Day: November 9, 2022

On December 15, 2006, Larsen, Scott D.; Hester, Matthew R.; Ruble, J. Craig; Kamilar, Gregg M.; Romero, Donna L.; Wakefield, Brian; Melchior, Earline P.; Sweeney, Michael T.; Marotti, Keith R. published an article.Computed Properties of 52537-00-5 The title of the article was Discovery and initial development of a novel class of antibacterials: Inhibitors of Staphylococcus aureus transcription/translation. And the article contained the following:

The novel bacterial transcription/translation (TT) inhibitor 1 was identified through a combination of high throughput screening and exploratory medicinal chem. Initial optimization of the anthranilic acid moiety and sulfonamide amine diversity was accomplished via 1- and two-dimensional solution phase libraries, resulting in an improvement in the MIC of the lead from 64 to 8 μg/mL (compound 4l). Subsequent modification of the central aromatic ring and further refinement of the sulfonamide amines required the development of a solid phase route on Wang resin. The resulting libraries generated a number of potent antibacterials with MICs of ≤1 μg/mL (e.g., 10b, 12, and 13). During the course of this work, it became apparent that the antibacterial activity of the series is not fully correlated with TT inhibition, suggesting that at least one addnl. mechanism of action is operative. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Computed Properties of 52537-00-5

The Article related to antibacterial staphylococcus aureus anthranilic acid derivative sar preparation, Pharmacology: Structure-Activity and other aspects.Computed Properties 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 March 10, 2016, Pelz, Nicholas F.; Bian, Zhiguo; Zhao, Bin; Shaw, Subrata; Tarr, James C.; Belmar, Johannes; Gregg, Claire; Camper, DeMarco V.; Goodwin, Craig M.; Arnold, Allison L.; Sensintaffar, John L.; Friberg, Anders; Rossanese, Olivia W.; Lee, Taekyu; Olejniczak, Edward T.; Fesik, Stephen W. published an article.Recommanded Product: 79815-20-6 The title of the article was Discovery of 2-Indole-acylsulfonamide Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors Using Fragment-Based Methods. And the article contained the following:

Myeloid cell leukemia-1 (Mcl-1) is a member of the Bcl-2 family of proteins responsible for the regulation of programmed cell death. Amplification of Mcl-1 is a common genetic aberration in human cancer whose overexpression contributes to the evasion of apoptosis and is one of the major resistance mechanisms for many chemotherapies. Mcl-1 mediates its effects primarily through interactions with pro-apoptotic BH3 containing proteins that achieve high affinity for the target by utilizing four hydrophobic pockets in its binding groove. Here we describe the discovery of Mcl-1 inhibitors using fragment-based methods and structure-based design. These novel inhibitors exhibit low nanomolar binding affinities to Mcl-1 and >500-fold selectivity over Bcl-xL. X-ray structures of lead Mcl-1 inhibitors when complexed to Mcl-1 provided detailed information on how these small-mols. bind to the target and were used extensively to guide compound optimization. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Recommanded Product: 79815-20-6

The Article related to preparation indoleacylsulfonamide antitumor myeloid leukemia, crystal structure, Pharmacology: Structure-Activity and other aspects.Recommanded Product: 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

On October 8, 2015, Cleghorn, Laura A. T.; Albrecht, Sebastien; Stojanovski, Laste; Simeons, Frederick R. J.; Norval, Suzanne; Kime, Robert; Collie, Iain T.; De Rycker, Manu; Campbell, Lorna; Hallyburton, Irene; Frearson, Julie A.; Wyatt, Paul G.; Read, Kevin D.; Gilbert, Ian H. published an article.Safety of H-Idc-OH The title of the article was Discovery of Indoline-2-carboxamide Derivatives as a New Class of Brain-Penetrant Inhibitors of Trypanosoma brucei. And the article contained the following:

There is an urgent need for new, brain penetrant small mols. that target the central nervous system second stage of human African trypanosomiasis (HAT). We report that a series of novel indoline-2-carboxamides have been identified as inhibitors of Trypanosoma brucei from screening of a focused protease library against Trypanosoma brucei brucei in culture. We describe the optimization and characterization of this series. Potent antiproliferative activity was observed The series demonstrated excellent pharmacokinetic properties, full cures in a stage 1 mouse model of HAT, and a partial cure in a stage 2 mouse model of HAT. Lack of tolerability prevented delivery of a fully curative regimen in the stage 2 mouse model and thus further progress of this series. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Safety of H-Idc-OH

The Article related to trypanosomicide indolinecarboxamide preparation structure activity brain penetrant trypanosomiasis, Pharmacology: Structure-Activity and other aspects.Safety of 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 24, 1997, Bromidge, Steven M.; Duckworth, Malcolm; Forbes, Ian T.; Ham, Peter; King, Frank D.; Thewlis, Kevin M.; Blaney, Frank E.; Naylor, Christopher B.; Blackburn, Thomas P.; Kennett, Guy A.; Wood, Martyn D.; Clarke, Stephen E. published an article.Computed Properties of 52537-00-5 The title of the article was 6-Chloro-5-methyl-1-[[2-[(2-methyl-3- pyridyl)oxy]-5-pyridyl]carbamoyl]indoline (SB-242084): The First Selective and Brain Penetrant 5-HT2C Receptor Antagonist. And the article contained the following:

The synthesis and biol. activity of a number of substituted 1-(3-pyridylcarbamoyl)indolines is reported. These compounds are potent and selective 5-HT2C/2B receptor antagonists and illustrate the use of 5,6-disubstitution as a replacement for a fused 5-membered ring in this context. Unfortunately, some compounds were also found to be very potent inhibitors of a number of human cytochrome P 450 enzymes which precluded their development as potential anxiolytic agents. Elaboration of the left hand side pyridyl ring abolished the inhibitory activity, leading to bipyridylethers such as SB-242084 which is the first reported brain penetrant, 5-HT2C receptor antagonist with selectivity over both the 5-HT2A and 5-HT2B receptor subtypes. Furthermore, SB-242084 was found to exert marked anxiolytic-like responses in rat models, confirming that these responses are mediated by 5-HT2C receptor blockade. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Computed Properties of 52537-00-5

The Article related to pyridylcarbamoyl indoline preparation structure 5ht2c antagonist, sb242084 serotoninergic s2c receptor antagonist, Pharmacology: Structure-Activity and other aspects.Computed Properties 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 September 1, 2015, Gehling, Victor S.; Vaswani, Rishi G.; Nasveschuk, Christopher G.; Duplessis, Martin; Iyer, Priyadarshini; Balasubramanian, Srividya; Zhao, Feng; Good, Andrew C.; Campbell, Robert; Lee, Christina; Dakin, Les A.; Cook, Andrew S.; Gagnon, Alexandre; Harmange, Jean-Christophe; Audia, James E.; Cummings, Richard T.; Normant, Emmanuel; Trojer, Patrick; Albrecht, Brian K. published an article.Quality Control of Methyl 2-methyl-1H-indole-3-carboxylate The title of the article was Discovery, design, and synthesis of indole-based EZH2 inhibitors. And the article contained the following:

The discovery and optimization of a series of small mol. EZH2 inhibitors is described. Starting from dimethylpyridone HTS hit, a series of indole-based EZH2 inhibitors were identified. Biochem. potency and microsomal stability were optimized during these studies and afforded compound (I). Compound I demonstrates nanomolar levels of biochem. potency (IC50 = 0.002 μM), cellular potency (EC50 = 0.080 μM), and afforded tumor regression when dosed (200 mpk SC BID) in an EZH2 dependent tumor xenograft model. The experimental process involved the reaction of Methyl 2-methyl-1H-indole-3-carboxylate(cas: 65417-22-3).Quality Control of Methyl 2-methyl-1H-indole-3-carboxylate

The Article related to indole derivative preparation sar ezh2 inhibitor anticancer mao cell, ezh2, epigenetics, histone methyltransferase, prc2, pyridone, Pharmacology: Structure-Activity and other aspects.Quality Control of Methyl 2-methyl-1H-indole-3-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 January 7, 2019, Nakamura, Hidemitsu; Hirabayashi, Kei; Miyakawa, Takuya; Kikuzato, Ko; Hu, Wenqian; Xu, Yuqun; Jiang, Kai; Takahashi, Ikuo; Niiyama, Ruri; Dohmae, Naoshi; Tanokura, Masaru; Asami, Tadao published an article.Recommanded Product: 6-Chloro-2,3-dihydro-1H-indole The title of the article was Triazole Ureas Covalently Bind to Strigolactone Receptor and Antagonize Strigolactone Responses. And the article contained the following:

Strigolactones, a class of plant hormones with multiple functions, mediate plant-plant and plant-microorganism communications in the rhizosphere. In this study, we developed potent strigolactone antagonists, which covalently bind to the strigolactone receptor D14, by preparing an array of triazole urea compounds Using yeast two-hybrid and rice-tillering assays, we identified a triazole urea compound KK094 as a potent inhibitor of strigolactone receptors. Liquid chromatog.-tandem mass spectrometry anal. and X-ray crystallog. revealed that KK094 was hydrolyzed by D14, and that a reaction product of this degradation covalently binds to the Ser residue of the catalytic triad of D14. Furthermore, we identified two triazole urea compounds KK052 and KK073, whose effects on D14-D53/D14-SLR1 complex formation were opposite due to the absence (KK052) or presence (KK073) of a trifluoromethyl group on their Ph ring. These results demonstrate that triazole urea compounds are potentially powerful tools for agricultural application and may be useful for the elucidation of the complicated mechanism underlying strigolactone perception. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Recommanded Product: 6-Chloro-2,3-dihydro-1H-indole

The Article related to oryza tillering triazole urea strigolactone signaling, covalent antagonist, crystal structure, strigolactone, triazole urea, Agrochemical Bioregulators: Plant and other aspects.Recommanded Product: 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

On July 4, 2007, Hartikka, Antti; Slosarczyk, Adam T.; Arvidsson, Per I. published an article.Recommanded Product: H-Idc-OH The title of the article was Application of novel sulfonamides in enantioselective organocatalyzed cyclopropanation. And the article contained the following:

Three novel aryl sulfonamides derived from (2S)-indoline-2-carboxylic acid have been obtained and used as organocatalysts. The catalysts incorporate diverse functionality on the Ph ring, enabling steric, and electronic fine tuning of the catalysts. The catalysts facilitate the reaction between a range of α,β-unsaturated aldehydes and sulfur ylides, thus providing cyclopropane products in enantiomeric excesses of up to 99%. E.g., reaction of (E)-MeCH:CHCHO and Me2S+C-HCOPh gave 45% cyclopropane I (88% ee). The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Recommanded Product: H-Idc-OH

The Article related to enantioselective cyclopropanation unsaturated aldehyde sulfur ylide arylsulfonamide catalyst, Alicyclic Compounds: Cyclopropanes 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

Demerson, Christopher A.; Humber, Leslie G.; Philipp, Adolph H.; Martel, Rene R. published an article in 1976, the title of the article was Etodolic acid and related compounds. Chemistry and antiinflammatory actions of some potent di- and trisubstituted 1,3,4,9-tetrahydropyrano[3,4-b]indole-1-acetic acids.Safety of 7-Isopropyl-1H-indole And the article contains the following content:

Of 37 title compounds, prepared by the condensation of a substituted tryptophol with the appropriate β-keto ester, etodolic acid (I) [41340-25-4], II [57817-27-3], III [57817-28-4], and IV [57817-29-5] were considerably more active than phenylbutazone [50-33-9] and approached the activity of indomethacin [53-86-1] against a chronic rat model of inflammation. The compounds, which were more potent against chronic inflammation than in the carrageenin paw edema test, had relatively low acute ulcerogenic potential in rats. Structure-activity relations were discussed. The experimental process involved the reaction of 7-Isopropyl-1H-indole(cas: 57817-04-6).Safety of 7-Isopropyl-1H-indole

The Article related to inflammation inhibitor tetrahydropyranoindoleacetate, pyranoindoleacetate antiinflammatory, Pharmacodynamics: Structure-Activity and other aspects.Safety of 7-Isopropyl-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

Sau, Abhijit; Misra, Anup Kumar published an article in 2011, the title of the article was Environmentally Benign Preparation of Benzylidene Acetal of Carbohydrate Derivatives in PEG 600.Formula: C16H19NO6S And the article contains the following content:

An environmentally benign preparation of benzylidene acetal of carbohydrate derivatives catalyzed by HClO4-SiO2 in PEG 600 as solvent has been developed. Yields were excellent in every case. 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).Formula: C16H19NO6S

The Article related to benzylidene acetal glycoside preparation, Carbohydrates: Monosaccharides, Glycals and other aspects.Formula: C16H19NO6S

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

Furuta, Kenjiro; Yoshida, Shuhei; Fujita, Norihiro; Yamada, Naotaka; Kuwano, Eiichi published an article in 2009, the title of the article was Ethyl 4-[(1-substituted indol-2-yl)methoxy]benzoates and indoline derivatives: anti-juvenile hormone and juvenile hormone activities.Name: H-Idc-OH And the article contains the following content:

A number of Et 4-[(1-substituted indol-2-yl)methoxy]benzoates and indoline derivatives were prepared as rigid congeners of Et 4-(2-benzylhexyloxy)benzoate (KF-13), an anti-juvenile hormone (anti-JH) agent, and tested for both anti-JH and JH activities in silkworm larvae. In contrast to KF-13, the precocious metamorphosis-inducing activity of which decreased by increasing the applied doses, 1-Pr, 1-Bu (1c) and 1-benzyl (1d) derivatives were found to induce higher percentages of precocious metamorphosis at high doses. Compounds 1c and 1d also exhibited JH activity when topically applied to allatectomized 4 th instar larvae. Et 4-[(S)-(1-n-butylindolin-2-yl)methoxy]benzoate, which showed precocious metamorphosis-inducing activity at high doses, had no JH activity. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Name: H-Idc-OH

The Article related to ethyl indolylmethoxybenzoate indoline derivative juvenile hormone, anti juvenile hormone juvenile hormone indole indoline precocious metamorphosis, Agrochemical Bioregulators: Invertebrate and other aspects.Name: 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