Month: October 2022

In 2019,Applied Microbiology and Biotechnology included an article by Kannappan, Arunachalam; Srinivasan, Ramanathan; Nivetha, Arumugam; Annapoorani, Angusamy; Pandian, Shunmugiah Karutha; Ravi, Arumugam Veera. Recommanded Product: 2-Hydroxy-4-methoxybenzaldehyde. The article was titled 《Anti-virulence potential of 2-hydroxy-4-methoxybenzaldehyde against methicillin-resistant Staphylococcus aureus and its clinical isolates》. The information in the text is summarized as follows:

Burgeoning antibiotic resistance among bacterial pathogens necessitates the alternative treatment options to control the multidrug-resistant bacterial infections. Plant secondary metabolites, a significant source of structurally diverse compounds, posses several biol. activities. The present study was designed to investigate the anti-virulence potential of least explored phytocompound 2-hydroxy-4-methoxybenzaldehyde (HMB) against methicillin-resistant Staphylococcus aureus (MRSA) and its clin. isolates. The min. inhibitory concentration of HMB was found to be 1024 μg/mL. HMB at sub-MIC (200 μg/mL) exhibited a profound staphyloxanthin inhibitory activity against MRSA and its clin. isolates. Besides, growth curve anal. revealed the non-bactericidal activity of HMB at its sub-MIC. Other virulences of MRSA such as lipase, nuclease, and hemolysin were also significantly inhibited upon HMB treatment. The observations made out of blood and H2O2 sensitivity assay suggested that HMB treatment sensitized the test pathogens and aided the functions of host immune responses. Transcriptomic anal. revealed that HMB targets the virulence regulatory genes such as sigB and saeS to attenuate the production of virulence arsenal in MRSA. Further, the result of in vitro cytotoxicity assay using PBMC cells portrayed the non-toxic nature of HMB. To our knowledge, for the first time, the present study reported the virulence inhibitory property of HMB against MRSA along with plausible mol. mechanisms. Addnl. studies incorporating in vivo anal. and omics technologies are required to explore the anti-virulence potential of HMB and its mode of action during MRSA infections. In addition to this study using 2-Hydroxy-4-methoxybenzaldehyde, there are many other studies that have used 2-Hydroxy-4-methoxybenzaldehyde(cas: 673-22-3Recommanded Product: 2-Hydroxy-4-methoxybenzaldehyde) was used in this study.

2-Hydroxy-4-methoxybenzaldehyde(cas: 673-22-3) is employed in the synthesis of Schiff base ligand. It is applied as a reactant in the synthesis of LPA1R antagonists used in the inhibition of LPA-induced proliferation and contraction of normal human lung fibroblasts. Also used in the synthesis of tyrosine kinase 6 proteinase inhibitors.Recommanded Product: 2-Hydroxy-4-methoxybenzaldehyde

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

In 2019,Angewandte Chemie, International Edition included an article by Todorovic, Mihajlo; Schwab, Katerina D.; Zeisler, Jutta; Zhang, Chengcheng; Benard, Francois; Perrin, David M.. Reference of 2-(Benzyloxy)acetaldehyde. The article was titled 《Fluorescent isoindole crosslink (FlICk) chemistry: A rapid, user-friendly stapling reaction》. The information in the text is summarized as follows:

The stabilization of peptide secondary structure via stapling is a ubiquitous goal for creating new probes, imaging agents, and drugs. Inspired by indole-derived crosslinks found in natural peptide toxins, we employed ortho-phthalaldehydes to create isoindole staples, thus transforming inactive linear and monocyclic precursors into bioactive monocyclic and bicyclic products. Mild, metal-free conditions give an array of macrocyclic α-MSH (α-MSH) derivatives, of which several isoindole-stapled α-MSH analogs (Ki ≈ 1 nM) are found to be as potent as α-MSH. Analogously, late-stage intra-annular isoindole stapling furnished a bicyclic peptide mimic of α-amanitin that is cytotoxic to CHO cells (IC50=70 μM). Given its user-friendliness, we have termed this approach FlICk (fluorescent isoindole crosslink) chem. In the experimental materials used by the author, we found 2-(Benzyloxy)acetaldehyde(cas: 60656-87-3Reference of 2-(Benzyloxy)acetaldehyde)

2-(Benzyloxy)acetaldehyde(cas: 60656-87-3) may be used in the following syntheses: (3S,5S)-methyl 6-benzyloxy-3,5-dihydroxyhexanoate ,(S)-5-benzyloxy-4-hydroxypentan-2-one, myxothiazols.Reference of 2-(Benzyloxy)acetaldehyde

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

The author of 《Transition Metal-Free Oxidative Coupling of Primary Amines in Polyethylene Glycol at Room Temperature: Synthesis of Imines, Azobenzenes, Benzothiazoles, and Disulfides》 were Hudwekar, Abhinandan D.; Verma, Praveen K.; Kour, Jaspreet; Balgotra, Shilpi; Sawant, Sanghapal D.. And the article was published in European Journal of Organic Chemistry in 2019. Recommanded Product: 882-33-7 The author mentioned the following in the article:

A transition metal-free protocol has been developed for the oxidative coupling of primary amines to imines and azobenzenes, thiols to disulfides, and 2-aminothiophenols to benzothiazoles, offering excellent yields. The advantageous features of the present environmentally benign methodol. include the usage of biocompatible and green reaction conditions such as, solvent, room temperature reactions and transition metal-free approach. Moreover, it offers a broader substrate scope. In the part of experimental materials, we found many familiar compounds, such as 1,2-Diphenyldisulfane(cas: 882-33-7Recommanded Product: 882-33-7)

1,2-Diphenyldisulfane(cas: 882-33-7) belongs to ethers.Oxygen is more electronegative than carbon, thus the alpha hydrogens of ethers are more acidic than those of simple hydrocarbons. They are far less acidic than alpha hydrogens of carbonyl groups (such as in ketones or aldehydes), however. Recommanded Product: 882-33-7

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

《Novel anti-Alzheimer phenol-lipoyl hybrids: synthesis, physico-chemical characterization, and biological evaluation》 was published in European Journal of Medicinal Chemistry in 2020. These research results belong to Pagoni, Aikaterini; Marinelli, Lisa; Di Stefano, Antonio; Ciulla, Michele; Turkez, Hasan; Mardinoglu, Adil; Vassiliou, Stamatia; Cacciatore, Ivana. Recommanded Product: tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate The article mentions the following:

To date, drugs that hit a single target are inadequate for the treatment of neurodegenerative diseases, such as Alzheimer’s or Parkinson’s diseases. The development of multitarget ligands, able to interact with the different pathways involved in the progression of these disorders, represents a great challenge for medicinal chemists. In this context, we report here the synthesis and biol. evaluation of phenol-lipoyl hybrids (SV1-13), obtained via a linking strategy, to take advantage of the synergistic effect due to the antioxidant portions and anti-amyloid properties of the single constituents present in the hybrid mol. Biol. results showed that SV5 (I) and SV10 (II) possessed the best protective activity against Aβ1-42 induced neurotoxicity in differentiated SH-SY5Y cells. SV9 (III) and II showed remarkable antioxidant properties due to their ability to counteract the damage caused by H2O2 in SHSY-5Y-treated cells. Hovewer, I, showing moderate antioxidant and good neuroprotective activities, resulted the best candidate for further experiments since it also resulted stable both simulated and plasma fluids.tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate(cas: 139115-91-6Recommanded Product: tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate) was used in this study.

tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate(cas: 139115-91-6) belongs to ethers.Although ethers resist hydrolysis, they are cleaved by hydrobromic acid and hydroiodic acid. Hydrogen chloride cleaves ethers only slowly. Recommanded Product: tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

《Efficacy and Safety of a Fixed-Dose Clindamycin Phosphate 1.2%, Benzoyl Peroxide 3.1%, and Adapalene 0.15% Gel for Moderate-to-Severe Acne: A Randomized Phase II Study of the First Triple-Combination Drug.》 was written by Stein Gold, Linda; Baldwin, Hilary; Kircik, Leon H; Weiss, Jonathan S; Pariser, David M; Callender, Valerie; Lain, Edward; Gold, Michael; Beer, Kenneth; Draelos, Zoe; Sadick, Neil; Pillai, Radhakrishnan; Bhatt, Varsha; Tanghetti, Emil A. Recommanded Product: 106685-40-9 And the article was included in American journal of clinical dermatology in 2021. The article conveys some information:

BACKGROUND: A three-pronged approach to acne treatment-combining an antibiotic, antibacterial, and retinoid-could provide greater efficacy and tolerability than single or dyad treatments, while potentially improving patient compliance and reducing antibiotic resistance. OBJECTIVES: We aimed to evaluate the efficacy and safety of triple-combination, fixed-dose topical clindamycin phosphate 1.2%/benzoyl peroxide (BPO) 3.1%/adapalene 0.15% (IDP-126) gel for the treatment of acne. METHODS: In a phase II, double-blind, multicenter, randomized, 12-week study, eligible participants aged ≥ 9 years with moderate-to-severe acne were equally randomized to once-daily IDP-126, vehicle, or one of three component dyad gels: BPO/adapalene; clindamycin phosphate/BPO; or clindamycin phosphate/adapalene. Coprimary endpoints were treatment success at week 12 (participants achieving a ≥ 2-grade reduction from baseline in Evaluator’s Global Severity Score and clear/almost clear skin) and least-squares mean absolute changes from baseline in inflammatory and noninflammatory lesion counts to week 12. Treatment-emergent adverse events and cutaneous safety/tolerability were also assessed. RESULTS: A total of 741 participants were enrolled. At week 12, 52.5% of participants achieved treatment success with IDP-126 vs vehicle (8.1%) and dyads (range 27.8-30.5%; P ≤ 0.001, all). IDP-126 also provided significantly greater absolute reductions in inflammatory (29.9) and noninflammatory (35.5) lesions compared with vehicle or dyads (range inflammatory, 19.6-26.8; noninflammatory, 21.8-30.0; P < 0.05, all), corresponding to > 70% reductions with IDP-126. IDP-126 was well tolerated, with most treatment-emergent adverse events of mild-to-moderate severity. CONCLUSIONS: Once-daily treatment with the novel fixed-dose triple-combination clindamycin phosphate 1.2%/BPO 3.1%/adapalene 0.15% gel demonstrated superior efficacy to vehicle and all three dyad component gels, and was well tolerated over 12 weeks in pediatric, adolescent, and adult participants with moderate-to-severe acne. CLINICAL TRIAL REGISTRATION: ClinicalTrials.gov identifier NCT03170388 (registered 31 May, 2017).6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas: 106685-40-9Recommanded Product: 106685-40-9) was used in this study.

6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas:106685-40-9) may be used as a pharmaceutical reference standard for the quantification of the analyte in topical gel formulations using high-performance liquid chromatography technique.Recommanded Product: 106685-40-9

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Ritchie, Nina F. C.; Zahara, Adam J.; Wilkerson-Hill, Sidney M. published an article in 2022. The article was titled 《Divergent Reactivity of α,α-Disubstituted Alkenyl Hydrazones: Bench Stable Cyclopropylcarbinyl Equivalents》, and you may find the article in Journal of the American Chemical Society.Application In Synthesis of 1-Bromo-3-methoxybenzene The information in the text is summarized as follows:

The divergent reactivity of 2,2-dialkyl-3-(E)-alkenyl N-tosylhydrazones using Pd-catalyzed cross-coupling conditions, which enabled the Z-selective synthesis of 3-aryl-1,4-dienes and gem-dialkyl vinylcyclopropanese. It was found that the dialkylbiaryl phosphine ligand SPhos was the optimal ligand for this transformation producing skipped dienes in up to 83% isolated yield. The ratio of skipped diene to vinylcyclopropane was dependent on both the structure of the α,α-disubstituted hydrazones and the aryl halide component. Using sterically encumbered aryl bromides provided the trans-cyclopropane products selectively in up to 69% yield. The reaction was stereospecific and stereoselective and occurs alongside a competing 1,2-vinyl group migration pathway. The results came from multiple reactions, including the reaction of 1-Bromo-3-methoxybenzene(cas: 2398-37-0Application In Synthesis of 1-Bromo-3-methoxybenzene)

1-Bromo-3-methoxybenzene(cas: 2398-37-0) is a compound useful in organic synthesis and other chemical processes. It is an intermediate used for pharmaceuticals, perfumes and agrochemicals.Application In Synthesis of 1-Bromo-3-methoxybenzene

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Safety of tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamateIn 2015 ,《Covalent Protein Labeling by Enzymatic Phosphocholination》 appeared in Angewandte Chemie, International Edition. The author of the article were Heller, Katharina; Ochtrop, Philipp; Albers, Michael F.; Zauner, Florian B.; Itzen, Aymelt; Hedberg, Christian. The article conveys some information:

We present a new protein labeling method based on the covalent enzymic phosphocholination of a specific octapeptide amino acid sequence in intact proteins. The bacterial enzyme AnkX from Legionella pneumophila has been established to transfer functional phosphocholine moieties from synthetically produced CDP-choline derivatives to N-termini, C-termini, and internal loop regions in proteins of interest. Furthermore, the covalent modification can be hydrolytically removed by the action of the Legionella enzyme Lem3. Only a short peptide sequence (eight amino acids) is required for efficient protein labeling and a small linker group (PEG-phosphocholine) is introduced to attach the conjugated cargo. In addition to this study using tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate, there are many other studies that have used tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate(cas: 139115-91-6Safety of tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate) was used in this study.

tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate(cas: 139115-91-6) belongs to ethers. Ethers lack the hydroxyl groups of alcohols. Safety of tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate Without the strongly polarized O―H bond, ether molecules cannot engage in hydrogen bonding with each other.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

《Control of Crystallinity and Stereocomplexation of Synthetic Carbohydrate Polymers from D- and L-Xylose》 was written by McGuire, Thomas M.; Bowles, Jessica; Deane, Edward; Farrar, Elliot H. E.; Grayson, Matthew N.; Buchard, Antoine. Quality Control of 1,4,7,10,13-PentaoxacyclopentadecaneThis research focused onxylose polymer crystallinity stereocomplexation; carbohydrates; polyether; polysaccharide mimics; ring-opening polymerisation; stereocomplex; xylose. The article conveys some information:

Manipulating the stereochem. of polymers is a powerful method to alter their phys. properties. Despite the chirality of monosaccharides, reports on the impact of stereochem. in natural polysaccharides and synthetic carbohydrate polymers remain absent. Herein, we report the cocrystn. of regio- and stereoregular polyethers derived from D- and L-xylose, leading to enhanced thermal properties compared to the enantiopure polymers. To the best of our knowledge, this is the first example of a stereocomplex between carbohydrate polymers of opposite chirality. In contrast, atactic polymers obtained from a racemic mixture of monomers are amorphous. We also show that the polymer hydroxyl groups are amenable to post-polymerization functionalization. These strategies afford a family of carbohydrate polyethers, the phys. and chem. properties of which can both be controlled, and which opens new possibilities for polysaccharide mimics in biomedical applications or as advanced materials. The experimental part of the paper was very detailed, including the reaction process of 1,4,7,10,13-Pentaoxacyclopentadecane(cas: 33100-27-5Quality Control of 1,4,7,10,13-Pentaoxacyclopentadecane)

1,4,7,10,13-Pentaoxacyclopentadecane(cas: 33100-27-5) is a member of crown ether Ligands. Crown-ethers are macrocyclic polyethers capable of forming host-guest complexes, especially with inorganic and organic cations. Crown-ethers can incorporate protonated primary amine compounds by formation of ion-dipole bonds with the oxygen atoms of the chiral selector. Crown-ethers have been widely used for the separation of several pharmaceuticals both in aqueous and non-aqueous media. Quality Control of 1,4,7,10,13-Pentaoxacyclopentadecane

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

In 2012,Fujishima, Sho-hei; Yasui, Ryosuke; Miki, Takayuki; Ojida, Akio; Hamachi, Itaru published 《Ligand-Directed Acyl Imidazole Chemistry for Labeling of Membrane-Bound Proteins on Live Cells》.Journal of the American Chemical Society published the findings.SDS of cas: 139115-91-6 The information in the text is summarized as follows:

Chem.-based protein labeling in living cells is undoubtedly useful for understanding natural protein functions and for biol./pharmaceutical applications. Here, the authors report a novel approach for endogenous membrane-bound protein labeling for both in vitro and live cell conditions. A moderately reactive alkyloxyacyl imidazole (AI) assisted by ligand-binding affinity (ligand-directed AI (LDAI)) chem. allowed the authors to selectively modify natural proteins, such as dihydrofolate reductase (DHFR) and folate receptor (FR), neither of which could be efficiently labeled using the recently developed ligand-directed tosylate approach. It was clear that LDAI selectively labeled a single Lys(K32) in DHFR, proximal to the ligand-binding pocket. The authors also demonstrate that the fluorescein-labeled (endogenous, by LDAI) FR works as a fluorescent biosensor on the live KB cell surface, which allowed the authors to carry out unprecedented in situ kinetic anal. of ligand binding to FR. The experimental part of the paper was very detailed, including the reaction process of tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate(cas: 139115-91-6SDS of cas: 139115-91-6)

tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate(cas: 139115-91-6) belongs to ethers.The C-O bonds that comprise simple ethers are strong. SDS of cas: 139115-91-6 They are unreactive toward all but the strongest bases. Although generally of low chemical reactivity, they are more reactive than alkanes.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

In 2012,Takahashi, Michiko; Kawamura, Akie; Kato, Nobuo; Nishi, Tsuyoshi; Hamachi, Itaru; Ohkanda, Junko published 《Phosphopeptide-Dependent Labeling of 14-3-3 ζ Proteins by Fusicoccin-Based Fluorescent Probes》.Angewandte Chemie, International Edition published the findings.Reference of tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate The information in the text is summarized as follows:

The authors hypothesized that a chem. modified fusicoccin (FC) bearing a fluorescent tag that is attached by a reactive spacer, and a phosphopeptide that contains a V residue at position i+1 would bind to 14-3-3 and form a ternary complex. The formation of the complex would in turn trigger the spacer to react with nucleophilic residues on the protein surface to covalently attach the tag. Labeling through formation of a ternary complex with the consensus peptide should be kinetically more favorable than labeling with the probe alone, because of the stabilizing effect imparted by van der Waals interactions. The authors developed such fluorescent probes that are capable of labeling 14-3-3ζ, in a site-specific, 14-3-3-selective, and most importantly, highly ligand-dependent manner. The FC anchor precisely recognizes the structural difference of the residue at position i+1 in the phosphopeptide, thus enabling selective 14-3-3 labeling which depends on the shape of the ligand.tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate(cas: 139115-91-6Reference of tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate) was used in this study.

tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate(cas: 139115-91-6) belongs to ethers.Oxygen is more electronegative than carbon, thus the alpha hydrogens of ethers are more acidic than those of simple hydrocarbons. They are far less acidic than alpha hydrogens of carbonyl groups (such as in ketones or aldehydes), however. Reference of tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem