Tag: 100-200

Discovery, synthesis and in combo studies of Schiff闂備胶鍋ㄩ崕鎶芥倶?bases as promising dipeptidyl peptidase-IV inhibitors was written by Abu Khalaf, Reema;Awad, Maha;Al-Essa, Luay;Mefleh, Sara;Sabbah, Dima;Al-Shalabi, Eveen;Shabeeb, Ihsan. And the article was included in Molecular Diversity in 2022.Application In Synthesis of Methyl 5-fluoro-1H-indole-2-carboxylate This article mentions the following:

Diabetes mellitus is a main global health apprehension. Macrovascular illnesses, neuropathy, retinopathy, and nephropathy are considered some of its severe hitches. Gliptins are a group of hypoglycemic agents that inhibit dipeptidyl peptidase-IV (DPP-IV) enzyme and support blood glucose-lowering effect of incretins. In the current research, synthesis, characterization, docking, and biol. evaluation of fourteen Schiff闂備胶鍋ㄩ崕鎶芥倶?bases 5a-f and 9a-h were carried out. Compound 9f revealed the best in vitro anti-DPP-IV activity of 35.7% inhibition at a concentration of 100 濠电偞鎸鹃幏? Compounds 9c and 9f with the highest in vitro DPP-IV inhibition were subjected to the in vivo glucose-lowering test using vildagliptin as a pos. inhibitor. Vildagliptin, 9c, and 9f showed significant reduction in the blood glucose levels of the treated mice after 30 min of glucose administration. Moreover, induced fit docking showed that these derivatives accommodated the enzyme binding site with comparable docking scores. Schiff闂備胶鍋ㄩ崕鎶芥倶?bases can serve as promising lead for the development of new DPP-IV inhibitors. In the experiment, the researchers used many compounds, for example, Methyl 5-fluoro-1H-indole-2-carboxylate (cas: 167631-84-7Application In Synthesis of Methyl 5-fluoro-1H-indole-2-carboxylate).

Methyl 5-fluoro-1H-indole-2-carboxylate (cas: 167631-84-7) 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.Application In Synthesis of Methyl 5-fluoro-1H-indole-2-carboxylate

Referemce:
Indole alkaloid derivatives as building blocks of natural products from闂佽壈浜崹淇沜illus thuringiensis闂佽壈浜粋鍧闂佽壈浜崹淇沜illus velezensis闂佽壈浜粋鍧 their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Synthesis and anticancer activity evaluation of 3-(4-oxo-2-thioxothiazolidin-5-yl)-1H-indole-carboxylic acids derivatives was written by Kryshchyshyn-Dylevych, Anna;Garazd, Myroslav;Karkhut, Andrew;Polovkovych, Sviatoslav;Lesyk, Roman. And the article was included in Synthetic Communications in 2020.Recommanded Product: 167631-84-7 This article mentions the following:

A mild and efficient method for the synthesis of 1-oxo-9H-thiopyrano[3,4-b]indole-3-carboxylic acids I (R = F, H, OMe) and dimerized 3-(4-carboxy-1H-3-indolyl)-2-propenoic acids II (R¹ = Me, Et) via alk. hydrolysis of 3-(rhodanin-5-yl)-1H-indole-2-carboxylic acids derivatives III (R² = H, methoxycarbonyl; R³ = H, methoxycarbonyl, carboxy; R⁴ = H, Me, Et) was elaborated. Anticancer activity screening in NCI60-cell lines assay allowed identification of III (R = F; R² = R⁴ = H; R³ = methoxycarbonyl) with significant antimitotic activity at micromolar and submicromolar concentrations In the experiment, the researchers used many compounds, for example, Methyl 5-fluoro-1H-indole-2-carboxylate (cas: 167631-84-7Recommanded Product: 167631-84-7).

Methyl 5-fluoro-1H-indole-2-carboxylate (cas: 167631-84-7) belongs to indole derivatives. Indole is an important structural motif of various drugs, therapeutic leads besides its prevalence in numerous natural products, agrochemicals, perfumery, and dyes. Due to this activity, the indole ring system has become an important component or intermediate in the synthesis of heterocycles.Recommanded Product: 167631-84-7

Referemce:
Indole alkaloid derivatives as building blocks of natural products from闂佽壈浜崹淇沜illus thuringiensis闂佽壈浜粋鍧闂佽壈浜崹淇沜illus velezensis闂佽壈浜粋鍧 their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Discovery of Indole- and Indazole-acylsulfonamides as Potent and Selective Na_V1.7 Inhibitors for the Treatment of Pain was written by Luo, Guanglin;Chen, Ling;Easton, Amy;Newton, Amy;Bourin, Clotilde;Shields, Eric;Mosure, Kathy;Soars, Matthew G.;Knox, Ronald J.;Matchett, Michele;Pieschl, Rick L.;Post-Munson, Debra J.;Wang, Shuya;Herrington, James;Graef, John;Newberry, Kimberly;Sivarao, Digavalli V.;Senapati, Arun;Bristow, Linda J.;Meanwell, Nicholas A.;Thompson, Lorin A.;Dzierba, Carolyn. And the article was included in Journal of Medicinal Chemistry in 2019.Category: indole-building-block This article mentions the following:

3-Aryl-indole and 3-aryl-indazole derivatives were identified as potent and selective Na_v1.7 inhibitors. Compound I was shown to be efficacious in the mouse formalin assay and also reduced complete Freund’s adjuvant (CFA)-induced thermal hyperalgesia and chronic constriction injury (CCI) induced cold allodynia and models of inflammatory and neuropathic pain, resp., following i.p. (IP) doses of 30 mg/kg. The observed efficacy could be correlated with the mouse dorsal root ganglion exposure and Na_V1.7 potency associated with I. In the experiment, the researchers used many compounds, for example, 1H-Pyrrolo[2,3-b]pyridine-6-carboxylic acid (cas: 898746-35-5Category: indole-building-block).

1H-Pyrrolo[2,3-b]pyridine-6-carboxylic acid (cas: 898746-35-5) belongs to indole derivatives. Indole is an important structural motif of various drugs, therapeutic leads besides its prevalence in numerous natural products, agrochemicals, perfumery, and dyes. They are capable of binding to a variety of receptors with high affinity and thus have applications in a wide range of therapeutic areas.Category: indole-building-block

Referemce:
Indole alkaloid derivatives as building blocks of natural products from闂佽壈浜崹淇沜illus thuringiensis闂佽壈浜粋鍧闂佽壈浜崹淇沜illus velezensis闂佽壈浜粋鍧 their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Synthesis, cytotoxic, antioxidant and anti-inflammatory activity of 3-((3-((6-benzoyl-1H-benz [D]imidazol-2-YL) amino)-5-mercapto- 4H-1,2, 4-triazol-4-YL) imino)substituted indol-2-ones was written by Rani, B. Shoba;Blessi, Priyanka K.;Sammaiah, G.. And the article was included in American Journal of PharmTech Research in 2016.HPLC of Formula: 112656-95-8 This article mentions the following:

In the present study novel series of 3-((3-((6-benzoyl-1H-benz[d]imidazol-2-yl) amino)-5- mercapto-4H-1, 2, 4-triazol-4-yl)imino)substituted indolin-2-ones have been synthesized in good yields and characterized by IR, NMR and Mass spectral analyses. Compounds were evaluated for their preliminary in vitro cytotoxic activity against HCT-116 (colon), MCF-7 (breast), HeLa (cervical) and HepG2 (hepatocellular) cancer cell lines by standard MTT assay method, antioxidant activity by standard DPPH assay method and also were screened for in vitro antiinflammatory activity. In the experiment, the researchers used many compounds, for example, 7-Nitroindoline-2,3-dione (cas: 112656-95-8HPLC of Formula: 112656-95-8).

7-Nitroindoline-2,3-dione (cas: 112656-95-8) belongs to indole derivatives. Indole is an important structural motif of various drugs, therapeutic leads besides its prevalence in numerous natural products, agrochemicals, perfumery, and dyes. They are capable of binding to a variety of receptors with high affinity and thus have applications in a wide range of therapeutic areas.HPLC of Formula: 112656-95-8

Referemce:
Indole alkaloid derivatives as building blocks of natural products from闂佽壈浜崹淇沜illus thuringiensis闂佽壈浜粋鍧闂佽壈浜崹淇沜illus velezensis闂佽壈浜粋鍧 their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

New Generation of Selective Androgen Receptor Degraders: Our Initial Design, Synthesis, and Biological Evaluation of New Compounds with Enzalutamide-Resistant Prostate Cancer Activity was written by Hwang, Dong-Jin;He, Yali;Ponnusamy, Suriyan;Mohler, Michael L.;Thiyagarajan, Thirumagal;McEwan, Iain J.;Narayanan, Ramesh;Miller, Duane D.. And the article was included in Journal of Medicinal Chemistry in 2019.Electric Literature of C8H6N2O2 This article mentions the following:

In our effort to find small-mol. treatments of advanced prostate cancers (PCs), a novel series of indolyl and indolinyl propanamides (series II and III) were discovered as selective androgen receptor degraders (SARDs). Initial studies of androgen receptor (AR) antagonist (1) and agonist (2) propanamides yielded a tertiary aniline (3) with novel SARD activity but poor metabolic stability. Cyclization to II and III produced submicromolar AR antagonism and protein degradation selective to AR and AR splice variant (AR SV). II and III maintained potency against enzalutamide-resistant (Enz-R) mutant ARs and PC cells and were efficacious in Enz-R xenografts, suggesting their potential to treat advanced PCs. Design, synthesis, and biol. activity of novel SARDs that could potentially be used for the treatment of a wide spectrum of PCs including castration-resistant, Enz-R, and/or AR SV-dependent advanced PCs that are often untreatable with known hormone therapies are discussed. In the experiment, the researchers used many compounds, for example, 6-Nitro-1H-indole (cas: 4769-96-4Electric Literature of C8H6N2O2).

6-Nitro-1H-indole (cas: 4769-96-4) belongs to indole derivatives. Indole is an important structural motif of various drugs, therapeutic leads besides its prevalence in numerous natural products, agrochemicals, perfumery, and dyes. In addition to indole, the strain-release chemistry worked for numerous substrates including amines, alcohols, thiols, carboxylic acids, imidazoles, and pyrazoles.Electric Literature of C8H6N2O2

Referemce:
Indole alkaloid derivatives as building blocks of natural products from闂佽壈浜崹淇沜illus thuringiensis闂佽壈浜粋鍧闂佽壈浜崹淇沜illus velezensis闂佽壈浜粋鍧 their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Synthesis of Quinoline-4-carboxamides and Quinoline-4-carboxylates via a Modified Pfitzinger Reaction of N-Vinylisatins was written by Mijangos, Marco V.;Amador-Sanchez, Yoarhy A.;Miranda, Luis D.. And the article was included in European Journal of Organic Chemistry in 2021.Recommanded Product: 150560-58-0 This article mentions the following:

A synthetic approach for the accelerated assembly of quinoline-4-carboxamide and quinoline-4-carboxylate nuclei is presented. The methodol. is based on the rearrangement of N-vinylisatins promoted by different types of amines (or ethanol) in a Pfitzinger-type mechanism that, in turn, builds the quinoline ring system. The reaction took place only by heating the starting materials in ethanol, without any additive. In the experiment, the researchers used many compounds, for example, 5-Isopropylindoline-2,3-dione (cas: 150560-58-0Recommanded Product: 150560-58-0).

5-Isopropylindoline-2,3-dione (cas: 150560-58-0) belongs to indole derivatives. Indole is an important structural motif of various drugs, therapeutic leads besides its prevalence in numerous natural products, agrochemicals, perfumery, and dyes. They are capable of binding to a variety of receptors with high affinity and thus have applications in a wide range of therapeutic areas.Recommanded Product: 150560-58-0

Referemce:
Indole alkaloid derivatives as building blocks of natural products from闂佽壈浜崹淇沜illus thuringiensis闂佽壈浜粋鍧闂佽壈浜崹淇沜illus velezensis闂佽壈浜粋鍧 their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Synthesis of 1-(3-aminopropyl)indoles and 3-indol-1-ylpropionic acids was written by Basanagoudar, L. D.;Siddappa, S.. And the article was included in Journal of the Chemical Society [Section] C: Organic in 1967.Synthetic Route of C11H11NO2 This article mentions the following:

Various substituted indoles and their derivatives were condensed with acrylonitrile in the presence of trimethylbenzylammonium hydroxide to give the corresponding 3-indol-1-ylpropionitriles. These nitriles were reduced catalytically with Raney nickel to the corresponding 1-(3-aminopropyl)indoles, or hydrolyzed to the corresponding 3-indol-1-ylpropionic acids. Some of the nitriles were formylated to give the corresponding 1-(2-cyanoethyl)indole-3-carboxaldehydes. In the experiment, the researchers used many compounds, for example, 3-(1H-Indol-1-yl)propanoic acid (cas: 6639-06-1Synthetic Route of C11H11NO2).

3-(1H-Indol-1-yl)propanoic acid (cas: 6639-06-1) 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 C11H11NO2

Referemce:
Indole alkaloid derivatives as building blocks of natural products from闂佽壈浜崹淇沜illus thuringiensis闂佽壈浜粋鍧闂佽壈浜崹淇沜illus velezensis闂佽壈浜粋鍧 their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Synthesis and screening N-(2, 4-dioxo-1, 2-dihydro-3H-spiro [indole-3, 2-[1,3]thiazolidin]-3-yl)-2-hydroxybenzamides for anti-bacterial activity was written by Devi, N. Saritha;Srinivas, B.;Sarangapani, Manda. And the article was included in International Journal of Pharmaceutical Sciences and Research in 2019.Name: 7-Nitroindoline-2,3-dione This article mentions the following:

A novel synthesis of N-(2, 4-dioxo-1, 2-dihydro-3H-spiro [indole-3, 2-[1, 3] thiazolidin]-3-yl)-2-hydroxybenzamide derivatives were synthesized by cyclization of isatin hydrazones with thioglycolic acid. The synthesized compounds were characterized by spectral data (IR, 1H-NMR, Mass) and evaluated for antibacterial activity against various strains of bacteria at the concentrations of 200濠电偞鎸鹃幐?mL. Among the tested compounds X(i) is highly active against E. coli, X(f) is active against B. subtilis, X(h) is active against S. aureus and X(c) is active against S. typhi. In the experiment, the researchers used many compounds, for example, 7-Nitroindoline-2,3-dione (cas: 112656-95-8Name: 7-Nitroindoline-2,3-dione).

7-Nitroindoline-2,3-dione (cas: 112656-95-8) 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.Name: 7-Nitroindoline-2,3-dione

Referemce:
Indole alkaloid derivatives as building blocks of natural products from闂佽壈浜崹淇沜illus thuringiensis闂佽壈浜粋鍧闂佽壈浜崹淇沜illus velezensis闂佽壈浜粋鍧 their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Cyclocondensation reactions of heterocyclic carbonyl compounds. I. Synthesis of some 6-substituted 2,3-dihydro-5H-1,2,4-triazino[5,6-b]indole-3-thiones was written by Hlavac, Jan;Slouka, Jan. And the article was included in Acta Universitatis Palackianae Olomucensis, Facultas Rerum Naturalium in 1993.Category: indole-building-block This article mentions the following:

Condensation of 7-nitroisatin and 7-methylisatin with thiosemicarbazide in acetic acid gave the corresponding 闁?thiosemicarbazones. These 闁?thiosemicarbazones were converted into 1,2,4-triazino[6,5-b]indole-3-thiones I (R = NO₂, Me). In the experiment, the researchers used many compounds, for example, 7-Nitroindoline-2,3-dione (cas: 112656-95-8Category: indole-building-block).

7-Nitroindoline-2,3-dione (cas: 112656-95-8) 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.Category: indole-building-block

Referemce:
Indole alkaloid derivatives as building blocks of natural products from闂佽壈浜崹淇沜illus thuringiensis闂佽壈浜粋鍧闂佽壈浜崹淇沜illus velezensis闂佽壈浜粋鍧 their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Revisiting the reduction of indoles by hydroboranes: A combined experimental and computational study was written by Jayaraman, Arumugam;Powell-Davies, Henry;Fontaine, Frederic-Georges. And the article was included in Tetrahedron in 2019.Synthetic Route of C8H6N2O2 This article mentions the following:

A combined exptl. and d. functional computational study was used to probe the mechanism for the reduction of indoles using simple borane BH₃闁荤姾娅ｉ弸宄係 (DMS = di-Me sulfide). Exptl. and computational studies all steer to the formation of the reduced species 1-BH₂-indolines as the resting state for this reaction, as opposed to the historically presumed formation of the unreduced 1-BH₂-indoles, before the addition of a proton source to form the final product indolines. Furthermore, it was observed that mol. H₂ was generated and consumed in the reaction. Computations put forward hydroboration followed by protodeborylation as the very reasonable mechanistic route for the formation of exptl. observed major intermediate 1-BH₂ indolines. For the H₂ consumption in the reaction, computations suggest the frustrated Lewis pair-type heterolytic splitting of H₂ by a bis(3-indolinyl)borane intermediate. In the experiment, the researchers used many compounds, for example, 6-Nitro-1H-indole (cas: 4769-96-4Synthetic Route of C8H6N2O2).

6-Nitro-1H-indole (cas: 4769-96-4) 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). Synthetic Route of C8H6N2O2

Referemce:
Indole alkaloid derivatives as building blocks of natural products from闂佽壈浜崹淇沜illus thuringiensis闂佽壈浜粋鍧闂佽壈浜崹淇沜illus velezensis闂佽壈浜粋鍧 their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles