Tag: 100-200

Safety of 1H-IndoleIn 2021 ,《Recent advances in indole dimers and hybrids with antibacterial activity against methicillin-resistant Staphylococcus aureus》 appeared in Archiv der Pharmazie (Weinheim, Germany). The author of the article were Meng, Tingting; Hou, Yani; Shang, Congshan; Zhang, Jing; Zhang, Bo. The article conveys some information:

A review. Methicillin-resistant Staphylococcus aureus (MRSA), one of the major and most dangerous pathogens in humans, is a causative agent of severe pandemic of mainly skin and soft tissue and occasionally fatal infections. Therefore, it is imperative to develop potent and novel anti-MRSA agents. Indole derivatives could act against diverse enzymes and receptors in bacteria, occupying a salient place in the development of novel antibacterial agents. Dimerization and hybridization are common strategies to discover new drugs, and a number of indole dimers and hybrids possess potential antibacterial activity against a panel of clin. important pathogens including MRSA. Accordingly, indole dimers and hybrids are privileged scaffolds for the discovery of novel anti-MRSA agents. This outlines the recent development of indole dimers and hybrids with a potential activity against MRSA, covering articles published between 2010 and 2020. The structure-activity relationship and the mechanism of action are also discussed to facilitate further rational design of more effective candidates. In the experiment, the researchers used 1H-Indole(cas: 120-72-9Safety of 1H-Indole)

1H-Indole(cas: 120-72-9) belongs to indole. Indole, also called Benzopyrrole, a heterocyclic organic compound occurring in some flower oils, such as jasmine and orange blossom, in coal tar, and in fecal matter. It is used in perfumery and in making tryptophan, an essential amino acid, and indoleacetic acid (heteroauxin), a hormone that promotes the development of roots in plant cuttings.Safety of 1H-Indole

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

In 2019,Advanced Synthesis & Catalysis included an article by Pillaiyar, Thanigaimalai; Uzair, Muhammad; Ullah, Saif; Schnakenburg, Gregor; Mueller, Christa E.. Application In Synthesis of 5-Fluoro-1H-indole. The article was titled 《Decarboxylative Coupling Reaction of 2-(1H-indol-3-yl)acetic Acids with Indole, Azaindole, Benzimidazole and Indazole Derivatives》. The information in the text is summarized as follows:

A new, mild and efficient copper(II)-promoted decarboxylative coupling reaction of 2-(1H-indol-3-yl)acetic acid derivatives I (R = H, 4-Cl, 5-OCH3, 6-F, 5-Cl, 6-Cl; R1 = H, CH3) with a variety of (substituted) indoles II (R2 = H, Ph, CO2Et; R3 = H, CH3; R4 = H, Me, F, Br, MeO, CHO; R5 = H, MeO, CHO, F; R6 = H, Cl, Br, MeO, Et, CN; R7 = H, Br; R6R7 = CH=CH-CH=CH) yielding (un)sym. substituted 3,3′-diindolylmethanes (DIMs) III have been reported. Reaction of 2-(1H-indol-3-yl)acetic acid I (R = R1 = H) with 7-azaindole led to 3-((1H-indol-3-yl)methyl)-1H-pyrrolo[2,3-b]pyridine, while 4-, 5-, and 6-azaindoles and benzimidazole reacted at the N1-nitrogen atom. Reaction of I (R = R1 = H) with 1H-indazole led to a mixture of 1-((1H-indol-3-yl)methyl)-1H-indazole and 2-((1H-indol-3-yl)methyl)-2H-indazole. The new method allows large-scale synthesis of biol. active DIMs. After reading the article, we found that the author used 5-Fluoro-1H-indole(cas: 399-52-0Application In Synthesis of 5-Fluoro-1H-indole)

5-Fluoro-1H-indole(cas: 399-52-0) is a member of aromaticfluorinated building blocks. Fluorine-containing aromatics have been incorporated into crop-protection chemicals (herbicides, insecticides, fungicides). Liquid crystals, positron emission tomography, and imaging systems represent new areas where fluoroaromatics and fluoroheterocyclics have gained attention.Application In Synthesis of 5-Fluoro-1H-indole

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

Recommanded Product: 1H-IndoleIn 2020 ,《Recent Development in Indole Derivatives as Anticancer Agents for Breast Cancer》 appeared in Anti-Cancer Agents in Medicinal Chemistry. The author of the article were Kaur, Kamalpreet; Jaitak, Vikas. The article conveys some information:

A review. Background: Breast Cancer (BC) is the second most common cause of cancer related deaths in women. Due to severe side effects and multidrug resistance, current therapies like hormonal therapy, surgery, radiotherapy and chemotherapy become ineffective. Also, the existing drugs for BC treatment are associated with several drawbacks such as poor oral bioavailability, non-selectivity and poor pharmacodynamics properties. Therefore, there is an urgent need for the development of more effective and safer anti BC agents. Objective: This article explored in detail the possibilities of indole-based heterocyclic compounds as anticancer agents with breast cancer as their major target. Methods: Recent literature related to indole derivatives endowed with encouraging anti BC potential is reviewed. With special focus on BC, this review offers a detailed account of multiple mechanisms of action of various indole derivatives: aromatase inhibitor, tubulin inhibitor, microtubule inhibitor, targeting estrogen receptor, DNA-binding mechanism, induction of apoptosis, inhibition of PI3K/AkT/NFkB/mTOR, and HDAC inhibitors, by which these derivatives have shown promising anticancer potential. Results: Exhaustive literature survey indicated that indole derivatives are associated with properties of inducing apoptosis and disturbing tubulin assembly. Indoles are also associated with the inhibition of NFkB/mTOR/PI3K/AkT and regulation of estrogen-mediated activity. Furthermore, indole derivatives have been found to modulate critical targets such as topoisomerase and HDAC. These derivatives have shown significant activity against breast cancer cells. Conclusion: In BC, indole derivatives seem to be quite competent and act through various mechanisms that are well established in case of BC. This review has shown that indole derivatives can further be explored for the betterment of BC chemotherapy. A lot of potential is still hidden which demands to be discovered for upgrading BC chemotherapy. In addition to this study using 1H-Indole, there are many other studies that have used 1H-Indole(cas: 120-72-9Recommanded Product: 1H-Indole) was used in this study.

1H-Indole(cas: 120-72-9) belongs to indole. Indole, also called Benzopyrrole, a heterocyclic organic compound occurring in some flower oils, such as jasmine and orange blossom, in coal tar, and in fecal matter. It is used in perfumery and in making tryptophan, an essential amino acid, and indoleacetic acid (heteroauxin), a hormone that promotes the development of roots in plant cuttings.Recommanded Product: 1H-Indole

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

Reference of 1H-IndoleIn 2022 ,《Diet-Microbiota Interplay: An Emerging Player in Macrophage Plasticity and Intestinal Health》 appeared in International Journal of Molecular Sciences. The author of the article were O’Mahony, Cian; Amamou, Asma; Ghosh, Subrata. The article conveys some information:

A review. Inflammatory bowel diseases (IBD) are chronic disorders of the gastrointestinal tract with an increasing prevalence worldwide. Targeted therapies for IBD are limited by several factors, including the therapeutic ceiling and the high incidence of non-responders or loss-of-response. In order to improve therapeutic efficacy, there is critical need to decipher disease pathogenesis, currently not well understood. Macrophages, innate immune cells that exhibit high plasticity, perpetuate inflammatory signalling in IBD through excessive release of inflammatory mediators. In recent years, pioneering research has revealed the importance of the interplay between macrophages and gut microbiota in maintaining intestinal homeostasis. Particular attention is focusing on microbiota-derived metabolites, believed to possess immunomodulatory properties capable of manipulating macrophage plasticity. Microbiota-derived short-chain fatty acids (SCFAs) and indole compounds, along with dietary sourced omega-3 (ω-3) polyunsaturated fatty acids (PUFA), exert anti-inflammatory effects, attributable to interactions with macrophages. Before we can effectively incorporate these metabolites into IBD therapies, a deeper understanding of microbiota-macrophage interactions at a mol. level is necessary. Therefore, the aim of this review is firstly to detail current knowledge regarding how diet and microbiota-derived metabolites modify macrophage plasticity. Later, we discuss the concept of therapeutic strategies directed at microbiota-macrophage interactions, which could be highly valuable for IBD therapies in the future. After reading the article, we found that the author used 1H-Indole(cas: 120-72-9Reference of 1H-Indole)

1H-Indole(cas: 120-72-9) belongs to indole. Indole, also called Benzopyrrole, a heterocyclic organic compound occurring in some flower oils, such as jasmine and orange blossom, in coal tar, and in fecal matter. It is used in perfumery and in making tryptophan, an essential amino acid, and indoleacetic acid (heteroauxin), a hormone that promotes the development of roots in plant cuttings.Reference of 1H-Indole

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

In 2022,Dai, Chunxiao; Ma, Fang; Ma, Qiao; Yang, Jing; Li, Yan; Yang, Bingyu; Qu, Yuanyuan published an article in Environmental Science and Pollution Research. The title of the article was 《Investigation of indole biodegradation by Cupriavidus sp. strain IDO with emphases on downstream biotransformation and indigo production》.Safety of 1H-Indole The author mentioned the following in the article:

Indole, as a typical N-heterocyclic aromatic pollutant, poses risks to living things; however, indole-biotransformation mechanisms remain under-discussed, especially those related to its downstream biotransformation. Here, we systematically investigated the characteristics of indole degradation by strain Cupriavidus sp. IDO. We found that Cupriavidus sp. IDO could utilize 25 to 150 mg/L indole within 40 h and identified three intermediates (2-oxindole, indigo, and isatin). Addnl., integrated genomics and proteomics anal. of the indole biotransformation mechanism in strain IDO revealed 317 proteins showing significant changes (262 upregulated and 55 downregulated) in the presence of indole. Among these, three clusters containing indole oxidoreductase, CoA-thioester ligase, and gentisate 1,2-oxidoreductase were identified as potentially responsible for upstream and downstream indole metabolism Moreover, HPLC-MS and -omics anal. offered insight into the indole-degradation pathway in strain IDO. Furthermore, the indole oxidoreductase IndAB, which initiates indole degradation, was heterologously expressed in Escherichia coli BL21(DE3). Optimization by the response surface methodol. resulted in a maximal production of 135.0 mg/L indigo by the recombination strains in tryptophan medium. This work enriches our understanding of the indole-biodegradation process and provides new insights into multiple indole-degradation pathways in natural environments. The experimental part of the paper was very detailed, including the reaction process of 1H-Indole(cas: 120-72-9Safety of 1H-Indole)

1H-Indole(cas: 120-72-9) belongs to indole. Indole, also called Benzopyrrole, a heterocyclic organic compound occurring in some flower oils, such as jasmine and orange blossom, in coal tar, and in fecal matter. It is used in perfumery and in making tryptophan, an essential amino acid, and indoleacetic acid (heteroauxin), a hormone that promotes the development of roots in plant cuttings.Safety of 1H-Indole

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

The author of 《Structure-based redesign of a self-sufficient flavin-containing monooxygenase towards indigo production》 were Loncar, Nikola; van Beek, Hugo L.; Fraaije, Marco W.. And the article was published in International Journal of Molecular Sciences in 2019. Product Details of 120-72-9 The author mentioned the following in the article:

Indigo is currently produced by a century-old petrochem.-based process, therefore it is highly attractive to develop a more environmentally benign and efficient biotechnol. process to produce this timeless dye. Flavin-containing monooxygenases (FMOs) are able to oxidize a wide variety of substrates. In this paper we show that the bacterial mFMO can be adapted to improve its ability to convert indole into indigo. The improvement was achieved by a combination of computational and structure-inspired enzyme redesign. We showed that the thermostability and the kcat for indole could be improved 1.5-fold by screening a relatively small number of enzyme mutants. This project not only resulted in an improved biocatalyst but also provided an improved understanding of the structural elements that determine the activity of mFMO and provides hints for further improvement of the monooxygenase as biocatalyst. The experimental part of the paper was very detailed, including the reaction process of 1H-Indole(cas: 120-72-9Product Details of 120-72-9)

1H-Indole(cas: 120-72-9) belongs to indole. Indole, also called Benzopyrrole, a heterocyclic organic compound occurring in some flower oils, such as jasmine and orange blossom, in coal tar, and in fecal matter. It is used in perfumery and in making tryptophan, an essential amino acid, and indoleacetic acid (heteroauxin), a hormone that promotes the development of roots in plant cuttings.Product Details of 120-72-9

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

Pillaiyar, Thanigaimalai; Sedaghati, Masoud; Mahardhika, Andhika B.; Wendt, Lukas L.; Mueller, Christa E. published their research in Beilstein Journal of Organic Chemistry in 2021. The article was titled 《Iodine-catalyzed electrophilic substitution of indoles: synthesis of (un)symmetrical diindolylmethanes with a quaternary carbon center》.Related Products of 399-52-0 The article contains the following contents:

A novel, versatile approach for the synthesis of unsym. 3,3′-diindolylmethanes (DIMs) with a quaternary carbon center has been developed via iodine-catalyzed coupling of trifluoromethyl(indolyl)phenylmethanols with indoles. In contrast to previously reported methods, the new procedure is characterized by chemoselectivity, mild conditions, high yields, and scalability to obtain gram amounts for biol. studies. Selected compounds were found to display affinity for cannabinoid receptors, which are promising drug targets for the treatment of inflammatory and neurodegenerative diseases. The results came from multiple reactions, including the reaction of 5-Fluoro-1H-indole(cas: 399-52-0Related Products of 399-52-0)

5-Fluoro-1H-indole(cas: 399-52-0) is a member of aromaticfluorinated building blocks. Fluorine-containing aromatics have been incorporated into crop-protection chemicals (herbicides, insecticides, fungicides). Liquid crystals, positron emission tomography, and imaging systems represent new areas where fluoroaromatics and fluoroheterocyclics have gained attention.Related Products of 399-52-0

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

Liu, Xiaoyu; He, Kun; Gao, Na; Jiang, Peiyun; Lin, Jun; Jin, Yi published their research in Chemical Communications (Cambridge, United Kingdom) in 2021. The article was titled 《A radical-mediated multicomponent cascade reaction for the synthesis of azide-biindole derivatives》.Formula: C8H6FN The article contains the following contents:

A radical-mediated, one-pot, multicomponent cascade reaction was developed for the synthesis of azide-biindole derivatives Mechanistic studies demonstrated that the nitrogen-centered free radical were formed by the reaction of heterocyclic N-H with CuII and PIFA and initiated the cascade reaction with indole to obtain the biindole intermediate. The obtained biindole intermediate then reacted with sodium azide in the presence of CuII catalyst and PIFA which then resulted in final products. This methodol. was useful for constructing other azido heterocycles. In the part of experimental materials, we found many familiar compounds, such as 5-Fluoro-1H-indole(cas: 399-52-0Formula: C8H6FN)

5-Fluoro-1H-indole(cas: 399-52-0) is a member of aromaticfluorinated building blocks. Fluorine-containing aromatics have been incorporated into crop-protection chemicals (herbicides, insecticides, fungicides). Liquid crystals, positron emission tomography, and imaging systems represent new areas where fluoroaromatics and fluoroheterocyclics have gained attention.Formula: C8H6FN

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

《The copper(II)-catalyzed and oxidant-promoted regioselective C-2 difluoromethylation of indoles and pyrroles》 was published in Chemical Communications (Cambridge, United Kingdom) in 2020. These research results belong to Zhang, Dong; Fang, Zheng; Cai, Jinlin; Liu, Chengkou; He, Wei; Duan, Jindian; Qin, Ning; Yang, Zhao; Guo, Kai. Reference of 5-Fluoro-1H-indole The article mentions the following:

A novel and efficient approach for the highly selective C-2 difluoromethylation of indole derivatives was developed by using sodium difluoromethylsulfinate (HCF2SO2Na) as the source of difluoromethyl groups and a Cu(II) complex as the catalyst. Various substrates were well tolerated in this transformation and the desired products, such as I [R = H, 3-Me, 4-Me, etc.] were obtained in moderate to good yields. Moreover, the late-stage C-2 difluoromethylation of bioactive mols. containing an indole ring was achieved in good yields. Generally, this reaction features excellent functional group compatibility, broad substrate scope and excellent C-2 selectivity. In the experiment, the researchers used 5-Fluoro-1H-indole(cas: 399-52-0Reference of 5-Fluoro-1H-indole)

5-Fluoro-1H-indole(cas: 399-52-0) is a member of aromaticfluorinated building blocks. Fluorine-containing aromatics have been incorporated into crop-protection chemicals (herbicides, insecticides, fungicides). Liquid crystals, positron emission tomography, and imaging systems represent new areas where fluoroaromatics and fluoroheterocyclics have gained attention.Reference of 5-Fluoro-1H-indole

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis 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 electrosynthesis of C2-quaternary indolin-3-ones》 was written by Lu, Fo-Yun; Chen, Yu-Jue; Chen, Yuan; Ding, Xuan; Guan, Zhi; He, Yan-Hong. COA of Formula: C8H6FN And the article was included in Chemical Communications (Cambridge, United Kingdom) in 2020. The article conveys some information:

A highly enantioselective and direct synthesis of C2-quaternary indolin-3-ones from 2-arylindoles by combining electrochem. and organocatalysis is described. Excellent enantioselectivities (up to 99% ee) and diastereoselectivities (>20 : 1) can be obtained through anodic oxidation in combination with asym. proline-catalyzed alkylation in an undivided cell under constant-current conditions. Thus, e.g., 2-phenylindole + cyclohexanone → I (67%, > 20:1 d.r., 98% ee) in presence of L-proline as chiral organic catalyst using DMF as solvent, TFE as cosolvent, TEMPO as mediator, benzoic acid as additive and tetrabutylammonium perchlorate as electrolyte in undivided cell with Pt anode and cathode. In the experiment, the researchers used 5-Fluoro-1H-indole(cas: 399-52-0COA of Formula: C8H6FN)

5-Fluoro-1H-indole(cas: 399-52-0) is a member of aromaticfluorinated building blocks. Fluorine-containing aromatics have been incorporated into crop-protection chemicals (herbicides, insecticides, fungicides). Liquid crystals, positron emission tomography, and imaging systems represent new areas where fluoroaromatics and fluoroheterocyclics have gained attention.COA of Formula: C8H6FN

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