Category: amides-buliding-blocks

Some reactions of substituted 2-bromopyridines was written by Berrie, A. H.;Newbold, G. T.;Spring, F. S.. And the article was included in Journal of the Chemical Society in 1952.Recommanded Product: 3-Aminopicolinamide This article mentions the following:

2-Hydroxy-3-nitropyridine (I) (14 g.), added to 50 g. PBr₃ and 16 g. Br, heated 5 hrs. at 100°, cooled, treated dropwise with 100 cc. MeOH and then with 300 cc. H₂O, and extracted with boiling C₆H₆ and the residue from the C₆H₆ extracted with petr. ether (b. 60-80°), gives 10 g. 2-bromo-3-nitropyridine (II), m. 125°; the 5-Cl derivative of I yields 59% of the 5-Cl derivative (III) of II, m. 75°; the 5-Br derivative of I gives 80% of 2,5-dibromo-3-nitropyridine (IV), m. 93°. II (1 g.) and 10 cc. conductivity HCl in 10 cc. AcOH, refluxed 3 hrs., give 0.5 g. 2-hydroxy-3-nitropyridine (V), pale yellow, m. 224°; III yields 54% of the 5-Cl derivative (VI) of V, yellow, m. 235°; IV, HCl, and AcOH give 64% of the 5-Br derivative (VII) of V, pale yellow, m. 242°; 10 g. 2-amino-5-bromo-3-nitropyridine (VIII) in 25 cc. H₂SO₄ (d. 1.84) at 0°, treated with 6 g. NaNO₂ in 15 cc. H₂O, kept 30 min. at 0°, and diluted with 150 cc. H₂O, gives 6.05 g. VII. V (0.7 g.), 2 g. PCl₅, and 1.5 cc. POCl₃, heated 2 hrs. at 100°, give 0.2 g. 2-chloro-3-nitropyridine (IX), m. 101°; VI gives 52% 2,5-dichloro-3-nitropyridine (X), m. 43°; X results in 1.3 g. yield from 2-amino-5-chloro-3-nitropyridine. VII, PCl₅, and POCl₃ give 45% 5-bromo-2-chloro-3-nitropyridine (XI), m. 68° (51% from VIII). II (0.75 g.) and 0.7 g. CuCN, gradually heated to 150°, the pressure reduced to 1 mm., and the heat source removed after 15 sec., give 0.3 g. 3-nitropicolinonitrile (XII), m. 78°; III yields the 5-Cl derivative (XIII) of XII, m. 98°. IV gives 66% of the 5-Br derivative (XIV) of XII, m. 102°. 3-Amino-2-bromopyridine yields 32% 3-aminopicolinonitrile (XIVA), m. 149°; 5-Cl derivative (XIVB), m. 175°, 25%. XII (100 mg.) and 0.2 cc. H₂SO₄ (d. 1.84), heated 2 hrs. at 100°, give 50 mg. 3-nitropicolinamide (XV), m. 211°; XIII yields 55% of the 5-Cl derivative of XV, m. 230° and XIV gives-56% of the 5-Br derivative (XVA), m. 232-3° (decompn). II (1.45 g.), 2 g. Fe filings, and 12 cc. AcOH, heated 2 hrs. at 100°, diluted with 15 cc. H₂O, basified with 30% NaOH, and the cooled product extracted with CHCl₃, give 0.8 g. 3-amino-2-bromopyridine (XVI), m. 79°; 1.1 g. III yields 0.1 g. of the 2-Cl analog (XVII) of XVI, m. 79-80°; 1 g. XVI in 10 cc. HCl (d. 1.19), refluxed 3 hrs., gives 0.5 g. XVII. XV (20 mg.), 20 mg. Fe filings, and 0.12 cc. AcOH, heated 2 hrs. at 100°, give 10 mg. 3-aminopicolinamide (XVIII), m. 175-7°, sublimes at 100°/10^-1 mm.; 120 mg. XIVA and 0.24 g. concentrated H₂SO₄, heated 2 hrs. at 100°, give 10 mg. XVIII. XIII, reduced in AcOH with Fe, gives 67% of the 5-Cl derivative (XIX) of XVIII, m. 168°; XIVB yields 11% XIX; 5-Br derivative of XVIII, m. 168°, 72 and 18% yield, resp. XI gives 81% 3-amino-2-bromo-5-chloropyridine (XX), m. 142°, absorption maximum at 2520 and 3140 A. (ε 11,500 and 5700); IV gives 84% 3-amino-2,5-dibromopyridine (XXI), m. 153°; 2,5-di-Cl analog, m. 129°; it results in 87% on reduction of X and in 0.2-g. yield on refluxing 2 hrs. 0.5 g. 3-amino-5-bromo-2-chloropyridine (XXII) in 10 cc. concentrated HCl. Reduction of XI with Fe in AcOH gives 85% XXII, m. 131°, absorption maximum at 2510 and 3140 A. (ε 7200 and 4700); 1 part XXI and 20 parts concentrated HCl, refluxed 2 hrs., give 35% XXII; 2.82 g. IV, 7 g. Sn, and 30 cc. HCl, refluxed until solution results, give 0.2 g. XXII. 2-Amino-5-bromo-3-nitropyridine, reduced with Sn and HCl, gives 21% 2,3-diamino-5-bromo-4(6)-chloropyridine, m. 164° (quinoxaline derivative from phenanthraquinone, C₁₉H₉N₃ClBr, m. 270-2°). XXII (0.3 g.) in 10 cc. concentrated HCl, treated at 0° with 0.55 g. NaNO₂ in 1.5 cc. H₂O and then with 1.1 g. Cu, shaken 1 hr., almost neutralized with 30% NaOH, and the precipitate extracted with Me₂CO and the residue from the Me₂CO extracted with petr. ether, gives 100 mg. 5-bromo-2,3-dichloropyridine, m. 30-1°. XXI (1.26 g.) with NaNO₂ in concentrated H₂SO₄ gives 0.6 g. 2,5-dibromo-3-hydroxypyridine, m. 195-7°. XVA (12.1 g.) and KOBr give 7 g. 2-amino-5-bromo-3-nitropyridine, yellow, m. 205°. In the experiment, the researchers used many compounds, for example, 3-Aminopicolinamide (cas: 50608-99-6Recommanded Product: 3-Aminopicolinamide).

3-Aminopicolinamide (cas: 50608-99-6) 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 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.Recommanded Product: 3-Aminopicolinamide

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

Antiallergic Properties of Biflavonoids Isolated from the Flowers of Mesua ferrea Linn. was written by Manse, Yoshiaki;Sakamoto, Yusuke;Miyachi, Taiki;Nire, Mitsuyo;Hashimoto, Yoshinori;Chaipech, Saowanee;Pongpiriyadacha, Yutana;Morikawa, Toshio. And the article was included in Separations in 2022.Recommanded Product: 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid This article mentions the following:

The methanolic extract from the flowers of Mesua ferrea Linn. (Calophyllaceae) showed significant hyaluronidase inhibitory activity. Following a bioassay-guided separation of the extract, two biflavonoids, viz., mesuaferrone-A (1) and mesuaferrone-B (2), were isolated, along with ten flavonoids (3-12), two xanthones (13 and 14), three triterpenes (15-17), a phenylpropanoid (18), and five aromatics (19-24). Among the isolates, 1 and 2 (IC₅₀ = 51.1μM and 54.7μM, resp.) exhibited hyaluronidase inhibitory activity equivalent to that of the com. available antiallergic agents disodium cromoglycate (64.8μM) and ketotifen fumarate (76.5μM). These biflavonoids (1 and 2) are 8-8″ linked dimers that are composed of naringenin (1a) or apigenin (3), with their corresponding monomers lacking inhibitory activity (IC₅₀ > 300μM). In addition, 1 and 2 (IC₅₀ = 49.4μM and 49.2μM, resp.) inhibited the release of β-hexosaminidase, which is a marker of antigen-IgE-mediated degranulation, in rat basophilic leukemia (RBL-2H3) cells. These inhibitory activities were more potent than those of the antiallergic agents tranilast and ketotifen fumarate (IC₅₀ = 282μM and 158μM, resp.), as well as one of the corresponding monomers (1a; IC₅₀ > 100μM). Nonetheless, these effects were weaker than those of the other monomer (3; IC₅₀ = 6.1μM). In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8Recommanded Product: 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid).

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 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.Recommanded Product: 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid

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

Iridium-catalyzed C-H methylation and d₃-methylation of benzoic acids with application to late-stage functionalizations was written by Weis, Erik;Hayes, Martin A.;Johansson, Magnus J.;Martin-Matute, Belen. And the article was included in iScience in 2021.Electric Literature of C18H17NO5 This article mentions the following:

An iridium-catalyzed carboxylate-directed ortho C-H methylation and d₃-methylation of benzoic acids was reported. The method used com. available reagents and precatalyst and requires no inert atm. or exclusion of moisture. Substrates bearing electron-rich and electron-poor groups were successfully methylated, including compounds with competing directing/coordinating groups. The method was also applied to the LSF of several marketed drugs, forming analogs with increased metabolic stability compared with the parent drug. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8Electric Literature of C18H17NO5).

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 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.Electric Literature of C18H17NO5

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

Metformin effect in models of inflammation is associated with activation of ATP-dependent potassium channels and inhibition of tumor necrosis factor-α production was written by Augusto, Paulo S. A.;Matsui, Tamires C.;Braga, Alysson V.;Rodrigues, Felipe F.;Morais, Marcela I.;Dutra, Marcela M. G. B.;Batista, Carla R. A.;Melo, Ivo S. F.;Costa, Sarah O. A. M.;Bertollo, Caryne M.;Coelho, Marcio M.;Machado, Renes R.. And the article was included in Inflammopharmacology in 2022.Category: amides-buliding-blocks This article mentions the following:

Metformin is an oral hypoglycemic drug widely used in the management of type 2 diabetes mellitus. We have recently demonstrated that metformin exhibits activity in models of nociceptive and neuropathic pain. However, little is known about its effects in exptl. models of inflammation and inflammatory pain. Thus, the present study aimed to evaluate the activity of metformin in exptl. models of inflammation and inflammatory pain in mice, as well as the underlying mechanisms. Previous (1 h) per os (p.o.) administration of metformin (250, 500 or 1000 mg/kg) inhibited the mech. allodynia and paw edema induced by intraplantar (i.pl.) injection of carrageenan (600μg) and also the pleurisy induced by this stimulus (200μg, intrapleural). In the model of mech. allodynia and paw edema induced by carrageenan, metformin also exhibited activity when administered after (1 h) the inflammatory stimulus. Metformin (1000 mg/kg) reduced the production of tumor necrosis factor-α induced by i.pl. injection of carrageenan. Metformin antiallodynic effect was not affected by previous administration of naltrexone (5 or 10 mg/kg, i.p.) or cyproheptadine (5 or 10 mg/kg, p.o). However, this effect was abolished by previous administration of glibenclamide (20 or 40 mg/kg, p.o). In conclusion, the results demonstrate the activity of metformin in models of inflammation and inflammatory pain. In addition, the results indicate that the activity of metformin may be mediated by activation of ATP-sensitive potassium channels and reduction of production of inflammatory mediators. Altogether, these results stimulate the conduction of studies aiming to evaluate whether metformin may be repositioned in the treatment of patients with painful and inflammatory disorders. In the experiment, the researchers used many compounds, for example, 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8Category: amides-buliding-blocks).

5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8) 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′Râ€? or, equivalently, an acyl (alkanoyl) group RC(=O)âˆ?joined to an amine group. The presence of the amide group –C(=O)Nâ€?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 cmâˆ?. 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.Category: amides-buliding-blocks

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

The investigation of oxidative bleaching performance of peripherally Schiff base substituted tri-nuclear cobalt-phthalocyanine complexes was written by Sen, Pinar;Yildiz, S. Zeki. And the article was included in Inorganica Chimica Acta in 2017.Name: N,N-(Ethane-1,2-diyl)bis(N-acetylacetamide) This article mentions the following:

This study covers the functional complexes of tetrakis [4-(salicylhydrazone)phenoxy] phthalocyaninato cobalt (II) (5) which was the macro mol. Schiff base ligand and synthesized through a multistep reaction sequence starting first with the cyclotetramerization of 4-[4-(1,3-Dioxolan-2-yl)phenoxy]-phthalonitrile (2). Then, the de-protection of tetra acetal groups of Tetrakis[4-(1,3-dioxolan-2-yl)phenoxy]phthalocyaninato cobalt (II) (3) to the aldehyde functionality in acetic acid/FeCl₃ system to yield the Tetrakis(4-formylphenoxy)phthalocyaninato cobalt(II) (4) and then its condensation with salicylhydrazide gave to 5. Finally, CoPc-bis(salicylhydrazone)phenoxymanganese (III) (6), CoPc-bis(salicylhydrazone) phenoxycobalt(III) (7) and CoPc-bis (salicylhydrazone)phenoxy nickel(II) (8) were synthesized using with the related MnCl₂·4H₂O, CoCl₂·6H₂O, Ni(CH₃COO)₂ salt in basic conditions in DMF. FTIR, UV-visible, MS spectra and elemental anal. were applied to characterize to prepared compounds The bleaching performances of the prepared phthalocyanine compounds (3–8) were examined by the degradation of Morin as the hydrophilic dye which characterized the wine stains on the fabrics. Progress of the degradations in the catalysts (3–8)/H₂O₂ combination in basic aqueous solution conditions was investigated by using online spectrophotometric method (OSM). The prepared catalysts showed better bleaching performance at 25° than to that of tetraacetylethylenediamine (TAED) bleach activator com. used in powder detergent formulations. In the experiment, the researchers used many compounds, for example, N,N-(Ethane-1,2-diyl)bis(N-acetylacetamide) (cas: 10543-57-4Name: N,N-(Ethane-1,2-diyl)bis(N-acetylacetamide)).

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. 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: N,N-(Ethane-1,2-diyl)bis(N-acetylacetamide)

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

Hydrolysis of naptalam and structurally related amides: inhibition by dissolved metal ions and metal (hydr)oxide surfaces was written by Huang, Ching-Hua;Stone, Alan T.. And the article was included in Journal of Agricultural and Food Chemistry in 1999.Synthetic Route of C11H15NO2 This article mentions the following:

In metal ion-free solutions, the secondary amide naptalam hydrolyzes more rapidly as the pH is decreased; intramol. nucleophilic attack by a carboxylate side group is very likely involved. Millimolar levels of dissolved Cu^II and Zn^II inhibit hydrolysis between pH 3.6 and pH 6.5. Metal ion-naptalam complex formation is important since addition of the competitive ligand citrate lessens the inhibitory effect. The metal (hydr)oxide surfaces Al₂O₃ and FeOOH inhibit naptalam hydrolysis to a lesser degree; inhibition is proportional to the extent of naptalam adsorbed. Secondary amides (propanil, salicylanilide, and N-1-naphthylacetamide) and tertiary amides (N-methyl-N-1-naphthylacetamide, furalaxyl, and N,N-diethylsalicylamide) that lack carboxylate side groups do not hydrolyze within 45 days of reaction, even when millimolar Cu^II concentrations are present. Tertiary amides possessing carboxylate side groups (N,N-diethyl-3,6-difluorophthalamic acid and N,N-dimethylsuccinamic acid) do hydrolyze but are insensitive to the presence or absence of Cu^II. The inhibitory effect is believed to occur via metal coordination of (1) the carbonyl group of naptalam, which induces deprotonation of the amide group and makes the substrate less reactive toward nucleophilic attack; (2) the free carboxylate group of naptalam, which blocks intramol. nucleophilic attack; or (3) a combination of the two. In the experiment, the researchers used many compounds, for example, N,N-Diethylsalicylamide (cas: 19311-91-2Synthetic Route of C11H15NO2).

N,N-Diethylsalicylamide (cas: 19311-91-2) 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. 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 C11H15NO2

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

Improved chromatographic method for purification of lactoperoxidase from different milk sources was written by Koksal, Zeynep;Usanmaz, Hande;Bayrak, Songul;Ozdemir, Hasan. And the article was included in Preparative Biochemistry & Biotechnology in 2017.Application of 53297-70-4 This article mentions the following:

Our previous studies showed that sulfanilamide is a new competitive inhibitor of and can be used in the purification of lactoperoxidase (LPO, EC1.11.1.7) from milk. However, this method has some disadvantages like a lower purification factor. The aim of the present study is to improve the purification process of milk LPO from different sources. For this purpose, 16 com. sulfanilamide derivatives were selected for inhibition studies to determine the best inhibitor of bovine LPO by calculating kinetic parameters. A cyanogen bromide-activated Sepharose 4B affinity matrix was synthesized by coupling with each competitive inhibitor. Among the inhibitors, 5-amino-2-methylbenzenesulfonamide and 2-chloro-4-sulfamoylaniline were used as ligands for the purification of LPO from bovine, buffalo, cow, and goat milks with 1059.37, 509.09, 232.55, and 161.90, and 453.12-, 151.86-, 869.00-, and 447.57-fold, resp. Our results show that 5-amino-2-methylbenzenesulfonamide, 2-chloro-4-sulfamoylaniline, and 5-amino-1-naphthalenesulfonamide are the best inhibitors for one-step purification of the enzyme. In the experiment, the researchers used many compounds, for example, 4-Amino-3-methylbenzenesulfonamide (cas: 53297-70-4Application of 53297-70-4).

4-Amino-3-methylbenzenesulfonamide (cas: 53297-70-4) 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)Nâ€?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 cmâˆ?. 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.Application of 53297-70-4

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

High-performance liquid chromatographic control of drugs containing caffeine was written by Alary, J.;Vergnes, M. F.. And the article was included in Annales Pharmaceutiques Francaises in 1984.Category: amides-buliding-blocks This article mentions the following:

Pharmaceutical dosage forms containing caffeine (I) [58-08-2] and other drugs were analyzed by reversed-phase HPLC. All the dosage forms except the oral solutions were extracted with CHCl₃ or water and I was determined at 273 nm. The mobile phase was a mixture of MeCN-HOAc (either 10:90 or 50:50). The other drugs were detected either at 273 nm or other wavelengths. The oral solutions were measured directly. The recovery was 98-100%. The method is applicable to various pharmaceutical forms. In the experiment, the researchers used many compounds, for example, N,N-Diethylsalicylamide (cas: 19311-91-2Category: amides-buliding-blocks).

N,N-Diethylsalicylamide (cas: 19311-91-2) 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.Category: amides-buliding-blocks

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

The Discovery of Novel ACA Derivatives as Specific TRPM2 Inhibitors that Reduce Ischemic Injury Both In Vitro and In Vivo was written by Zhang, Han;Yu, Peilin;Lin, Hongwei;Jin, Zefang;Zhao, Siqi;Zhang, Yi;Xu, Qingxia;Jin, Hongwei;Liu, Zhenming;Yang, Wei;Zhang, Liangren. And the article was included in Journal of Medicinal Chemistry in 2021.HPLC of Formula: 13255-50-0 This article mentions the following:

The transient receptor potential melastatin 2 (TRPM2) channel is associated with ischemia/reperfusion injury, inflammation, cancer, and neurodegenerative diseases. However, the limit of specific inhibitors impedes the development of TRPM2-targeted therapeutic agents. To discover more potent and selective TRPM2 inhibitors, 59 N-(p-amylcinnamoyl) anthranilic acid (ACA) derivatives were synthesized and evaluated using calcium imaging and electrophysiol. approaches. Systematic structure-activity relationship studies resulted in some potent compounds inhibiting the TRPM2 channel with sub-micromolar half-maximal inhibitory concentration values. Among them, the preferred compound A23 (I) exhibited TRPM2 selectivity over TRPM8 and TRPV1 channels as well as phospholipase A2 and showed neuroprotective activity in vitro. Following pharmacokinetic studies, I was further evaluated in a transient middle cerebral artery occlusion model in vivo, which significantly reduced cerebral infarction. These data indicate that A23 might serve as a useful tool for TRPM2-related research as well as a lead compound for the development of therapeutic agents for ischemic injury. In the experiment, the researchers used many compounds, for example, 4-Formyl-N-isopropylbenzamide (cas: 13255-50-0HPLC of Formula: 13255-50-0).

4-Formyl-N-isopropylbenzamide (cas: 13255-50-0) 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)Nâ€?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 cmâˆ?. 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.HPLC of Formula: 13255-50-0

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

Neuroprotective effects of Lasmiditan and Sumatriptan in an experimental model of post-stroke seizure in mice: Higher effects with concurrent opioid receptors or K_ATP channels inhibitors was written by Shayan, Maryam;Eslami, Faezeh;Amanlou, Arash;Solaimanian, Shahabaddin;Rahimi, Nastaran;Rashidian, Amir;Ejtemaei-Mehr, Shahram;Ghasemi, Mehdi;Dehpour, Ahmad-Reza. And the article was included in Toxicology and Applied Pharmacology in 2022.Electric Literature of C23H28ClN3O5S This article mentions the following:

Early post-stroke seizure frequently occurs in stroke survivors within the first few days and is associated with poor functional outcomes. Therefore, efficient treatments of such complications with less adverse effects are pivotal. In this study, we investigated the possible beneficial effects of lasmiditan and sumatriptan against post-stroke seizures in mice and explored underlying mechanisms in their effects. Stroke was induced by double ligation of the right common carotid artery in mice. Immediately after the ligation, lasmiditan (0.1 mg/kg, i.p. [i.p.]) or sumatriptan (0.03 mg/kg, i.p.) were administered. Twenty-four hours after the stroke induction, seizure susceptibility was evaluated using the pentylenetetrazole (PTZ)-induced clonic seizure model. In sep. experiments, naltrexone (a non-specific opioid receptor antagonist) and glibenclamide (a K_ATP channel blocker) were administered 15 min before lasmiditan or sumatriptan injection. To evaluate the underlying signaling pathways, ELISA anal. of inflammatory cytokines (TNF-α and IL-1β) and western blot anal. of anti- and pro-apoptotic markers (Bcl-2 and Bax) were performed on mice isolated brain tissues. Lasmiditan (0.1 mg/kg, i.p.) and sumatriptan (0.03 mg/kg, i.p.) remarkably decreased seizure susceptibility in stroke animals by reducing inflammatory cytokines and neuronal apoptosis. Concurrent administration of naltrexone (10 mg/kg, i.p.) or glibenclamide (0.3 mg/kg, i.p.) with lasmiditan or sumatriptan resulted in a higher neuroprotection against clonic seizures and efficiently reduced the inflammatory and apoptotic markers. Lasmiditan and sumatriptan significantly increased post-stroke seizure thresholds in mice by suppressing inflammatory cytokines and neuronal apoptosis. Lasmiditan and sumatriptan seem to exert higher effects on seizure threshold with concurrent administration of the opioid receptors or K_ATP channels modulators. In the experiment, the researchers used many compounds, for example, 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8Electric Literature of C23H28ClN3O5S).

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. 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.Electric Literature of C23H28ClN3O5S

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