(4H)-imidazolone derivatives as cytotoxic agents and COX-2/LOX inhibitors. And the article contained the following:

A new series of 1,2-diaryl-4-substituted-benzylidene-5(4H)-imidazolone derivatives I (R = H, Me; R1 = H, OMe, Cl; X = O, S) was synthesized. Their cytotoxic activities in vitro were evaluated against breast, ovarian, and liver cancer cell lines and also against normal human skin fibroblasts. Cyclooxygenase (COX)-1, COX-2 and lipoxygenase (LOX) inhibitory activities were measured. The synthesized compounds showed selectivity toward COX-2 rather than COX-1, and the IC50 values (0.25-1.7 μM) were lower than that of indomethacin (IC50 = 9.47 μM) and somewhat higher than that of celecoxib (IC50 = 0.071 μM). The selectivity index for COX-2 of the oxazole derivative I (R = Me; R1 = OMe; X = O) (SI = 3.67) was nearly equal to that of celecoxib (SI = 3.66). For the LOX inhibitory activity, the new compounds showed IC50 values of 0.02-74.03 μM, while the IC50 of the reference zileuton was 0.83 μM. The most active compound I (R = H; R1 = Cl; X = O) was found to have dual COX-2/LOX activity. All the synthesized compounds were docked inside the active site of the COX-2 and LOX enzymes. They linked to COX-2 through the N atom of the azole scaffold, while C=O of the oxazolone moiety was responsible for the binding to amino acids inside the LOX active site. The experimental process involved the reaction of 2-(4-Methylbenzamido)acetic acid(cas: 27115-50-0).Application In Synthesis of 2-(4-Methylbenzamido)acetic acid

The Article related to benzylidene imidazolone preparation antiinflammatory antitumor mol docking human, cyclooxygenase lipoxygenase inhibitor, anti-inflammatory, cytotoxicity, diaryl imidazolone derivatives, molecular docking study and other aspects.Application In Synthesis of 2-(4-Methylbenzamido)acetic acid

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

Dobashi, Yasuo; Dobashi, Akira; Hara, Shoji published an article in 1984, the title of the article was Chiral recognition conducted by tartaric acid derivatives in nonaqueous media.SDS of cas: 65645-88-7 And the article contains the following content:

Chiral recognition of hydroxycarboxylic acids, amino acids and 1,2-diols using diastereomeric complexation based on H bonding with L-(+)-N,N’-diisopropyltartramide is described (liquid-solid chromatog.). The experimental process involved the reaction of (S)-2-Hydroxy-N-methyl-2-phenylacetamide(cas: 65645-88-7).SDS of cas: 65645-88-7

The Article related to chiral recognition tartramide, tartaric acid chiral recognition, chromatog tartaric chirality, hydrogen bond tartramide, hydroxycarboxylase enantiomerism chromatog, amino acid enantiomerism, diol enantiomerism and other aspects.SDS of cas: 65645-88-7

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

On October 25, 2021, Rimnacova, Lucie; Moos, Martin; Opekar, Stanislav; Vodrazka, Petr; Pejchal, Vladimir; Mraz, Jaroslav; Simek, Petr published an article.Computed Properties of 27115-50-0 The title of the article was Ethyl chloroformate mediated gas chromatographic-mass spectrometric biomonitoring of acidic biomarkers of occupational exposure and endogenous metabolites in human urine. And the article contained the following:

Numerous industrial organic pollutants such as aromates, alkoxyalcs., other organic solvents and monomers are absorbed, metabolized, and finally excreted in urine mostly as carboxylic acids that are determined as biomarkers of exposure. For a number of these xenometabolites, biol. limits (levels of biomarkers in biol. material) have been established to prevent damage to human health. Till now, most of the anal. procedures used have been optimized for one or a few analytes. Here, we report a more comprehensive approach enabling rapid GC-MS screening of sixteen acidic biomarkers in urine that are metabolized in the human body from several important industrial chems.; benzene, toluene, styrene, xylenes, alkoxyalcs., carbon disulfide, furfural and N,N-dimethylformamide. The new method involves immediate in situ derivatization – liquid liquid microextraction of urine by an Et chloroformate-ethanol-chloroform-pyridine medium and GC-MS anal. of the derivatized analytes in the lower organic phase. The xenometabolite set represents diverse chem. structures and some of hippuric and mercapturic acids also provided unusual derivatives that were unambiguously elucidated by means of new Et chloroformates labeled with stable isotopes and by synthesis of the missing reference standards In the next step, an automated routine was developed for GC-MS/MS anal. using a MetaboAuto sample preparation workstation and the new method was validated for fourteen metabolites over the relevant concentration range of each analyte in the spiked pooled human urine. It shows good linearity (R2 ≥ 0.982), accuracy (from 85% to 120%), precision (from 0.7% to 20%) and recovery (from 89% to 120%). The method performance was further successfully proved by GC-MS/MS anal. of the certified IP45 and RM6009 reference urines. Moreover, we show that the new method opens up the possibility for biomonitoring of combined and cumulative occupational exposures as well as for urinary metabolite profiling of persons exposed to harmful industrial chems. The experimental process involved the reaction of 2-(4-Methylbenzamido)acetic acid(cas: 27115-50-0).Computed Properties of 27115-50-0

The Article related to ethyl chloroformate gcms occupational exposure acidic biomarker metabolite urine, biomarker of occupational exposure, endogenous metabolites, ethyl chloroformate mediated derivatization, urine, xenometabolite and other aspects.Computed Properties of 27115-50-0

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