Tag: 100-200

Quality Control of 1H-IndoleIn 2019 ,《Effective removal of nitrogen compounds from model diesel fuel by easy-to-prepare ionic liquids》 appeared in Separation and Purification Technology. The author of the article were Fan, Yunchang; Cai, Dongxu; Zhang, Sheli; Wang, Huiying; Guo, Kaigang; Zhang, Lei; Yang, Lei. The article conveys some information:

The removal of nitrogen compounds by liquid-liquid extraction using ionic liquids (ILs) as extraction solvents has been limited by the lack of easy-to-prepare, low cost and highly efficient ILs. To overcome this limitation, the present work synthesized protic ILs (PILs) via acid-base reaction and investigated their extraction ability for nitrogen compounds (quinoline, indole and carbazole) from model fuel (n-dodecane). Exptl. results suggested that the PIL, triethylammonium p-toluenesulfonate (TEA-TSA), exhibited higher extraction ability for indole and carbazole as compared to the 1-butyl-3-methylimidazolium ([C4mim]+) based ILs due to the stronger π-π interaction between TEA-TSA and nitrogen compounds Among a number of ILs, TEA-TSA containing a slight excess of p-toluenesulfonic acid (2%, molar percent) was particularly promising as extractant because of its excellent extraction performance for the basic and neutral nitrogen compounds Furthermore, the suggested PIL could be easily regenerated and reused via a back extraction process. The results showed that extractive denitrogenation using PILs as extractants was a potential technique to produce clean fuel considering their stronger extraction ability, lower-cost and easy-to-prepare characteristics. In the experiment, the researchers used many compounds, for example, 1H-Indole(cas: 120-72-9Quality Control 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.Quality Control 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 《Antistaphylococcal evaluation of indole-naphthalene hybrid analogs》 were Ashraf, Kerolos; Yasrebi, Kaveh; Adeniyi, Emmanuel Tola; Hertlein, Tobias; Ohlsen, Knut; Lalk, Michael; Erdmann, Frank; Hilgeroth, Andreas. And the article was published in Drug Design, Development and Therapy in 2019. Quality Control of 1H-Indole The author mentioned the following in the article:

Resistance developments against established antibiotics are an emerging problem for antibacterial therapies. Infections with Staphylococcus aureus and methicillin-resistant S. aureus (MRSA) have become more difficult to treat with standard antibiotics that often fail, especially against MRSA. In consequence, novel antibiotics are urgently needed. Antibiotics from natural sources own complicated structures that cause difficulties for a chem. synthetic production We developed novel small-mol. antibacterials that are easily accessible in a simple one-pot synthesis. The central indolonaphthalene core is substituted with indole residues at various positions. Both the varied indole substitutions and their positions at the mol. scaffold influence the determined antibacterial activity against the evaluated Staphylococcus strains. Best activities have been found for 5-chloro, -cyano, and -hydroxyl indole substitutions. Therefore, first promising lead compounds could be identified that are nontoxic in human HEK and SH-SY5Y cells and exceed the activity of used standard antibiotics, especially against MRSA. In the experiment, the researchers used 1H-Indole(cas: 120-72-9Quality Control 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.Quality Control 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

Name: 4-Chloro-1H-indol-7-amineOn June 5, 2000, Owa, Takashi; Okauchi, Tatsuo; Yoshimatsu, Kentaro; Sugi, Naoko Hata; Ozawa, Yoichi; Nagasu, Takeshi; Koyanagi, Nozomu; Okabe, Tadashi; Kitoh, Kyosuke; Yoshino, Hiroshi published an article in Bioorganic & Medicinal Chemistry Letters. The article was 《A focused compound library of novel N-(7-indolyl)benzenesulfonamides for the discovery of potent cell cycle inhibitors》. The article mentions the following:

A series of compounds containing an N-(7-indolyl)benzenesulfonamide pharmacophore, e.g. I, was synthesized and evaluated as a potential antitumor agent. Cell cycle anal. with P388 murine leukemia cells revealed that there were two different classes of potent cell cycle inhibitors; one disrupted mitosis and the other caused G1 accumulation. The structure-activity relationships of the substituent patterns on this pharmacophore template are described. In the experimental materials used by the author, we found 4-Chloro-1H-indol-7-amine(cas: 292636-12-5Name: 4-Chloro-1H-indol-7-amine)

4-Chloro-1H-indol-7-amine(cas: 292636-12-5) belongs to anime. Large quantities of aliphatic amines are made synthetically. The most widely used industrial method is the reaction of alcohols with ammonia at a high temperature, catalyzed by metals or metal oxide catalysts (e.g., nickel or copper). Mixtures of primary, secondary, and tertiary amines are thereby produced.Name: 4-Chloro-1H-indol-7-amine

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

Category: indole-building-blockIn 2019 ,《Identification and functional study of an iif2 gene cluster for indole degradation in Burkholderia sp. IDO3》 was published in International Biodeterioration & Biodegradation. The article was written by Ma, Qiao; Yang, Bingyu; Qu, Hui; Gao, Zhen; Qu, Yuanyuan; Sun, Yeqing. The article contains the following contents:

Burkholderia sp. IDO3 is an indole-degrading bacterium isolated from activated sludge. A previous genomic clone library assay identified an iif1 gene cluster for indole metabolism in strain IDO3. To further explore the underlying indole degradation mechanisms, the complete genome of strain IDO3 was sequenced (8,003,806 bp). The genome contained three circular chromosomes and one plasmid, and 7550 genes were predicted. Interestingly, in addition to iif1 on chromosome 3, bioinformatic analyses identified a second indole oxygenase gene cluster, iif2, on chromosome 1. Both iif clusters were up-regulated in response to indole. Heterologous expression of iifC1D1 and iifC2D2 in Escherichia coli BL21(DE3) demonstrated that these genes were capable of oxidizing indole to indigo. Gene knockout assays provided addnl. evidence that iifC2 played crucial roles in indole metabolism In addition, we identified a novel gene (iifF) in the iif2 cluster. This gene was shown to encode an isatin hydrolase. IifF was expressed in E. coli, and a purified his-tagged enzyme preparation was obtained. IifF converted isatin to isatinate with Km of 4.4 ± 0.7μM and kcat of 95.5 ± 4 s-1. This is the first study to show that indole can be degraded by two iif gene clusters, and that isatin hydrolase is involved in indole metabolism, improving our understanding of indole metabolic processes. The results came from multiple reactions, including the reaction of 1H-Indole(cas: 120-72-9Category: indole-building-block)

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.Category: indole-building-block

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

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

Category: indole-building-blockIn 2021 ,《Indole scaffolds as a promising class of the aryl hydrocarbon receptor ligands》 appeared in European Journal of Medicinal Chemistry. The author of the article were Dvorak, Zdenek; Poulikova, Karolina; Mani, Sridhar. The article conveys some information:

A review. The aryl hydrocarbon receptor (AhR), deemed initially as a xenobiotic sensor, plays multiple physiol. roles and is involved in various pathophysiol. processes and many diseases etiol. Therefore, the therapeutic and chemopreventive targeting of AhR is a fundamental issue. To date, thousands of structurally diverse ligands of AhR have been identified. The bottleneck in targeting the AhR is that it is a Janus-faced player with beneficial vs. harmful effects in the ligand-specific context. A distinct structural class of the AhR ligands is those with indole-based scaffolds. The present review summarizes the knowledge on the existing indole-derived AhR ligands, comprising natural and dietary compounds, synthetic compounds including clin. used drugs, endogenous intermediary metabolites, and catabolites produced by human microbiota. The examples of novel, indole ring containing, rational design based AhR ligands are presented. The mol., in vitro, and in vivo effects are described. In the experiment, the researchers used many compounds, for example, 1H-Indole(cas: 120-72-9Category: indole-building-block)

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.Category: indole-building-block

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

Name: 1H-IndoleIn 2021 ,《An insight in anti-malarial potential of indole scaffold: A review》 appeared in European Journal of Medicinal Chemistry. The author of the article were Chauhan, Mehak; Saxena, Anjali; Saha, Biswajit. The article conveys some information:

A review. Malaria is a major parasitic disease in tropical and sub-tropical regions. Pertaining to the sustaining resistance in malarial parasite against the available drugs, novel treatment options are the need of the hour. In this resolve recently, focus has shifted to finding the natural alternatives that possess anti-plasmodial activity for combating malaria. Drawing on the text written in ancient scriptures and Ayurveda, natural compounds are now being screened for their therapeutic properties. Indole is one such natural compound, present in all living organisms, it displays a range of therapeutic activities including anticancer, anti-inflammatory, antimalarial etc. In this review, we have discussed various indole scaffold as well as the semi-synthetic drugs containing indole moiety that have been synthesized for malaria treatment. The experimental part of the paper was very detailed, including the reaction process of 1H-Indole(cas: 120-72-9Name: 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.Name: 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

Name: 4-Chloro-1H-indol-7-amineOn June 5, 2000, Owa, Takashi; Okauchi, Tatsuo; Yoshimatsu, Kentaro; Sugi, Naoko Hata; Ozawa, Yoichi; Nagasu, Takeshi; Koyanagi, Nozomu; Okabe, Tadashi; Kitoh, Kyosuke; Yoshino, Hiroshi published an article in Bioorganic & Medicinal Chemistry Letters. The article was 《A focused compound library of novel N-(7-indolyl)benzenesulfonamides for the discovery of potent cell cycle inhibitors》. The article mentions the following:

A series of compounds containing an N-(7-indolyl)benzenesulfonamide pharmacophore, e.g. I, was synthesized and evaluated as a potential antitumor agent. Cell cycle anal. with P388 murine leukemia cells revealed that there were two different classes of potent cell cycle inhibitors; one disrupted mitosis and the other caused G1 accumulation. The structure-activity relationships of the substituent patterns on this pharmacophore template are described. In the experimental materials used by the author, we found 4-Chloro-1H-indol-7-amine(cas: 292636-12-5Name: 4-Chloro-1H-indol-7-amine)

4-Chloro-1H-indol-7-amine(cas: 292636-12-5) belongs to anime. Large quantities of aliphatic amines are made synthetically. The most widely used industrial method is the reaction of alcohols with ammonia at a high temperature, catalyzed by metals or metal oxide catalysts (e.g., nickel or copper). Mixtures of primary, secondary, and tertiary amines are thereby produced.Name: 4-Chloro-1H-indol-7-amine

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

Category: indole-building-blockIn 2019 ,《Identification and functional study of an iif2 gene cluster for indole degradation in Burkholderia sp. IDO3》 was published in International Biodeterioration & Biodegradation. The article was written by Ma, Qiao; Yang, Bingyu; Qu, Hui; Gao, Zhen; Qu, Yuanyuan; Sun, Yeqing. The article contains the following contents:

Burkholderia sp. IDO3 is an indole-degrading bacterium isolated from activated sludge. A previous genomic clone library assay identified an iif1 gene cluster for indole metabolism in strain IDO3. To further explore the underlying indole degradation mechanisms, the complete genome of strain IDO3 was sequenced (8,003,806 bp). The genome contained three circular chromosomes and one plasmid, and 7550 genes were predicted. Interestingly, in addition to iif1 on chromosome 3, bioinformatic analyses identified a second indole oxygenase gene cluster, iif2, on chromosome 1. Both iif clusters were up-regulated in response to indole. Heterologous expression of iifC1D1 and iifC2D2 in Escherichia coli BL21(DE3) demonstrated that these genes were capable of oxidizing indole to indigo. Gene knockout assays provided addnl. evidence that iifC2 played crucial roles in indole metabolism In addition, we identified a novel gene (iifF) in the iif2 cluster. This gene was shown to encode an isatin hydrolase. IifF was expressed in E. coli, and a purified his-tagged enzyme preparation was obtained. IifF converted isatin to isatinate with Km of 4.4 ± 0.7μM and kcat of 95.5 ± 4 s-1. This is the first study to show that indole can be degraded by two iif gene clusters, and that isatin hydrolase is involved in indole metabolism, improving our understanding of indole metabolic processes. The results came from multiple reactions, including the reaction of 1H-Indole(cas: 120-72-9Category: indole-building-block)

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.Category: indole-building-block

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