Month: February 2023

Tranilast as an Adjunctive Therapy in Hospitalized Patients with Severe COVID- 19: A Randomized Controlled Trial was written by Saeedi-Boroujeni, Ali;Nashibi, Roohangiz;Ghadiri, Ata A.;Nakajima, Motowo;Salmanzadeh, Shokrollah;Mahmoudian-Sani, Mohammad-Reza;Hanafi, Mohammad Ghasem;Sharhani, Asaad;Khodadadi, Ali. And the article was included in Archives of Medical Research in 2022.Quality Control of 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid This article mentions the following:

Tranilast is a potential NLRP3 inflammasome inhibitor that may relieve progressive inflammation due to COVID-19. To evaluate the therapeutic effects of Tranilast in combination with antiviral drugs in non-ICU-admitted hospitalized patients with COVID-19. This study was an open-label clin. trial that included 72 hospitals admitted patients with severe COVID-19 at Razi Hospital, Ahvaz, Iran, from July 2020-August 2020. These patients were randomly assigned in a 1:1 ratio to control (30) and intervention groups (30). Patients in the control group received antiviral therapy, while patients in the intervention group received Tranilast (300 mg daily) in addition to the antiviral drugs for Seven days. The collected data, including the expression of inflammatory cytokine, laboratory tests, and clin. findings, was used for intragroup comparisons. The intervention group showed significantly lower levels of NLR (p = 0.001), q-CRP (p = 0.002), IL-1 (p = 0.001), TNF (p = 0.001), and LDH (p = 0.046) in comparison with the control group. The effect of intervention was significant in increasing the o2 saturation (F = 7.72, p = 0.007). Long hospitalization (four days or above) was 36.6% in the Tranilast and 66.6% in the control group (RR = 0.58; 95% CI: 0.38-1.06, p = 0.045). In the Tranilst and control groups, one and four deaths or hospitalization in ICU were observed resp. (RR = 0.31; 95% CI: 0.03-2.88, p = 0.20). Tranilast might be used as an effective and safe adjuvant therapy and enhance the antiviral therapy′s efficacy for managing patients with COVID-19. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8Quality Control of 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid).

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 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.Quality Control of 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid

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

Design, synthesis and biological activities of 2,3-dihydroquinazolin-4(1H)-one derivatives as TRPM2 inhibitors was written by Zhang, Han;Liu, Huan;Luo, Xiao;Wang, Yuxi;Liu, Yuan;Jin, Hongwei;Liu, Zhenming;Yang, Wei;Yu, Peilin;Zhang, Liangren;Zhang, Lihe. And the article was included in European Journal of Medicinal Chemistry in 2018.Electric Literature of C7H7ClN2O This article mentions the following:

In this study, a series of novel 2,3-dihydroquinazolin-4(1H)-one derivatives, e.g. I was subsequently synthesized and characterized. Their inhibitory activity against the TRPM2 channel was evaluated by calcium imaging and electrophysiol. approaches. Some of the compounds exhibited significant inhibitory activity, especially 6-bromo-8-methyl-2-[3-(2-naphthyl)-1H-pyrazol-4-yl]-2,3-dihydro-1H-quinazolin-4-one which showed an IC₅₀ of 3.7μM against TRPM2 and did not affect the TRPM8 channel. The summarized structure-activity relationship (SAR) provided valuable insights for further development of specific TRPM2 targeted inhibitors. In the experiment, the researchers used many compounds, for example, 6-Chloro-2-aminobenzamide (cas: 54166-95-9Electric Literature of C7H7ClN2O).

6-Chloro-2-aminobenzamide (cas: 54166-95-9) 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.Electric Literature of C7H7ClN2O

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

Reactions of OH-radicals with procarbazine. A pulse radiolysis and computer simulation study was written by Delipetar-Grudl, A.;Solar, S.;Getoff, N.. And the article was included in Anticancer Research in 2006.Recommanded Product: 13255-50-0 This article mentions the following:

Pulse radiolysis was applied to study the reactivity of ^·OH radicals with procarbazine (PC), a cytostatic agent widely used in radiation- and chemotherapy. An overall rate constant of k(^·OH+PC)=3.7×10⁹ l.mol^-1.s^-1 was determined The thereby formed transients had a strong absorption at 350 nm, ε₃₅₀=4.46×10³ l.mol^-1.cm^-1, and a weak absorption band around 530 nm. Computer simulation studies to elucidate the most probable sites of ^·OH attack on the PC mol. showed that ^·OH radical addition to the aromatic ring had the highest probability. These transients decayed by a first order reaction, k=1.75×10³ s^-1, whereby species having a maximum absorption at 300 nm and broad shoulder at 340-380 nm were formed. Similar absorptions were observed after gamma radiolysis of PC. A reaction mechanism is suggested. For the reaction of H-atoms with PC, a rate constant k(^·H+PC)=6.4×10⁸ l.mol^-1.s^-1 was determined In the experiment, the researchers used many compounds, for example, 4-Formyl-N-isopropylbenzamide (cas: 13255-50-0Recommanded Product: 13255-50-0).

4-Formyl-N-isopropylbenzamide (cas: 13255-50-0) 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 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.Recommanded Product: 13255-50-0

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

A general palladium-catalyzed cross-coupling of aryl fluorides and organotitanium (IV) reagents was written by He, Xiao-Yun. And the article was included in Monatshefte fuer Chemie in 2021.Reference of 383-31-3 This article mentions the following:

Pd(OAc)₂/1-[2-(di-tert-butylphosphanyl)phenyl]-4-methoxy-piperidine was demonstrated to effectively catalyze cross-coupling of aryl fluoride and aryl(alkyl) titanium reagent. Both electron-deficient and electron-rich aryl fluoride reacted effectively with nucleophile and provided extensive functional groups tolerance. 2-Arylated product was realized by selective activation of the C-F bond. In the experiment, the researchers used many compounds, for example, 4-Fluoro-N,N-dimethylbenzenesulfonamide (cas: 383-31-3Reference of 383-31-3).

4-Fluoro-N,N-dimethylbenzenesulfonamide (cas: 383-31-3) 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.Reference of 383-31-3

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

Halogenation of N-substituted p-quinone imines and p-quinone oxime esters: IV. Chlorination and bromination of N-arylsulfonyl-2(3)-methyl(2-chloro)-1,4-benzoquinone monoimines was written by Avdeenko, A. P.;Konovalova, S. A.. And the article was included in Russian Journal of Organic Chemistry in 2006.Application of 1146-43-6 This article mentions the following:

The addition of halogens to N-arylsulfonyl-1,4-benzoquinone imines (e.g. N-(4-oxo-2,5-cyclohexadien-1-ylidene)benzenesulfonamide), which exist in a solution as Z and E isomers, is controlled by steric factors. Z-E isomerization strongly affects the stability of cyclohexene structures formed by halogenation of 1,4-benzoquinone imines. The halogenation of N-arylsulfonyl-1,4-benzoquinone imines is accompanied by prototropic rearrangement. The halogenation of analogous phenols, e.g. N-(4-hydroxyphenyl)benzenesulfonamide, which were also obtained in the halogenation of the quinone imines, was also examined In the experiment, the researchers used many compounds, for example, N-(4-Hydroxyphenyl)-4-methylbenzenesulfonamide (cas: 1146-43-6Application of 1146-43-6).

N-(4-Hydroxyphenyl)-4-methylbenzenesulfonamide (cas: 1146-43-6) belongs to amides. Amides can be viewed as a derivative of a carboxylic acid RC(=O)OH with the hydroxyl group –OH replaced by an amine group −NR′R″; or, equivalently, an acyl (alkanoyl) group RC(=O)− joined to an amine group. 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 1146-43-6

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

Analogues of Fenarimol Are Potent Inhibitors of Trypanosoma cruzi and Are Efficacious in a Murine Model of Chagas Disease was written by Keenan, Martine;Abbott, Michael J.;Alexander, Paul W.;Armstrong, Tanya;Best, Wayne M.;Berven, Bradley;Botero, Adriana;Chaplin, Jason H.;Charman, Susan A.;Chatelain, Eric;von Geldern, Thomas W.;Kerfoot, Maria;Khong, Andrea;Nguyen, Tien;McManus, Joshua D.;Morizzi, Julia;Ryan, Eileen;Scandale, Ivan;Thompson, R. Andrew;Wang, Sen Z.;White, Karen L.. And the article was included in Journal of Medicinal Chemistry in 2012.COA of Formula: C10H10F3NO2 This article mentions the following:

We report the discovery of nontoxic fungicide fenarimol (1, I) as an inhibitor of Trypanosoma cruzi (T. cruzi), the causative agent of Chagas disease, and the results of structure-activity investigations leading to potent analogs with low nM IC₅₀s in a T. cruzi whole cell in vitro assay. Lead compounds suppressed blood parasitemia to virtually undetectable levels after once daily oral dosing in mouse models of T. cruzi infection. Compounds are chem. tractable, allowing rapid optimization of target biol. activity and drug characteristics. Chem. and biol. studies undertaken in the development of the fenarimol series toward the goal of delivering a new drug candidate for Chagas disease are reported. In the experiment, the researchers used many compounds, for example, N-Methoxy-N-methyl-4-(trifluoromethyl)benzamide (cas: 116332-61-7COA of Formula: C10H10F3NO2).

N-Methoxy-N-methyl-4-(trifluoromethyl)benzamide (cas: 116332-61-7) 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.COA of Formula: C10H10F3NO2

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

¹H NMR determination of 1,3-dicyclohexylurea, glutaric acid and triethylamine in medical four-arm poly(ethylene glycol)-N-hydroxysuccinimide-glutarate for better quality control was written by Li, Fei-Fei;Liu, Hui-Xiang;Zhang, Yan-Li;Wang, Shu-Qi. And the article was included in Analytical Methods in 2019.Application In Synthesis of 1,3-Dicyclohexylurea This article mentions the following:

Absorbable vascular sealing medical glue, which belongs to Class III medical devices, is a special new material for preventing the leakage of cerebrospinal fluid. Medical four-arm poly(ethylene glycol)-N-hydroxysuccinimide-glutarate (4-arm-PEG-SG) with a mol. weight of 20 000 is the main component of the absorbable medical glue. According to its quality standard, the quality control of residues 1,3-dicyclohexylurea (DCU), glutaric acid (GA) and triethylamine (TEA) is required. A rapid anal. method of quant. ¹H NMR (¹H NMR) for the determination of residues DCU, GA and TEA in medical 4-arm-PEG-SG was established in the present study. The peaks at δ 1.56 (4H, m), δ 2.71 (4H, t, J = 6.7 Hz), and δ 2.42 (6H, q, J = 7.2 Hz) were selected for quantifying DCU, GA and TEA, resp., with deuterated pyridine as the solvent and tetramethylsilane as the internal standard The ¹H NMR assay was validated by several exptl. parameters including specificity, linearity, accuracy, precision, robustness, limit of detection (LOD), limit of quantification (LOQ) and stability. The average recoveries obtained were in the range of 99.48-102.02% for all three residues. Compared with the HPLC and GC approaches, the proposed ¹H NMR method proved to be a powerful tool for quantification due to its unique advantages of simplicity, rapidity and high robustness, especially not requiring standard compounds for calibration curve preparation In the experiment, the researchers used many compounds, for example, 1,3-Dicyclohexylurea (cas: 2387-23-7Application In Synthesis of 1,3-Dicyclohexylurea).

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. 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.Application In Synthesis of 1,3-Dicyclohexylurea

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

Neuroprotective Effects of Cannabidiol but Not Δ9-Tetrahydrocannabinol in Rat Hippocampal Slices Exposed to Oxygen-Glucose Deprivation: Studies with Cannabis Extracts and Selected Cannabinoids was written by Landucci, Elisa;Mazzantini, Costanza;Lana, Daniele;Davolio, Pier Luigi;Giovannini, Maria Grazia;Pellegrini-Giampietro, Domenico E.. And the article was included in International Journal of Molecular Sciences in 2021.SDS of cas: 53902-12-8 This article mentions the following:

Over the past 10 years, a number of scientific studies have demonstrated the therapeutic potential of cannabinoid compounds present in the Cannabis Sativa and Indica plants. However, their role in mechanisms leading to neurodegeneration following cerebral ischemia is yet unclear. We investigated the effects of Cannabis extracts (Bedrocan, FM2) or selected cannabinoids (Δ9-tetrahydrocannabinol (THC), cannabidiol (CBD), and cannabigerol) in rat organotypic hippocampal slices exposed to oxygen-glucose deprivation (OGD), an in vitro model of forebrain global ischemia. Cell death in the CA1 subregion of slices was quantified by propidium iodide fluorescence, and morphol. anal. and tissue organization were examined by immunohistochem. and confocal microscopy. Incubation with the Bedrocan extract or THC exacerbated, whereas incubation with the FM2 extract or cannabidiol attenuated CA1 injury induced by OGD. Δ9-THC toxicity was prevented by CB1 receptor antagonists, the neuroprotective effect of cannabidiol was blocked by TRPV2, 5-HT1A, and PPARγ antagonists. Confocal microscopy confirmed that CBD, but not THC, had a significant protective effect toward neuronal damage and tissue disorganization caused by OGD in organotypic hippocampal slices. Our results suggest that cannabinoids play different roles in the mechanisms of post-ischemic neuronal death. In particular, appropriate concentrations of CBD or CBD/THC ratios may represent a valid therapeutic intervention in the treatment of post-ischemic neuronal death. 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 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. 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

Visible light mediated synthesis of 4-aryl-1,2-dihydronaphthalene derivatives via single-electron oxidation or MHAT from methylenecyclopropanes was written by Liu, Jiaxin;Wei, Yin;Shi, Min. And the article was included in Organic Chemistry Frontiers in 2021.HPLC of Formula: 192436-83-2 This article mentions the following:

A direct single-electron oxidation of methylenecyclopropanes (MCPs) I (R = H, 2-Me, 3-OMe, 4-F, etc.; R¹ = H, 2-Me, 3-Cl, 4-F, etc.) for the rapid construction of 4-aryl-1,2-dihydronaphthalene derivatives II (R² = H, 5-Me, 6-OMe, 7-F, etc.; R³ = H, F) and III (R⁴ = R⁵ = H, F) by merging visible light photoredox catalysis and cobalt catalysis was reported. In MeCN with Et₃N·3HF (1.0 equivalent), the fluorination of MCPs I can be realized in the presence of 9-mesityl-10-methylacridinium perchlorate and Co(dmgH)₂PyCl, affording fluorinated 4-aryl-1,2-dihydronaphthalene derivatives II (R³ = F) in moderate yields. In MeCN/HFIP (7 : 3), 4-aryl-1,2-dihydronaphthalene derivatives II (R³ = H) and III were obtained in good yields through a metal-catalyzed hydrogen atom transfer process under similar conditions. In the experiment, the researchers used many compounds, for example, 4-Bromo-N-methoxy-N-methylbenzamide (cas: 192436-83-2HPLC of Formula: 192436-83-2).

4-Bromo-N-methoxy-N-methylbenzamide (cas: 192436-83-2) 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. 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.HPLC of Formula: 192436-83-2

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

Synthesis and nematicidal activities of 1,2,3-benzotriazin-4-one derivatives containing benzo[d][1,2,3]thiadiazole against Meloidogyne incognita was written by Zhang, Ruifeng;Guo, Wei;Wang, Gaolei;Chen, Xiulei;Li, Zhong;Xu, Xiaoyong. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2020.Application In Synthesis of 2-Amino-4-fluorobenzamide This article mentions the following:

Based on the characteristic of benzo[d][1,2,3]thiadiazole to induce the systemic acquired resistance and improve the immunity of plants, benzo[d][1,2,3]thiadiazole was introduced into 1,2,3-benzotriazin-4-one, thirty-one novel 1,2,3-benzotriazin-4-one derivatives containing benzo[d][1,2,3]thiadiazole were designed and synthesized. Nematicidal activity showed that most of the synthesized compounds exhibited great inhibitory activity in vivo against Meloidogyne incognita at 20 mg/L. Among 31 tested compounds, I and II showed an excellent nematicidal activity with the inhibition rate of 50.4% and 53.1% at the concentration of 1.0 mg/L, resp. The influence of substituent type and position was studied. The relation between structure and activity was also preliminary analyzed. In the experiment, the researchers used many compounds, for example, 2-Amino-4-fluorobenzamide (cas: 119023-25-5Application In Synthesis of 2-Amino-4-fluorobenzamide).

2-Amino-4-fluorobenzamide (cas: 119023-25-5) 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. 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.Application In Synthesis of 2-Amino-4-fluorobenzamide

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