Author: Jessica.F

Kawada, Hatsuo published the artcileLead optimization of a dihydropyrrolopyrimidine inhibitor against phosphoinositide 3-kinase (PI3K) to improve the phenol glucuronic acid conjugation, Recommanded Product: N-Methyl-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzamide, the publication is Bioorganic & Medicinal Chemistry Letters (2013), 23(3), 673-678, database is CAplus and MEDLINE.

Lead compound I, for a phosphoinositide 3-kinase (PI3K) inhibitor, was metabolically unstable because of rapid glucuronidation of the phenol moiety. Based on structure-activity relationship (SAR) information and a FlexSIS docking simulation score, aminopyrimidine was identified as a bioisostere of phenol. An X-ray structure study revealed a hydrogen bonding pattern of aminopyrimidine derivatives Finally, aminopyrimidine derivative II showed strong tumor growth inhibition against a KPL-4 breast cancer xenograft model in vivo.

Bioorganic & Medicinal Chemistry Letters published new progress about 1197171-76-8. 1197171-76-8 belongs to amides-buliding-blocks, auxiliary class Boronic acid and ester,Amine,Benzene,Amide,Boronate Esters,Boronic Acids,Boronic acid and ester,, name is N-Methyl-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzamide, and the molecular formula is C14H20BNO3, Recommanded Product: N-Methyl-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzamide.

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

Dyachenko, Ivan V. published the artcileNovel multicomponent synthesis of 6,7-dihydro-5H-cyclopenta[b]pyridine derivatives, Formula: C2H4ClNO, the publication is Chemistry of Heterocyclic Compounds (New York, NY, United States) (2020), 56(12), 1592-1598, database is CAplus.

The multicomponent condensation of malononitrile, hydrogen sulfide, aldehydes RCHO (R = Et, cyclohex-3-en-1-yl, Ph, 4-hydroxyphenyl, etc.), 1-(cyclopent-1-en-1-yl)pyrrolidine, and alkylating agents XCH₂Z (X = Br, Cl, I; Z = H, ethoxycarbonyl, CN, Ph, etc.) leads to the formation of 6,7-dihydro-5H-cyclopenta[b]pyridine derivatives, e.g., I.

Chemistry of Heterocyclic Compounds (New York, NY, United States) published new progress about 79-07-2. 79-07-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Aliphatic hydrocarbon chain,Amide,Inhibitor, name is 2-Chloroacetamide, and the molecular formula is C2H4ClNO, Formula: C2H4ClNO.

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

Dyachenko, I. V. published the artcileSynthesis of functionalized tetrahydropyridones by the tandem Knoevenagel-Michael-intramolecular ammonolysis-alkylation reaction, SDS of cas: 79-07-2, the publication is Russian Chemical Bulletin (2021), 70(11), 2145-2155, database is CAplus.

The tandem Knoevenagel-Michael-intramol. ammonolysis-alkylation reaction was used to synthesize functionalized tetrahydropyridones. The mol. and crystal structures of four pyridone derivatives were studied by X-ray diffraction.

Russian Chemical Bulletin published new progress about 79-07-2. 79-07-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Aliphatic hydrocarbon chain,Amide,Inhibitor, name is 2-Chloroacetamide, and the molecular formula is C2H4ClNO, SDS of cas: 79-07-2.

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

Moreno-Sanz, Guillermo published the artcileSynthesis and Structure-Activity Relationship Studies of O-Biphenyl-3-yl Carbamates as Peripherally Restricted Fatty Acid Amide Hydrolase Inhibitors, COA of Formula: C14H20BNO3, the publication is Journal of Medicinal Chemistry (2013), 56(14), 5917-5930, database is CAplus and MEDLINE.

The peripherally restricted fatty acid amide hydrolase (FAAH) inhibitor URB937 (I, cyclohexylcarbamic acid 3′-carbamoyl-6-hydroxybiphenyl-3-yl ester) is extruded from the brain and spinal cord by the Abcg2 efflux transporter. Despite its inability to enter the central nervous system (CNS), I exerts profound antinociceptive effects in mice and rats, which result from the inhibition of FAAH in peripheral tissues and the consequent enhancement of anandamide signaling at CB₁ cannabinoid receptors localized on sensory nerve endings. In the present study, we examined the structure-activity relationships (SAR) for the biphenyl region of compound I, focusing on the carbamoyl and hydroxyl groups in the distal and proximal Ph rings. Our SAR studies generated a new series of peripherally restricted FAAH inhibitors and identified compound II (cyclohexylcarbamic acid 3′-carbamoyl-5-hydroxybiphenyl-3-yl ester) as the most potent brain-impermeant FAAH inhibitor disclosed to date.

Journal of Medicinal Chemistry published new progress about 1197171-76-8. 1197171-76-8 belongs to amides-buliding-blocks, auxiliary class Boronic acid and ester,Amine,Benzene,Amide,Boronate Esters,Boronic Acids,Boronic acid and ester,, name is N-Methyl-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzamide, and the molecular formula is C14H20BNO3, COA of Formula: C14H20BNO3.

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

Salives, Richard published the artcileSolid-phase syntheses of 6-arylpyridazin-3(2H)-ones, COA of Formula: C11H16BNO3, the publication is Journal of Combinatorial Chemistry (2005), 7(3), 414-420, database is CAplus and MEDLINE.

The 3-chloropyridazine moiety was immobilized on a Wang resin, using two different methodologies. The first of these involved direct nucleophilic substitution of 3,6-dichloropyridazine with the alcoholate of Wang resin. The exptl. conditions were optimized. The second method involved a Mitsunobu reaction between the Wang resin and 6-chloropyridazin-3-ol during which a problem of regioselectivity was observed The so-obtained chloropyridazine-containing resins were subsequently reacted with various arylboronic acids under Suzuki conditions. Acid cleavage yielded 6-arylpyridazin-3(2H)-ones, e.g., I, with high chem. purity.

Journal of Combinatorial 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, COA of Formula: C11H16BNO3.

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

Zhou, Wanyi published the artcileGlucose and MMP-9 dual-responsive hydrogel with temperature sensitive self-adaptive shape and controlled drug release accelerates diabetic wound healing, Safety of 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, the publication is Bioactive Materials (2022), 1-17, database is CAplus and MEDLINE.

Chronic diabetic wounds are an important healthcare challenge. High concentration glucose, high level of matrix metalloproteinase-9 (MMP-9), and long-term inflammation constitute the special wound environment of diabetic wounds. Tissue necrosis aggravates the formation of irregular wounds. All the above factors hinder the healing of chronic diabetic wounds. To solve these issues, a glucose and MMP-9 dual-response temperature-sensitive shape self-adaptive hydrogel (CBP/GMs@Cel&INS) was designed and constructed with polyvinyl alc. (PVA) and chitosan grafted with phenylboric acid (CS-BA) by encapsulating insulin (INS) and gelatin microspheres containing celecoxib (GMs@Cel). Temperature-sensitive self-adaptive CBP/GMs@Cel&INS provides a new way to balance the fluid-like mobility (self-adapt to deep wounds quickly, approx. 37°C) and solid-like elasticity (protect wounds against external forces, approx. 25°C) of self-adaptive hydrogels, while simultaneously releasing insulin and celecoxib on-demand in the environment of high-level glucose and MMP-9. Moreover, CBP/GMs@Cel&INS exhibits remodeling and self-healing properties, enhanced adhesion strength (39.65 ± 6.58 kPa), down-regulates MMP-9, and promotes cell proliferation, migration, and glucose consumption. In diabetic full-thickness skin defect models, CBP/GMs@Cel&INS significantly alleviates inflammation and regulates the local high-level glucose and MMP-9 in the wounds, and promotes wound healing effectively through the synergistic effect of temperature-sensitive shape-adaptive character and the dual-responsive system.

Bioactive Materials 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 C20H28B2O4S2, Safety of 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide.

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

Zhao, Yanbin published the artcileVanadium-catalyzed Oxidative Conversion of Primary Aromatic Alcohols into Amides and Nitriles with Molecular Oxygen, SDS of cas: 1453-82-3, the publication is Chemistry – An Asian Journal (2022), 17(11), e202200224, database is CAplus and MEDLINE.

Herein, a vanadium-based material V-N-C-700 was prepared via a simple and convenient method, and employed for liquid-phase catalytic ammoxidation of alcs. RCH₂OH (R = n-Bu, Ph, pyridin-2-yl, etc.) with mol. oxygen. By using V-N-C-700/2-picolinic acid, primary aromatic alcs. were smoothly converted into the amides RC(O)NH₂ and nitriles RCN in the presence of urea. The corresponding aldehydes RCHO are the key intermediates, and 2-picolinic acid could significantly enhance oxidation of alcs. into aldehydes. The amides were formed simultaneously along with nitriles, rather than only from nitriles via successive hydration. This work further expands non-noble metal catalysts for the preparation of amides and nitriles.

Chemistry – An Asian Journal published new progress about 1453-82-3. 1453-82-3 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is Isonicotinamide, and the molecular formula is C20H19NO4, SDS of cas: 1453-82-3.

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

Zhang, Jing published the artcileEffect of Sacubitril/Valsartan on the Right Ventricular Function and Pulmonary Hypertension in Patients With Heart Failure With Reduced Ejection Fraction: A Systematic Review and Meta-Analysis of Observational Studies., Product Details of C24H29N5O3, the publication is Journal of the American Heart Association (2022), 11(9), e024449, database is MEDLINE.

Background Sacubitril/valsartan (S/V) demonstrated significant effects in improving left ventricular performance and remodeling in patients with heart failure with reduced ejection fraction. However, its effects on the right ventricle remain unclear. This systematic review and meta-analysis aimed to assess the impact of S/V on right ventricular function and pulmonary hypertension. Methods and Results We searched PubMed, Embase, Cochrane Library, and Web of Science from January 2010 to April 2021 for studies reporting right ventricular and pulmonary pressure indexes following S/V treatment. The quality of included studies was assessed using the Newcastle-Ottawa scale. Variables were pooled using a random-effects model to estimate weighted mean differences with 95% CIs. We identified 10 eligible studies comprising 875 patients with heart failure with reduced ejection fraction (mean age, 62.2 years; 74.0% men), all of which were observational. Significant improvements on right ventricular function and pulmonary hypertension after S/V initiation were observed, including tricuspid annular plane systolic excursion (weighted mean difference, 1.26 mm; 95% CI, 0.33-2.18 mm; P=0.008), tricuspid annular peak systolic velocity (weighted mean difference, 0.85 cm/s; 95% CI, 0.25-1.45 cm/s; P=0.005), and systolic pulmonary arterial pressure (weighted mean difference, 7.21 mm Hg; 95% CI, 5.38-9.03 mm Hg; P<0.001). Besides, S/V had a significant beneficial impact on left heart function, which was consistent with previous studies. The quadratic regression model revealed a certain correlation between tricuspid annular plane systolic excursion and left ventricular ejection fraction after excluding the inappropriate data (P=0.026). Conclusions This meta-analysis verified that S/V could improve right ventricular performance and pulmonary hypertension in heart failure with reduced ejection fraction, which did not seem to be fully dependent on the reverse remodeling of left ventricle. Registration URL: https://www.crd.york.ac.uk/prospero; Unique identifier: CRD42021247970.

Journal of the American Heart Association 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 C27H39ClN2, Product Details of C24H29N5O3.

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

Hua, Guoxiong published the artcileSynthesis and Structural Study of Novel Selenation Derivatives of N, N-Dialkylcyanamides, Quality Control of 2451-91-4, the publication is ChemistrySelect (2016), 1(21), 6810-6817, database is CAplus.

The reaction of 2,4-bis(phenyl)-1,3-diselenadiphosphetane-2,4-diselenide {[PhP(Se)(μ-Se)]₂, Woollins’ reagent, WR} with N, N-dialkylcyanamides 1–3 in refluxing toluene solution led to the corresponding [2+3] cycloaddition products 4-dialkylamino-2,5-diphenyl-1,3,2,5-selenazadiphosphole 2,5-diselenides 4–6 in good yields, the latter were further treated with water resulting in the corresponding hydrolysis derivatives dialkyl-selenoureas 7–9, and phosphinodiselenoates 10 and 11. Selenourea 7 could be transferred into 1,3-selenazol-2-amines 12–15 in excellent yields by further cyclization with four different α-haloketones. All new compounds have been characterized by IR spectroscopy, multi-NMR (¹H, ¹³C, ³¹P, ⁷⁷Se) spectroscopy and accurate mass measurement. The single crystal X-ray structural features of nine new compounds are also discussed.

ChemistrySelect published new progress about 2451-91-4. 2451-91-4 belongs to amides-buliding-blocks, auxiliary class Nitrile,Amine,Benzene, name is N,N-Dibenzylcyanamide, and the molecular formula is C15H14N2, Quality Control of 2451-91-4.

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

Giliomee, Johnel published the artcileEvaluation of composition effects on the physicochemical and biological properties of polypeptide-based hydrogels for potential application in wound healing, Recommanded Product: H-Lys(Boc)-OH, the publication is Polymers (Basel, Switzerland) (2021), 13(11), 1828, database is CAplus and MEDLINE.

In this study, the effect of crosslinking and concentration on the properties of a new library of low-concentration poly(Lys₆₀-ran-Ala₄₀)-based hydrogels for potential application in wound healing was investigated in order to correlate the hydrogel composition with the desired physicochem. and biofunctional properties to expand the assortment of poly-L-lysine (PLL)-based hydrogels suitable for wound healing. Controlled ring-opening polymerization (ROP) and precise hydrogel compositions were used to customize the physicochem. and biofunctional properties of a library of new hydrogels comprising poly(L-lysine-ran-L-alanine) and four-arm poly(ethylene glycol) (P(KA)/4-PEG). The chem. composition and degree of crosslinking via free amine quantification were analyzed for the P(KA)/4-PEG hydrogels. In addition, the rheol. properties, pore morphol., swelling behavior and degradation time were characterized. Subsequently, in vitro cell studies for evaluation of the cytotoxicity and cell adhesion were performed. The 4 wt% 1:1 functional molar ratio hydrogel with P(KA) concentrations as low as 0.65 wt% demonstrated low cytotoxicity and desirable cell adhesion towards fibroblasts and thus displayed a desirable combination of properties for wound healing application.

Polymers (Basel, Switzerland) 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, Recommanded Product: H-Lys(Boc)-OH.

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