Month: January 2023

Flagellin maintains eosinophils in intestine was written by Lv, Xiaodan;Chang, Qing;Wang, Qin;Jin, Qiao-Ruo;Liu, Hua-Zhen;Yang, Shao-Bo;Yang, Ping-Chang;Yang, Gui. And the article was included in Cytokine+ in 2022.Safety of 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid This article mentions the following:

Eosinophils (Eos) are the major effector cells in allergic response. The regulation of Eo is not fully understood yet. Flagellin (FGN) has immune regulatory functions. This study aims to elucidate the role of FGN in maintaining Eo at the static status in the intestinal tissues. A mouse food allergy (FA) model was developed. Eo mediator levels in the serum or culture supernatant or intestinal lavage fluids were assessed and used as an indicator of Eo activation. The results showed that less FGN amounts were detected in the FA mouse intestinal tissues, that were neg. correlated with the Eo activation. Mast cell-derived chymase bound FGN to induce FGN degradation FGN formed complexes with FcγRI on Eos to prevent specific antigens from binding FcγRI, and thus, to prevent Eo activation. Administration of FGN efficiently alleviated exptl. FA. In conclusion, FGN plays a critical role in maintaining Eos at static status in the intestine. Administration of FGN can alleviate exptl. FA. FGN may be a novel drug candidate to be used in the treatment of Eo-related diseases. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8Safety of 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid).

2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8) belongs to amides. Because of the greater electronegativity of oxygen, the carbonyl (C=O) is a stronger dipole than the N–C dipole. The presence of a C=O dipole and, to a lesser extent a N–C dipole, allows amides to act as H-bond acceptors. Amides can be recrystallised from large quantities of water, ethanol, ethanol/ether, aqueous ethanol, chloroform/toluene, chloroform or acetic acid. The likely impurities are the parent acids or the alkyl esters from which they have been made. The former can be removed by thorough washing with aqueous ammonia followed by recrystallisation, whereas elimination of the latter is by trituration or recrystallisation from an organic solvent.Safety of 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid

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

SynAggreg: A Multifunctional High-Throughput Technology for Precision Study of Amyloid Aggregation and Systematic Discovery of Synergistic Inhibitor Compounds was written by Aviolat, Hubert;Nomine, Yves;Gioria, Sophie;Bonhoure, Anna;Hoffmann, David;Ruhlmann, Christine;Nierengarten, Helene;Ruffenach, Frank;Villa, Pascal;Trottier, Yvon;Klein, Fabrice A. C.. And the article was included in Journal of Molecular Biology in 2018.HPLC of Formula: 53902-12-8 This article mentions the following:

Numerous proteins can coalesce into amyloid self-assemblies, which are responsible for a class of diseases called amyloidoses, but which can also fulfill important biol. functions and are of great interest for biotechnol. Amyloid aggregation is a complex multi-step process, poorly prone to detailed structural studies. Therefore, small mols. interacting with amyloids are often used as tools to probe the amyloid aggregation pathway and in some cases to treat amyloidoses as they prevent pathogenic protein aggregation. Here, we report on SynAggreg, an in vitro high-throughput (HT) platform dedicated to the precision study of amyloid aggregation and the effect of modulator compounds SynAggreg relies on an accurate bi-fluorescent amyloid-tracer readout that overcomes some limitations of existing HT methods. It allows addressing diverse aspects of aggregation modulation that are critical for pathomechanistic studies, such as the specificity of compounds toward various amyloids and their effects on aggregation kinetics, as well as the co-assembly propensity of distinct amyloids and the influence of prion-like seeding on self-assembly. Furthermore, SynAggreg is the first HT technol. that integrates tailored methodol. to systematically identify synergistic compound combinations-an emerging strategy to improve fatal amyloidoses by targeting multiple steps of the aggregation pathway. To this end, we apply anal. combinatorial scores to rank the inhibition efficiency of couples of compounds and to readily detect synergism. Finally, the SynAggreg platform should be suited for the characterization of a broad class of amyloids, whether of interest for drug development purposes, for fundamental research on amyloid functions, or for biotechnol. applications. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8HPLC of Formula: 53902-12-8).

2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8) belongs to amides. The solubilities of amides and esters are roughly comparable. Typically amides are less soluble than comparable amines and carboxylic acids since these compounds can both donate and accept hydrogen bonds. Tertiary amides, with the important exception of N,N-dimethylformamide, exhibit low solubility in water. Amides can be freed from solvent or water by drying below their melting points. These purifications can also be used for sulfonamides and acid hydrazides.HPLC of Formula: 53902-12-8

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

Selective Cell Penetrating Peptide-Functionalized Polymersomes Mediate Efficient and Targeted Delivery of Methotrexate Disodium to Human Lung Cancer In Vivo was written by Yang, Weijing;Xia, Yifeng;Fang, Yuan;Meng, Fenghua;Zhang, Jian;Cheng, Ru;Deng, Chao;Zhong, Zhiyuan. And the article was included in Advanced Healthcare Materials in 2018.Application of 7413-34-5 This article mentions the following:

It is a long challenge to develop nanomedicines that simultaneously possess tumor cell selectivity and penetration functions. Here, it is reported that selective cell penetrating peptide (RLWMRWYSPRTRAYGC)-functionalized polymersomes (SCPP-PS) mediate efficient and targeted delivery of methotrexate disodium (MTX) to human lung cancer in vivo. SCPP-PS with an SCPP d. of 18.7% is self-crosslinked, has a small size (63-65 nm), and high MTX loading (up to 19.4 wt%), shows selective uptake and fast penetration into A549 lung cancer cells, and efficiently releases MTX intracellularly. Interestingly, MTX-loaded SCPP-PS (MTX-SCPP-PS) displays much lower IC₅₀ than those of MTX-PS and free MTX. Installing SCPP to polymersomes has no detrimental effect to their long blood circulation time but significantly increases drug accumulation in A549 tumor (5.3% injected dose per g at 8 h post injection). Remarkably, SCPP-PS exhibits deep penetration in to A549 tumors. MTX-SCPP-PS completely inhibits tumor progression and significantly improves survival rates in mice bearing A549 lung tumor xenografts as compared to MTX-PS and free MTX groups (median survival time: 75 vs 45 and 38 d, resp.), without causing noticeable adverse effects. These results highlight that functionalization of nanomedicines with SCPP is a feasible strategy to achieve efficient and targeted tumor therapy. In the experiment, the researchers used many compounds, for example, Sodium (S)-2-(4-(((2,4-diaminopteridin-6-yl)methyl)(methyl)amino)benzamido)pentanedioate (cas: 7413-34-5Application of 7413-34-5).

Sodium (S)-2-(4-(((2,4-diaminopteridin-6-yl)methyl)(methyl)amino)benzamido)pentanedioate (cas: 7413-34-5) belongs to amides. In primary and secondary amides, the presence of N–H dipoles allows amides to function as H-bond donors as well. Thus amides can participate in hydrogen bonding with water and other protic solvents; the oxygen atom can accept hydrogen bonds from water and the N–H hydrogen atoms can donate H-bonds. Amides are stable compounds. The lower-melting members (such as acetamide) can be readily purified by fractional distillation. Most amides are solids which have low solubilities in water.Application of 7413-34-5

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

Screening for contaminant hotspots in the marine environment of Kuwait using ecotoxicological and chemical screening techniques was written by Smith, A. J.;McGowan, T.;Devlin, M. J.;Massoud, M. S.;Al-Enezi, M.;Al-Zaidan, A. S.;Al-Sarawi, H. A.;Lyons, B. P.. And the article was included in Marine Pollution Bulletin in 2015.Application of 10543-57-4 This article mentions the following:

Kuwait is a country with low rainfall and highly concentrated industrial and domestic effluents entering its coastal waters. These can be both treated and untreated. In this study we sampled a series of coastal and open-sea sites and used a variety of analyses to identify those sites requiring the most attention. We used a high throughput GC-MS screen to look for over 1000 chems. in the samples. Estrogen and androgen screens assessed the potential to disrupt endocrine activity. An oyster embryo development screen was used to assess biol. effect potential. The chem. screen identified sites which had high numbers of identified industrial and domestic chems. The oyster screen showed that these sites had also caused high levels of developmental abnormalities with 100% of embryos affected at some sites. The yeast screen showed that estrogenic chems. were present in outfalls at 2-3 ng/l E2 equiv, and detectable even in some open water sites. In the experiment, the researchers used many compounds, for example, N,N-(Ethane-1,2-diyl)bis(N-acetylacetamide) (cas: 10543-57-4Application of 10543-57-4).

N,N-(Ethane-1,2-diyl)bis(N-acetylacetamide) (cas: 10543-57-4) belongs to amides. The amide group is called a peptide bond when it is part of the main chain of a protein, and an isopeptide bond when it occurs in a side chain, such as in the amino acids asparagine and glutamine. Amides are not in general accessible by the direct condensation of amines with carboxylic acids for two reasons: first, both components are readily deactivated by a transfer of a proton from the acid to the amine and second, the hydroxy unit on the carbonyl of the acid is a relatively poor leaving group. Nevertheless, the formation of five- and six-membered rings is often surprisingly simple provided that other factors can be brought into play to assist in the condensation.Application of 10543-57-4

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

Synthesis and pharmacological and conformational studies of 4-benzylisoquinolines, papaverine analogs was written by Bouvier, Philippe;Branceni, Dan;Prouteau, Monique;Prudhommeaux, Elie;Viel, Claude. And the article was included in European Journal of Medicinal Chemistry in 1976.SDS of cas: 61189-99-9 This article mentions the following:

Benzylisoquinolines I (R = Ph, 4-ClC6H4, 2-FC6H4, 3-FC6H4, 4-FC6H4, 2-ClC6H4, 2,6-Cl2C6H3, 3,4-Cl2C6H3, 4-MeOC6H4, 3,4-(MeO)2C6H3, 3,4,5-(MeO)3C6H2, 3,4-(methylenedioxy)phenyl, 4-HCOC6H4, 4-Me2NC6H4, 4-O2NC6H4; R1 = 6-OMe, R2 = 7-OMe, R3 = H; R1 = 7-OMe, R2 = R3 = H; R1 = 5-OMe, 7-OMe, R2 = 8-OMe, R3 = H; R1 = 5-OMe, R2 = 6-OMe, R3 = 7-OMe; R1R2 = 6,7-OCH2O, R3 = H) were prepared by treating (EtO)2CHCO2Et with NH3, reducing (EtO)2CHCONH2, treating H2NCH2CH(OEt)2 with R1R2R3C6H2CHO followed by hydrogenation, and cyclizing R1R2R3C6H2CH2NHCH2CH(OEt)2 with RCHO. In the experiment, the researchers used many compounds, for example, 2,2-Diethoxyacetamide (cas: 61189-99-9SDS of cas: 61189-99-9).

2,2-Diethoxyacetamide (cas: 61189-99-9) belongs to amides. Amides include many other important biological compounds, as well as many drugs like paracetamol, penicillin and LSD. Low-molecular-weight amides, such as dimethylformamide, are common solvents. Ionic, or saltlike, amides are strongly alkaline compounds ordinarily made by treating ammonia, an amine, or a covalent amide with a reactive metal such as sodium.SDS of cas: 61189-99-9

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

Infrared spectra of N-substituted sulfonamides was written by Goldstein, Michael;Russell, Maurice Alan;Willis, H. A.. And the article was included in Spectrochimica Acta, Part A: Molecular and Biomolecular Spectroscopy in 1969.Name: N-Isopropylbenzenesulfonamide This article mentions the following:

The ir spectra of 25 sulfonamides of the types MeSO2NHR (R = Me, iso-Pr, tert-Bu) MeSO2NR2 (R = Me,Et,iso-Pr), ArSO2NHR (Ar = Ph, p-tolyl; R = Me, Et, Pr, iso-Pr, Bu, iso-Bu, sec-Bu, tert-Bu), and PhSO2NR2 (R = Me, Et, iso-Pr) have been studied. Assignments are discussed for stretching and deformation vibrations of the NH and SO2 groups and for SN, CS and CN stretching modes. Some consideration is also given to vibrations of the hydrocarbon residues. In the experiment, the researchers used many compounds, for example, N-Isopropylbenzenesulfonamide (cas: 5339-69-5Name: N-Isopropylbenzenesulfonamide).

N-Isopropylbenzenesulfonamide (cas: 5339-69-5) belongs to amides. In primary and secondary amides, the presence of N–H dipoles allows amides to function as H-bond donors as well. Thus amides can participate in hydrogen bonding with water and other protic solvents; the oxygen atom can accept hydrogen bonds from water and the N–H hydrogen atoms can donate H-bonds. Amides are not in general accessible by the direct condensation of amines with carboxylic acids for two reasons: first, both components are readily deactivated by a transfer of a proton from the acid to the amine and second, the hydroxy unit on the carbonyl of the acid is a relatively poor leaving group. Nevertheless, the formation of five- and six-membered rings is often surprisingly simple provided that other factors can be brought into play to assist in the condensation.Name: N-Isopropylbenzenesulfonamide

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

Discovery of BMS-986202: A Clinical Tyk2 Inhibitor that Binds to Tyk2 JH2 was written by Liu, Chunjian;Lin, James;Langevine, Charles;Smith, Daniel;Li, Jianqing;Tokarski, John S.;Khan, Javed;Ruzanov, Max;Strnad, Joann;Zupa-Fernandez, Adriana;Cheng, Lihong;Gillooly, Kathleen M.;Shuster, David;Zhang, Yifan;Thankappan, Anil;McIntyre, Kim W.;Chaudhry, Charu;Elzinga, Paul A.;Chiney, Manoj;Chimalakonda, Anjaneya;Lombardo, Louis J.;Macor, John E.;Carter, Percy H.;Burke, James R.;Weinstein, David S.. And the article was included in Journal of Medicinal Chemistry in 2021.Electric Literature of C8H9ClN2O This article mentions the following:

A search for structurally diversified Tyk2 JH2 ligands from 6 (BMS-986165), a pyridazine carboxamide-derived Tyk2 JH2 ligand as a clin. Tyk2 inhibitor currently in late development for the treatment of psoriasis, began with a survey of six-membered heteroaryl groups in place of the N-Me triazolyl moiety in 6. The x-ray co-crystal structure of an early lead (12) revealed a potential new binding pocket. Exploration of the new pocket resulted in two front-runners for a clin. candidate. The potential hydrogen bonding interaction with Thr599 in the pocket was achieved with a tertiary amide moiety, confirmed by the x-ray co-crystal structure of 29. When the diversity search was extended to nicotinamides, a single fluorine atom addition was found to significantly enhance the permeability, which directly led to the discovery of 7 (BMS-986202) as a clin. Tyk2 inhibitor that binds to Tyk2 JH2. The preclin. studies of 7, including efficacy studies in mouse models of IL-23-driven acanthosis, anti-CD40-induced colitis, and spontaneous lupus, will also be presented. In the experiment, the researchers used many compounds, for example, 6-Chloro-N,N-dimethylnicotinamide (cas: 54864-83-4Electric Literature of C8H9ClN2O).

6-Chloro-N,N-dimethylnicotinamide (cas: 54864-83-4) belongs to amides. The amide group is called a peptide bond when it is part of the main chain of a protein, and an isopeptide bond when it occurs in a side chain, such as in the amino acids asparagine and glutamine. Amides are stable compounds. The lower-melting members (such as acetamide) can be readily purified by fractional distillation. Most amides are solids which have low solubilities in water.Electric Literature of C8H9ClN2O

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

Benzylic Aroylation of Toluenes Mediated by a LiN(SiMe₃)₂/Cs⁺ System was written by Gu, Yuanyun;Zhang, Zhen;Wang, Yan-En;Dai, Ziteng;Yuan, Yaqi;Xiong, Dan;Li, Jie;Walsh, Patrick J.;Mao, Jianyou. And the article was included in Journal of Organic Chemistry in 2022.Product Details of 192436-83-2 This article mentions the following:

Chemoselective deprotonative functionalization of benzylic C-H bonds is challenging, because the arene ring contains multiple aromatic C(sp²)-H bonds, which can be competitively deprotonated and lead to selectivity issues. Recently it was found that bimetallic [MN(SiMe₃)₂ M = Li, Na]/Cs⁺ combinations exhibit excellent benzylic selectivity. Herein, is reported the first deprotonative addition of toluenes to Weinreb amides mediated by LiN(SiMe₃)₂/CsF for the synthesis of a diverse array of 2-arylacetophenones. Surprisingly, simple Me benzoates also react with toluenes under similar conditions to form 2-arylacetophenones without double addition to give tertiary alc. products. This finding greatly increases the practicality and impact of this chem. Some challenging substrates with respect to benzylic deprotonations, such as fluoro and methoxy substituted toluenes, are selectively transformed to 2-aryl acetophenones. The value of benzylic deprotonation of 3-fluorotoluene is demonstrated by the synthesis of a key intermediate in the preparation of Polmacoxib. In the experiment, the researchers used many compounds, for example, 4-Bromo-N-methoxy-N-methylbenzamide (cas: 192436-83-2Product Details of 192436-83-2).

4-Bromo-N-methoxy-N-methylbenzamide (cas: 192436-83-2) belongs to amides. The solubilities of amides and esters are roughly comparable. Typically amides are less soluble than comparable amines and carboxylic acids since these compounds can both donate and accept hydrogen bonds. Tertiary amides, with the important exception of N,N-dimethylformamide, exhibit low solubility in water. The presence of the amide group –C(=O)N– is generally easily established, at least in small molecules. It can be distinguished from nitro and cyano groups in IR spectra. Amides exhibit a moderately intense νCO band near 1650 cm−1. By 1H NMR spectroscopy, CONHR signals occur at low fields. In X-ray crystallography, the C(=O)N center together with the three immediately adjacent atoms characteristically define a plane.Product Details of 192436-83-2

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

Application and investigation of TAED advanced oxidation in the polyester/cotton fabric desizing process was written by Ding, Wei;Zhou, Rong;Zheng, Qing-kang. And the article was included in Qingdao Daxue Xuebao, Gongcheng Jishuban in 2009.Computed Properties of C10H16N2O4 This article mentions the following:

TAED oxidation system was employed in order to remove PVA from the polyester/cotton fabric and to make it degrade into small degradable organic compound Effects of TAED/H₂O₂ molar ratio, TAED and H₂ O₂ amounts, initial pH value of the desizing solution, desizing temperature and desizing time in TAED/H₂O₂ oxidation system were investigated in order to remove PVA from the fabric and improve its biodegradability. The optimal operation condition determined by orthogonal test method were: temperature of 80°C, time of 60 min, pH value of 7, TAED/H₂O₂ molar ratio of 1/3, TAED amount of 0.06 mol/L and liquor ratio of 1:30. Under this optimal operation condition, the desizing rate is 99.7%, which shows a good desizing result. In the experiment, the researchers used many compounds, for example, N,N-(Ethane-1,2-diyl)bis(N-acetylacetamide) (cas: 10543-57-4Computed Properties of C10H16N2O4).

N,N-(Ethane-1,2-diyl)bis(N-acetylacetamide) (cas: 10543-57-4) belongs to amides. Amides are pervasive in nature and technology. Proteins and important plastics like Nylons, Aramid, Twaron, and Kevlar are polymers whose units are connected by amide groups (polyamides); these linkages are easily formed, confer structural rigidity, and resist hydrolysis. The presence of the amide group –C(=O)N– is generally easily established, at least in small molecules. It can be distinguished from nitro and cyano groups in IR spectra. Amides exhibit a moderately intense νCO band near 1650 cm−1. By 1H NMR spectroscopy, CONHR signals occur at low fields. In X-ray crystallography, the C(=O)N center together with the three immediately adjacent atoms characteristically define a plane.Computed Properties of C10H16N2O4

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

Acetic Acid-Catalyzed Regioselective C(sp²)-H Bond Functionalization of Indolizines: Concomitant Involvement of Synthetic and Theoretical Studies was written by Mane, Kishor D.;Mukherjee, Anirban;Das, Gourab Kanti;Suryavanshi, Gurunath. And the article was included in Journal of Organic Chemistry in 2022.HPLC of Formula: 1146-43-6 This article mentions the following:

An atom economical and environmentally benign protocol has been developed for the regioselective C(sp²)-H bond functionalization of indolizines. The acetic acid-catalyzed cross-coupling reaction proceeds under metal-free conditions, producing a wide range of synthetically useful indolizine derivatives The present protocol showed good functional group tolerance and broad substrate scope in good to excellent yields. Quantum mech. investigation using d. functional theory (DFT) has played a crucial role in understanding that acetic acid is the key player in determining the actual pathway as the catalyst and its ultrafast nature. Different pathways involving inter- and intramol. proton transfer, with or without acetic acid, were investigated. Calculated results revealed that a proton shuttle mechanism is involved for the least energetic, most favorable acetic acid-catalyzed pathway. Furthermore, regioselectivity has also been explained theor. In the experiment, the researchers used many compounds, for example, N-(4-Hydroxyphenyl)-4-methylbenzenesulfonamide (cas: 1146-43-6HPLC of Formula: 1146-43-6).

N-(4-Hydroxyphenyl)-4-methylbenzenesulfonamide (cas: 1146-43-6) belongs to amides. The solubilities of amides and esters are roughly comparable. Typically amides are less soluble than comparable amines and carboxylic acids since these compounds can both donate and accept hydrogen bonds. Tertiary amides, with the important exception of N,N-dimethylformamide, exhibit low solubility in water. Amides are stable compounds. The lower-melting members (such as acetamide) can be readily purified by fractional distillation. Most amides are solids which have low solubilities in water.HPLC of Formula: 1146-43-6

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