Tag: M.W=100-150

Shen, Ji; Qiao, Juan; Zhang, Xinya; Qi, Li published the artcile< Dual-stimuli-responsive porous polymer enzyme reactor for tuning enzymolysis efficiency>, COA of Formula: C7H5NO2, the main research area is porous polymer enzyme reactor enzymolysis efficiency; Capillary electrophoresis; D-amino acid oxidase; Dual-stimuli-response; Porous polymer membrane enzyme reactor; Tuning enzymolysis efficiency.

A strategy for preparing a dual-stimuli-responsive porous polymer membrane enzyme reactor (D-PPMER) is described, consisting of poly(styrene-maleic anhydride-N-isopropylacrylamide-acrylate-3′,3′-dimethyl-6-nitro-spiro[2H-1-benzopyran-2,2′-indoline]-1′-esterspiropyran ester) [P(S-M-N-SP)] and D-amino acid oxidase. Tunable control via “”on/off”” 365 nm UV light irradiation and temperature variation was used to change the membrane surface configuration and adjust the enzymolysis efficiency of the D-PPMER. A chiral capillary electrophoresis technique was developed for evaluation of the enzymic efficiency of D-PPMER with a Zn(II)-dipeptide complex as the chiral selector and D,L-serine as the substrate. Interestingly, the enzymic kinetic reaction rate of D-PPMER under UV irradiation at 36°C (9.2 x 10-2 mM·min-1) was 3.2-fold greater than that of the free enzyme (2.9 x 10-2 mM·min-1). This was because upon UV irradiation at high temperature, the P(SP) and P(N) moieties altered from a “”stretched”” to a “”curled”” state to encapsulate the enzyme in smaller cavities. The confinement effect of the cavities further improved the enzymic efficiency of the D-PPMER. This protocol highlights the outstanding potential of smart polymers, enables tunable control over the kinetic rates of stimuli-responsive enzyme reactors, and establishes a platform for adjusting enzymolysis efficiency using two different stimuli.

Microchimica Acta published new progress about Contact angle. 21725-69-9 belongs to class isoxazole, and the molecular formula is C7H5NO2, COA of Formula: C7H5NO2.

Referemce:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

Ueda, Mitsuru; Oikawa, Hideaki; Kawaharasaki, Naomi; Imai, Yoshio published the artcile< N,N'-Carbonyldi[1,2-benzisoxazol-3(2H)-one]: new, reactive condensing agent>, COA of Formula: C7H5NO2, the main research area is carbonyldibenzisoxazolone preparation peptide condensing agent; condensing agent carbonyldibenzisoxazolone amide peptide; ester carbonyldibenzisoxazolone condensing agent; benzisoxazolone carbonyldi preparation condensing agent.

The title compound (I) was prepared in 73% yield by treating 1,2-benzisoxazol-3-ol (II) with ClCO2CCl3 in refluxing toluene for 1 day. I was used as a condensing agent for the synthesis of amides, esters, and dipeptides under mild conditions. Thus, BzOH was condensed with H2NPh and HOPh by I in N-methyl-2-pyrrolidone containing pyridine to give 94% BzNHPh and 86% BzOPh, resp., whereas PhCH2O2C-Val-OH was condensed with H-Gly-OEt by I in CH2Cl2 at room temperature to give 87% PhCH2O2C-Val-Gly-OEt. I was also used as a reagent for the one-pot polycondensation of isophthalic acid with diamines to give polyamides.

Bulletin of the Chemical Society of Japan published new progress about Condensation reaction. 21725-69-9 belongs to class isoxazole, and the molecular formula is C7H5NO2, COA of Formula: C7H5NO2.

Referemce:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

Anand, Mohanam; Selvaraj, Vaithialingam; Alagar, Muthukaruppan published the artcile< Synthesis, characterization and evaluation of antioxidant and anticancer activities of novel benzisoxazole-substituted-allyl derivatives>, Recommanded Product: Benzo[d]isoxazol-3-ol, the main research area is allylbenzisoxazolone preparation antioxidant anticancer activity human green chem; benzoisoxazolone allyl bromide chloride cesium carbonate catalyst.

A novel series of various 2-allylbenzo[d]isoxazol-3(2H)-ones I [R = allyl, cinnamyl, benzyl, etc.] were synthesized using benzo[d]isoxazol-3(2H)-one treated with different allyl bromides/chlorides in the presence of water-mediated cesium carbonate as a new catalyst. The structures of the allylated benzisoxazolones I were characterized by spectroscopic methods and mass spectrometry. These synthesized compounds I were evaluated for their in vitro antioxidant and anticancer activity. Compounds I [R = 2-pentynyl, 3-methyl-2-butenyl, benzyl, 4-phenyl-2-butynyl] were identified as the best hit against HT-29 Human colon cancer cells, and showed significant antioxidant activity compared to the standard drug butylated hydroxy toluene (BHT).

Korean Journal of Chemical Engineering published new progress about Allylic halides Role: RCT (Reactant), RACT (Reactant or Reagent) (bromides, chlorides). 21725-69-9 belongs to class isoxazole, and the molecular formula is C7H5NO2, Recommanded Product: Benzo[d]isoxazol-3-ol.

Referemce:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

Csakai, Adam; Smith, Christina; Davis, Emily; Martinko, Alexander; Coulup, Sara; Yin, Hang published the artcile< Saccharin Derivatives as Inhibitors of Interferon-Mediated Inflammation>, Product Details of C7H5NO2, the main research area is saccharin derivative suppressant interferon mediated inflammation SAR.

A series of novel, saccharin-based antagonists have been identified for the interferon signaling pathway. Through in vitro high-throughput screening with the Colorado Center for Drug Discovery (C2D2) Pilot Library, we identified isothiazolone 1,1-dioxides as the basis for extensive structure-activity relationship studies. Our efforts produced a lead anti-inflammatory compound, tert-Bu N-(furan-2-ylmethyl)-N-{4-[(1,1,3-trioxo-2,3-dihydro-1λ6,2-benzisothiazol-2-yl)methyl]benzoyl}carbamate CU-CPD103 (I), as a potent inhibitor using an established nitric oxide (NO) signaling assay. With further studies of its inhibitory mechanisms, we demonstrated that I carries out this inhibition through the JAK/STAT1 pathway, providing a drug-like small mol. inflammation suppressant for possible therapeutic uses.

Journal of Medicinal Chemistry published new progress about Animal gene Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (Cebpb, modified gene consistent with modulation of STAT1 signaling). 21725-69-9 belongs to class isoxazole, and the molecular formula is C7H5NO2, Product Details of C7H5NO2.

Referemce:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

Deering, Robert W.; Whalen, Kristen E.; Alvarez, Ivan; Daffinee, Kathryn; Beganovic, Maya; LaPlante, Kerry L.; Kishore, Shreya; Zhao, Sijing; Cezairliyan, Brent; Yu, Shen; Rosario, Margaret; Mincer, Tracy J.; Rowley, David C. published the artcile< Identification of a bacteria-produced benzisoxazole with antibiotic activity against multi-drug resistant Acinetobacter baumannii>, Electric Literature of 21725-69-9, the main research area is Acinetobacter benzisoxazole antibiotic activity.

Abstract: The emergence of multi-drug resistant pathogenic bacteria represents a serious and growing threat to national healthcare systems. Most pressing is an immediate need for the development of novel antibacterial agents to treat Gram-neg. multi-drug resistant infections, including the opportunistic, hospital-derived pathogen, Acinetobacter baumannii. Herein we report a naturally occurring 1,2-benzisoxazole with min. inhibitory concentrations as low as 6.25μg ml-1 against clin. strains of multi-drug resistant A. baumannii and investigate its possible mechanisms of action. This mol. represents a new chemotype for antibacterial agents against A. baumannii and is easily accessed in two steps via de novo synthesis. In vitro testing of structural analogs suggest that the natural compound may already be optimized for activity against this pathogen. Our results demonstrate that supplementation of 4-hydroxybenzoate in minimal media was able to reverse 1,2-benzisoxazoles antibacterial effects in A. baumannii. A search of metabolic pathways involving 4-hydroxybenzoate coupled with mol. modeling studies implicates two enzymes, chorismate pyruvate-lyase and 4-hydroxybenzoate octaprenyltransferase, as promising leads for the target of 3,6-dihydroxy-1,2-benzisoxazole.

Journal of Antibiotics published new progress about 16S rRNA Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 21725-69-9 belongs to class isoxazole, and the molecular formula is C7H5NO2, Electric Literature of 21725-69-9.

Referemce:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

Ueda, Mitsuru; Harada, Toshiaki; Aoyama, Shigeto; Imai, Yoshio published the artcile< Synthesis of polyamides from active diacyl derivatives of 3-hydroxy-1,2-benzisoxazole and diamines under mild conditions>, COA of Formula: C7H5NO2, the main research area is benzisoxazole ester amide polymer; polyamide benzisoxazole; aminolysis benzoisoxazole ester amide.

New active diesters and diamides derived by O- or N-acylation of 3-hydroxy-1,2-benzisoxazole [21725-69-9] were prepared for use in polyamide synthesis. The active esters and amides reacted readily with amines to give quant. yields of amides. The high reactivity of these active esters and amides was discussed in relation to the electron-withdrawing effect of the leaving group and intramol. general-base catalysis. Solution polycondensation of the new diesters and diamides with aliphatic and aromatic diamines proceeded slowly under mild conditions to produce polyamides with inherent viscosities up to 1.5.

Journal of Polymer Science, Polymer Chemistry Edition published new progress about Aminolysis. 21725-69-9 belongs to class isoxazole, and the molecular formula is C7H5NO2, COA of Formula: C7H5NO2.

Referemce:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

Urban, Frank J.; Breitenbach, Ralph; Murtiashaw, Charles W.; Vanderplas, Brian C. published the artcile< Synthesis of an optically active octahydro-2H-pyrido[1,2-a]pyrazine based CNS agent>, Recommanded Product: Benzo[d]isoxazol-3-ol, the main research area is pyridopyrazine octahydro optically active.

A synthesis of an optically active octahydro-2H-pyrido[1,2-a]pyrazine (I) is presented. The key sequence involved the equilibration of an optically active cis-aldehyde to give the thermodn. trans-aldehyde that was trapped by nitromethane anion.

Tetrahedron: Asymmetry published new progress about 21725-69-9. 21725-69-9 belongs to class isoxazole, and the molecular formula is C7H5NO2, Recommanded Product: Benzo[d]isoxazol-3-ol.

Referemce:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

Lalut, Julien; Payan, Hugo; Davis, Audrey; Lecoutey, Cedric; Legay, Remi; Sopkova-de Oliveira Santos, Jana; Claeysen, Sylvie; Dallemagne, Patrick; Rochais, Christophe published the artcile< Rational design of novel benzisoxazole derivatives with acetylcholinesterase inhibitory and serotoninergic 5-HT4 receptors activities for the treatment of Alzheimer's disease>, COA of Formula: C7H5NO2, the main research area is benzisoxazole preparation; acetylcholinesterase inhibitory Alzheimer’s disease.

Abstract: A rigidification strategy was applied to the preclin. candidate donecopride, an acetylcholinesterase inhibitor possessing 5-HT4R agonist activity. Inspired by promising bioactive benzisoxazole compounds, we have conducted a pharmacomodulation study to generate a novel series of multitarget directed ligands. The chem. synthesis of the ligand was optimized and compounds were evaluated in vitro against each target and in cellulo. Structure-activity relationship was supported by docking anal. in human acetylcholinesterase binding site. Among the synthesized compounds, we have identified a novel hybrid 32a (3-[2-[1-(cyclohexylmethyl)-4-piperidyl]ethyl]-4-methoxy-1,2-benzoxazole) able to display nanomolar acetylcholinesterase inhibitory effects and nanomolar Ki for 5-HT4R.

Scientific Reports published new progress about 5-HT4 receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 21725-69-9 belongs to class isoxazole, and the molecular formula is C7H5NO2, COA of Formula: C7H5NO2.

Referemce:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

Sieser, Janice E.; Singer, Robert A.; McKinley, Jason D.; Bourassa, Dennis E.; Teixeira, John J.; Long, James published the artcile< Synthesis of a bicyclic piperazine from l-aspartic acid and application of a fluoride-promoted SNAr coupling>, Electric Literature of 21725-69-9, the main research area is benzoisoxazolyloctahydropyridopyrazinylmethanol preparation chem resolution nucleophilic aromatic substitution.

The process development is reported of a pivotal C-N bond formation involving ((7R,9aS)-octahydro-1H-pyrido[1,2-a]pyrazin-7-yl)methanol I undergoing nucleophilic aromatic substitution with 3-chlorobenzo[d]isoxazole to furnish ((7R,9aS)-2-(benzo[d]isoxazol-3-yl)octahydro-1H-pyrido[1,2-a]pyrazin-7-yl)methanol II(R = H) as a key intermediate for a family of compounds II(R =aryl). Essential to the success of the coupling is the use of fluoride in combination with a phase transfer catalyst. The development of an alternative route to bicyclic piperazine II (R = H) that uses L-aspartic acid as a starting material to avoid the need for a classical salt resolution is described.

Organic Process Research & Development published new progress about Cyclization. 21725-69-9 belongs to class isoxazole, and the molecular formula is C7H5NO2, Electric Literature of 21725-69-9.

Referemce:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

Zhang, Xuqing; Qiu, Yuhong; Li, Xiaojie; Bhattacharjee, Sheela; Woods, Morgan; Kraft, Patricia; Lundeen, Scott G.; Sui, Zhihua published the artcile< Discovery and structure-activity relationships of a novel series of benzopyran-based KATP openers for urge urinary incontinence>, Computed Properties of 21725-69-9, the main research area is hydroxybenzopyran stereoselective preparation sulfonylurea receptor modulator potassium channel opener; structure hydroxybenzopyran potassium channel opening activity selectivity sulfonylurea receptor.

Substituted hydroxybenzopyrans such as hydroxybenzopyranyl benzoisoxazolone I are prepared as selective modulators of sulfonylurea receptors (SUR) in ATP-sensitive potassium channels for use as potassium channel openers for treatment of urinary incontinence. The structure-activity relationships of 4-substituted benzopyranols are evaluated. I shows EC50 values of 0.67 μM in SUR2B-containing cells, 99.8 μM in SUR1-containing cells, and 1.67 μM in SUR2A-containing cells; in two rat models of myogenic bladder overactivity, I inhibits spontaneous bladder contractions.

Bioorganic & Medicinal Chemistry published new progress about ATP-sensitive potassium channels Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 21725-69-9 belongs to class isoxazole, and the molecular formula is C7H5NO2, Computed Properties of 21725-69-9.

Referemce:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem