Tag: 200-300

COA of Formula: C10H22N2O2In 2018 ,《Design and Synthesis of Quenched Activity-based Probes for Diacylglycerol Lipase and α,β-Hydrolase Domain Containing Protein 6》 appeared in Chemistry – An Asian Journal. The author of the article were van Rooden, E. J.; Kohsiek, M.; Kreekel, R.; van Esbroeck, A. C. M.; van den Nieuwendijk, A. M. C. H.; Janssen, A. P. A.; van den Berg, R. J. B. H. N.; Overkleeft, H. S.; van der Stelt, M.. The article conveys some information:

Diacylglycerol lipases (DAGL) are responsible for the biosynthesis of the endocannabinoid 2-arachidonoylglycerol. The fluorescent activity-based probes (ABPs) DH379 and HT-01 have been previously shown to label DAGLs and to cross-react with the serine hydrolase ABHD6. Here, we report the synthesis and characterization of two new quenched activity-based probes (qABPs) 1 and 2, the design of which was based on the structures of DH379 and HT-01, resp. Probe 1 contains a BODIPY-FL and a 2,4-dinitroaniline moiety as a fluorophore-quencher pair, whereas probe 2 employs a Cy5-fluorophore and a cAB40-quencher. The fluorescence of both probes was quenched with relative quantum yields of 0.34 and 0.0081, resp. The probes showed target inhibition as characterized in activity-based protein profiling assays using human cell- and mouse brain lysates, but were unfortunately not active in living cells, presumably due to limited cell permeability. The results came from multiple reactions, including the reaction of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3COA of Formula: C10H22N2O2)

Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).COA of Formula: C10H22N2O2

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

In 2022,Li, Steven A.; Cadelis, Melissa M.; Deed, Rebecca C.; Douafer, Hana; Bourguet-Kondracki, Marie-Lise; Michel Brunel, Jean; Copp, Brent R. published an article in Bioorganic & Medicinal Chemistry. The title of the article was 《Valorisation of the diterpene podocarpic acid – Antibiotic and antibiotic enhancing activities of polyamine conjugates》.Reference of N-Boc-1,6-Diaminohexane The author mentioned the following in the article:

As part of our search for new antimicrobials and antibiotic adjuvants, a series of podocarpic acid-polyamine conjugates have been synthesized. The library of compounds made use of the phenolic and carboxylic acid moieties of the diterpene allowing attachment of polyamines (PA) of different lengths to afford a structurally-diverse set of analogs. Evaluation of the conjugates for intrinsic antimicrobial properties identified two derivatives of interest: a PA3-4-3 (spermine) amide-bonded variant 7a that was a non-cytotoxic, non-hemolytic potent growth inhibitor of Gram-pos. Staphylococcus aureus (MRSA) and 9d, a PA3-8-3 carbamate derivative that was a non-toxic selective antifungal towards Cryptococcus neoformans. Of the compound set, only one example exhibited activity towards Gram-neg. bacteria. However, in the presence of sub-therapeutic amounts of either doxycycline (4.5 μM) or erythromycin (2.7 μM) several analogs were observed to exhibit weak to modest antibiotic adjuvant properties against Pseudomonas aeruginosa and/or Escherichia coli. The observation of strong cytotoxicity and/or hemolytic properties for subsets of the library, in particular those analogs bearing Me ester or n-pentylamide functionality, highlighted the fine balance of structural requirements and lipophilicity for antimicrobial activity as opposed to mammalian cell toxicity. The results came from multiple reactions, including the reaction of N-Boc-1,6-Diaminohexane(cas: 51857-17-1Reference of N-Boc-1,6-Diaminohexane)

N-Boc-1,6-Diaminohexane(cas: 51857-17-1) can be used as a linear hexyl spacer (C6-spacer) to synthesize biodegradable poly(disulfide amine)s for gene delivery, a multifunctional dendrimer for theranostics and so on.Reference of N-Boc-1,6-Diaminohexane

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Chan, Hwai-Chien; Bueno, Bianca; Le Roch, Adrien; Gagnon, Alexandre published their research in Chemistry – A European Journal in 2021. The article was titled 《Copper-promoted N-arylation of the imidazole side chain of protected histidine by using triarylbismuth reagents》.SDS of cas: 7524-52-9 The article contains the following contents:

The N-arylation of the side chain of histidine by using triarylbismuthines is reported. The reaction is promoted by copper(II) acetate in dichloromethane at 40°C under oxygen in the presence of diisopropylethylamine and 1,10-phenanthroline and allows the transfer of aryl groups with substituents at any position of the aromatic ring. The reaction shows excellent functional group tolerance and is applicable to dipeptides where the histidine is located at the N terminus. A histidine-guided backbone N-H arylation was observed in dipeptides where the histidine occupies the C terminus. In the experiment, the researchers used H-Trp-OMe.HCl(cas: 7524-52-9SDS of cas: 7524-52-9)

H-Trp-OMe.HCl(cas:7524-52-9) is one of amino acid derivatives. Amino acid derivatives represent an important category of skin penetration promoters. These compounds possess hydrophobic chains attached to an amino acid headgroup via a biodegradable ester bond. Due to the amphiphilic nature of these derivatives, it is possible for them to enter into the SC lipid barrier and significantly disorganize skin membrane lipids.SDS of cas: 7524-52-9

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

In 1976,Journal of the Chemical Society included an article by Clark, John C.; Phillipps, Gordon H.; Steer, Margaret R.; Stephenson, Leslie; Cooksey, A. Roy. Recommanded Product: H-Phg-OEt.HCl. The article was titled 《Resolution of esters of phenylglycine with (+)-tartaric acid》. The information in the text is summarized as follows:

The Me, Et, and iso-Pr esters of DL-PhCH(NH2)CO2H were resolved with 1 mol. equivalent of (+)-tartaric acid in aqueous alcs. to give 25-42% D-ester hydrogen (+)-tartrate salts. The L-salts in the filtrates from the resolutions were racemized in EtOH containing polar cosolvents. The resolution and racemization stages can be combined so that DL-PhCH(NH2)CO2Et underwent a second order asymmetric transformation to give 65% Et D-phenylglycinate hydrogen (+)-tartrate. The resolved salts were hydrolyzed to give 66-91% D-PhCH(NH2)CO2H. In the experiment, the researchers used H-Phg-OEt.HCl(cas: 59410-82-1Recommanded Product: H-Phg-OEt.HCl)

H-Phg-OEt.HCl(cas: 59410-82-1) belongs to esters. They are important in biology, being one of the main classes of lipids and comprising the bulk of animal fats and vegetable oils.Recommanded Product: H-Phg-OEt.HCl Polyesters are important plastics, with monomers linked by ester moieties.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Petrachenko, N. E.; Vovna, V. I.; Furin, G. G. published an article in Zhurnal Organicheskoi Khimii. The title of the article was 《He(I) photoelectron spectra of fluorinated benzoic acid derivatives》.Name: Ethyl 2,3,4,5,6-pentafluorobenzoate The author mentioned the following in the article:

Photoelectron spectra of RC6H4CONH2 (R = 3-F, 2-F), 2,6-F2C6H3CONH2, 4-RC6X4CONHOH (R = F, X = H; R = H, X = F), C6F5CONHX (X = H, OH), and C6F5COR1 (R1 = OEt, C6F5) were obtained and interpreted with the aid of MNDO calculations Increasing the extent of fluorination leads to approx. equal stabilization of π MO and orbitals localized on the heteroatoms of the substituents.Ethyl 2,3,4,5,6-pentafluorobenzoate(cas: 4522-93-4Name: Ethyl 2,3,4,5,6-pentafluorobenzoate) was used in this study.

Ethyl 2,3,4,5,6-pentafluorobenzoate(cas: 4522-93-4) belongs to esters. Esters are more polar than ethers but less polar than alcohols. Name: Ethyl 2,3,4,5,6-pentafluorobenzoate They participate in hydrogen bonds as hydrogen-bond acceptors, but cannot act as hydrogen-bond donors, unlike their parent alcohols.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Quality Control of H-Trp-OMe.HClIn 2021 ,《Chemoselective peptide backbone diversification and bioorthogonal ligation by ruthenium-catalyzed C-H activation/annulation》 was published in Advanced Synthesis & Catalysis. The article was written by Song, Liangliang; Ojeda-Carralero, Gerardo M.; Parmar, Divyaakshar; Gonzalez-Martinez, David A.; Van Meervelt, Luc; Van der Eycken, Johan; Goeman, Jan; Rivera, Daniel G.; Van der Eycken, Erik V.. The article contains the following contents:

The field of peptide derivatization by metal-catalyzed C-H activation has been mostly directed to modify the side chains, but poor attention has been given to the peptide backbone. Here we report a ruthenium-catalyzed C-H activation/annulation process that can chemoselectively modify the peptide backbone producing functionalized isoquinolone scaffolds with high regioselectivity in a rapid and step-economical manner. This strategy is characterized by racemization-free conditions and the production of fluorescent peptides, and peptide conjugates to drugs, natural products and other peptide fragments, providing a chem. approach for the construction of novel peptide-pharmacophore conjugates. Mechanistic studies suggest that amide bonds of peptide backbone act as the bidentate directing group to promote the C-H activation/annulation process. This report provides an unprecedented example of peptide backbone diversification and bioorthogonal ligation exploiting the power of ruthenium-catalyzed C-H activation. The results came from multiple reactions, including the reaction of H-Trp-OMe.HCl(cas: 7524-52-9Quality Control of H-Trp-OMe.HCl)

H-Trp-OMe.HCl(cas:7524-52-9) is one of amino acid derivatives. Amino acid derivatives represent an important category of skin penetration promoters. These compounds possess hydrophobic chains attached to an amino acid headgroup via a biodegradable ester bond. Due to the amphiphilic nature of these derivatives, it is possible for them to enter into the SC lipid barrier and significantly disorganize skin membrane lipids.Quality Control of H-Trp-OMe.HCl

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Name: Methyl 2-(3-fluoro-4-nitrophenyl)acetateOn September 15, 2007 ,《α-Substituted N-(4-tert-butylbenzyl)-N’-[4-(methylsulfonylamino)benzyl]thiourea analogues as potent and stereospecific TRPV1 antagonists》 was published in Bioorganic & Medicinal Chemistry. The article was written by Chung, Jae-Uk; Kim, Su Yeon; Lim, Ju-Ok; Choi, Hyun-Kyung; Kang, Sang-Uk; Yoon, Hae-Seok; Ryu, HyungChul; Kang, Dong Wook; Lee, Jeewoo; Kang, Bomi; Choi, Sun; Toth, Attila; Pearce, Larry V.; Pavlyukovets, Vladimir A.; Lundberg, Daniel J.; Blumberg, Peter M.. The article contains the following contents:

A series of α-substituted N-(4-tert-butylbenzyl)-N’-[4-(methylsulfonylamino)benzyl]thiourea analogs have been investigated as TRPV1 receptor antagonists. α-Me substituted analogs showed potent and stereospecific antagonism to the action of capsaicin on rat TRPV1 heterologously expressed in Chinese hamster ovary cells. In particular, compounds (I and II), which possess the R-configuration, exhibited excellent potencies (resp., Ki = 41 and 39.2 nM and Ki(ant) = 4.5 and 37 nM).Methyl 2-(3-fluoro-4-nitrophenyl)acetate(cas: 169339-41-7Name: Methyl 2-(3-fluoro-4-nitrophenyl)acetate) was used in this study.

Methyl 2-(3-fluoro-4-nitrophenyl)acetate(cas: 169339-41-7) belongs to esters.Name: Methyl 2-(3-fluoro-4-nitrophenyl)acetate They are important in biology, being one of the main classes of lipids and comprising the bulk of animal fats and vegetable oils.Esters typically have a pleasant smell; those of low molecular weight are commonly used as fragrances and are found in essential oils and pheromones.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Product Details of 51857-17-1In 2021 ,《A PROTAC targets splicing factor 3B1》 appeared in Cell Chemical Biology. The author of the article were Gama-Brambila, Rodrigo A.; Chen, Jie; Zhou, Jun; Tascher, Georg; Muench, Christian; Cheng, Xinlai. The article conveys some information:

The proteolysis-targeting chimeras (PROTACs) are a new technol. to degrade target proteins. However, their clin. application is limited currently by lack of chem. binders to target proteins. For instance, it is still unknown whether splicing factor 3B subunit 1 (SF3B1) is targetable by PROTACs. We recently identified a 2-aminothiazole derivative (herein O4I2) as a promoter in the generation of human pluripotent stem cells. In this work, proteomic anal. on the biotinylated O4I2 revealed that O4I2 targeted SF3B1 and pos. regulated RNA splicing. Fusing thalidomide-the ligand of the cereblon ubiquitin ligase-to O4I2 led to a new PROTAC-O4I2, which selectively degraded SF3B1 and induced cellular apoptosis in a CRBN-dependent manner. In a Drosophila intestinal tumor model, PROTAC-O4I2 increased survival by interference with the maintenance and proliferation of stem cell. Thus, our finding demonstrates that SF3B1 is PROTACable by utilizing noninhibitory chems., which expands the list of PROTAC target proteins. The experimental process involved the reaction of N-Boc-1,6-Diaminohexane(cas: 51857-17-1Product Details of 51857-17-1)

N-Boc-1,6-Diaminohexane(cas: 51857-17-1) is used to prepare 1,3-Bis[6-(Boc-amino)hexyl]urea by reacting with carbonyl dichloride in the presence of triethylamine. Further, it is used as a reagent for the introduction of a C6-spacer.Product Details of 51857-17-1

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Computed Properties of C10H22N2O2In 2022 ,《Turning Nonselective Inhibitors of Type I Protein Arginine Methyltransferases into Potent and Selective Inhibitors of Protein Arginine Methyltransferase 4 through a Deconstruction-Reconstruction and Fragment-Growing Approach》 appeared in Journal of Medicinal Chemistry. The author of the article were Iannelli, Giulia; Milite, Ciro; Marechal, Nils; Cura, Vincent; Bonnefond, Luc; Troffer-Charlier, Nathalie; Feoli, Alessandra; Rescigno, Donatella; Wang, Yalong; Cipriano, Alessandra; Viviano, Monica; Bedford, Mark T.; Cavarelli, Jean; Castellano, Sabrina; Sbardella, Gianluca. The article conveys some information:

Protein arginine methyltransferases (PRMTs) are important therapeutic targets, playing a crucial role in the regulation of many cellular processes and being linked to many diseases. Yet, there is still much to be understood regarding their functions and the biol. pathways in which they are involved, as well as on the structural requirements that could drive the development of selective modulators of PRMT activity. Here we report a deconstruction-reconstruction approach that, starting from a series of type I PRMT inhibitors previously identified by us, allowed for the identification of potent and selective inhibitors of PRMT4, which regardless of the low cell permeability show an evident reduction of arginine methylation levels in MCF7 cells and a marked reduction of proliferation. We also report crystal structures with various PRMTs supporting the observed specificity and selectivity. In the experiment, the researchers used many compounds, for example, tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Computed Properties of C10H22N2O2)

Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Computed Properties of C10H22N2O2

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On April 22, 1999, Takahashi, Kanji; Sugiura, Tsuneyuki published a patent.Quality Control of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate The title of the patent was Preparation of aminobutanoic acid derivatives as inhibitors of matrix metalloproteinases. And the patent contained the following:

Aminobutanoic acid derivatives represented by general formula (I) and salts thereof [wherein R1 = CO2R10, CONHOR10, CONHNHR10, (CH2)nSR50, Y-P(:O)(OR51)2; R10 = H, C1-8 alkyl, Ph, phenyl- or C1-8 alkoxy-C1-8 alkyl, PhO2C, PhCH2O2C, C1-8 alkoxycarbonyl; wherein n = 0-3; R50 = H, C1-8 alkyl, C1-8-alkyl-carbonyl, PhCO, SH, C1-8 alkylthio, SPh; R51 = H, C1-8 alkyl, Ph; Y = single bond, CH2, O; R2-R7 = H, C2-8 alkenyl, (un)substituted SH, OH, or NH2, CO2H, C1-8 alkyl-carbonyl, C1-8 alkoxy-carbonyl, (un)substituted carbocyclyl or heterocyclyl, (un)substituted C1-8 alkyl or C2-8 alkenyl; or R3 and R4 or R5 and R6 together represents C1-8 alkylene; or R2 and R3, R4 and R5, or R6 and R7 together represent C2-8 alkylene; when R8 = H, (un)substituted C1-8 alkyl, or C1-8 alkoxy-carbonyl, R9 = (un)substituted carbocyclyl; or when R8 = (un)substituted carbocyclyl or heterocyclyl, R9 = (un)substituted C1-8 alkyl or C1-8 alkoxy, (un)substituted carbocyclyl; M = C1-8 alkylene; J = single bond, O, S, NH, C1-8 alkyl-N] are prepared and claimed. Also claimed are matrix metalloproteinases containing I as the active ingredients and drugs containing I as the active ingredients for the prevention and/or treatment of rheumatism, osteoarthritis, pathol. bone resorption, osteoporosis, periodontal diseases, interstitial nephritis, arteriosclerosis, pulmonary emphysema, hepatic cirrhosis, corneal injury, diseases due to metastasis and infiltration of cancer cells or proliferation thereof, autoimmune diseases (such as Crohn’s disease and Sjogren’s disease), diseases due to transmigration of white blood cells or infiltration thereof, neovascularization, multiple sclerosis, aortic aneurysm, or endometritis. For example, the title compound (II) showed IC50 of 26 nM against human stromelysin. A table and an ampule formulation containing II were described. The experimental process involved the reaction of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate(cas: 53838-27-0).Quality Control of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate

The Article related to antiarteriosclerotics, antirheumatic agents, antitumor agents, aortic aneurysm, autoimmune disease, bone resorption, cirrhosis, corneal injury, crohn disease, endometritis, interstitial nephritis, leukocyte, metastasis inhibitors, multiple sclerosis, neovascularization, osteoarthritis, osteoporosis, periodontal disease and other aspects.Quality Control of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics