Tag: 100-200

Selective Inhibition of Carboxylesterases by Isatins, Indole-2,3-diones was written by Hyatt, Janice L.;Moak, Teri;Hatfield, M. Jason;Tsurkan, Lyudmila;Edwards, Carol C.;Wierdl, Monika;Danks, Mary K.;Wadkins, Randy M.;Potter, Philip M.. And the article was included in Journal of Medicinal Chemistry in 2007.Formula: C10H9NO2 The following contents are mentioned in the article:

Carboxylesterases (CE) are ubiquitous enzymes thought to be responsible for the metabolism and detoxification of xenobiotics. Numerous clin. used drugs including Demerol, lidocaine, capecitabine, and CPT-11 are hydrolyzed by these enzymes. Hence, the identification and application of selective CE inhibitors may prove useful in modulating the metabolism of esterified drugs in vivo. Having recently identified benzil (diphenylethane-1,2-dione) as a potent selective inhibitor of CEs, we sought to evaluate the inhibitory activity of related 1,2-diones toward these enzymes. Biochem. assays and kinetic studies demonstrated that isatins (indole-2,3-diones), containing hydrophobic groups attached at a variety of positions within these mols., could act as potent, specific CE inhibitors. Interestingly, the inhibitory potency of the isatin compounds was related to their hydrophobicity, such that compounds with clogP values of <1.25 were ineffective at enzyme inhibition. Conversely, analogs demonstrating clogP values >5 routinely yielded K_i values in the nM range. Furthermore, excellent 3D QSAR correlates were obtained for 2 human CEs, hCE1 and hiCE. While the isatin analogs were generally less effective at CE inhibition than the benzils, the former may represent valid lead compounds for the development of inhibitors for use in modulating drug metabolism in vivo. This study involved multiple reactions and reactants, such as 4,7-Dimethylindoline-2,3-dione (cas: 15540-90-6Formula: C10H9NO2).

4,7-Dimethylindoline-2,3-dione (cas: 15540-90-6) belongs to indole derivatives. Indole produced by Proteus, Pseudomonas, Escherichia and other species was shown to be a growth promoting factor in Arabidopsis thaliana. In addition to indole, the strain-release chemistry worked for numerous substrates including amines, alcohols, thiols, carboxylic acids, imidazoles, and pyrazoles.Formula: C10H9NO2

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

Catalyst-Free Convergent Approach for the Synthesis of Spiro[imidazo[2,1-b][1,3]oxazine-7,3′-indoline] was written by Siddiqui, I. R.;Srivastava, Anushree;Rai, Pragati;Srivastava, Arjita;Srivastava, Anjali. And the article was included in Journal of Heterocyclic Chemistry in 2015.Recommanded Product: 4,7-Dimethylindoline-2,3-dione The following contents are mentioned in the article:

Strategies to address mounting environmental concerns with current approaches include an operationally simple and highly efficient one-pot three-component approach for the synthesis of spiro[imidazo[2,1-b][1,3]oxazine-7,3′-indoline] derivatives, e. g., I, which has been developed via Huisgen zwitter ion intermediate. The significant advantages of this protocol are short reaction time, excellent yields, and facile formation of three new bonds in one operation from easily available starting materials. This study involved multiple reactions and reactants, such as 4,7-Dimethylindoline-2,3-dione (cas: 15540-90-6Recommanded Product: 4,7-Dimethylindoline-2,3-dione).

4,7-Dimethylindoline-2,3-dione (cas: 15540-90-6) belongs to indole derivatives. Indole produced by Proteus, Pseudomonas, Escherichia and other species was shown to be a growth promoting factor in Arabidopsis thaliana. More than 200 indole derivatives have already been marketed as drugs or are under advanced stages of clinical trials.Recommanded Product: 4,7-Dimethylindoline-2,3-dione

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

Reductive Coupling of Acrylates with Ketones and Ketimines by a Nickel-Catalyzed Transfer-Hydrogenative Strategy was written by Buxton, Craig S.;Blakemore, David C.;Bower, John F.. And the article was included in Angewandte Chemie, International Edition in 2017.Quality Control of 4,7-Dimethylindoline-2,3-dione The following contents are mentioned in the article:

Nickel-catalyzed coupling of benzyl acrylates with activated ketones and imines provides γ-butyrolactones and lactams, resp. The benzyl alc. byproduct released during the lactonization/lactamization event is relayed to the next cycle where it serves as the reductant for C-C bond formation. This strategy represents a conceptually unique approach to transfer-1′- C-C bond formation, thus providing examples of reductive heterocyclizations where hydrogen embedded within an alc. leaving group facilitates turnover. This study involved multiple reactions and reactants, such as 4,7-Dimethylindoline-2,3-dione (cas: 15540-90-6Quality Control of 4,7-Dimethylindoline-2,3-dione).

4,7-Dimethylindoline-2,3-dione (cas: 15540-90-6) belongs to indole derivatives. Indole produced by Proteus, Pseudomonas, Escherichia and other species was shown to be a growth promoting factor in Arabidopsis thaliana.Indole was synthesized in moderate yield via an o-naphthoquinone catalyzed tandem cross-coupling of substituted aniline and benzylamine under aerobic oxidation conditions.Quality Control of 4,7-Dimethylindoline-2,3-dione

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

Dicyclooctabiphenylene. Synthesis and properties was written by Wilcox, Charles F. Jr.;Farley, Erik N.. And the article was included in Journal of the American Chemical Society in 1984.Recommanded Product: 15540-90-6 The following contents are mentioned in the article:

The preparation and properties of the “antiarom.” hydrocarbon dicycloocta[1,2,3,4-def:1′,2′,3′,4′-jkl]biphenylene (I) are described. The observed electronic and ¹H NMR spectra of I agree well with previous predictions. The series of polycycles comprising I, biphenylene (II), and cycloocta[def]biphenylene (III), is examined in terms of resonance energy and qual. aromaticity models. This study involved multiple reactions and reactants, such as 4,7-Dimethylindoline-2,3-dione (cas: 15540-90-6Recommanded Product: 15540-90-6).

4,7-Dimethylindoline-2,3-dione (cas: 15540-90-6) 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. 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). Recommanded Product: 15540-90-6

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

Synthesis of novel 3-acyloxy-1,3-dihydro-2H-indol-2-ones and isomeric 4-acyl-1,4-dihydro-3,1-benzoxazin-2-ones: double rearrangement of 3-hydroxyquinoline-2,4(1H,3H)-diones was written by Klasek, Antonin;Koristek, Kamil;Polis, Jiri;Kosmrlj, Janez. And the article was included in Tetrahedron in 2000.Recommanded Product: 15540-90-6 The following contents are mentioned in the article:

Substituted 3-hydroxyquinoline-2,4(1H,3H)-diones were transformed into 3-acyloxy-1,3-dihydro-2H-indol-2-ones and isomeric 4-acyl-1,4-dihydro-3,1-benzoxazin-2-ones. The influence of the substituents and the reaction conditions on the course of the reaction was studied. In the proposed mechanism, a double rearrangement takes place; α-ketol rearrangement, leading to a α-hydroxy β-diketone intermediate, is followed by a rearrangement to the isomeric α-ketol esters. This study involved multiple reactions and reactants, such as 4,7-Dimethylindoline-2,3-dione (cas: 15540-90-6Recommanded Product: 15540-90-6).

4,7-Dimethylindoline-2,3-dione (cas: 15540-90-6) 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. 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: 15540-90-6

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

Face selective reduction of the exocyclic double bond in isatin derived spirocyclic lactones was written by Rana, Sandeep;Natarajan, Amarnath. And the article was included in Organic & Biomolecular Chemistry in 2013.Application of 15540-90-6 The following contents are mentioned in the article:

We report an unusual face selective reduction of the exocyclic double bond in the α-methylene-γ-butyrolactone motif of spiro-oxindole systems I and II [R¹ = H, Me, R² = H; R¹ =H, R² = Me]. The spiro-oxindoles were assembled by an indium metal mediated Barbier-type reaction followed by an acid catalyzed lactonization. This study involved multiple reactions and reactants, such as 4,7-Dimethylindoline-2,3-dione (cas: 15540-90-6Application of 15540-90-6).

4,7-Dimethylindoline-2,3-dione (cas: 15540-90-6) 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. Due to this activity, the indole ring system has become an important component or intermediate in the synthesis of heterocycles.Application of 15540-90-6

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 Baeyer-Villiger oxidation of ketones and aldehydes was written by Krow, Grant R.. And the article was included in Organic Reactions (Hoboken, NJ, United States) in 1993.Safety of 4,7-Dimethylindoline-2,3-dione The following contents are mentioned in the article:

A review of the article The Baeyer-Villiger oxidation of ketones and aldehydes. This study involved multiple reactions and reactants, such as 4,7-Dimethylindoline-2,3-dione (cas: 15540-90-6Safety of 4,7-Dimethylindoline-2,3-dione).

4,7-Dimethylindoline-2,3-dione (cas: 15540-90-6) 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. More than 200 indole derivatives have already been marketed as drugs or are under advanced stages of clinical trials.Safety of 4,7-Dimethylindoline-2,3-dione

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

Decamethylanthracene and its 9,10-‘Dewar’ isomer was written by Hart, Harold;Ruge, Bernd. And the article was included in Tetrahedron Letters in 1977.COA of Formula: C10H9NO2 The following contents are mentioned in the article:

Decamethylanthracene (I) was prepared from 4,7-dimethylisatin by sequential addition of Br (Br, boiling EtOH), bromination (Br/AlBr₃ in fuming H₂SO₄, 24 h), treatment with H₂O₂/OH^–, diazotization, cycloaddition of hexamethyl-2,4-cyclohexadienone (ClCH₂CH₂Cl containing propylene oxide, 70-80°), reduction (LiAlH₄), reflux in mesitylene, cycloaddition of N-butyltetramethylpyrrole (room temperature, BuLi/C₆H₁₃, 1 h), and oxidation with m-ClC₆H₄C(O)OOH in CHCl₃/aqueous Na₂CO₃. Treatment of I in CH₂Cl₂ with one drop of CF₃CO₂H gave tautomer II. Irradiation of I in C₆H₆ or Et₂O gave th 9,10-‘Dewar’ isomer III. This study involved multiple reactions and reactants, such as 4,7-Dimethylindoline-2,3-dione (cas: 15540-90-6COA of Formula: C10H9NO2).

4,7-Dimethylindoline-2,3-dione (cas: 15540-90-6) 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. In addition to indole, the strain-release chemistry worked for numerous substrates including amines, alcohols, thiols, carboxylic acids, imidazoles, and pyrazoles.COA of Formula: C10H9NO2

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

Structure-Activity Relationship (SAR) Optimization of 6-(Indol-2-yl)pyridine-3-sulfonamides: Identification of Potent, Selective, and Orally Bioavailable Small Molecules Targeting Hepatitis C (HCV) NS4B was written by Zhang, Nanjing;Zhang, Xiaoyan;Zhu, Jin;Turpoff, Anthony;Chen, Guangming;Morrill, Christie;Huang, Song;Lennox, William;Kakarla, Ramesh;Liu, Ronggang;Li, Chunshi;Ren, Hongyu;Almstead, Neil;Venkatraman, Srikanth;Njoroge, F. George;Gu, Zhengxian;Clausen, Valerie;Graci, Jason;Jung, Stephen P.;Zheng, Yingcong;Colacino, Joseph M.;Lahser, Fred;Sheedy, Josephine;Mollin, Anna;Weetall, Marla;Nomeir, Amin;Karp, Gary M.. And the article was included in Journal of Medicinal Chemistry in 2014.Computed Properties of C9H8FN The following contents are mentioned in the article:

Nonracemic (aminosulfonyl)pyridinyl indolecarbonitriles such as I were prepared as inhibitors of the hepatitis C viral protein NS4B for use as antihepatitis C agents. The substitution patterns on the indole rings were modified to limit oxidative metabolism of the indolecarbonitriles and to avoid potential liver damage and cytochrome P₄₅₀ inhibition; the compounds were also optimized to improve their oral bioavailabilities. I was potent against the HCV 1b replicon, with an EC₅₀ value of 2 nM and a selectivity of >5000 with respect to cellular glyceraldehyde-3-phosphate dehydrogenase. I had a favorable pharmacokinetic profile with oral bioavailabilities of 62%, 78%, and 18% in rats, dogs, and monkeys, resp., and favorable tissue distribution properties (liver to plasma exposure ratio in rats of 25). This study involved multiple reactions and reactants, such as 5-Fluoro-6-methyl-1H-indole (cas: 1000343-16-7Computed Properties of C9H8FN).

5-Fluoro-6-methyl-1H-indole (cas: 1000343-16-7) 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). Computed Properties of C9H8FN

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

Ninhydrin as a building block in scaffold-linked chromophoric dyad construction was written by Margetic, Davor;Mann, David A.;Warrener, Ronald N.. And the article was included in ARKIVOC (Gainesville, FL, United States) in 2014.Reference of 15540-90-6 The following contents are mentioned in the article:

The reaction of ninhydrin with ester-activated cyclobutene epoxide (CE) containing the fused 1,4-dimethoxynaphthalene (DMN) chromophore, gave adducts formed by 1,3-dipolar cycloaddition at the central (C₂)-CO (major) and the outer (C_1,3)-CO (minor) positions. Conversion of the minor adduct to quinoxalines (QIN) by reaction with o-phenylenediamines at the α-dione moiety, albeit in poor yield, led to spiro-DMN-1,4σ-QIN dyad in which the plane of the chromophore was orthogonally oriented yet angled to the plane of the DMN chromophore. Reaction of ninhydrin with o-phenylenediamines yielded the corresponding 11-oxoindeno[1,2-b]quinoxalines which were coupled with CE-BLOCKs to form spiro adducts by reaction at the carbonyl site, the product from CE-1 was identical with that formed above. This study involved multiple reactions and reactants, such as 4,7-Dimethylindoline-2,3-dione (cas: 15540-90-6Reference of 15540-90-6).

4,7-Dimethylindoline-2,3-dione (cas: 15540-90-6) 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. More than 200 indole derivatives have already been marketed as drugs or are under advanced stages of clinical trials.Reference of 15540-90-6

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