Tag: M.W=250-300

El-Gendy, Adel A. published the artcileSynthesis and antihypertensive activity of certain Mannich bases of 2-ethoxycarbonylindoles and 5H-pyridazino[4,5-b]indoles, SDS of cas: 100123-25-9, the publication is Archives of Pharmacal Research (2001), 24(1), 21-26, database is CAplus and MEDLINE.

The synthesis of 3-(aminomethyl)-1H-indole-2-carboxylic acid Et ester derivatives and of 3-(aminomethyl)-3,5-dihydro-4H-pyridazino[4,5-b]indol-4-one derivatives was reported. Fourteen of the synthesized Mannich bases were screened as antihypertensive agents in normotensive anesthetized rats. The effect of 3-[(diethylamino)methyl]-1H-indole-2-carboxylic acid Et ester hydrochloride in normotensive anesthetized dogs was also studied.

Archives of Pharmacal Research published new progress about 100123-25-9. 100123-25-9 belongs to indole-building-block, auxiliary class Indole,Bromide,Ester,Aldehyde, name is Ethyl 5-bromo-3-formyl-1H-indole-2-carboxylate, and the molecular formula is C12H10BrNO3, SDS of cas: 100123-25-9.

Referemce:
https://www.nature.com/articles/s41429-020-0333-2,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

De Mauri, Andreana published the artcileProbiotics-addicted low-protein diet for microbiota modulation in patients with advanced chronic kidney disease (ProLowCKD): A protocol of placebo-controlled randomized trial, Recommanded Product: Potassium 1H-indol-3-yl sulfate, the publication is Journal of Functional Foods (2020), 104133, database is CAplus.

Microbiota is a term coined to describe the population of bacteria, viruses and fungi that inhabit in symbiosis within a living host. A connection between unbalanced microbiota and chronic kidney disease has been established. In these patients, high levels of urea reach the intestine promoting the overgrowth of bacterial species that are prone to generate uremic toxins. Due to the high morbidity and mortality of this condition, a large number of therapeutic approaches to reduce inflammation and microbial uremic toxins have been proposed, with controversial results. A low protein diet, with a protein intake of 0.6-0.8 g/kg of body weight, is a useful and historically pursued option with this regard. The aim of our study is to evaluate, among patients with advanced renal failure not on dialysis, the synergic beneficial effects of this diet and the selected probiotics Bifidobacterium longum (mix DLBL) and Lactobacillus reuteri LRE02 (DSM 23878).

Journal of Functional Foods published new progress about 2642-37-7. 2642-37-7 belongs to indole-building-block, auxiliary class Indole,Salt,Sulfonate,Inhibitor,Inhibitor, name is Potassium 1H-indol-3-yl sulfate, and the molecular formula is C8H6KNO4S, Recommanded Product: Potassium 1H-indol-3-yl sulfate.

Referemce:
https://www.nature.com/articles/s41429-020-0333-2,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Matsuo, Yusuke published the artcileFacile synthesis of fluorescent hetero[8]circulene analogues with tunable solubilities and optical properties, COA of Formula: C14H17BClNO2, the publication is Chemical Science (2019), 10(48), 11006-11012, database is CAplus and MEDLINE.

Hetero[8]circulenes are an interesting class of polycyclic heteroaromatic mols. having rigid and planar structures, which are promising in light of their potential applications for OLEDs, OFETs and so forth. Although their synthetic methods have been developed in some specific cases, a facile synthetic protocol of novel hetero[8]circulenes with tunable properties is highly desirable. We herein report the unexpected formation of methoxy-substituted quasi-aza[8]circulene and its conversion into unprecedented triazaoxa[8]circulene. The structures and optical properties were comparatively studied. Remarkably, triazaoxa[8]circulene is highly soluble in THF, acetone and DMSO mainly because of effective hydrogen-bonding of the NH moieties to these solvents. Their highly soluble nature in various solvents enabled us to study the solvent effects of these mols. In particular, triazaoxa[8]circulene displays a high fluorescence quantum yield of 0.72 in DMSO. Furthermore, enantiomeric separation of highly distorted quasi-aza[8]circulene was successfully achieved by chiral HPLC. Thus, these novel hetero[8]circulene derivatives are practically useful fluorescent nanographene-like mols. with intriguing optical properties.

Chemical Science published new progress about 1256358-91-4. 1256358-91-4 belongs to indole-building-block, auxiliary class Indole,Chloride,Boronic acid and ester,Boronate Esters,Boronic Acids,Boronic acid and ester, name is 5-Chloro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole, and the molecular formula is C14H17BClNO2, COA of Formula: C14H17BClNO2.

Referemce:
https://www.nature.com/articles/s41429-020-0333-2,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Matsuo, Yusuke published the artcileFacile synthesis of fluorescent hetero[8]circulene analogues with tunable solubilities and optical properties, Synthetic Route of 683229-62-1, the publication is Chemical Science (2019), 10(48), 11006-11012, database is CAplus and MEDLINE.

Hetero[8]circulenes are an interesting class of polycyclic heteroaromatic mols. having rigid and planar structures, which are promising in light of their potential applications for OLEDs, OFETs and so forth. Although their synthetic methods have been developed in some specific cases, a facile synthetic protocol of novel hetero[8]circulenes with tunable properties is highly desirable. We herein report the unexpected formation of methoxy-substituted quasi-aza[8]circulene and its conversion into unprecedented triazaoxa[8]circulene. The structures and optical properties were comparatively studied. Remarkably, triazaoxa[8]circulene is highly soluble in THF, acetone and DMSO mainly because of effective hydrogen-bonding of the NH moieties to these solvents. Their highly soluble nature in various solvents enabled us to study the solvent effects of these mols. In particular, triazaoxa[8]circulene displays a high fluorescence quantum yield of 0.72 in DMSO. Furthermore, enantiomeric separation of highly distorted quasi-aza[8]circulene was successfully achieved by chiral HPLC. Thus, these novel hetero[8]circulene derivatives are practically useful fluorescent nanographene-like mols. with intriguing optical properties.

Chemical Science published new progress about 683229-62-1. 683229-62-1 belongs to indole-building-block, auxiliary class Indole,Boronic acid and ester,Ether,Boronate Esters,Boronic Acids,Boronic acid and ester, name is 5-Methoxy-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole, and the molecular formula is C15H20BNO3, Synthetic Route of 683229-62-1.

Referemce:
https://www.nature.com/articles/s41429-020-0333-2,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Zhu, Wei published the artcileDesign, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer, COA of Formula: C14H18BNO3, the publication is Journal of Medicinal Chemistry (2017), 60(14), 6018-6035, database is CAplus and MEDLINE.

A novel series of pyridin-3-amine derivatives were designed, synthesized, and evaluated as multitargeted protein kinase inhibitors for the treatment of non-small cell lung cancer (NSCLC). Hit 1 was first disclosed by in silico screening against fibroblast growth factor receptors (FGFR), which was subsequently validated by in vitro experiments The structure-activity relationship (SAR) of its analogs was then explored to afford novel FGFR inhibitors. Among them, I showed potent inhibition against FGFR1, 2, and 3. Interestingly, compound I not only inhibited various phosphorylation and downstream signaling across different oncogenic forms in FGFR-overactivated cancer cells but also showed nanomolar level inhibition against several other NSCLC-related oncogene kinases, including RET, EGFR, EGFR/T790M/L858R, DDR2, and ALK. Finally, in vivo pharmacol. evaluations of I showed significant antitumor activity (TGI = 66.1%) in NCI-H1581 NSCLC xenografts with a good pharmacokinetic profile.

Journal of Medicinal Chemistry published new progress about 837392-64-0. 837392-64-0 belongs to indole-building-block, auxiliary class Indoline,Boronic acid and ester,Amide,Boronate Esters, name is 5-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)indolin-2-one, and the molecular formula is C5H6N2O2, COA of Formula: C14H18BNO3.

Referemce:
https://www.nature.com/articles/s41429-020-0333-2,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Paul, Sulagna published the artcileIr-catalyzed functionalization of 2-substituted indoles at the 7-position: Nitrogen-directed aromatic borylation, Recommanded Product: 2-Methyl-7-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole, the publication is Journal of the American Chemical Society (2006), 128(49), 15552-15553, database is CAplus and MEDLINE.

Ir-catalyzed borylation of 2-substituted indoles selectively yielded 7-borylated products, e.g., I (R = H, Cl or OMe) in good yields. N-Protection, required for previous functionalizations of 2-substituted indoles, was unnecessary.

Journal of the American Chemical Society published new progress about 919119-59-8. 919119-59-8 belongs to indole-building-block, auxiliary class Indole,Boronic acid and ester,Boronate Esters,Boronic Acids,Boronic acid and ester, name is 2-Methyl-7-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole, and the molecular formula is C15H20BNO2, Recommanded Product: 2-Methyl-7-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole.

Referemce:
https://www.nature.com/articles/s41429-020-0333-2,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Liu, Hong published the artcileDesign and evaluation of novel tetracyclic benzofurans as palm site allosteric inhibitors of HCV NS5B polymerase, Name: 4-Fluoro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole, the publication is Bioorganic & Medicinal Chemistry Letters (2019), 29(24), 126104, database is CAplus and MEDLINE.

Hepatitis C virus (HCV) NS5B polymerase is a prime target for the development of direct-acting antiviral drugs for the treatment of chronic HCV infection. Several novel and potent HCV NS5B non-nucleoside inhibitors with unique tetracyclic benzofuran-based structures were prepared and evaluated. Similar to clin. developmental compound MK-8876, N-linked (compounds 1 and 2) and C-linked (compounds 3 and 4) tetracyclic structures maintained broad spectrum anti-replicon potency profiles and demonstrated moderate to excellent oral bioavailability and pharmacokinetic parameters across the three preclin. animal species. To better understand the importance of tetracyclic structures related to pan genotypic potency profiles especially against clin. relevant GT1a variants, the teracycles with different ring size were prepared and in vitro evaluations suggested compounds with six number ring have better overall potency profiles.

Bioorganic & Medicinal Chemistry Letters published new progress about 1256359-96-2. 1256359-96-2 belongs to indole-building-block, auxiliary class Indole,Fluoride,Boronic acid and ester,Boronic Acids,Boronate Esters,Boronate Esters, name is 4-Fluoro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole, and the molecular formula is C14H17BFNO2, Name: 4-Fluoro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole.

Referemce:
https://www.nature.com/articles/s41429-020-0333-2,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Podevin, R. A. published the artcileConcentrative PAH transport by rabbit kidney slices in the absence of metabolic energy, Category: indole-building-block, the publication is American Journal of Physiology (1978), 235(4), F278-F285, database is CAplus and MEDLINE.

Characteristics of p-aminohippurate (PAH) transport in the absence of intracellular metabolism were studied with Na⁺,K⁺-depleted and ouabain-poisoned rabbit kidney cortex slices. The imposition of a NaCl gradient (out to in) resulted in specific stimulation of PAH uptake. PAH accumulated against its concentration gradient when cell Na⁺ concentration [Na⁺] was less than medium [Na⁺]. Conversely, renal cells extruded PAH when cell [Na⁺] exceeded medium [Na⁺]. Membrane potential measured with triphenylmethylphosphonium revealed that conditions which created an interior-pos. membrane potential inhibited the Na⁺-dependent transport of PAH but caused stimulation of the Na⁺-independent component. Characteristics of the Na⁺-dependent PAH transport system in ouabain-poisoned slices were similar to those previously described in metabolically active tissues.

American Journal of Physiology published new progress about 2642-37-7. 2642-37-7 belongs to indole-building-block, auxiliary class Indole,Salt,Sulfonate,Inhibitor,Inhibitor, name is Potassium 1H-indol-3-yl sulfate, and the molecular formula is C8H6KNO4S, Category: indole-building-block.

Referemce:
https://www.nature.com/articles/s41429-020-0333-2,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Velezheva, Valeriya published the artcileSynthesis and antituberculosis activity of indole-pyridine derived hydrazides, hydrazide-hydrazones, and thiosemicarbazones, Category: indole-building-block, the publication is Bioorganic & Medicinal Chemistry Letters (2016), 26(3), 978-985, database is CAplus and MEDLINE.

We describe the design, synthesis, and in vitro antimycobacterial activity of a series of novel simple hybrid hydrazides and hydrazide-hydrazones combining indole and pyridine nuclei. The compounds are derivatives of 1-acetylindoxyl or substituted indole-3-carboxaldehydes tethered via a hydrazine group by simple C-N or double C:N bonds with 3- and 4-pyridines, 1-oxide 3- and 4-pyridine carbohydrazides. The most active of the 15 compounds showed MICs values against an INH-sensitive strain of Mycobacterium tuberculosis H37Rv equal to that of INH (0.05-2 μg/mL). Five compounds demonstrated appreciable activity against the INH-resistant M. tuberculosis CN-40 clin. isolate (MICs: 2-5 μg/mL), providing justification for further in vivo studies.

Bioorganic & Medicinal Chemistry Letters published new progress about 100123-25-9. 100123-25-9 belongs to indole-building-block, auxiliary class Indole,Bromide,Ester,Aldehyde, name is Ethyl 5-bromo-3-formyl-1H-indole-2-carboxylate, and the molecular formula is C15H24O2, Category: indole-building-block.

Referemce:
https://www.nature.com/articles/s41429-020-0333-2,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Mondal, Pravat published the artcileEnantioselective Total Synthesis of Desbromoarborescidines A-C and the Formal Synthesis of (S)-Deplancheine, Recommanded Product: tert-Butyl 3-(2-aminoethyl)-1H-indole-1-carboxylate, the publication is Journal of Organic Chemistry (2013), 78(13), 6802-6808, database is CAplus and MEDLINE.

Starting from Boc-protected tryptamine and (S)-tetrahydro-5-oxo-2-furancarboxylic acid, facile enantioselective total synthesis of desbromoarborescidines A-C and the formal synthesis of (S)-deplancheine have been accomplished via a common intermediate (S)-indolo[2,3-a]quinolizine (I). Synthesis of enantiomerically pure (S)-acetoxyglutarimide (II), stereoselective reductive intramol. cyclization, hydroxyl group-assisted in situ N-Boc-deprotection, selective deoxygenation of the xanthate ester, and lactam hydrolysis followed by an appropriate exchange of nitrogen regioselectivity in intramol. cyclization were the decisive steps.

Journal of Organic Chemistry published new progress about 167015-84-1. 167015-84-1 belongs to indole-building-block, auxiliary class Indols, name is tert-Butyl 3-(2-aminoethyl)-1H-indole-1-carboxylate, and the molecular formula is C15H20N2O2, Recommanded Product: tert-Butyl 3-(2-aminoethyl)-1H-indole-1-carboxylate.

Referemce:
https://www.nature.com/articles/s41429-020-0333-2,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles