Author: Jessica.F

Micovic, Tijana published the artcileIn vitro, in vivo and in silico evaluation of the anti-inflammatory potential of Hyssopus officinalis L. subsp. aristatus (Godr.) Nyman (Lamiaceae), Recommanded Product: 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, the publication is Journal of Ethnopharmacology (2022), 115201, database is CAplus and MEDLINE.

Medicinal properties of hyssop have been used in traditional medicine since ancient times, inter alia, in diseases/conditions with an inherent inflammatory process. Aim of the study: Accordingly, the aim of this study was to investigate the anti-inflammatory properties of hyssop herb preparations (essential oil and methanol extracts) in vivo, in vitro and in silico. For in vitro testing of essential oils and extracts of hyssop herb, the cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) enzyme assays were used. In vivo anti-inflammatory potential of the extracts (at doses of 50, 100 and 200 mg/kg) was assessed using the carrageenan-induced rat paw edema test. Mol. docking and dynamics were used for in silico testing of the inhibitory activity of chlorogenic (CA) and rosmarinic (RA) acids, as the dominant compounds in the tested methanol extracts against COX-1 and COX-2 enzymes. Significant inhibitory activity was shown in the COX-2 test regarding extracts (essential oils did not exhibit any significant activity). Namely, all analyzed extracts, at a concentration of 20μg/mL, showed a percentage of inhibition of COX-2 enzyme (54.04-63.04%), which did not indicate a statistically significant difference from the pos. control of celecoxib (61.60%) at a concentration of 8.8μM. In vivo testing showed that all methanol extracts of hyssop herb, at the highest test dose of 200 mg/kg in the third and fourth hours, after carrageenan administration, exhibited a statistically significant (p < 0.05) inhibitory effect on the increase in rat paw edema in relation to control. This activity is comparable or higher in relation to the reference substance, indomethacin, at a concentration of 8 mg/kg. The preliminary in silico results suggest that investigated compounds (RA and CA) showed better inhibitory activity against COX-1 and COX-2 than standard non-steroidal anti-inflammatory drug (NSAID), ibuprofen, as evident from the free binding energy (δGbind in kJ mol^-1). The binding energies of the docked compounds to COX-1 and -2 were found to be in the range between -47.4 and -49.2 kJ mol^-1. Ibuprofen, as the one NSAID, for the same receptors targets, showed remarkably higher binding energy (ΔG_bind = -31.3 kJ mol^-1 to COX-1, and ΔG_bind = -30.9 kJ mol^-1 to COX-2). The results obtained not only support the traditional use of hyssop herb in inflammatory conditions in folk medicine, but also open the door to and the need for further in vivo testing of extracts in order to examine the mol. mechanism of anti-inflammatory activity in living systems and possibly develop a new anti-inflammatory drug or supplement.

Journal of Ethnopharmacology published new progress about 169590-42-5. 169590-42-5 belongs to amides-buliding-blocks, auxiliary class Sulfamide,Immunology/Inflammation,COX, name is 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, and the molecular formula is C17H14F3N3O2S, Recommanded Product: 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Beletskiy, Evgeny V. published the artcileSelective binding and extraction of aqueous dihydrogen phosphate solutions via three-armed thiourea receptors, Related Products of amides-buliding-blocks, the publication is Organic & Biomolecular Chemistry (2015), 13(38), 9844-9849, database is CAplus and MEDLINE.

A series of neutral anion receptors with one to three thiourea arms were synthesized and their binding to tetrabutylammonium chloride, acetate, and dihydrogen phosphate salts in aqueous DMSO mixtures was examined The three-armed thiourea host was found to strongly and selectively bind H₂PO₄^– even in DMSO solutions containing up to 30% water. This enabled the dihydrogen phosphate salt to be extracted from water into chloroform in its dibasic form despite the high heat of the hydration of HPO₄^2-.

Organic & Biomolecular Chemistry published new progress about 146140-95-6. 146140-95-6 belongs to amides-buliding-blocks, auxiliary class Boronic acid and ester,Amine,Benzene,Amide,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (2-Pivalamidophenyl)boronic acid, and the molecular formula is C11H16BNO3, Related Products of amides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Stockmann, Vegar published the artcileStudies on reactive pyridylketones formed by Weinreb transformations, Application of N-Methoxy-N-methylisonicotinamide, the publication is Journal of Heterocyclic Chemistry (2012), 49(3), 613-620, database is CAplus.

A method was developed to allow the preparation of reactive pure vinyl pyridyl ketones and activated vinyl ketones, in general, to be used in further reactions, such as cycloadditions The process is based on the Weinreb’s amide transformation and includes a quaternary ammonium intermediate and subsequent elimination. Addnl., based on the authors’ previous results on the malonate alkylation of 3-nitropyridines and subsequent synthetic applications, they present studies on the transformation of Me 4-(methoxycarbonyl)-3-pyridineacetate via the corresponding Weinreb amide and reactive methylpyridyl- and allyl pyridyl ketones into isoquinoline derivatives

Journal of Heterocyclic Chemistry published new progress about 100377-32-0. 100377-32-0 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is N-Methoxy-N-methylisonicotinamide, and the molecular formula is C6H3ClFNO2, Application of N-Methoxy-N-methylisonicotinamide.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Piskov, V. B. published the artcileConversion of carboxylic acids to amides, Related Products of amides-buliding-blocks, the publication is Zhurnal Prikladnoi Khimii (Sankt-Peterburg, Russian Federation) (1973), 46(1), 220-1, database is CAplus.

Pelargonic, lauric, and (10) benzoic acid derivatives were converted to the resp. amides (≤99%) by heating with ≥2 equivalent of H2NSO3H in oleum or polyphosphoric acid at 100-20°; 3-02NC6H4CO2H and MeNHSO3H gave 89% 3-O2NC6H4CONHMe under similar conditions.

Zhurnal Prikladnoi Khimii (Sankt-Peterburg, Russian Federation) published new progress about 2447-79-2. 2447-79-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Benzene,Amide, name is 2,4-Dichlorobenzamide, and the molecular formula is C7H5Cl2NO, Related Products of amides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Sathe, Pratima A. published the artcileTandem synthesis of aromatic amides from styrenes in water, SDS of cas: 2447-79-2, the publication is Tetrahedron Letters (2018), 59(29), 2820-2823, database is CAplus.

An expedient one-pot synthesis of aromatic amides from styrenes in the presence of N-bromosuccinimide and iodine by using aqueous ammonia in water is reported. The reaction proceeds through the formation of a α-bromoketone as an intermediate in the presence of NBS and water. The α-bromoketone on reaction with iodine forms bromodiiodoketone which on nucleophilic substitution with aqueous ammonia gives aromatic amide. Substituted aromatic amides were obtained in good yields with wide functional group compatibility.

Tetrahedron Letters published new progress about 2447-79-2. 2447-79-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Benzene,Amide, name is 2,4-Dichlorobenzamide, and the molecular formula is C7H5Cl2NO, SDS of cas: 2447-79-2.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Krajsovszky, Gabor published the artcileSuzuki-aza-Wittig, Suzuki-condensation and aza-Wittig-electrocyclic ring-closure tandem reactions for synthesis of fused nitrogen-containing ring systems, Recommanded Product: (2-Pivalamidophenyl)boronic acid, the publication is ARKIVOC (Gainesville, FL, United States) (2011), 229-253, database is CAplus.

Tandem combinations of Suzuki-aza-Wittig, Suzuki-condensation, and aza-Wittig-electrocyclic ring closure reactions for the synthesis of new pyridazino[4,5-c]isoquinolinone, pyridazino[4,5-c]quinolinone, and pyrimido[5,4-c]quinoline derivatives were described.

ARKIVOC (Gainesville, FL, United States) published new progress about 146140-95-6. 146140-95-6 belongs to amides-buliding-blocks, auxiliary class Boronic acid and ester,Amine,Benzene,Amide,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (2-Pivalamidophenyl)boronic acid, and the molecular formula is C11H16BNO3, Recommanded Product: (2-Pivalamidophenyl)boronic acid.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Paulsen, Marianne H. published the artcileAn amphipathic cyclic tetrapeptide scaffold containing halogenated β^2,2-amino acids with activity against multiresistant bacteria, Product Details of C11H22N2O4, the publication is Journal of Peptide Science (2018), 24(10), n/a, database is CAplus and MEDLINE.

The present study describes the synthesis and biol. studies of a small series of head-to-tail cyclic tetrapeptides of the general structure c(Lys-β^2,2-Xaa-Lys) containing one lipophilic β^2,2-amino acid and Lys, Gly, Ala, or Phe as the Xaa residue in the sequence. The peptides were investigated for antimicrobial activity against gram-pos. and gram-neg. reference strains and 30 multiresistant clin. isolates including strains with extended spectrum β-lactamase-carbapenemase (ESBL-CARBA) production Toxicity was determined against human red blood cells. The most potent peptides showed high activity against the gram-pos. clin. isolates with min. inhibitory concentrations of 4-8 μg/mL and low hemolytic activity. The combination of high antimicrobial activity and low toxicity shows that these cyclic tetrapeptides containing lipophilic β^2,2-amino acids form a valuable scaffold for designing novel antimicrobial agents.

Journal of Peptide Science published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C11H22N2O4, Product Details of C11H22N2O4.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Rakugi, Hiromi published the artcileEfficacy of sacubitril/valsartan versus olmesartan in Japanese patients with essential hypertension: a randomized, double-blind, multicenter study, Computed Properties of 137862-53-4, the publication is Hypertension Research (2022), 45(5), 824-833, database is CAplus and MEDLINE.

This phase III study assessed the efficacy and safety of sacubitril/valsartan compared with those of olmesartan in Japanese patients with essential hypertension. Patients (n = 1161, aged ≥20 years) with mild to moderate hypertension (mean sitting systolic blood pressure [msSBP] ≥150 to <180 mmHg) were randomized to receive sacubitril/valsartan 200 mg (n = 387), sacubitril/valsartan 400 mg (n = 385), or olmesartan 20 mg (n = 389) once daily for 8 wk. The primary assessment was a reduction in msSBP from baseline with sacubitril/valsartan 200 mg vs. olmesartan 20 mg at Week 8. Secondary assessments included msSBP reduction with sacubitril/valsartan 400 mg vs. olmesartan at Week 8 and reductions in mean sitting diastolic blood pressure (msDBP), mean sitting pulse pressure (msPP), and overall blood pressure (BP) control rate for all treatment groups at Week 8. Sacubitril/valsartan 200 mg provided a significantly greater reduction in msSBP from baseline than olmesartan at Week 8 (between-treatment difference: -5.01 mmHg [95% confidence interval: -6.95 to -3.06 mmHg, P < 0.001 for noninferiority and superiority]). Greater reductions in msSBP with sacubitril/valsartan 400 mg vs. olmesartan, as well as in msDBP and msPP with both doses of sacubitril/valsartan vs. olmesartan (P < 0.05 for all), were also observed Patients treated with sacubitril/valsartan achieved an overall higher BP control rate. The safety and tolerability profiles of sacubitril/valsartan were generally comparable to those of olmesartan. The adverse event rate with sacubitril/valsartan was not dose-dependent. Treatment with sacubitril/valsartan was effective and provided superior BP reduction, with a higher proportion of patients achieving target BP goals than treatment with olmesartan in Japanese patients with mild to moderate essential hypertension.

Hypertension Research published new progress about 137862-53-4. 137862-53-4 belongs to amides-buliding-blocks, auxiliary class GPCR/G Protein,Angiotensin Receptor, name is (S)-2-(N-((2′-(1H-Tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid, and the molecular formula is C24H29N5O3, Computed Properties of 137862-53-4.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Keshari, Twinkle published the artcileCarbon tetrabromide mediated oxidative cyclocondensation of ketones and thioureas: an easy access to 2-aminothiazoles, COA of Formula: C5H10N2OS, the publication is Tetrahedron Letters (2015), 56(41), 5623-5627, database is CAplus.

A simple, mild, and efficient one-pot method for the synthesis of substituted 2-aminothiazoles has been reported. The reaction involves the formation of sulfenyl bromide as an umpolung intermediate of nucleophilic sulfur, which is responsible for C-S bond formation leading to oxidative cyclization of ketones and thioureas to furnish the desired products. Carbon tetrabromide was used as a convenient and mild brominating reagent under basic condition at room temperature to give 2-aminothiazoles in good to excellent yields.

Tetrahedron Letters published new progress about 14294-10-1. 14294-10-1 belongs to amides-buliding-blocks, auxiliary class Morpholine,Thiourea,Amine,Amide, name is Morpholine-4-carbothioamide, and the molecular formula is C5H10N2OS, COA of Formula: C5H10N2OS.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Solankee, Anjani published the artcile2-Substituted phenyl-5-(ω-methoxycarbonyl propyl/pentyl)-Δ²-thiazolin-4-one. Part IV, HPLC of Formula: 14294-10-1, the publication is Journal of the Institution of Chemists (India) (1994), 66(3), 91-2, database is CAplus.

The title compounds I (R = substituted Ph, 3-pyridyl, morpholino, n = 3, 5) were prepared by treatment of 2-bromoadipic and 2-bromosuberic acid with thioamides followed by esterification of the corresponding acids. with MeOH and thionyl chloride.

Journal of the Institution of Chemists (India) published new progress about 14294-10-1. 14294-10-1 belongs to amides-buliding-blocks, auxiliary class Morpholine,Thiourea,Amine,Amide, name is Morpholine-4-carbothioamide, and the molecular formula is C9H8F2O2, HPLC of Formula: 14294-10-1.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics