Month: February 2023

The effect of immunosuppressive and anti-inflammatory drugs on monocyte function in vitro was written by Norris, David A.;Weston, William L.;Sams, W. Mitchell Jr.. And the article was included in Journal of Laboratory and Clinical Medicine in 1977.Formula: C20H20N8Na2O5 This article mentions the following:

Monocytes (MNL) cellular chemotaxis, bacterial killing and phagocytosis, and Oil Red O phagocytosis were studied in vitro in the presence of 8 anti-inflammatory or immunosuppressive drugs. Inhibition of Boyden Chamber migration of MNL’s in a MNL-lymphocyte mixture was achieved after 0.5 h incubation by 10-3 and 10-4 mol/L concentrations of chloroquine [54-05-7] (maximum inhibition 63%), dexamethasone [50-02-2] (58%), 6-mercaptopurine [50-44-2] (62%), Na methotrexate [7413-34-5] (66%) , and vinblastine [865-21-4] (100%). Bacterial killing was not significantly affected by any of the drugs studied. Bacterial phagocytosis was improved by vinblastine at 10-3 and 10-4M and by 6-mercaptopurine at 10-5M, but there was apparent interference with the assay at high drug concentrations Modification of the Oil Red O technique showed inhibitions of MNL phagocytosis by vinblastine at 10-3M (69% inhibition), chloroquine at 10-3M (49%), and mercaptopurine at 10-3M (32.5%). Cyclophosphamide [50-18-0], although reported to require hepatic conversion in vivo, may be partially activated in a lymphocyte-MNL mixture in vitro, producing a decrease in cell viability but no statistically significant impairment of MNL function. These results support direct inhibition of MNL cellular function as 1 of the mechanisms of the anti-inflammatory action of chloroquine, dexamethasone, methotrexate, 6-mercaptopurine, and vinblastine. 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: 7413-34-5Formula: C20H20N8Na2O5).

Sodium (S)-2-(4-(((2,4-diaminopteridin-6-yl)methyl)(methyl)amino)benzamido)pentanedioate (cas: 7413-34-5) 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.Formula: C20H20N8Na2O5

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

Mass spectra of N-aryl(arylsulfonyl)-4-aminophenols (-naphthols) was written by Avdeenko, A. P.. And the article was included in Voprosy Khimii i Khimicheskoi Tekhnologii in 1988.COA of Formula: C13H13NO3S This article mentions the following:

The mass spectra of title compounds I (R = Ph, p-tolyl, 2-naphthyl; R¹ = H, Cl, CHMe₂; R² = H, Cl; R³ = H, Me), II (R = H, Me; R¹ = H, SO₂Ph, Cl), and III (R = R¹ = H, Cl; R = Cl, R¹ = H) at 12 and 70 eV were analyzed. The most characteristic decomposition path for the mol. ions of I is ejection of the arylsulfonyl radical. In the experiment, the researchers used many compounds, for example, N-(4-Hydroxyphenyl)-4-methylbenzenesulfonamide (cas: 1146-43-6COA of Formula: C13H13NO3S).

N-(4-Hydroxyphenyl)-4-methylbenzenesulfonamide (cas: 1146-43-6) 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 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.COA of Formula: C13H13NO3S

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

Compensation mechanism for membrane potential against hypoosmotic stress in the Onchidium neuron was written by Nishi, Takako;Sakamoto, Katsuhiko;Matsuo, Ryota. And the article was included in Comparative Biochemistry and Physiology, Part A: Molecular & Integrative Physiology in 2022.Name: 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide This article mentions the following:

The effect of acute hypoosmotic stress on the neural response was investigated using the neurons identified in the abdominal ganglion of the amphibious mollusk Onchidium. The membrane potential of an identified neuron (Ip-1/2) was not significantly altered in 50% hypoosmotic artificial sea water. In isotonic 50% artificial seawater (ASW) with osmolarity that was compensated for using glycerol or urea, the membrane potentials of Ip-1/2 were also not altered compared to those in 50% hypoosmotic ASW. However, hyperpolarization was induced in isotonic 50% ASW when osmolarity was compensated for using sucrose or mannose. In the presence of volume-regulated anion channel (VRAC) inhibitors (niflumic acid and glibenclamide), the Ip-1/2 membrane potentials were hyperpolarized in 50% hypoosmotic ASW. These results suggest that there is a compensatory mechanism involving aquaglyceroporin and VRAC-like channels that maintains membrane potential under hypoosmotic conditions. Here, we detected the expression of aquaglyceroporin mRNA in neural tissues of Onchidium. In the experiment, the researchers used many compounds, for example, 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8Name: 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide).

5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8) 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.Name: 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide

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

Magnesium Aldimines Prepared by Addition of Organomagnesium Halides to 2,4,6-Trichlorophenyl Isocyanide: Synthesis of 1,2-Dicarbonyl Derivatives was written by Schwaerzer, Kuno;Bellan, Andreas;Zoeschg, Maximilian;Karaghiosoff, Konstantin;Knochel, Paul. And the article was included in Chemistry – A European Journal in 2019.Category: amides-buliding-blocks This article mentions the following:

The selective addition of organomagnesium reagents to 2,4,6-trichlorophenyl isocyanide leading to magnesiated aldimines I [R = n-Bu, Ph, Me₂NC₆H₄, etc.] was reported. These aldimines reacted with Weinreb amides, ketones or carbonates to provide the corresponding carbonyl derivatives after acidic cleavage. This allowed for an efficient synthesis of 1,2-dicarbonyl compounds II [R¹ = c-hexyl, Ph, 4-MeOC₆H₄, etc.] and α-hydroxy ketones III [R²R³ = (CH₂)₅, R² = R³ = Ph, R² = c-Pr, R³ = 4-FC₆H₄]. In the experiment, the researchers used many compounds, for example, N-Methoxy-N-methyl-4-(trifluoromethyl)benzamide (cas: 116332-61-7Category: amides-buliding-blocks).

N-Methoxy-N-methyl-4-(trifluoromethyl)benzamide (cas: 116332-61-7) 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 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

Intermolecular cyclotrimerization of haloketoalkynes and internal alkynes: facile access to arenes and phthalides was written by Silvestri, A. P.;Oakdale, J. S.. And the article was included in Chemical Communications (Cambridge, United Kingdom) in 2020.Recommanded Product: 2387-23-7 This article mentions the following:

A highly chemo- and regioselective cyclo(co)trimerization between 3-halopropiolamides RC(O)CCX [R = dimethylaminyl, morpholin-4-yl, 4-(ethoxycarbonyl)piperidin-1-yl, 4-([3-(propan-2-yloxy)propyl]carbamoyl)piperidin-1-yl, etc.; X = H, Br, Cl] and internal alkynes R¹CCR² [R¹ = H, n-Bu, 4-cyanophenyl, thiophen-3-yl, etc.; R² = H, Me, 4-methoxyphenyl, thiophen-3-yl, etc.; R¹R² = -(CH₂)₁₀-] is reported. The reaction is catalyzed by CpRuCl(COD) and proceeds under air at ambient temperature in ethanol with no addnl. precautions. Iodo-, bromo-, and chloropropiolamides, esters, and ketones are viable coupling partners and, in a 2:1 stoichiometry relative to internal alkyne, yield fully-substituted arenes I and II in a single step. The highest regioselectivities (96% single isomer) were observed when employing 2° and 3°-halopropiolamides. A mechanistic hypothesis accounting for this selectivity is proposed. Notably, by using 1,4-butynediol as the internal alkyne, in situ lactonization following [2+2+2]-cycloaddition generates therapeutically-relevant phthalide pharmacophores III directly. In the experiment, the researchers used many compounds, for example, 1,3-Dicyclohexylurea (cas: 2387-23-7Recommanded Product: 2387-23-7).

1,3-Dicyclohexylurea (cas: 2387-23-7) 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. 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.Recommanded Product: 2387-23-7

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

Enantioselective sulfoxide-directed preparation of 1,2-diols from oxalic compounds: formal synthesis of the 10-membered lactone core of ascidiatrienolides and didemnilactones was written by Izzo, Irene;Crumbie, Robin;Solladie, Guy;Hanquet, Gilles. And the article was included in Tetrahedron: Asymmetry in 2005.Synthetic Route of C6H12N2O4 This article mentions the following:

The synthesis of diene I, which is available in both possible absolute configurations is described. This diene constitutes the key intermediate of a previous synthesis of the 10-membered lactone core of the marine natural products ascidiatrienolides and didemnilactones. Intermediate I is available via two successive highly diastereoselective sulfoxide-directed reductions of oxalic diamide II. In the experiment, the researchers used many compounds, for example, N1,N2-Dimethoxy-N1,N2-dimethyloxalamide (cas: 106675-70-1Synthetic Route of C6H12N2O4).

N1,N2-Dimethoxy-N1,N2-dimethyloxalamide (cas: 106675-70-1) 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.Synthetic Route of C6H12N2O4

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

Predicting the Loading Capability of mPEG-PDLLA to Hydrophobic Drugs Using Solubility Parameters was written by Sun, Jiali;Wei, Qi;Shen, Na;Tang, Zhaohui;Chen, Xuesi. And the article was included in Chinese Journal of Chemistry in 2020.Application of 53902-12-8 This article mentions the following:

Summary of main observation and conclusion : Phys. encapsulation of drugs into polymer micelles is a common method of loading hydrophobic drugs. Methoxy polyethylene glycol-poly(D,L-lactide) (mPEG-PDLLA) is one of the most commonly used drug carrier. At present, whether a carrier is suitable for the loading of a certain drug is determined by drug loading experiments This process costs a lot of time. Therefore, an efficient predicting method to avoid time-consuming tests is critical In this study, we prepared mPEG_5k-PDLLA_5k and used it to load a series of drugs. Three parameters were used to test the miscibility of mPEG_5k-PDLLA_5k with drugs, including absolute difference in Hildebrand solubility parameters (|Δδ|), Flory-Huggins interaction parameter (Χ) and the distance (D value) calculated from the two-dimensional solubility parameters. We found the two-dimensional solubility parameters obtained from JB2013 group contribution (GC) method was useful. By comparing the drug loading content (DLC) with the D value, we found that when the D value was less than 5.0 (MJ/m³)^1/2, the miscibility of drug and mPEG_5k-PDLLA_5k was good and drug loading capability was high; when the D value was more than 8.0 (MJ/m³)^1/2, the drug was barely loaded. Thus, this work provided a rationale to qual. predict the loading capability of mPEG_5k-PDLLA_5k for hydrophobic drugs. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8Application of 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 freed from solvent or water by drying below their melting points. These purifications can also be used for sulfonamides and acid hydrazides.Application of 53902-12-8

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

Transamidation of primary amides with amines catalyzed by zirconocene dichloride was written by Atkinson, Benjamin N.;Chhatwal, A. Rosie;Lomax, Helen V.;Walton, James W.;Williams, Jonathan M. J.. And the article was included in Chemical Communications (Cambridge, United Kingdom) in 2012.Application of 61189-99-9 This article mentions the following:

Zirconocene dichloride has been shown to be an effective catalyst for the transamidation of primary amides with amines in cyclohexane at 80° in 5-24 h. For favorable substrates, the reaction can be performed at temperatures as low as 30°. In the experiment, the researchers used many compounds, for example, 2,2-Diethoxyacetamide (cas: 61189-99-9Application of 61189-99-9).

2,2-Diethoxyacetamide (cas: 61189-99-9) 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 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 61189-99-9

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

Copper-Catalyzed Reactions of Alkenyl Boronic Esters via Chan-Evans-Lam Coupling/Annulation Cascades: Substrate Selective Synthesis of Dihydroquinazolin-4-ones and Polysubstituted Quinolines was written by Li, Yuge;Cao, Zifeng;Wang, Zhijun;Xu, Liang;Wei, Yu. And the article was included in Organic Letters in 2022.COA of Formula: C7H7FN2O This article mentions the following:

Copper-catalyzed cascade cyclization reactions between alkenyl boronic esters BpinC(R)=CH(R¹) [R = H, Me; R¹ = Me; RR¹ = -(CH₂)₅-, -(CH₂)₂O(CH₂)₂-, -(CH₂)₂N(C(O)Ot-Bu)(CH₂)₂-] and N-H-based nucleophiles R²C(O)NHR³ (R² = 2-amino-5-fluorophenyl, 2-amino-3-bromophenyl, 2-aminophenyl, etc.; R³ = H, Me, Ph, Bn, etc.) have been established, providing new approaches for one-pot assembly of azacycles. Following the Chan-Evans-Lam C-N couplings, the cyclization processes occur via divergent pathways based on the utilized substrates, affording hydroamination product dihydroquinazolin-4-ones I (R⁴ = H, 6-Me, 8-Br, 7-F, etc.) or aromatization product quinolines II (R⁵ = Ph, 4-chlorophenyl, Me, etc.; X = H, Cl, Br, F). Via this one-pot C-N coupling/annulation cascade, the target substituted azacycles can be obtained in moderate to good yields in each case. In the experiment, the researchers used many compounds, for example, 2-Amino-4-fluorobenzamide (cas: 119023-25-5COA of Formula: C7H7FN2O).

2-Amino-4-fluorobenzamide (cas: 119023-25-5) 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. 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.COA of Formula: C7H7FN2O

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

The Effect of Tranilast 8% Liposomal Gel Versus Placebo on Post-Cesarean Surgical Scars: A Prospective Double-Blind Split-Scar Study was written by Kohavi, Libi;Sprecher, Eli;Zur, Eyal;Artzi, Ofir. And the article was included in Dermatologic Surgery in 2017.Related Products of 53902-12-8 This article mentions the following:

Background: Tranilast (N-[3, 4-dimethoxycinnamoyl] anthranilic acid), an antiallergic drug, has been shown to attenuate scar formation possibly through inhibition of transforming growth factor beta 1 activity and consequent suppression of collagen synthesis in fibroblasts. Objective: The authors aimed at evaluating the efficacy and safety of tranilast 8% gel in improving the appearance and symptoms of new post-cesarean section surgical wounds. Methods: In this prospective double-blind split-scar study, the authors treated each half scar of 26 women with either tranilast 8% liposomal gel or tranilast-free liposomal gel (placebo). Treatment was applied twice daily for 3 mo. Twenty women completed the trial. Scar halves were evaluated by 2 investigators and by the patients 9 mo after the last application using the Patient and Observer Scar Assessment Scale (POSAS). The participants also rated overall satisfaction and recorded side effects of the treatment. Results: The mean POSAS scores at 9 mo post-treatment were significantly lower for tranilast-treated half scars compared with placebo-treated half scars (p < .001). The women were significantly more satisfied with the tranilast-treated half-scar appearance (p = .002). Three participants reported itching and erythema on the tranilast-treated side. Conclusion: Topical tranilast 8% gel provided significantly better post cesarian section scar cosmesis and user satisfaction compared with placebo. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8Related Products of 53902-12-8).

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

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