Day: February 22, 2023

A copper iodide-catalyzed coupling reaction of benzofuran-3(2H)-ones with amines: an approach to 伪-ketoamides was written by Chen, Rongxiang;Jia, Ruo-Ling;Li, Wenbo;Zhao, Wei;Wang, Kai-Kai;Wang, Zhan-Yong;Ma, Xueji;Dai, Wei;Sun, Aili. And the article was included in Organic & Biomolecular Chemistry in 2021.Product Details of 16800-68-3 This article mentions the following:

A CuI-catalyzed coupling reaction of benzofuran-3(2H)-ones with amines has been well established for the direct synthesis of 伪-ketoamides. This process involves C-O bond cleavage and C=O/C-N bond formation. Mechanism studies indicated that this 伪-ketoamide formation reaction may involve a free radical process. In the experiment, the researchers used many compounds, for example, 1-Acetylindolin-3-one (cas: 16800-68-3Product Details of 16800-68-3).

1-Acetylindolin-3-one (cas: 16800-68-3) belongs to indole derivatives. Indole exists overwhelmingly in the 1H-indole form as do other simple indoles. Indole plays a fundamental role for QS in E. coli, being one of the signal molecules responsible for the transcription of a variety of genes (gabT, and tnaB ASTD). Product Details of 16800-68-3

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Chiral Protein-Covalent Organic Framework 3D-Printed Structures as Chiral Biosensors was written by Wang, Lujun;Gao, Wanli;Ng, Siowwoon;Pumera, Martin. And the article was included in Analytical Chemistry (Washington, DC, United States) in 2021.Electric Literature of C11H12N2O2 This article mentions the following:

Three-dimensional (3D) printing technol. has attracted great attention for prototyping different electrochem. sensor devices. However, chiral recognition remains a crucial challenge for electrochem. sensors with similar physicochem. properties such as enantiomers. In this work, a magnetic covalent organic framework (COF) and bovine serum albumin (BSA) (as the chiral surface) functionalized 3D-printed electrochem. chiral sensor is reported for the first time. The characterization of the chiral biomol.-COF 3D-printed constructure was performed by SEM (SEM), XPS, and energy-dispersive X-ray spectroscopy (EDX). A tryptophan (Trp) enantiomer was chosen as the model chiral mol. to estimate the chiral recognition ability of the magnetic COF and BSA-based 3DE (Fe₃O₄@COF@BSA/3DE). We have demonstrated that the Fe₃O₄@COF@BSA/3DE exhibited excellent chiral recognition to L-Trp as compared to D-Trp. The chiral protein-COF sensing interface was used to determine the concentration of L-Trp in a racemic mixture of D-Trp and L-Trp. This strategy of on-demand fabrication of 3D-printed protein-COF-modified electrodes opens up new approaches for enantiomer recognition. In the experiment, the researchers used many compounds, for example, H-D-Trp-OH (cas: 153-94-6Electric Literature of C11H12N2O2).

H-D-Trp-OH (cas: 153-94-6) belongs to indole derivatives. In addition to tryptophan, indigo, and indoleacetic acid, numerous compounds obtainable from plant or animal sources contain the indole molecular structure.Indole was synthesized in moderate yield via an o-naphthoquinone catalyzed tandem cross-coupling of substituted aniline and benzylamine under aerobic oxidation conditions.Electric Literature of C11H12N2O2

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Design, synthesis and antitumor activity of novel indolin-2-one derivatives containing 4-thiazolidinone moiety was written by Liu, Zijian;Hou, Yunlei;Zhang, Guogang;Xu, Ning;Mi, Bin;Gong, Ping;Zhao, Yanfang. And the article was included in Chemical Research in Chinese Universities in 2015.Quality Control of 5,6-Difluoroindolin-2-one This article mentions the following:

A series of novel indolin-2-one derivatives containing 4-thiazolidinone moiety(7a-7r) were synthesized and evaluated for their in vitro antitumor activities against MDA-MB-231(human breast cancer), H460(human lung cancer) and HT-29(human colon cancer) cell lines by standard 3-(4,5-dimethylthiazae-2-yl)-2,5-diphenyltetrazolium bromide(MTT) assay. Representative compounds(7d, 7k, 7m, 7p) with higher cytotoxicity were further examined against one normal cell line(WI-38, human fetal lung fibroblasts). The preliminary investigation shows that most of the compounds display moderate to excellent potency and high selectivity against different human cancer cell lines. In particular, the most potent compound 7m shows promising cytotoxicity against MDA-MB-231, H460 and HT-29 cell lines with IC₅₀ values of 0.78, 0.056 and 0.018 渭mol/L, resp. The potency is much higher than that of Sunitinib(IC₅₀=3.46 渭mol/L against MDA-MB-231, IC₅₀=2.59 渭mol/L against H460, IC₅₀=1.50 渭mol/L against HT-29) by 4.4, 46.3 and 83.3 fold. In the experiment, the researchers used many compounds, for example, 5,6-Difluoroindolin-2-one (cas: 71294-07-0Quality Control of 5,6-Difluoroindolin-2-one).

5,6-Difluoroindolin-2-one (cas: 71294-07-0) belongs to indole derivatives. Indole produced by Proteus, Pseudomonas, Escherichia and other species was shown to be a growth promoting factor in Arabidopsis thaliana. Due to this activity, the indole ring system has become an important component or intermediate in the synthesis of heterocycles.Quality Control of 5,6-Difluoroindolin-2-one

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

The Application of Vinamidinium Salt to the Synthesis of 3-Chloro-伪-carbolines was written by Tian, Shaixiao;Mao, Yu;Jiang, Yongjun;Xu, Guangyu. And the article was included in Synlett in 2018.Recommanded Product: 5-Fluoroindolin-2-one This article mentions the following:

A convenient synthesis of 3-chloro-伪-carbolines, e.g., I by the condensation of vinamidinium salt with 2-indolinones via two steps is reported. This protocol has the advantages of readily available starting materials, high yields and easy workup. In the experiment, the researchers used many compounds, for example, 5-Fluoroindolin-2-one (cas: 56341-41-4Recommanded Product: 5-Fluoroindolin-2-one).

5-Fluoroindolin-2-one (cas: 56341-41-4) belongs to indole derivatives. Indole produced by Proteus, Pseudomonas, Escherichia and other species was shown to be a growth promoting factor in Arabidopsis thaliana. Moreover, it is known that it controls biofilm formation. However, the role of indole in the cell has not been fully elucidated.Recommanded Product: 5-Fluoroindolin-2-one

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Highly Enantioselective Synthesis of Spiro[cyclohexanone-oxindoles] and Spiro[cyclohexanone-pyrazolones] by Asymmetric Cascade [5+1] Double Michael Reactions was written by Wu, Bin;Chen, Jian;Li, Mei-Qiu;Zhang, Jin-Xin;Xu, Xiao-Ping;Ji, Shun-Jun;Wang, Xing-Wang. And the article was included in European Journal of Organic Chemistry in 2012.Computed Properties of C8H5F2NO This article mentions the following:

The construction of spiro compounds through cascade [5+1] double Michael reactions between divinyl ketones and N-unprotected oxindoles or N-phenyl-protected pyrazolones catalyzed by a combination of the easily available 9-amino-9-deoxy-epi-quinine with N-Boc-D-phenylglycine. The desired multistereogenic spiro[cyclohexanone-oxindoles] and spiro[cyclohexanone-pyrazolones] were obtained with high yields (up to 98 %) and stereoselectivities (up to >20:1 dr, 99 % ee). In the experiment, the researchers used many compounds, for example, 5,6-Difluoroindolin-2-one (cas: 71294-07-0Computed Properties of C8H5F2NO).

5,6-Difluoroindolin-2-one (cas: 71294-07-0) belongs to indole derivatives. Indole produced by Proteus, Pseudomonas, Escherichia and other species was shown to be a growth promoting factor in Arabidopsis thaliana. In addition to indole, the strain-release chemistry worked for numerous substrates including amines, alcohols, thiols, carboxylic acids, imidazoles, and pyrazoles.Computed Properties of C8H5F2NO

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

A quick and regioselective access of spirooxindole-oxazoline by reaction of isatin and isocyanoacetate “on water” was written by Rankan, Chandran;Santhi Marimuthu, Prabhakaran;Tiwari, Keshri Nath. And the article was included in Journal of Heterocyclic Chemistry in 2020.Application of 723-89-7 This article mentions the following:

A greener, rapid and regioselective “on water” synthesis of spirooxindole-oxazoline by the reaction of isatin and isocyanoacetate at room temperature was described. The developed protocol has the advantage of being atom-economical, eco-friendly and benign reaction conditions. Broader substrate scope, exptl. simple procedures and easy purification of products with high yield further make this method attractive. The synthesized compounds were fully characterized with spectral anal. In the experiment, the researchers used many compounds, for example, 1-Phenylindoline-2,3-dione (cas: 723-89-7Application of 723-89-7).

1-Phenylindoline-2,3-dione (cas: 723-89-7) belongs to indole derivatives. Indole could be stereoselectively alkylated with chiral cyclopentyl sulfone reagent. In addition to indole, the strain-release chemistry worked for numerous substrates including amines, alcohols, thiols, carboxylic acids, imidazoles, and pyrazoles.Application of 723-89-7

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Pharmacophore modeling and 3D-QSAR study of indole and isatin derivatives as antiamyloidogenic agents targeting Alzheimer’s disease was written by Purgatorio, Rosa;Gambacorta, Nicola;Catto, Marco;de Candia, Modesto;Pisani, Leonardo;Espargaro, Alba;Sabate, Raimon;Cellamare, Saverio;Nicolotti, Orazio;Altomare, Cosimo D.. And the article was included in Molecules in 2020.Formula: C10H9NO2 This article mentions the following:

Thirty-six novel indole-containing compounds, mainly 3-(2-phenylhydrazono) isatins and structurally related 1H-indole-3-carbaldehyde derivatives, were synthesized and assayed as inhibitors of beta amyloid (A尾) aggregation, a hallmark of pathophysiol. of Alzheimer’s disease. The newly synthesized mols. spanned their IC₅₀ values from sub- to two-digit micromolar range, bearing further information into structure-activity relationships. Some of the new compounds showed interesting multitarget activity, by inhibiting monoamine oxidases A and B. A cell-based assay in tau overexpressing bacterial cells disclosed a promising addnl. activity. The accumulated data of either about ninety published and thirty-six newly synthesized mols. were used to generate a pharmacophore hypothesis of antiamyloidogenic activity exerted in a wide range of potencies, satisfactorily discriminating the ‘active’ compounds from the ‘inactive’ (poorly active) ones. An atom-based 3D-QSAR model was also derived for about 80% of ‘active’ compounds, i.e., those achieving finite IC₅₀ values lower than 100渭M. The 3D-QSAR model (encompassing 4 PLS factors), featuring acceptable predictive statistics either in the training set (n = 45, q² = 0.596) and in the external test set (n = 14, r²ext = 0.695), usefully complemented the pharmacophore model by identifying the physicochem. features mainly correlated with the A尾 anti-aggregating potency of the indole and isatin derivatives studied herein. In the experiment, the researchers used many compounds, for example, 5-Methoxy-1H-indole-3-carbaldehyde (cas: 10601-19-1Formula: C10H9NO2).

5-Methoxy-1H-indole-3-carbaldehyde (cas: 10601-19-1) belongs to indole derivatives. In addition to tryptophan, indigo, and indoleacetic acid, numerous compounds obtainable from plant or animal sources contain the indole molecular structure. In addition to indole, the strain-release chemistry worked for numerous substrates including amines, alcohols, thiols, carboxylic acids, imidazoles, and pyrazoles.Formula: C10H9NO2

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Ru-catalyzed oxidation and C-C bond formation of indoles for the synthesis of 2-indolyl indolin-3-ones under mild reaction conditions was written by Zhou, Xiao-Yu;Chen, Xia. And the article was included in Canadian Journal of Chemistry in 2020.Synthetic Route of C10H11NO This article mentions the following:

Herein, a ruthenium catalyzed oxidation and C-C bond formation reaction of 2-alkyl or 2-aryl substituted indoles using tert-Bu hydroperoxide (TBHP) as oxidant is described. Coupled with cascade transformation, it provided a mild catalytic oxidation system for the synthesis of 2-indolylindolin-3-ones I (R = Me, Ph, 4-FC₆H₄, etc.; R¹ = H, Me, Et; R² = 5-Me, 5-OMe, 5-Cl) . The reaction could readily occur using RuCl₃路3H₂O as catalyst, and the target product was obtained with medium to high yield. In the experiment, the researchers used many compounds, for example, 5-Methoxy-2-methyl-1H-indole (cas: 1076-74-0Synthetic Route of C10H11NO).

5-Methoxy-2-methyl-1H-indole (cas: 1076-74-0) belongs to indole derivatives. The indole subunit is an almost ubiquitous component of biologically active natural products, and its study has been the focus of research for decades. In addition to indole, the strain-release chemistry worked for numerous substrates including amines, alcohols, thiols, carboxylic acids, imidazoles, and pyrazoles.Synthetic Route of C10H11NO

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

The hemodynamic interactions of combination therapy with 伪-blockers and phosphodiesterase-5 inhibitors compared to monotherapy with 伪-blockers: a systematic review and meta-analysis was written by Adamou, Constantinos;Ntasiotis, Panteleimon;Athanasopoulos, Anastasios;Kallidonis, Panagiotis. And the article was included in International Urology and Nephrology in 2020.Recommanded Product: 160970-54-7 This article mentions the following:

The present study systematically reviewed the safety of combined treatment with an alpha blocker and phosphodiesterase-5 inhibitor. The study was performed according to the PRISMA statement. The included studies were randomized controlled trials that included at least one group on alpha-blocker monotherapy and one group on a combined treatment with an alpha blocker and phosphodiesterase-5 inhibitor. The primary endpoints were the hemodynamic effects of the two groups, specifically the clin. significant changes and a pos. orthostatic test. The secondary endpoints were the adverse events of the two treatment modalities. A total of 6687 studies were screened, and 19 randomized controlled trials were eligible for the meta-anal. The combined treatment more often produced a clin. significant hemodynamic change with an MD of 4.73 (CI 1.25, 17.94; I2 = 0%; p = 0.02), but the pos. orthostatic test was similar between the groups with an MD of 1.64 (CI 0.36, 7.47; I2 = 50%; p = 0.52). The meta-anal. of adverse events favored alpha-blocker monotherapy with an OD of 0.5 (CI 0.32, 0.78; I2 = 44%; p = 0.002). However, if we consider only the adverse events due to hypotension, the result was similar between the two groups with an OD of 0.97 (CI 0.58, 1.64; I2 = 0%; p = 0.92). The combined treatment may produce a clin. significant hemodynamic change. The combination of alpha blocker and phosphodiesterase-5 inhibitor was safe because it did not increase the rate of adverse events due to hypotension. In the experiment, the researchers used many compounds, for example, (-)-1-(3-Hydroxypropyl)-5-[(2R)-2-[[2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethyl]amino]propyl]-2,3-di-hydro-1H-indole-7-carboxamide (cas: 160970-54-7Recommanded Product: 160970-54-7).

(-)-1-(3-Hydroxypropyl)-5-[(2R)-2-[[2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethyl]amino]propyl]-2,3-di-hydro-1H-indole-7-carboxamide (cas: 160970-54-7) belongs to indole derivatives. Indole exists overwhelmingly in the 1H-indole form as do other simple indoles. Moreover, it is known that it controls biofilm formation. However, the role of indole in the cell has not been fully elucidated.Recommanded Product: 160970-54-7

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Spiropyran in situ switching: A real-time fluorescence strategy for tracking DNA G-quadruplexes in live cells was written by Li, Jin;Yin, Xinchi;Li, Bin;Li, Xiaokang;Pan, Yuanjiang;Li, Jian;Guo, Yuan. And the article was included in Analytical Chemistry (Washington, DC, United States) in 2019.SDS of cas: 118-12-7 This article mentions the following:

DNA G-quadruplexes (G4s) in vivo have been linked to cancer and other diseases such as neurol. disorders. Nondestructive fast detection of endogenous DNA G4s can provide specific real-time information, which is of particular interest for clinic accurate diagnosis. However, tools to probe live-cell endogenous DNA G4s in real time are very limited. Herein, we report the design and development of a fluorescent mol. QIN for the real-time detection of endogenous DNA G4s in live cells with the aid of a new spiropyran in situ switching (SIS) strategy. The lipophilic spiropyran-linked QIN differs from the other probes in that it can enter live cells readily within 15 s and can be in situ induced by DNA G4s to adopt its charged open form, causing a large red shift in the fluorescent emission wavelength. Live-cell super-resolution fluorescent imaging suggests that the SIS-based probe has high photostability and can be applied for the accurate detection of DNA G4s in complex biosystems with very high sensitivity and selectivity. In the experiment, the researchers used many compounds, for example, 1,3,3-Trimethyl-2-methyleneindoline (cas: 118-12-7SDS of cas: 118-12-7).

1,3,3-Trimethyl-2-methyleneindoline (cas: 118-12-7) belongs to indole derivatives. In addition to tryptophan, indigo, and indoleacetic acid, numerous compounds obtainable from plant or animal sources contain the indole molecular structure.Indole was synthesized in moderate yield via an o-naphthoquinone catalyzed tandem cross-coupling of substituted aniline and benzylamine under aerobic oxidation conditions.SDS of cas: 118-12-7

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles