Month: October 2022

Recommanded Product: 6381-59-5In 2020 ,《Synthesis and Biological Evaluation of Pyrroloindolines as Positive Allosteric Modulators of the α1β2γ2 GABAA Receptor》 appeared in ACS Medicinal Chemistry Letters. The author of the article were Blom, Annet E. M.; Su, Justin Y.; Repka, Lindsay M.; Reisman, Sarah E.; Dougherty, Dennis A.. The article conveys some information:

Here, the synthesis and functional evaluation of a novel series of pyrroloin-dolines, e.g., I that displayed significant modulation of the γ-aminobutyric acid type A (GABAA) receptor, acting as pos. allosteric modulators (PAMs) was described. It was found that halogen incorporation at the C5 position greatly increased the PAM potency relative to the parent ligand, while substitutions at other positions generally decreased potency. Mutagenesis studies suggested that the binding site lies at the top of the transmembrane domain. In the experimental materials used by the author, we found Potassium sodium (2R,3R)-2,3-dihydroxysuccinate tetrahydrate(cas: 6381-59-5Recommanded Product: 6381-59-5)

Potassium sodium (2R,3R)-2,3-dihydroxysuccinate tetrahydrate(cas: 6381-59-5) is a ferroelectric crystal with a high piezoelectric effect and electromechanical coupling coefficient. Recommanded Product: 6381-59-5 As a Biuret reagent, it is used to measure the protein concentration. Furthermore, it is used as laxative and is also used in food industry.

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Computed Properties of C3H8ClNOIn 2017 ,《Discovery and in vivo effects of novel human natriuretic peptide receptor A (NPR-A) agonists with improved activity for rat NPR-A》 appeared in Bioorganic & Medicinal Chemistry. The author of the article were Iwaki, Takehiko; Tanaka, Taisaku; Miyazaki, Kazuo; Suzuki, Yamato; Okamura, Yoshihiko; Yamaki, Akira; Iwanami, Makoto; Morozumi, Naomi; Furuya, Mayumi; Oyama, Yoshiaki. The article conveys some information:

Natriuretic peptide receptor A (NPR-A) agonists were evaluated in vivo by optimizing the structure of quinazoline derivatives to improve agonistic activity for rat NPR-A. A 1,4-Cis-aminocyclohexylurea moiety at 4-position and hydroxy group of D-alaninol at 2-position on the quinazoline ring were found to be important factors in improving rat NPR-A activity. The authors identified potent quinazoline and pyrido[2,3-d]pyrimidine derivatives against rat NPR-A, with double-digit nanomolar EC50 values. The in vivo results showed that compound 56b (1-((1S,4S)-4-((6-(3-fluorophenyl)-2-(((R)-1-hydroxypropan-2-yl)amino)pyrido[2,3-d]pyrimidin-4-yl)amino)cyclohexyl)-3-((R)-1-hydroxy-3-methylbutan-2-yl)urea) administered at 1.0 mg/kg/min significantly increased plasma cGMP concentration and urine volume in rats. The authors discovered novel potent NPR-A agonists that showed agonistic effects similar to those of atrial natriuretic peptide. After reading the article, we found that the author used Azetidin-3-ol hydrochloride(cas: 18621-18-6Computed Properties of C3H8ClNO)

Azetidin-3-ol hydrochloride(cas:18621-18-6) is one of azetidine.Azetidines (azacyclobutanes) constitute a well-known class of heterocyclic compounds. Azetidine scaffold has been discovered in several natural products.Computed Properties of C3H8ClNO Several pharmacologically important synthetic compounds also contain azetidine ring. Because of inherent ring strain, the synthesis of azetidines is a challenging endeavor.

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Recommanded Product: 26153-38-8In 2019 ,《Synthesis, anticancer activity and molecular docking studies of some novel quinoline hydrazide derivatives of substituted benzaldehydes》 appeared in Rasayan Journal of Chemistry. The author of the article were Gayam, Venkatareddy; Ravi, Subban; Ravikumar, G. M. V. N. A. R.; Thangamani, Arumugam. The article conveys some information:

A novel series of quinoline hydrazide bridged derivatives were synthesized by a multistep reaction from vanillic acid. The reactions involved esterification, O-alkylation, nitration, reduction, cyclization, to get 7-(3-hloropropoxy)-4-hydroxy-6-methoxyquinoline-3-carbonitrile 5 which further reacted with Et bromoacetate to yield the corresponding ester 6. Compound 6 react with hydrazine hydrate to afford the hydrazide 7, which then reacted with substituted benzaldehydes to afford the corresponding quinoline-hydrazides 8 – 19. The synthesized compounds were characterized by IR, NMR and MS data. Compounds 7-19 were tested for their cytotoxic activity by Trypan blue, MTT and LDH assays. All the tested compounds showed cytotoxic activity and the results are comparable with the standard compound bosutinib. Compound 12 showed an IC50 value of 26.93 ± 2.8 and 28.92 ± 1.6μg/mL by MTT and trypan blue assay resp. Structure activity relationship was discussed among the compounds 7-19. Mol. docking studies were carried out for all the compounds 7-19 against BCR-ABL T315I protein. Compound 12 showed very good interactions with the protein like any other tyrosine kinase inhibitors. After reading the article, we found that the author used 3,5-Dihydroxybenzaldehyde(cas: 26153-38-8Recommanded Product: 26153-38-8)

3,5-Dihydroxybenzaldehyde(cas: 26153-38-8) is a building block. It has been used in the synthesis of 2,4-dimethylbenzoylhydrazones with antileishmanial and antioxidant activities.Recommanded Product: 26153-38-8

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Quality Control of 3-HydroxybenzaldehydeIn 2020 ,《Synthesis, spectral characterization and biological activity of some novel quinoline-substituted thiazolo[4,5-e]azepine derivatives》 appeared in Research Journal of Chemical Sciences. The author of the article were Ravi, Sharma; Kishore, Dharam. The article conveys some information:

A novel series of quinoline-substituted thiazolo(hetero)azepines I (R = Ph, 3-ClC6H4, 3-HOC6H4; X = NH, O, S) was synthesized via condensation of thiazolidinones II with o-phenylenediamine, o-aminophenol or o-aminothiophenol in the presence of glacial acetic acid in methanol. The compounds II were in turn synthesized by condensation of N-(4-oxo-2-phenylthiazolidin-3-yl)-2-(quinolin-8-yloxy)acetamide with various aromatic aldehydes. All novel compounds were characterized by spectroscopic methods (MASS, IR, 1H NMR) and elemental anal. The antimicrobial activity of these compounds has been studied using the micro dilution format.3-Hydroxybenzaldehyde(cas: 100-83-4Quality Control of 3-Hydroxybenzaldehyde) was used in this study.

3-Hydroxybenzaldehyde(cas: 100-83-4) is used as an ionophore, during the development of an highly selective and sensitive PVC membrane sensor, which can be used as a Tb3+ ion selective electrode.Quality Control of 3-Hydroxybenzaldehyde

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Application In Synthesis of 5-Hexen-1-olIn 2021 ,《Photochemical intermolecular dearomative cycloaddition of bicyclic azaarenes with alkenes》 appeared in Science (Washington, DC, United States). The author of the article were Ma, Jiajia; Chen, Shuming; Bellotti, Peter; Guo, Renyu; Schaefer, Felix; Heusler, Arne; Zhang, Xiaolong; Daniliuc, Constantin; Brown, M. Kevin; Houk, Kendall N.; Glorius, Frank. The article conveys some information:

Dearomative cycloaddition reactions represent an ideal means of converting flat arenes into three-dimensional architectures of increasing interest in medicinal chem. Quinolines, isoquinolines, and quinazolines, despite containing latent diene and alkene subunits, are scarcely applied in cycloaddition reactions because of the inherent low reactivity of aromatic systems and selectivity challenges. Here, we disclose an energy transfer-mediated, highly regio- and diastereoselective intermol. [4 + 2] dearomative cycloaddition reaction of these bicyclic azaarenes with a plethora of electronically diverse alkenes. This approach bypasses the general reactivity and selectivity issues, thereby providing various bridged polycycles that previously have been inaccessible or required elaborate synthetic efforts. Computational studies with d. functional theory elucidate the mechanism and origins of the observed regio- and diastereoselectivities. In addition to this study using 5-Hexen-1-ol, there are many other studies that have used 5-Hexen-1-ol(cas: 821-41-0Application In Synthesis of 5-Hexen-1-ol) was used in this study.

5-Hexen-1-ol(cas: 821-41-0) is used in cyclization to a tetrahydropyran by phenylselenoetherification. It is also used as a building block in synthetic chemistry.Application In Synthesis of 5-Hexen-1-ol

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Quality Control of 3-HydroxybenzaldehydeIn 2020 ,《Synthesis and characterization of a novel and green rod-like magnetic ZnS/CuFe2O4/agar organometallic hybrid catalyst for the synthesis of biologically-active 2-amino-tetrahydro-4H-chromene-3-carbonitrile derivatives》 appeared in Applied Organometallic Chemistry. The author of the article were Bahrami, Shahrzad; Hassanzadeh-Afruzi, Fereshte; Maleki, Ali. The article conveys some information:

The magnetic biocompatible rod-like ZnS/CuFe2O4/agar organometallic hybrid catalyst was designed and prepared based on a natural macromol. (agar) through a green and convenient method using inexpensive, nontoxic, and easily available substances. Then, the as-prepared catalyst was characterized by several techniques such as Fourier transform-IR spectroscopy, energy-dispersive X-ray anal., SEM image, transmission electron microscopy, vibrating sample magnetometry curve, X-ray diffraction pattern, and thermogravimetric anal. Eventually, the catalytic application of the ZnS/CuFe2O4/agar nanobiocomposite was assessed in sequential Knoevenagel condensation-Michael addition reaction of dimedone, malononitrile, and different substituted aromatic aldehydes for the synthesis of 2-amino-tetrahydro-4H-chromene-3-carbonitrile derivatives Some notable strengths of this environmentally benign catalyst include simplicity of catalyst preparation and separation, affording desired products with satisfactory yields (81%-97%) in very short reaction times (3-18 min), and with no need for complicated work-up processes. Exptl. tests showed that the catalyst can be successfully reused after five sequential runs without significant reduction in its catalytic efficiency.3-Hydroxybenzaldehyde(cas: 100-83-4Quality Control of 3-Hydroxybenzaldehyde) was used in this study.

3-Hydroxybenzaldehyde(cas: 100-83-4) is used as an ionophore, during the development of an highly selective and sensitive PVC membrane sensor, which can be used as a Tb3+ ion selective electrode.Quality Control of 3-Hydroxybenzaldehyde

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Electric Literature of C6H13NOIn 2021 ,《Fragment-based Scaffold Hopping: Identification of Potent, Selective, and Highly Soluble Bromo and Extra Terminal Domain (BET) Second Bromodomain (BD2) Inhibitors》 was published in Journal of Medicinal Chemistry. The article was written by Seal, Jonathan T.; Atkinson, Stephen J.; Bamborough, Paul; Bassil, Anna; Chung, Chun-wa; Foley, James; Gordon, Laurie; Grandi, Paola; Gray, James R. J.; Harrison, Lee A.; Kruger, Ryan G.; Matteo, Jeanne J.; McCabe, Michael T.; Messenger, Cassie; Mitchell, Darren; Phillipou, Alex; Preston, Alex; Prinjha, Rab K.; Rianjongdee, Francesco; Rioja, Inmaculada; Taylor, Simon; Wall, Ian D.; Watson, Robert J.; Woolven, James M.; Wyce, Anastasia; Zhang, Xi-Ping; Demont, Emmanuel H.. The article contains the following contents:

The profound efficacy of pan-BET inhibitors is well documented, but these epigenetic agents have shown pharmacol.-driven toxicity in oncol. clin. trials. The opportunity to identify inhibitors with an improved safety profile by selective targeting of a subset of the eight bromodomains of the BET family has triggered extensive medicinal chem. efforts. In this article, we disclose the identification of potent and selective drug-like pan-BD2 inhibitors such as pyrazole 23 (GSK809) and furan 24 (GSK743) that were derived from the pyrrole fragment 6. We transpose the key learnings from a previous pyridone series (GSK620 2 as a representative example) to this novel class of inhibitors, which are characterized by significantly improved solubility relative to our previous research. The experimental process involved the reaction of trans-4-Aminocyclohexanol(cas: 27489-62-9Electric Literature of C6H13NO)

trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. Amine, any member of a family of nitrogen-containing organic compounds that is derived, either in principle or in practice, from ammonia (NH3). Naturally occurring amines include the alkaloids, which are present in certain plants; the catecholamine neurotransmitters (i.e., dopamine, epinephrine, and norepinephrine); and a local chemical mediator, histamine, that occurs in most animal tissues.Electric Literature of C6H13NO

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《A new heterocycles compound combined with focused ultrasound inhibits breast cancer cell proliferation and invasion》 was written by Qu, Chun-Ping; Xu, Qing-Ling. Formula: C3H6O2 And the article was included in Latin American Journal of Pharmacy in 2021. The article conveys some information:

The new (S)-oxiran-2-ylmethyl 3-nitrobenzenesulfonate (1), designed using (R)-3-chloropropane-1,2-diol and nitrobenzene as start material, was successfully obtained via multiple synthesis routes and finally characterized by IR, 1H NMR, and single crystal X-ray crystallog. Its application values on the breast cancer treatment were evaluated and the related mechanism was explored as well. The CCK-8 assay was firstly conducted and the inhibitory effect of the new compound on the breast cancer cells was measured. Then, the reduction effect of the new compound on the breast cancer migration and invasion activity was measured with trans-well assay. The experimental part of the paper was very detailed, including the reaction process of (R)-Oxiran-2-ylmethanol(cas: 57044-25-4Formula: C3H6O2)

(R)-Oxiran-2-ylmethanol(cas: 57044-25-4) is a chiral building block used to construct an epoxyvinyl iodide intermediate in a synthesis of a furanocembrane, a marine natural product.Formula: C3H6O2

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《EDTA-Functionalized Covalent Organic Framework for the Removal of Heavy-Metal Ions》 was written by Jiang, Yunzhe; Liu, Chuanyao; Huang, Aisheng. Recommanded Product: 2,4,6-Trihydroxybenzene-1,3,5-tricarbaldehydeThis research focused onwastewater treatment heavy metal ion adsorptive removal; EDTA functionalized covalent organic framework adsorbent wastewater treatment; Adsorption; Covalent organic framework (COF); Ethylenediaminetetraacetic acid (EDTA); Post-synthesis; Removal of heavy-metal ions. The article conveys some information:

Heavy metal ion removal from wastewater has gained intense attention due to metal toxicity, bioaccumulation tendency, and persistence. Adsorption is a most promise method because of its simplicity and efficiency. This work reports preparation of an EDTA-functionalized covalent organic framework (COF) for heavy metal ion removal. A COF, TpPa-NO2, was reduced to TpPa-NH2 using a Na2S2O4 reductant, then EDTA dianhydride was grafted on the TpPa-NH2 to form TpPa-NH2@EDTA via post-modification. COF morphol. and structure remained unchanged after post-modification. TpPa-NH2@EDTA displayed excellent heavy metal ion adsorption performance (e.g., soft Lewis acids [Ag+, Pd2+], hard Lewis acids [Fe3+, Cr3+], borderline Lewis acids [Cu2+, Ni2+]) with removal efficiencies all >85% within 5 min due to the EDTA strong chelation effect. TpPa-NH2@EDTA also showed high adsorption ability in a pH ≥3 environment with an adsorption capacity >50 mg/g for six representative heavy metal ions. This work provided an idea to use COF materials to remove heavy metal ions from wastewater. In addition to this study using 2,4,6-Trihydroxybenzene-1,3,5-tricarbaldehyde, there are many other studies that have used 2,4,6-Trihydroxybenzene-1,3,5-tricarbaldehyde(cas: 34374-88-4Recommanded Product: 2,4,6-Trihydroxybenzene-1,3,5-tricarbaldehyde) was used in this study.

2,4,6-Trihydroxybenzene-1,3,5-tricarbaldehyde(cas: 34374-88-4) is a member of phloroglucinol derivatives. Phloroglucinol derivatives are a major class of secondary metabolites. Phloroglucinol compounds can be classified into monomeric, dimeric, trimeric and higher phloroglucinols, and phlorotannins.Recommanded Product: 2,4,6-Trihydroxybenzene-1,3,5-tricarbaldehyde

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《Exploiting designed oxidase-peroxygenase mutual benefit system for asymmetric cascade reactions》 was written by Yu, Da; Wang, Jian-bo; Reetz, Manfred T.. Application of 133082-13-0 And the article was included in Journal of the American Chemical Society on April 10 ,2019. The article conveys some information:

A unique P 450 monooxygenase-peroxygenase mutual benefit system was designed as the core element in the construction of a biocatalytic cascade reaction sequence leading from 3-Ph propionic acid to (R)-Ph glycol. In this system, P 450 monooxygenase (P 450-BM3) and P 450 peroxygenase (OleTJE) not only function as catalysts for the crucial initial reactions, they also ensure an internal in situ H2O2 recycle mechanism that avoids its accumulation and thus prevents possible toxic effects. By directed evolution of P 450-BM3 as the catalyst in the enantioselective epoxidation of the styrene-intermediate, formed from 3-Ph propionic acid, and the epoxide hydrolase ANEH for final hydrolytic ring opening, (R)-Ph glycol and 9 derivatives thereof were synthesized from the resp. carboxylic acids in one-pot processes with high enantioselectivity. In the experiment, the researchers used many compounds, for example, (1S)-1-(2-chlorophenyl)ethane-1,2-diol(cas: 133082-13-0Application of 133082-13-0)

(1S)-1-(2-chlorophenyl)ethane-1,2-diol(cas: 133082-13-0) belongs to hydroxy-containing compounds. Hydroxy groups participate in the dehydration reactions that link simple biological molecules into long chains. The creation of a peptide bond to link two amino acids to make a protein removes the −OH from the carboxy group of one amino acid.Application of 133082-13-0

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