Day: November 7, 2022

On November 5, 2015, Okano, Tsubasa; Suzuki, Shinya published a patent.Product Details of 52537-00-5 The title of the patent was Preparation of imidazoline derivatives as selective adrenaline α1A receptor full agonists. And the patent contained the following:

Disclosed are compounds I [A = Q1, Q2 or Q3; R = halo; n = 1-4; or pharmaceutically acceptable salts thereof]. For example, II·2HCl was prepared via reaction of 5-chloroindolin-2-one with TMEDA/n-BuLi/1,2-dibromoethane, reduction, cyanomethylation with bromoacetonitrile, treatment with ethylenediamine/P2S5 and salt-formation. In adrenaline receptor α1 agonist activity test, the exemplified compound II·2HCl showed EC50 values (nmol/L) of 2.60 and >10000 for α1A and α1L, resp. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Product Details of 52537-00-5

The Article related to imidazoline preparation selective adrenaline alpha 1a receptor full agonist, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Product Details of 52537-00-5

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

On April 30, 2012, Sikorska, Emilia; Sobolewski, Dariusz; Kwiatkowska, Anna published an article.Recommanded Product: H-Idc-OH The title of the article was Conformational preferences of proline derivatives incorporated into vasopressin analogues: NMR and molecular modelling studies. And the article contained the following:

In this study, arginine vasopressin analogs modified with proline derivatives – indoline-2-carboxylic acid (Ica), (2S,4R)-4-(naphthalene-2-ylmethyl)pyrrolidine-2-carboxylic acid (Nmp), (2S,4S)-4-aminopyroglutamic acid (APy) and (2R,4S)-4-aminopyroglutamic acid, (Apy) – were examined using NMR spectroscopy and mol. modeling methods. The results have shown that Ica is involved in the formation of the cis peptide bond. Moreover, it reduces to a great extent the conformational flexibility of the peptide. In turn, incorporation of (2S,4R)-Nmp stabilizes the backbone conformation, which is heavily influenced by the pyrrolidine ring. However, the aromatic part of the Nmp side chain exhibits a high degree of conformational freedom. With analogs [(2S,4S)-4-aminopyroglutamic acid2-3]AVP and [(2R,4S)-4-aminopyroglutamic acid2-3]AVP, introduction of the 4-aminopyroglutamic acid reduces locally conformational space of the peptides, but it also results in weaker interactions with the dodecylphosphocholine/SDS micelle. Admittedly, both analogs are adsorbed on the micelle’s surface but they do not penetrate into its core. With analog [(2R,4S)-4-aminopyroglutamic acid2-3]AVP, the interactions between the peptide and the micelle seem to be so weak that conformational equilibrium is established between different bound states. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Recommanded Product: H-Idc-OH

The Article related to arginine vasopressin proline derivative nmr mol modeling conformation preference, Mammalian Hormones: Structure and Structure-Activity Relations and other aspects.Recommanded Product: H-Idc-OH

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

On October 13, 2011, Khan, Pasha M.; Correa, Ricardo G.; Divlianska, Daniela B.; Peddibhotla, Satyamaheshwar; Sessions, E. Hampton; Magnuson, Gavin; Brown, Brock; Suyama, Eigo; Yuan, Hongbin; Mangravita-Novo, Arianna; Vicchiarelli, Michael; Su, Ying; Vasile, Stefan; Smith, Layton H.; Diaz, Paul W.; Reed, John C.; Roth, Gregory P. published an article.Category: indole-building-block The title of the article was Identification of Inhibitors of NOD1-Induced Nuclear Factor-κB Activation. And the article contained the following:

NOD1 (nucleotide-binding oligomerization domain 1) protein is a member of the NLR (NACHT and leucine rich repeat domain containing proteins) protein family, which plays a key role in innate immunity as a sensor of specific microbial components derived from bacterial peptidoglycans and induction of inflammatory responses. Mutations in NOD proteins have been associated with various inflammatory diseases that affect NF-κB (nuclear factor κB) activity, a major signaling pathway involved in apoptosis, inflammation, and immune response. A luciferase-based reporter gene assay was utilized in a high-throughput screening program conducted under the NIH-sponsored Mol. Libraries Probe Production Center Network program to identify the active scaffolds. Herein, we report the chem. synthesis, structure-activity relationship studies, downstream counterscreens, secondary assay data, and pharmacol. profiling of the 2-aminobenzimidazole lead, I, as a potent and selective inhibitor of NOD1-induced NF-κB activation. The experimental process involved the reaction of 1-(Cyclopropanecarbonyl)indoline-5-sulfonyl chloride(cas: 879562-21-7).Category: indole-building-block

The Article related to indoline tetrahydroisoquinoline aminobenzimidazole preparation, structure activity relationship pharmacokinetics nod1 induced nfkappab activation inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.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

Soto, Sara; Vaz, Esther; Dell’Aversana, Carmela; Alvarez, Rosana; Altucci, Lucia; de Lera, Angel R. published an article in 2012, the title of the article was New synthetic approach to paullones and characterization of their SIRT1 inhibitory activity.Category: indole-building-block And the article contains the following content:

A series of 7,12-dihydroindolo[3,2-d][1]benzazepine-6(5H)-ones (paullones) substituted at C9/C10 (Br) and C2 (Me, CF3, CO2Me) have been synthesized by a one-pot Suzuki-Miyaura cross-coupling of an o-aminoarylboronic acid and Me 2-iodoindoleacetate followed by intramol. amide formation. Other approaches to the paullone scaffold based on Pd-catalyzed C-H activation were unsuccessful. In vitro enzymic assay with recombinant human SIRT-1 indicated a strong inhibitory profile for the series, in particular the analog with a methoxycarbonyl group at C2 and a bromine at C9. These compounds are, in general, inducers of granulocyte differentiation of the U937 acute leukemia cell line and cause a marked increase in pre-G1 of the cell cycle. The experimental process involved the reaction of Methyl 2-(6-bromo-1H-indol-3-yl)acetate(cas: 152213-63-3).Category: indole-building-block

The Article related to aminoarylboronic acid iodoindoleacetate suzuki amidation, Heterocyclic Compounds (One Hetero Atom): Higher-Membered Rings and other aspects.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

On June 18, 2002, Hester, Jackson B.; Rogers, Bruce N.; Jacobsen, Eric Jon; Ennis, Michael D.; Acker, Brad A.; Vander Velde, Susan L.; Frank, Kristine E. published a patent.Application In Synthesis of 6-Chloro-2,3-dihydro-1H-indole The title of the patent was Preparation of tetracyclic azepinoindoles as 5-HT receptor ligands for treatment of CNS disorders. And the patent contained the following:

Title compounds I [wherein R1 = independently OH, NO2, halo, CN CF3, CF3O, or (un)substituted alkyl, alkoxy, alkanoyl(oxy), alkoxycarbonyl, (hetero)aryl, sulfamoyl, amino, carbamoyl, or SOmRe; R2 = H, alkyl, alkanoyl, aryl(carbonyl), arylalkyl, alkoxycarbonyl, aryloxycarbonyl, arylsulfonyl, or arylalkoxycarbonyl; X and Y together = (un)substituted 2-3 membered saturated or partially unsaturated chain comprising 1 or more C’s and 1 O, S, SO, SO2, or NRf; m = independently 0-2; n = 0-3; Re = independently H, alkyl, (hetero)aryl, or (hetero)arylalkyl; Rf = H, alkyl, (hetero)aryl, (hetero)arylalkyl, or is a bond to a 2-4 membered alkylene chain that forms a ring fused to the ring comprising X and Y; with provisos; or a pharmaceutically acceptable salt thereof] were prepared as serotonin 5-HT receptor ligands. For example, a neat reaction between 1,2,3,4-tetrahydroquinoline and isoamylnitrile, followed by reduction of the N-nitroso intermediate with LiAlH4, afforded 3,4-dihydro-1(2H)-quinolinylamine•HCl. Cycloaddition with benzyl 4-oxo-1-azepanecarboxylate and deprotection using Pd/C gave the desired azepinopyrroloquinoline II•HCl. The latter exhibited binding to the 5HT2c receptor with Ki of 13 nM. I are useful for the treatment of central nervous system disorders, such as anxiety, obesity, depression, schizophrenia, stress related diseases, panic disorder, a phobia, obsessive compulsive disorder, post-traumatic stress syndrome, immune system depression, a stress induced problem with the gastrointestinal or cardiovascular system, or sexual dysfunction (no data). The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Application In Synthesis of 6-Chloro-2,3-dihydro-1H-indole

The Article related to cns agent azepinopyrroloquinoline preparation, azepinoindole tetracyclic preparation serotonin receptor ligand, Heterocyclic Compounds (One Hetero Atom): Higher-Membered Rings and other aspects.Application In Synthesis of 6-Chloro-2,3-dihydro-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

Sekhar, Abinitha S.; Saranya, T. S.; Baskar, Vaishnav; Manakadan, Asha Ashokan published an article in 2016, the title of the article was In silico approach of apoptosis induing ability of different indole derivatives by interaction with caspase9.Related Products of 256935-86-1 And the article contains the following content:

Indole compounds are well known for their wide variety of pharmacol. activities. It is the combination of benzene with pyrrole ring. Compounds having indole group are biol. important. They are used as antimicrobial, antiviral, antitubercular, antiinflammatory, anticancer, ant-diabetic and anticonvulsant agents. Because of the wide variety of biol. application, several substituted indole derivatives are studied for their mol. structure, mol. docking and bioavailability. The purpose of the study is to carry out the docking studies of indole derivatives containing electrophilic substitution and nucleophilic substitution with the anticancer target casp9. Fifty compounds were designed and by using Argus lab version 4.0.1. Their docking score was calculated and compared with the standard drug casodex. The drug likeness of compounds was performed using Lipinski rule of five. Result showed that 1,1′-(1H-indole-5,6-diyl)diethanone and 5-(trichloromethyl)-1H-indole and the phytoconstituent curcumin showed better docking score than that of the standard drug casodex. It is concluded that certain indole derivatives show greater affinity with casp9 protein. These compounds may be helpful in studying anticancer targets for casp9 protein. The experimental process involved the reaction of 6-Chloro-1H-indole-5-carboxylic acid(cas: 256935-86-1).Related Products of 256935-86-1

The Article related to indole derivative induce apoptosis ability anticancer target caspase protein, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Related Products of 256935-86-1

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

On December 31, 2014, Liu, Hong; Dai, Xing; Palani, Anandan; He, Shuwen; Nargund, Ravi; Xiao, Dong; Dang, Qun; Peng, Xuanjia; Li, Peng published a patent.Synthetic Route of 1256359-96-2 The title of the patent was Substituted benzofuran compounds and methods of use thereof for the treatment of viral diseases. And the patent contained the following:

Title compounds I [X = pyridinone, pyrimidinone, pyridazone, etc.; B = (un)substituted 5- to 6-membered monocyclic ring, 9- to 10-membered bicyclic ring or C(O)NHCR5R6; A = fluorophenyl; D = absent or NR3SO2R4; R2 = alkyl; R3 = alkyl; R4 = alkyl; R5 = H, alkyl, or hydroxyalkyl; R6 = H or R5 and R6 together with the carbon to which they are attached form cyclopropyl], and their pharmaceutically acceptable salts, are prepared and disclosed. Thus, e.g., II was prepared by Suzuki reaction of 2-(4-fluorophenyl)-N-methyl-6-(N-methylmethylsulfonylamino)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzofuran-3-carboxamide with 5-bromo-1-methylpyridin-2(1H)-one followed by bromination and Suzuki reaction with 4-fluoro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-lH-indole. Compounds of the invention were tested for their inhibitory activity using HCV replicon system, e.g., II showed IC50 value of 3.616 nM for genotypes 1a and 3.885 nM for genotype 1b. The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system. The experimental process involved the reaction of 4-Fluoro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole(cas: 1256359-96-2).Synthetic Route of 1256359-96-2

The Article related to benzofuran preparation hcv viral disease, Heterocyclic Compounds (One Hetero Atom): Areno- and Diarenofurans and other aspects.Synthetic Route of 1256359-96-2

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

On December 31, 2014, Liu, Hong; Dai, Xing; Palani, Anandan; He, Shuwen; Nargund, Ravi; Xiao, Dong; Dang, Qun; Peng, Xuanjia; Li, Peng published a patent.Application of 1256359-96-2 The title of the patent was Substituted benzofuran compounds and methods of use thereof for the treatment of viral diseases. And the patent contained the following:

Title compounds I [X = pyridinone, pyrimidinone, pyridazone, etc.; B = (un)substituted 5- to 6-membered monocyclic ring, 9- to 10-membered bicyclic ring or C(O)NHCR5R6; A = fluorophenyl; D = absent or NR3SO2R4; R2 = alkyl; R3 = alkyl; R4 = alkyl; R5 = H, alkyl, or hydroxyalkyl; R6 = H or R5 and R6 together with the carbon to which they are attached form cyclopropyl], and their pharmaceutically acceptable salts, are prepared and disclosed. Thus, e.g., II was prepared by Suzuki reaction of 2-(4-fluorophenyl)-N-methyl-6-(N-methylmethylsulfonylamino)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzofuran-3-carboxamide with 5-bromo-1-methylpyridin-2(1H)-one followed by bromination and Suzuki reaction with 4-fluoro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-lH-indole. Compounds of the invention were tested for their inhibitory activity using HCV replicon system, e.g., II showed IC50 value of 3.616 nM for genotypes 1a and 3.885 nM for genotype 1b. The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system. The experimental process involved the reaction of 4-Fluoro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole(cas: 1256359-96-2).Application of 1256359-96-2

The Article related to benzofuran preparation hcv viral disease, Heterocyclic Compounds (One Hetero Atom): Areno- and Diarenofurans and other aspects.Application of 1256359-96-2

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

On April 30, 1998, Ledvina, Miroslav; Zyka, Daniel; Jezek, Jan; Trnka, Tomas; Saman, David published an article.Category: indole-building-block The title of the article was New effective synthesis of (N-acetyl- and N-stearoyl-2-amino-2-deoxy-β-D-glucopyranosyl)-(1→4)-N-acetylnormuramoyl-L-2-aminobutanoyl-D-isoglutamine, analogs of GMDP with immunopotentiating activity. And the article contained the following:

Et 3,4,6-tri-O-benzyl-2-deoxy-2-phthalimido-1-thio-β-D-glucopyranoside (5), prepared by benzylation of Et 2-deoxy-2-phthalimido-1-thio-β-D-glucopyranoside, was transformed by reaction with bromine into 3,4,6-tri-O-benzyl-2-deoxy-2-phthalimido-β-D-glucopyranosyl bromide (6). Thioglycoside 5 in the presence of Me triflate and glycosyl bromide 6 in the presence of silver triflate were used as glycosyl donors for condensation with benzyl 2-acetamido-3-O-allyl-6-O-benzyl-2-deoxy-α-D-glucopyranoside, to give benzyl 2-acetamido-3-O-allyl-6-O-benzyl-4-O-(3,4,6-tri-O-benzyl-2-deoxy-2-phthalimido-β-D-glucopyranosyl)-2-deoxy-α-D-glucopyranoside (8). Its reductive dephthaloylation with NaBH4/AcOH afforded benzyl 2-acetamido-3-O-allyl-4-O-(2-amino-3,4,6-tri-O-benzyl-2-deoxy-β-D-glucopyranosyl)-6-O-benzyl-2-deoxy-α-D-glucopyranoside (11). Compound 11 was N-acylated to give benzyl 2-acetamido-4-O-(2-acylamino-3,4,6-tri-O-benzyl-2-deoxy-β-D-glucopyranosyl)-3-O-allyl-6-O-benzyl-2-deoxy-α-D-glucopyranosides. These compounds were converted into corresponding benzyl 2-acetamido-4-O-(2-acylamino-3,4,6-tri-O-benzyl-2-deoxy-β-D-glucopyranosyl)-6-O-benzyl-3-O-carboxymethyl-2-deoxy-α-D-glucopyranosides which, by condensation with H-L-Abu-D-isoGln(OBzl) followed by hydrogenolysis of protective benzyl groups, furnished the title glycopeptides. Intramol. O→N migration of the allyl protecting group followed by its reduction to the Pr residue by reaction of compound 8 with hydrazine or hydrazinium acetate, to give benzyl 2-acetamido-4-O-(3,4,6-tri-O-benzyl-2-deoxy-2-propylamino-β-D-glucopyranosyl)-6-O-benzyl-2-deoxy-α-D-glucopyranoside, is also described. The experimental process involved the reaction of Ethyl 2-deoxy-2-(1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)-1-thio-beta-D-glucopyranoside(cas: 130539-43-4).Category: indole-building-block

The Article related to glycopeptide gmdp analog preparation, Amino Acids, Peptides, and Proteins: Poly(Amino Acids) and Peptides and other aspects.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

Deb, Indubhusan; Coiro, Daniel J.; Seidel, Daniel published an article in 2011, the title of the article was Decarboxylative formation of N-alkyl pyrroles from 4-hydroxyproline.HPLC of Formula: 79815-20-6 And the article contains the following content:

N-Alkyl pyrroles are obtained in a single step from trans-4-hydroxyproline and aldehydes or ketones in just 15 min under microwave irradiation E.g., benzoic acid-catalyzed reaction of trans-4-hydroxyproline and 4-ClC6H4CHO gave 73% N-alkyl pyrrole I. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).HPLC of Formula: 79815-20-6

The Article related to hydroxyproline reaction aldehyde ketone, alkyl pyrrole decarboxylative preparation, Heterocyclic Compounds (One Hetero Atom): Pyrroles and Pyrrolizines and other aspects.HPLC of Formula: 79815-20-6

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