Category: 79815-20-6

Beury-Cirou, Amelie; Tannieres, Melanie; Minard, Corinne; Soulere, Laurent; Rasamiravaka, Tsiry; Dodd, Robert H.; Queneau, Yves; Dessaux, Yves; Guillou, Catherine; Vandeputte, Olivier M.; Faure, Denis published an article in 2013, the title of the article was At a supra-physiological concentration, human sexual hormones act as quorum-sensing inhibitors.Name: H-Idc-OH And the article contains the following content:

N-Acylhomoserine lactone (AHL)-mediated quorum-sensing (QS) regulates virulence functions in plant and animal pathogens such as Agrobacterium tumefaciens and Pseudomonas aeruginosa. A chemolibrary of more than 3500 compounds was screened using two bacterial AHL-biosensors to identify QS-inhibitors (QSIs). The purity and structure of 15 QSIs selected through this screening were verified using HPLC MS/MS tools and their activity tested on the A. tumefaciens and P. aeruginosa bacterial models. The IC50 value of the identified QSIs ranged from 2.5 to 90 渭g/mL, values that are in the same range as those reported for the previously identified QSI 4-nitropyridine-N-oxide (IC50 24 渭g/mL). Under the tested culture conditions, most of the identified QSIs did not exhibit bacteriostatic or bactericidal activities. One third of the tested QSIs, including the plant compound hordenine and the human sexual hormone estrone, decreased the frequency of the QS-regulated horizontal transfer of the tumor-inducing (Ti) plasmid in A. tumefaciens. Hordenine, estrone as well as its structural relatives estriol and estradiol, also decreased AHL accumulation and the expression of six QS-regulated genes (lasI, lasR, lasB, rhlI, rhlR, and rhlA) in cultures of the opportunist pathogen P. aeruginosa. Moreover, the ectopic expression of the AHL-receptors RhlR and LasR of P. aeruginosa in E. coli showed that their gene-regulatory activity was affected by the QSIs. Finally, modeling of the structural interactions between the human hormones and AHL-receptors LasR of P. aeruginosa and TraR of A. tumefaciens confirmed the competitive binding capability of the human sexual hormones. This work indicates potential interferences between bacterial and eukaryotic hormonal communications. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Name: H-Idc-OH

The Article related to human sex hormone quorum sensing inhibition agrobacterium pseudomonas, Microbial, Algal, and Fungal Biochemistry: Other and other aspects.Name: H-Idc-OH

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

On January 31, 2015, Holland, Mareike C.; Meemken, Fabian; Baiker, Alfons; Gilmour, Ryan published an article.Application In Synthesis of H-Idc-OH The title of the article was Chiral imidazolidinone and proline-derived surface modifiers for the Pt-catalyzed asymmetric hydrogenation of activated ketones. And the article contained the following:

A series of imidazolidinone and proline derivatives have been synthesized and tested with regard to their suitability for a chiral modification of platinum used for an asym. hydrogenation of activated ketones. Hydrogenation of ketopantolactone (KPL), Me benzoyl-formate (MBF) and trifluoroacetophenone (TFAP) performed at low hydrogen pressures (1 and 10 bar) were selected as test reactions. With some of these synthetic modifiers, encouraging levels of enantioselectivity were achieved (up to 73.5:26.5 e.r.) without optimization of the reaction conditions. Moreover, performance enhancement of L-proline derived-modifiers, as a consequence of mol. editing with fluorine, was found to be significant (OH éˆ?F, 螖ee up to 23%) contributing to the growing interest in modulating catalyst performance by fluorine introduction. The synthesis of the target compounds was achieved using Engelhard-4759 [i.e., a dihydrocinchonidine-modified 5% platinum-on-alumina catalyst (Engelhard Corp.)] as a catalyst. Chiral modifiers included (8ä¼?9R)-cinchonan-9-ol (cinchonidine), (5S)-2,2,3-trimethyl-5-[(3,4,5-trimethoxyphenyl)methyl]-4-imidazolidinone, (3S)-1-methyl-3-(phenylmethyl)-1,4-diazaspiro[4.4]nonan-2-one, (2S)-ä¼?ä¼?diphenyl-2-pyrrolidinemethanol (proline derivative), (2S)- 2-(fluorodiphenylmethyl)pyrrolidine, (2S)-2,3-dihydro-1H-indole-2-carboxylic acid. Starting materials included activated ketones, such as dihydro-4,4-dimethyl-2,3-furandione (furan-diketone), ä¼?(oxo)benzeneacetic acid Me ester (oxo carboxylic acid ester), 2,2,2-trifluoro-1-(phenyl)ethanone (trifluoromethyl ketone). The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Application In Synthesis of H-Idc-OH

The Article related to hydrogenation stereoselective enantioselective synthesis, Heterocyclic Compounds (One Hetero Atom): Furans and other aspects.Application In Synthesis of H-Idc-OH

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

Guerrero-Rubio, Maria Alejandra; Lopez-Llorca, Rosalia; Henarejos-Escudero, Paula; Garcia-Carmona, Francisco; Gandia-Herrero, Fernando published an article in 2019, the title of the article was Scaled-up biotechnological production of individual betalains in a microbial system.Safety of H-Idc-OH And the article contains the following content:

Summary : The recent interest in plant pigment betalains as bioactive compounds and chemopreventive agents has led to the search for a reliable and scalable process to obtain them. The cloning of the novel and efficient enzyme 4,5-DOPA-extradiol dioxygenase from Gluconacetobacter diazotrophicus in an expression vector, and the subsequent heterologous expression in Escherichia coli cultures has led to the start-up of a biotechnol. production system of individual pigments. The aim of this study was to search for the optimal conditions for the production of betalamic acid in microbial factories and the scaled-up obtention of the derived pigments. Four different betaxanthins and two betacyanins were obtained after the addition of non-transformable amines and amino acids and their condensation with the betalamic acid produced by the dioxygenase. The scaled-up obtention and purification of betalains improved the yields of the previous methodologies reaching quantities by up to 150 mg of pure compounds The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Safety of H-Idc-OH

The Article related to gluconacetobacter betalain biotechnol production microbial system, Fermentation and Bioindustrial Chemistry: Other and other aspects.Safety of H-Idc-OH

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

On August 31, 2016, Miller, Michael L.; Fishkin, Nathan E.; Li, Wei; Whiteman, Kathleen R.; Kovtun, Yelena; Reid, Emily E.; Archer, Katie E.; Maloney, Erin K.; Audette, Charlene A.; Mayo, Michele F.; Wilhelm, Alan; Modafferi, Holly A.; Singh, Rajeeva; Pinkas, Jan; Goldmacher, Victor; Lambert, John M.; Chari, Ravi V. J. published an article.Safety of H-Idc-OH The title of the article was A New Class of Antibody-Drug Conjugates with Potent DNA Alkylating Activity. And the article contained the following:

The promise of tumor-selective delivery of cytotoxic agents in the form of antibody-drug conjugates (ADC) has now been realized, evidenced by the approval of two ADCs, both of which incorporate highly cytotoxic tubulin-interacting agents, for cancer therapy. An ongoing challenge remains in identifying potent agents with alternative mechanisms of cell killing that can provide ADCs with high therapeutic indexes and favorable tolerability. Here, we describe the development of a new class of potent DNA alkylating agents that meets these objectives. Through chem. design, we changed the mechanism of action of our novel DNA crosslinking agent to a monofunctional DNA alkylator. This modification, coupled with linker optimization, generated ADCs that were well tolerated in mice and demonstrated robust antitumor activity in multiple tumor models at doses 1.5% to 3.5% of maximally tolerated levels. These properties underscore the considerable potential of these purpose-created, unique DNA-interacting conjugates for broadening the clin. application of ADC technol. Mol Cancer Ther; 15(8); 1870-8. æ¼?016 AACR. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Safety of H-Idc-OH

The Article related to antibody drug conjugate dna alkylating antitumor activity, Immunochemistry: Antibodies and Immunoglobulins and other aspects.Safety of H-Idc-OH

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

On December 20, 2020, Lee, Yesol; Kim, Ra Yun; Eom, In-Yong published an article.Product Details of 79815-20-6 The title of the article was Accuracy Improvement When Determining Copper(II) Ions With Zincon at Acidic Condition. And the article contained the following:

2-Carboxy-2′-hydorxy-5′-sulfoformazylbenzene has been widely used to determine Cu(II) ions. In general, basic pH condition is preferred to enhance the reactivity between metal ions and zincon. But acidic condition can be applied for copper determination because Cu(II) cannot lose reactivity at acidic condition. Also, pH = 5 condition can minimize the interference from zinc which is found together with copper in many samples. However, zincon can be precipitated at acidic condition. We minimized precipitation problem by adding cyclohexanone or the use of lower buffer concentration Using this approach, accuracy was improved from -17.7 to 242.5% to -0.4% to 22.0%. A very linear calibration curve (r2 = 0.9999) was obtained for the copper concentration range of 30-2002 ng/mL. This method was successfully applied to determine copper concentration from discharged water samples. No significant interference was observed and the estimated LOD (S/N = 3) is 5.5 ng/mL. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Product Details of 79815-20-6

The Article related to zincon copper ion acidic condition linear calibration curve, Water: Analysis and other aspects.Product Details of 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 November 4, 2002, Zhao, He; He, Xiaoshu; Thurkauf, Andrew; Hoffman, Diane; Kieltyka, Andrzej; Brodbeck, Robbin; Primus, Renee; Wasley, Jan W. F. published an article.Formula: C9H9NO2 The title of the article was Indoline and piperazine containing derivatives as a novel class of mixed D2/D4 receptor antagonists. Part 2: Asymmetric synthesis and biological evaluation. And the article contained the following:

A series of chiral benzylpiperazinyl-1-(2,3-dihydroindol-1-yl)ethanone derivatives were prepared and examined for their affinity at dopamine D2 and D4 receptors. Three compounds having D2/D4 affinity ratios approximating that found for the atypical neuroleptic clozapine were further evaluated in behavioral tests of antipsychotic efficacy and motor side effects. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Formula: C9H9NO2

The Article related to dopamine receptor antagonist antipsychotic indoline piperazine derivative, Pharmacology: Structure-Activity and other aspects.Formula: C9H9NO2

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 15, 2007, Perni, Robert B.; Chandorkar, Gurudatt; Cottrell, Kevin M.; Gates, Cynthia A.; Lin, Chao; Lin, Kai; Luong, Yu-Ping; Maxwell, John P.; Murcko, Mark A.; Pitlik, Janos; Rao, Govinda; Schairer, Wayne C.; Van Drie, John; Wei, Yunyi published an article.Related Products of 79815-20-6 The title of the article was Inhibitors of hepatitis C virus NS3·4A protease. Effect of P4 capping groups on inhibitory potency and pharmacokinetics. And the article contained the following:

Reversible tetrapeptide-based compounds have been shown to effectively inhibit the hepatitis C virus NS3·4A protease. Inhibition of viral replicon RNA production in Huh-7 cells has also been demonstrated. We show herein that the inclusion of hydrogen bond donors on the P4 capping group of tetrapeptide-based inhibitors result in increased binding potency to the NS3·4A protease. The capping groups also impart significant effects on the pharmacokinetic profile of these inhibitors. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Related Products of 79815-20-6

The Article related to hepatitis c virus protease inhibitor preparation structure activity, Pharmacology: Structure-Activity and other aspects.Related Products of 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 November 17, 2005, Ganellin, C. Robin; Bishop, Paul B.; Bambal, Ramesh B.; Chan, Suzanne M. T.; Leblond, Bertrand; Moore, Andrew N. J.; Zhao, Lihua; Bourgeat, Pierre; Rose, Christiane; Vargas, Froylan; Schwartz, Jean-Charles published an article.Related Products of 79815-20-6 The title of the article was Inhibitors of Tripeptidyl Peptidase II. 3. Derivation of Butabindide by Successive Structure Optimizations Leading to a Potential General Approach to Designing Exopeptidase Inhibitors. And the article contained the following:

The cholecystokinin-8 (CCK-8)-inactivating peptidase is a serine peptidase that has been shown to be a membrane-bound isoform of tripeptidyl peptidase II (EC 3.4.14.10). It cleaves the neurotransmitter CCK-8 sulfate at the Met-Gly bond to give Asp-Tyr(SO3H)-Met-OH + Gly-Trp-Met-Asp-Phe-NH2. Starting from Val-Pro-NHBu, a dipeptide of submicromolar affinity that had previously been generated to serve as a lead, successive optimization at P3, P1, and then P2 gave Abu-Pro-NHBu (18, Ki = 80 nM). Further transformation (by making a benzologue) gave the indoline analog, butabindide (33) as a reversible inhibitor having nanomolar affinity (Ki = 7 nM). Retrospective anal. suggested the possibility of a general approach to designing exopeptidase inhibitors starting from the structure of the first hydrolysis product. Application of this approach to CCK-8 led to Abu-Phe-NHBu (37), but this only had Ki = 9.4 μM. Mol. modeling, to determine the min. energy conformations and explain the 1000-fold better affinity of butabindide, indicated that 37 cannot access the likely active conformation of butabindide. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Related Products of 79815-20-6

The Article related to tripeptidyl peptidase butabindide designing exopeptidase, Pharmacology: Structure-Activity and other aspects.Related Products of 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 April 12, 2018, Lin, Hua; Long, Jonathan Z.; Roche, Alexander M.; Svensson, Katrin J.; Dou, Florence Y.; Chang, Mi Ra; Strutzenberg, Timothy; Ruiz, Claudia; Cameron, Michael D.; Novick, Scott J.; Berdan, Charles A.; Louie, Sharon M.; Nomura, Daniel K.; Spiegelman, Bruce M.; Griffin, Patrick R.; Kamenecka, Theodore M. published an article.Related Products of 79815-20-6 The title of the article was Discovery of Hydrolysis-Resistant Isoindoline N-Acyl Amino Acid Analogues that Stimulate Mitochondrial Respiration. And the article contained the following:

N-Acyl amino acids directly bind mitochondria and function as endogenous uncouplers of UCP1-independent respiration. The authors found that administration of N-acyl amino acids to mice improves glucose homeostasis and increases energy expenditure, indicating that this pathway might be useful for treating obesity and associated disorders. The authors report the full account of the synthesis and mitochondrial uncoupling bioactivity of lipidated N-acyl amino acids and their unnatural analogs. Unsaturated fatty acid chains of medium length and neutral amino acid head groups are required for optimal uncoupling activity on mammalian cells. A class of unnatural N-acyl amino acid analogs, characterized by isoindoline-1-carboxylate head groups, were resistant to enzymic degradation by PM20D1 and maintained uncoupling bioactivity in cells and in mice. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Related Products of 79815-20-6

The Article related to isoindoline acyl amino acid mitochondria respiration, Pharmacology: Structure-Activity and other aspects.Related Products of 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

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