Month: November 2022

On January 15, 2004, Seeberger, Peter H.; Hewitt, Michael C.; Snyder, Daniel published a patent.Formula: C16H19NO6S The title of the patent was Solid-phase and solution-phase synthesis of glycosylphosphatidylinositol glycans. And the patent contained the following:

One aspect of the present invention relates to solution-phase synthesis approaches to glycosylphosphatidylinositol (GPI) I, wherein, n is 1-4; R represents independently for each occurrence H, alkyl, aryl, CH2-aryl, C(O)-alkyl, C(O)-aryl, or Si(alkyl)3; R1 and R2 are independently H, CH2-aryl, C(O)-alkyl, C(O)-aryl, Si(alkyl)3; or R1 and R2 taken together are C(CH3)2, P(O)OH, or P(O)OR5; R3 is amino, N3, or NH3X; R4 represents independently for each occurrence H, alkyl, aryl, CH2-aryl, C(O)- alkyl, C(O)-aryl, Si(alkyl)3, or P(O)(OR5)2; R5 represents independently for each occurrence H, Li+, Na+, K+, Rb+, Cs+, aryl, or an optionally substituted alkyl group; and X is a halogen, alkyl carboxylate, or aryl carboxylate. Another aspect of the present invention relates to key building blocks, and syntheses thereof, useful for GPI assembly. Yet another aspect of the invention relates to an automated method for the synthesis of GPIs and fragments thereof. The synthesis of a pseudo-hexasaccharide glycosylphosphatidylinositol has been reduced to practice, both in solution and using a combination of solution and automated solid-phase methodologies. The material made in solution was covalently attached to a protein carrier and used to vaccinate mice. Inoculated mice were substantially protected against a subsequent challenge with Plasminodium parasites. This discovery further implicates GPI as the dominant toxin in malaria infections, and lays the groundwork for future trials in human volunteers. Combinations of solution and automated solid-phase synthetic methodologies will see continued usage in this context, and are expected to lead to the rapid generation of more potent vaccines for malaria and other maladies. 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 glycosylphosphatidylinositol oligosaccharide glycan solid phase synthesis vaccine human, Carbohydrates: Alditols, Cyclitols, Glycerides and other aspects.Formula: C16H19NO6S

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 7, 2012, Lagrange, Alain; Mignon, Marie published a patent.Electric Literature of 52537-00-5 The title of the patent was Hair dye composition comprising an indoline coupler in a medium rich in fatty substances. And the patent contained the following:

The present invention relates to a composition for dyeing keratin fibers, such as hair, comprising: a fatty substance, a surfactant; an oxidation base, one or more indoline couplers (I, R1 = e.g., H, C1-10 alkyl or alkenyl; R2 = halo, C1-10 alkyl or alkenyl, and 2 radicals R2 borne by adjacent carbon atoms forming a 5-8 membered ring; and n = 0-4; R3,R4 = H, halo halo, C1-10 alkyl or alkenyl, or C1-8 alkoxy); and the fatty substance content at 25% by weight The present invention also relates to a process of using this composition in the presence of a chem. oxidizing agent, and to multicompartment devices suitable for the implementation of the invention. Thus, a formulation containing 4-(3-aminopyrazolo[1,5-a]pyridin-2-yl)-1,1-dimethylpiperazin-1-ium chloride hydrochloride provides a raise in 螖Elab color much more important on 90% white hair and therefore a much better staining in the root than that obtained using a comparative composition The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Electric Literature of 52537-00-5

The Article related to hair dye indoline coupler fatty substance, Essential Oils and Cosmetics: Hair Preparations and other aspects.Electric Literature of 52537-00-5

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 6, 2012, Lagrange, Alain; Mignon, Marie published a patent.Application In Synthesis of 6-Chloro-2,3-dihydro-1H-indole The title of the patent was Hair dye composition comprising a (hydroxy)indoline coupler in a medium rich in fatty substances. And the patent contained the following:

The present invention relates to a composition for dyeing keratin fibers, such as hair, comprising: a fatty substance, a surfactant; an oxidation base, one or more indoline couplers (I, R1 = e.g., H, C1-10 alkyl, C2-10 alkenyl; R2 = OH, halo, C1-10 alkyl, C3-10 alkenyl; R2 being connected to a heterocycle via a C-C bond, a carboxyl or alkoxycarbonyl and n = 0-4; R3 = halo, C1-10 alkyl, C3-10 alkenyl, OH, C1-8 alkylthio, amino, and p = 0-3, and also salts, optical and geometrical isomers and tautomers, and hydrates thereof), and a basifying agent;and the fatty substance content at 25% by weight The present invention also relates to a process of using this composition in the presence of a chem. oxidizing agent, and to multicompartment devices suitable for the implementation of the invention. Thus, a formulation contained 2,3-diaminodihydropyrazolopyrazolone dimethosulfonate (oxidation base) 2×10-2 and 1-methylindolin-4-ol (coupler) 2×10-2 mol in addition to other cosmetic ingredients. 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 hair dye hydroxyindoline coupler fatty substance, Essential Oils and Cosmetics: Hair Preparations 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

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 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

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