Tag: 200-300

On December 15, 2019, Liu, Hong; Dai, Xing; He, Shuwen; Brockunier, Linda; Marcantonio, Karen; Ludmerer, Steven W.; Li, Fangbiao; Feng, Kung-I.; Nargund, Ravi P.; Palani, Anandan published an article.HPLC of Formula: 1256359-96-2 The title of the article was Design and evaluation of novel tetracyclic benzofurans as palm site allosteric inhibitors of HCV NS5B polymerase. And the article contained the following:

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. 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).HPLC of Formula: 1256359-96-2

The Article related to tetracyclic benzofuran hepatitis virus ns5b polymerase mk8876, hepatitis c virus, mk-8876, ns5b polymerase, non-nucleoside inhibitors (nni), tetracyclic structure, Pharmacology: Effects Of Antimicrobials and Parasiticides and other aspects.HPLC of Formula: 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 February 13, 2020, Na, Hyo Gyeong; Imran, Ali; Kim, Kyuneun; Han, Hong Sik; Lee, Young Jin; Kim, Myung-Jin; Yun, Chang-Soo; Jung, Young-Sik; Lee, Joo-Youn; Han, Soo Bong published an article.Name: Methyl 5-bromoindoline-7-carboxylate The title of the article was Discovery of a New Sulfonamide Hepatitis B Capsid Assembly Modulator. And the article contained the following:

Hepatitis B virus (HBV) remains a major health concern with 260 million people having been infected globally, and approx. 680,000 deaths have occurred annually from cirrhosis and liver cancer. The modulation of HBV capsid assembly has emerged as a promising therapeutic approach for curing chronic HBV infection. Small-mol. capsid assembly modulators (CAMs) can broadly be classified as heteroaryldihydropyrimidines and sulfamoylbenzamides (SBAs). SBAs are capsid activators that inhibit viral replication by achieving capsid assembly before polymerase encapsulation. Herein, we report a novel series of HBV CAMs based on NVR 3-778, a potent CAM belonging to the SBA class. The lead compound (KR-26556) exhibited improved pharmacol. activity and was examined through mol. docking studies. The experimental process involved the reaction of Methyl 5-bromoindoline-7-carboxylate(cas: 860624-88-0).Name: Methyl 5-bromoindoline-7-carboxylate

The Article related to hepatitis b capsid assembly antihbv mol docking studies, Pharmacology: Effects Of Antimicrobials and Parasiticides and other aspects.Name: Methyl 5-bromoindoline-7-carboxylate

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 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

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 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

On November 1, 2006, Baran, Phil S.; Shenvi, Ryan A. published an article.Application of 152213-63-3 The title of the article was Total Synthesis of (±)-Chartelline C. And the article contained the following:

The first total synthesis of (±)-chartelline C (I) in a concise 10-step sequence is reported. Highlights of the completion of this decades-old puzzle include (1) chemo- and position-selective installation of the heteroaromatic halogens, (2) halogen-sparing monoredn. of an alkyne linker, (3) a simple strategy for placement of the sensitive β-chloroenamide, (4) an unusually facile thermolysis of a vinyl carboxylic acid, and (5) a powerful ring contraction whose potential utility in heterocyclic chem. merits further investigation. The experimental process involved the reaction of Methyl 2-(6-bromo-1H-indol-3-yl)acetate(cas: 152213-63-3).Application of 152213-63-3

The Article related to chartelline c total synthesis, Alkaloids: Alkaloids Containing Three Or More Nitrogen Atoms and other aspects.Application of 152213-63-3

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 August 14, 2014, Dai, Xing; Liu, Hong; Palani, Anandan; He, Shuwen; Lai, Zhong; Nargund, Ravi; Marcantonio, Karen; Xiao, Dong; Brockunier, Linda L.; Zorn, Nicolas; Dang, Qun; Peng, Xuanjia; Li, Peng published a patent.Application of 1256359-96-2 The title of the patent was Preparation of tetracyclic heterocycle compounds and methods of use thereof for the treatment of hepatitis C. And the patent contained the following:

The 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. Compounds of formula I wherein A is C3-6 cycloalkyl, azetidin-1-ylcarbonyl and 5- to 6-membered aromatic ring system optionally containing heteroatoms; ring B is benzofuran, pyridinofuran pyrazolopyridine, etc.; Z1, Z2 and Z3 are independently CH and H, with the proviso that no more than one of Z1 – Z3 is N; Z4 is N, Z5 is CH and dashed bond to Z5 is double bond; Z4 is C, Z5 is NH and dashed bond is to Z5 is single bond; R2 is H, C1-6 alkyl, and C1-6 alkoxy; R3 is H and C1-6 alkyl; R4 is C1-6 alkyl and C1-6 alkoxy; R5 is H, C1-6 alkyl, CH2CO2H and derivatives, and SO2Me; R6 is H, C1-6 alkyl, C1-6 haloalkyl, etc.; R7 is H and C1-6 alkyl; R6R7 taken together to form C3-4 cycloalkyl; R8 is H, halo and CN; R9 and R10 are independently H and halo; dashed bond is single and double bond; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their anti-HCV activity. From the assay, it was determined that compound II exhibited IC50 values in the range of 4.006 nM to 6.558 nM. 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 tetracyclic heterocycle preparation antiviral treatment hepatitis c, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines 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 August 14, 2014, Dai, Xing; Liu, Hong; Palani, Anandan; He, Shuwen; Lai, Zhong; Nargund, Ravi; Marcantonio, Karen; Xiao, Dong; Brockunier, Linda L.; Zorn, Nicolas; Dang, Qun; Peng, Xuanjia; Li, Peng published a patent.Electric Literature of 1256359-96-2 The title of the patent was Preparation of tetracyclic heterocycle compounds and methods of use thereof for the treatment of hepatitis C. And the patent contained the following:

The 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. Compounds of formula I wherein A is C3-6 cycloalkyl, azetidin-1-ylcarbonyl and 5- to 6-membered aromatic ring system optionally containing heteroatoms; ring B is benzofuran, pyridinofuran pyrazolopyridine, etc.; Z1, Z2 and Z3 are independently CH and H, with the proviso that no more than one of Z1 – Z3 is N; Z4 is N, Z5 is CH and dashed bond to Z5 is double bond; Z4 is C, Z5 is NH and dashed bond is to Z5 is single bond; R2 is H, C1-6 alkyl, and C1-6 alkoxy; R3 is H and C1-6 alkyl; R4 is C1-6 alkyl and C1-6 alkoxy; R5 is H, C1-6 alkyl, CH2CO2H and derivatives, and SO2Me; R6 is H, C1-6 alkyl, C1-6 haloalkyl, etc.; R7 is H and C1-6 alkyl; R6R7 taken together to form C3-4 cycloalkyl; R8 is H, halo and CN; R9 and R10 are independently H and halo; dashed bond is single and double bond; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their anti-HCV activity. From the assay, it was determined that compound II exhibited IC50 values in the range of 4.006 nM to 6.558 nM. 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).Electric Literature of 1256359-96-2

The Article related to tetracyclic heterocycle preparation antiviral treatment hepatitis c, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Electric Literature 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 7, 2022, Borjesson, Ulf; Perry, Matthew William Dampier; Grebner, Christoph; Michaelides, Iacovos Neal; Hayhow, Thomas George Christopher; Kettle, Jason Grant; Collie, Gavin William; Storer, Robert Ian; Bagal, Sharanjeet Kaur; Fallan, Charlene published a patent.Recommanded Product: Methyl 2-(6-bromo-1H-indol-3-yl)acetate The title of the patent was Synthesis of heterocyclic substituted pyrimidine anticancer agents. And the patent contained the following:

The synthesis of heterocyclic substituted pyrimidine anticancer agents I, wherein A is a protein binder unit; Z can be a bicyclic heterocyclic ring system with multiple heteroaroms N, O, S; Y can be a pyrimidine dione moiety; R can be a substituent on any available C or N such that alkyl, alkenyl, alkynyl or related groups with optional halo, nitrile, amino or similar groups; L, as a linker, can be an (un)saturated framework comprising C and H atoms and at least one heteroatom; and n can be an integer between 0-3 are prepared as pharmaceutically acceptable salts. Of note, II demonstrated a Cereblon HTRF IC50 binding of 2.1μM and can be employed in the treatment of cancers in humans or animals such that solid tumors, BRD4-sensitive tumors. The experimental process involved the reaction of Methyl 2-(6-bromo-1H-indol-3-yl)acetate(cas: 152213-63-3).Recommanded Product: Methyl 2-(6-bromo-1H-indol-3-yl)acetate

The Article related to heterocyclic pyrimidine anticancer preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Recommanded Product: Methyl 2-(6-bromo-1H-indol-3-yl)acetate

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