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Jiang, Xiaohua et al. published their research in Journal of Medicinal Chemistry in 2012 | CAS: 754214-56-7

7-Azaindole-5-boronic Acid Pinacol Ester (cas: 754214-56-7) belongs to indole derivatives. Indole, first isolated in 1866, and it is commonly synthesized from phenylhydrazine and pyruvic acid, although several other procedures have been discovered. 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). Reference of 754214-56-7

Antiadhesion Therapy for Urinary Tract Infections-A Balanced PK/PD Profile Proved To Be Key for Success was written by Jiang, Xiaohua;Abgottspon, Daniela;Kleeb, Simon;Rabbani, Said;Scharenberg, Meike;Wittwer, Matthias;Haug, Martina;Schwardt, Oliver;Ernst, Beat. And the article was included in Journal of Medicinal Chemistry in 2012.Reference of 754214-56-7 This article mentions the following:

The initial step for the successful establishment of urinary tract infections (UTIs), predominantly caused by uropathogenic Escherichia coli, is the adhesion of bacteria to urothelial cells. This attachment is mediated by FimH, a mannose-binding adhesin, which is expressed on the bacterial surface. To date, UTIs are mainly treated with antibiotics, leading to the ubiquitous problem of increasing resistance against most of the currently available antimicrobials. Therefore, new treatment strategies are urgently needed, avoiding selection pressure and thereby implying a reduced risk of resistance. Here, we present a new class of highly active antimicrobials, targeting the virulence factor FimH. When the most potent representative, an indolinylphenyl mannoside, was administered in a mouse model at the low dosage of 1 mg/kg (corresponding to approx. 25 μg/mouse), the minimal therapeutic concentration to prevent UTI was maintained for more than 8 h. In a treatment study, the colony-forming units in the bladder could be reduced by almost 4 orders of magnitude, comparable to the standard antibiotic treatment with ciprofloxacin (8 mg/kg, s.c.). In the experiment, the researchers used many compounds, for example, 7-Azaindole-5-boronic Acid Pinacol Ester (cas: 754214-56-7Reference of 754214-56-7).

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

Lin, Aijun et al. published their research in Advanced Synthesis & Catalysis in 2011 | CAS: 14204-27-4

2-(Phenylthio)isoindoline-1,3-dione (cas: 14204-27-4) belongs to indole derivatives. Indole could be stereoselectively alkylated with chiral cyclopentyl sulfone reagent. 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). Reference of 14204-27-4

Organocatalytic Enantioselective Sulfenylation of β-Keto Phosphonates: A Convenient Approach to Construct Hetero-Quaternary Stereocenters was written by Lin, Aijun;Fang, Ling;Zhu, Xi;Zhu, Chengjian;Cheng, Yixiang. And the article was included in Advanced Synthesis & Catalysis in 2011.Reference of 14204-27-4 This article mentions the following:

The highly effective and enantioselective sulfenylation of β-keto phosphonates catalyzed by α,α-diaryl-L-prolinols has been developed. The optically active α-sulfenylated β-keto phosphonates could be obtained under mild reaction conditions in good yields (up to 92%) and with excellent enantioselectivities (up to 92% ee). In the experiment, the researchers used many compounds, for example, 2-(Phenylthio)isoindoline-1,3-dione (cas: 14204-27-4Reference of 14204-27-4).

Davies, Jacob et al. published their research in Angewandte Chemie, International Edition in 2017 | CAS: 14204-27-4

2-(Phenylthio)isoindoline-1,3-dione (cas: 14204-27-4) belongs to indole derivatives. Indole, first isolated in 1866, and it is commonly synthesized from phenylhydrazine and pyruvic acid, although several other procedures have been discovered. 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.HPLC of Formula: 14204-27-4

Photoredox Imino Functionalizations of Olefins was written by Davies, Jacob;Sheikh, Nadeem S.;Leonori, Daniele. And the article was included in Angewandte Chemie, International Edition in 2017.HPLC of Formula: 14204-27-4 This article mentions the following:

Shown herein is that polyfunctionalized nitrogen heterocycles can be easily prepared by a visible-light-mediated radical cascade process. This divergent strategy features the oxidative generation of iminyl radicals and subsequent cyclization/radical trapping, which allows the effective construction of highly functionalized heterocycles. The reactions proceed efficiently at room temperature, utilize an organic photocatalyst, use simple and readily available materials, and generate, in a single step, valuable building blocks that would be difficult to prepare by other methods. In the experiment, the researchers used many compounds, for example, 2-(Phenylthio)isoindoline-1,3-dione (cas: 14204-27-4HPLC of Formula: 14204-27-4).

Shao, Fangwei et al. published their research in Dyes and Pigments in 2011 | CAS: 146368-07-2

1-Ethyl-2,3,3-trimethyl-3H-indol-1-ium-5-sulfonate (cas: 146368-07-2) 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. 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). Category: indole-building-block

Facile synthesis of monofunctional pentamethine carbocyanine fluorophores was written by Shao, Fangwei;Yuan, Hushan;Josephson, Lee;Weissleder, Ralph;Hilderbrand, Scott A.. And the article was included in Dyes and Pigments in 2011.Category: indole-building-block This article mentions the following:

A high-yield route to sym., conjugatable pentamethine carbocyanine dyes with far-red/near IR (NIR) emission between 650 and 700 nm is reported. The dyes are prepared via condensation of indolium or benz[e]indolium inner salts with an alkyl carboxylic acid derivatized malonaldehyde dianil or alternatively in a one-pot reaction without isolation of the malonaldehyde intermediate. The fluorophores are water-soluble, have bright fluorescence emission, are easily prepared in good yield, and are promising candidates for use in a variety of biochem. and in vivo imaging applications. In the experiment, the researchers used many compounds, for example, 1-Ethyl-2,3,3-trimethyl-3H-indol-1-ium-5-sulfonate (cas: 146368-07-2Category: indole-building-block).

Chen, Changpeng et al. published their research in Organic Letters in 2017 | CAS: 1912-45-4

2-(5-Chloro-1H-indol-3-yl)acetic acid (cas: 1912-45-4) belongs to indole derivatives. Indole produced by Proteus, Pseudomonas, Escherichia and other species was shown to be a growth promoting factor in Arabidopsis thaliana. They are capable of binding to a variety of receptors with high affinity and thus have applications in a wide range of therapeutic areas.Product Details of 1912-45-4

Iridium-Catalyzed, Weakly Coordination-Assisted Ortho-Alkynylation of (Hetero)aromatic Carboxylic Acids without Cyclization was written by Chen, Changpeng;Liu, Pei;Tang, Jinghua;Deng, Gongda;Zeng, Xiaoming. And the article was included in Organic Letters in 2017.Product Details of 1912-45-4 This article mentions the following:

In the presence of [Cp^*IrCl₂]₂, arylcarboxylic acids and arylacetic acids such as 2-methylbenzoic acid or o-methylphenylacetic acid underwent regioselective directed alkynylation with i-Pr₃SiCCBr mediated by KHCO₃ and air in tert-amyl alc. to yield alkynylbenzoic acids and alkynylphenylacetic acids such as I (X = bond, CH₂) in 32-96% yields. Indolyl- and thienyl carboxylic and acetic acids and benzothiopheneacetic acids also underwent regioselective alkynylation. The reaction mechanism was studied using the alkynylation of potassium 2-methylbenzoate without added KHCO₃, deuterium labeling experiments, and the kinetic isotope effects on alkynylation. In the experiment, the researchers used many compounds, for example, 2-(5-Chloro-1H-indol-3-yl)acetic acid (cas: 1912-45-4Product Details of 1912-45-4).

Prager, Rolf H. et al. published their research in Journal of Heterocyclic Chemistry in 2000 | CAS: 5388-42-1

2-Phenylisoindolin-1-one (cas: 5388-42-1) belongs to indole derivatives. Indole could be stereoselectively alkylated with chiral cyclopentyl sulfone reagent. 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 5388-42-1

Carbene and radical pathways in pyrolysis of benzisoxazolones and benzotriazoles was written by Prager, Rolf H.;Baradarani, Mehdi M.;Khalafy, Jabbar. And the article was included in Journal of Heterocyclic Chemistry in 2000.Product Details of 5388-42-1 This article mentions the following:

Conference proceedings containing review material. A comparative study of the flash vacuum pyrolysis of a number of N-alkyl- and N-acylbenzotriazoles and -benzisoxazolones has confirmed that carbene-derived pathways predominate at lower temperatures, and radical pathways at higher temperatures Two new general unimol. thermal reactions are also highlighted. In the experiment, the researchers used many compounds, for example, 2-Phenylisoindolin-1-one (cas: 5388-42-1Product Details of 5388-42-1).

Hay, Duncan A. et al. published their research in Journal of the American Chemical Society in 2014 | CAS: 4583-55-5

5-Bromo-2,3-dimethyl-1H-indole (cas: 4583-55-5) belongs to indole derivatives. 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. Due to this activity, the indole ring system has become an important component or intermediate in the synthesis of heterocycles.Related Products of 4583-55-5

Discovery and Optimization of Small-Molecule Ligands for the CBP/p300 Bromodomains was written by Hay, Duncan A.;Fedorov, Oleg;Martin, Sarah;Singleton, Dean C.;Tallant, Cynthia;Wells, Christopher;Picaud, Sarah;Philpott, Martin;Monteiro, Octovia P.;Rogers, Catherine M.;Conway, Stuart J.;Rooney, Timothy P. C.;Tumber, Anthony;Yapp, Clarence;Filippakopoulos, Panagis;Bunnage, Mark E.;Muller, Susanne;Knapp, Stefan;Schofield, Christopher J.;Brennan, Paul E.. And the article was included in Journal of the American Chemical Society in 2014.Related Products of 4583-55-5 This article mentions the following:

Small-mol. inhibitors that target bromodomains outside of the bromodomain and extra-terminal (BET) sub-family are lacking. Here, the authors describe highly potent and selective ligands for the bromodomain module of the human lysine acetyl transferase CBP/p300, developed from a series of 5-isoxazolyl-benzimidazoles. The starting point was a fragment hit, which was optimized into a more potent and selective lead using parallel synthesis employing Suzuki couplings, benzimidazole-forming reactions, and reductive aminations. The selectivity of the lead compound against other bromodomain family members was investigated using a thermal stability assay, which revealed some inhibition of the structurally related BET family members. To address the BET selectivity issue, x-ray crystal structures of the lead compound bound to the CREB binding protein (CBP) and the first bromodomain of BRD4 (BRD4(1)) were used to guide the design of more selective compounds The crystal structures obtained revealed two distinct binding modes. By varying the aryl substitution pattern and developing conformationally constrained analogs, selectivity for CBP over BRD4(1) was increased. The optimized compound is highly potent (K_d = 21 nM) and selective, displaying 40-fold selectivity over BRD4(1). Cellular activity was demonstrated using fluorescence recovery after photo-bleaching (FRAP) and a p53 reporter assay. The optimized compounds are cell-active and have nanomolar affinity for CBP/p300; therefore, they should be useful in studies investigating the biol. roles of CBP and p300 and to validate the CBP and p300 bromodomains as therapeutic targets. In the experiment, the researchers used many compounds, for example, 5-Bromo-2,3-dimethyl-1H-indole (cas: 4583-55-5Related Products of 4583-55-5).

Silveira, Claudio C. et al. published their research in Tetrahedron Letters in 2010 | CAS: 14204-27-4

2-(Phenylthio)isoindoline-1,3-dione (cas: 14204-27-4) 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. Moreover, it is known that it controls biofilm formation. However, the role of indole in the cell has not been fully elucidated.Formula: C14H9NO2S

The use of anhydrous CeCl₃ as a catalyst for the synthesis of 3-sulfenyl indoles was written by Silveira, Claudio C.;Mendes, Samuel R.;Wolf, Lucas;Martins, Guilherme M.. And the article was included in Tetrahedron Letters in 2010.Formula: C14H9NO2S This article mentions the following:

Anhydrous CeCl₃ was successfully used as a catalyst for the synthesis of several 3-sulfenyl indoles in good to excellent yields through the reaction of indoles with N-(alkylthio) and N-(arylthio)phthalimides in DMF. In the experiment, the researchers used many compounds, for example, 2-(Phenylthio)isoindoline-1,3-dione (cas: 14204-27-4Formula: C14H9NO2S).

Wu, Yinrong et al. published their research in Organic Letters in 2021 | CAS: 1912-45-4

2-(5-Chloro-1H-indol-3-yl)acetic acid (cas: 1912-45-4) 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. Due to this activity, the indole ring system has become an important component or intermediate in the synthesis of heterocycles.Computed Properties of C10H8ClNO2

Copper-Mediated Decarboxylative Coupling between Arylacetic Acids and 1,3-Dicarbonyl Compounds was written by Wu, Yinrong;Wen, Kangmei;Chen, Jiewen;Shi, Jie;Yao, Xingang;Tang, Xiaodong. And the article was included in Organic Letters in 2021.Computed Properties of C10H8ClNO2 This article mentions the following:

A copper-mediated decarboxylative coupling reaction between arylacetic acids and 1,3-dicarbonyl compounds was described for the synthesis of ((indolyl)methyl)-oxocycloalkyl-esters, e.g., I. Significantly, methanocycloocta[b]indoles II [R = COOEt, CONHEt, SO₂Ph, etc.; R¹ = H, 4-Cl, 5-Br, etc.] were also obtained by sequential intramol. dehydrocyclization process in some cases. This protocol featured a broad substrate scope, simple operations, and good yields. Moreover, the products exhibited potent antiproliferative activity against the human cancer cell lines by a MTT assay. In the experiment, the researchers used many compounds, for example, 2-(5-Chloro-1H-indol-3-yl)acetic acid (cas: 1912-45-4Computed Properties of C10H8ClNO2).

Mironov, Yu. V. et al. published their research in Russian Chemical Bulletin in 2010 | CAS: 14204-27-4

A study of the mechanism of the azidophenylselenylation of glycals was written by Mironov, Yu. V.;Grachev, A. A.;Lalov, A. V.;Sherman, A. A.;Egorov, M. P.;Nifantiev, N. E.. And the article was included in Russian Chemical Bulletin in 2010.Computed Properties of C14H9NO2S This article mentions the following:

Chem. and physicochem. studies of homogeneous azidophenylselenylation of glycols with diacetoxyiodobenzene, trimethylsilyl azide, and di-Ph diselenide in dichloromethane revealed that the most probable key reaction step is the formation of phenylselenyl azide, an azide radical donor. A method for azidophenylsulfenylation of glycals, e.g. I, with diacetoxyiodobenzene, di-Ph diselenide, and sodium azide to give the corresponding glycosides, e.g. II, was proposed. In the experiment, the researchers used many compounds, for example, 2-(Phenylthio)isoindoline-1,3-dione (cas: 14204-27-4Computed Properties of C14H9NO2S).