Month: December 2022

A formal synthesis of althiomycin was written by Toogood, Peter L.;Hollenbeck, Jessica J.;Lam, Huong M.;Li, Li. And the article was included in Bioorganic & Medicinal Chemistry Letters in 1996.HPLC of Formula: 61189-99-9 This article mentions the following:

The thiazolecarboxylate and amine fragments previously used in the preparation of althiomycin were prepared in a formal synthesis of althiomycin for studies of its interaction with prokaryotic ribosomes. In the experiment, the researchers used many compounds, for example, 2,2-Diethoxyacetamide (cas: 61189-99-9HPLC of Formula: 61189-99-9).

2,2-Diethoxyacetamide (cas: 61189-99-9) 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. 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.HPLC of Formula: 61189-99-9

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

Clinical safety and efficacy of neoadjuvant combination chemotherapy of tranilast in advanced esophageal squamous cell carcinoma: Phase I/II study (TNAC) was written by Shiozaki, Atsushi;Kudou, Michihiro;Fujiwara, Hitoshi;Konishi, Hirotaka;Shimizu, Hiroki;Arita, Tomohiro;Kosuga, Toshiyuki;Yamamoto, Yusuke;Morimura, Ryo;Ikoma, Hisashi;Kuriu, Yoshiaki;Kubota, Takeshi;Okamoto, Kazuma;Otsuji, Eigo. And the article was included in Medicine (Philadelphia, PA, United States) in 2020.SDS of cas: 53902-12-8 This article mentions the following:

Transient receptor potential vanilloid 2 (TRPV2) was previously shown to play an important role in the maintenance of cancer stem cells, and its specific inhibitor, tranilast, also has potential as a targeted therapeutic agent for esophageal squamous cell carcinoma (ESCC). The present study is being conducted to confirm the safety and efficacy of the addnl. use of tranilast with conventional preoperative adjuvant chemotherapy for patients with advanced ESCC. Between 56 and 59 patients aged between 20 and 74 years with clin. diagnosed Stage II or Stage III ESCC will be enrolled. Eligible patients will receive preoperative adjuvant chemotherapy, 2 cycles of combination therapy with cisplatin, 5-fluorouracil, and tranilast. Recruitment started in Nov. 2019, with the final follow-up being planned for March 2029. One subject has been enrolled since Oct. 21, 2020. The pathol. therapeutic effect is the primary endpoint. The objective response rate, safety of preoperative adjuvant chemotherapy, recurrence-free survival (RFS), and overall survival (OS) are the secondary endpoints. RFS and OS will be calculated as the time from surgery to first recurrence and all-cause death, resp. This protocol has been approved by the Institutional Review Boards of Kyoto Prefectural University of Medicine and all participating hospitals in August 30, 2019 (Number: CRB5180001). Written informed consent will be obtained from all patients before their registration, which is in accordance with the Declaration of Helsinki. The results of the present study will be disseminated via publication in peer-reviewed journals. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8SDS of cas: 53902-12-8).

2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8) 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. 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.SDS of cas: 53902-12-8

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

Palladium-Catalyzed One-Pot Synthesis of Quinazolinones via tert-Butyl Isocyanide Insertion was written by Jiang, Xiao;Tang, Ting;Wang, Jin-Mei;Chen, Zhong;Zhu, Yong-Ming;Ji, Shun-Jun. And the article was included in Journal of Organic Chemistry in 2014.Quality Control of 2-Amino-4-fluorobenzamide This article mentions the following:

A novel palladium-catalyzed three-component reaction for the synthesis of quinazolin-4(3H)-ones from readily available 2-aminobenzamides and aryl halides via a palladium-catalyzed isocyanide insertion/cyclization sequence has been developed. This methodol. efficiently constructs quinazolin-4(3H)-ones in moderate to excellent yields with the advantages of operational simplicity. E.g., in presence of PdCl₂, DPPP, CaCl₂, and t-BuONa in toluene at 145 °C, reaction of IPh, anthranilamide, and t-BuNC gave 93% quinazolin-4(3H)-one derivative (I). In the experiment, the researchers used many compounds, for example, 2-Amino-4-fluorobenzamide (cas: 119023-25-5Quality Control of 2-Amino-4-fluorobenzamide).

2-Amino-4-fluorobenzamide (cas: 119023-25-5) 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. 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.Quality Control of 2-Amino-4-fluorobenzamide

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

Potassium tert-butoxide-mediated metal-free synthesis of sulfonamides from sodium sulfinates and N,N-disubstituted formamides was written by Bao, Xiaodong;Rong, Xiaona;Liu, Zhiguo;Gu, Yugui;Liang, Guang;Xia, Qinqin. And the article was included in Tetrahedron Letters in 2018.Category: amides-buliding-blocks This article mentions the following:

A new protocol was developed for KO-t-Bu mediated metal-free direct S-N bond formation from sodium sulfinates and formamides as amine sources. This protocol provided a simple and green approach for the preparation of sulfonamide derivatives RSO₂NR¹R² [R = 2-thienyl, Ph, 1-naphthyl, etc.; R¹ = Me, Et, Bn; R² = Me, Et; R¹R₂ = (CH₂)₅, (CH₂)₂O(CH₂)₂] from sodium sulfinates and N,N-disubstituted formamides. The reaction utilized readily available starting materials under metal-free conditions, thus providing an alternative and attractive route to sulfonamides. In the experiment, the researchers used many compounds, for example, 4-Fluoro-N,N-dimethylbenzenesulfonamide (cas: 383-31-3Category: amides-buliding-blocks).

4-Fluoro-N,N-dimethylbenzenesulfonamide (cas: 383-31-3) 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 can be freed from solvent or water by drying below their melting points. These purifications can also be used for sulfonamides and acid hydrazides.Category: amides-buliding-blocks

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

Repurposing of Tranilast for Potential Neuropathic Pain Treatment by Inhibition of Sepiapterin Reductase in the BH₄ Pathway was written by Moore, Benjamin J. R.;Islam, Barira;Ward, Sean;Jackson, Olivia;Armitage, Rebecca;Blackburn, Jack;Haider, Shozeb;McHugh, Patrick C.. And the article was included in ACS Omega in 2019.Reference of 53902-12-8 This article mentions the following:

Tetrahydrobiopterin (BH₄) is a cofactor in the production of various signaling mols. including nitric oxide, dopamine, adrenaline, and noradrenaline. BH₄ levels are critical for processes associated with cardiovascular function, inflammation, mood, pain, and neurotransmission. Increasing pieces of evidence suggest that BH₄ is upregulated in chronic pain. Sepiapterin reductase (SPR) catalyzes both the reversible reduction of sepiapterin to dihydrobiopterin (BH₂) and 6-pyruvoyl-tetrahydrobiopterin to BH₄ within the BH₄ pathway. Therefore, inhibition of SPR by small mols. can be used to control BH₄ production and ultimately alleviate chronic pain. Here, we have used various in silico and in vitro experiments to show that tranilast, licensed for use in bronchial asthma, can inhibit sepiapterin reduction by SPR. Docking and mol. dynamics simulations suggest that tranilast can bind to human SPR (hSPR) at the same site as sepiapterin including S157, one of the catalytic triad residues of hSPR. Colorimetric assays revealed that tranilast was nearly twice as potent as the known hSPR inhibitor, N-acetyl serotonin. Tranilast was able to inhibit hSPR activity both intracellularly and extracellularly in live cells. Triple quad mass spectrophotometry of cell lysates showed a proportional decrease of BH₄ in cells treated with tranilast. Our results suggest that tranilast can act as a potent hSPR inhibitor and therefore is a valid candidate for drug repurposing in the treatment of chronic pain. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8Reference of 53902-12-8).

2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8) 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 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.Reference of 53902-12-8

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

Ce(III) immobilised on aminated epichlorohydrin-activated agarose matrix – “green” and efficient catalyst for transamidation of carboxamides was written by Zarei, Zeinab;Akhlaghinia, Batool. And the article was included in Chemical Papers in 2015.Recommanded Product: 2670-38-4 This article mentions the following:

The present study reports the preparation and characterization of Ce(III) immobilized on an aminated epichlorohydrin-activated agarose matrix (CAEA) as a green catalyst. The catalyst was synthesized by the reaction of the epichlorohydrin-activated agarose matrix with ammonia solution, which was then treated with Ce(NO₃)₃·6H₂O. The catalyst (CAEA) was characterized by FT-IR, far IR, elemental anal., XRD, TGA and ICP techniques. CAEA was found to be an effective and reusable heterogeneous catalyst for the transamidation of carboxamides with amines under solvent-free conditions. The catalyst was successfully applied to the synthesis of a wide range of aromatic and aliphatic amides. High efficiency, mild reaction conditions, easy work-up and simple separation were the important advantages of this catalyst. In the experiment, the researchers used many compounds, for example, 3,4-Dichlorobenzamide (cas: 2670-38-4Recommanded Product: 2670-38-4).

3,4-Dichlorobenzamide (cas: 2670-38-4) belongs to amides. Compared to amines, amides are very weak bases and do not have clearly defined acid–base properties in water. On the other hand, amides are much stronger bases than esters, aldehydes, and ketones. 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.Recommanded Product: 2670-38-4

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

Synthesis and Investigation of Therapeutic Potential of Isoform-Specific HDAC8 Inhibitors for the Treatment of Cutaneous T Cell Lymphoma was written by Umamaheswari, Appavoo;Puratchikody, Ayarivan;Hari, Natarajan. And the article was included in Anti-Cancer Agents in Medicinal Chemistry in 2019.Related Products of 2387-23-7 This article mentions the following:

The aim of this paper was to synthesis and evaluates HDAC8 isoform specific inhibitors. Based on the preliminary report on the design and in-silico studies of 52 hydroxamic acid derivatives bearing multi-substituent heteroaromatic rings with chiral amine linker, five compounds were shortlisted and synthesized by microwave assisted approach and high yielding synthetic protocol. A series of in-vitro assays in addition to HDAC8 inhibitory activity was used to evaluate the synthesized compounds Serine derivatives I [R = H, MeO, OH; R¹ = H, Br; R² = Me, NH₂, MeO] and II exerted the anti-proliferative activities against CTCL cell lines at 20- 100 μM concentrations Both the compounds I and II exhibited μM inhibitory activity against HDAC8. The compound I [R = OH, R¹ = Br, R² = Me] displayed remarkable HDAC8 selectivity superior to that of the standard drug, SAHA with an IC50 at 0.1μM. Simple modifications at different portions of pharmacophore in the hydroxamic acid analogs were effective for improving both HDAC8 inhibitory activity and isoform selectivity. Potent and highly isoform-selective HDAC8 inhibitors were identified. These findings were expedient for further development of HDAC8-selective inhibitors. In the experiment, the researchers used many compounds, for example, 1,3-Dicyclohexylurea (cas: 2387-23-7Related Products of 2387-23-7).

1,3-Dicyclohexylurea (cas: 2387-23-7) 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. As a result of interactions such as these, the water solubility of amides is greater than that of corresponding hydrocarbons. These hydrogen bonds are also have an important role in the secondary structure of proteins.Related Products of 2387-23-7

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

Kraft pulp bleaching with a P-stage catalyzed by both bicarbonate and TAED was written by Das, N.;Bose, S. K.;Francis, R. C.. And the article was included in Tappi Journal in 2019.Formula: C10H16N2O4 This article mentions the following:

Peroxide bleaching of softwood and hardwood (eucalypt) kraft pulps was performed in solutions of sodium bicarbonate (NaHCO₃), sodium carbonate (Na₂CO₃), and sodium hydroxide (NaOH). The conventional P stage (hydrogen peroxide + sodium hydroxide; H₂O₂ + NaOH) was the most effective brightening system without an addnl. activator. However, peroxide activation by bicarbonate anion (HCO₃^–) was obvious in all cases where NaHCO₃ or Na₂CO₃ was used. When N,N,N’,N’-tetraacetylethylenediamine (TAED) was added to the bleaching system, Na₂CO₃ as the alkali source afforded equal or slightly higher bleached brightness compared to NaOH usage for both the softwood and hardwood pulps. This outcome is attributed to simultaneous peroxide activation by HCO₃^– and TAED. When applied to the eucalypt pulp, the H₂O₂/Na₂CO₃/TAED bleaching system also decreased the brightness loss due to thermal reversion. In the experiment, the researchers used many compounds, for example, N,N-(Ethane-1,2-diyl)bis(N-acetylacetamide) (cas: 10543-57-4Formula: C10H16N2O4).

N,N-(Ethane-1,2-diyl)bis(N-acetylacetamide) (cas: 10543-57-4) 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. In simple aromatic amides, fragmentation occurs on both sides of the carbonyl group. If a hydrogen is available in N-substituted aromatic amides, it tends to migrate and form an aromatic amine and the loss of a ketene.Formula: C10H16N2O4

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

Bleaching of Cotton/polyamide fabrics with enzymes and peracetic acid was written by Usluoglu, Ayse;Arabaci, Gulnur. And the article was included in Asia-Pacific Journal of Chemical Engineering in 2014.Reference of 10543-57-4 This article mentions the following:

Presently biotechnol. plays an important role especially in the field of environmental protection. In the textile industry, enzymes are often used in many technol. processes as they are ecol. This study attempted to introduce the bio-processes in the conventional scouring and bleaching preparation of cotton/polyamide (PA) fabric. We investigated the utilization of peracetic acid formed in situ from reaction of tetraacetylethylenediamine with sodium perborate to affecting bleaching process by using lipase, protease, cellulase, pectinase enzymes. Fabric wettability, tensile strength, whiteness index were taken as a measure of the extent of cotton/PA bleaching. The optimized bleaching recipe and processing were compared with conventional process. Results obtained that, cotton/PA fabric bleached with peracetic acid and either lipase, protease, cellulase or pectinase enzyme shows excellent wettability and acceptable whiteness index. The optimum bleaching recipe consists of 20 g/L, tetraacetylethylenediamine; 12 g/L, sodium perborate; 2 g/L, enzymes; and 1 g/L non-ionic wetting agent; the treatment was carried out at 60 °C for 45 min. This bio-process achieved high quality cotton/PA fabric whiteness to the conventional system at much shorter batch times and with significantly reduced fabric strange lost and alkali consumption, which would be beneficial to the textile industry. © 2014 Curtin University of Technol. and John Wiley & Sons, Ltd. In the experiment, the researchers used many compounds, for example, N,N-(Ethane-1,2-diyl)bis(N-acetylacetamide) (cas: 10543-57-4Reference of 10543-57-4).

N,N-(Ethane-1,2-diyl)bis(N-acetylacetamide) (cas: 10543-57-4) 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. In simple aromatic amides, fragmentation occurs on both sides of the carbonyl group. If a hydrogen is available in N-substituted aromatic amides, it tends to migrate and form an aromatic amine and the loss of a ketene.Reference of 10543-57-4

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

SARS-CoV-2 infection: NLRP3 inflammasome as plausible target to prevent cardiopulmonary complications? was written by Quagliariello, V;Bonelli, A;Caronna, A;Lombari, M C;Conforti, G;Libutti, M;Iaffaioli, R V;Berretta, M;Botti, G;Maurea, N. And the article was included in European review for medical and pharmacological sciences in 2020.Computed Properties of C18H17NO5 This article mentions the following:

NLRP3 (NOD-, LRR- and pyrin domain-containing protein 3) inflammasome has recently become an intriguing target of several chronic and viral diseases. Here, we argue that targeting NLRP3 inflammasome could be a strategy to prevent cardiovascular outcomes [fulminant myocarditis, heart failure, venous thromboembolism (VTE)] and acute respiratory distress syndrome (ARDS) in patients with SARS-CoV-2 infection. We discuss the rationale for NLRP3 targeting in clinical trials as an effective therapeutic strategy aimed to improve prognosis of COVID-19, analyzing the potential of two therapeutic options (tranilast and OLT1177) currently available in clinical practice. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8Computed Properties of C18H17NO5).

2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8) 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. 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 C18H17NO5

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