Tag: 200-300

《Phidianidine A and Synthetic Analogues as Naturally Inspired Marine Antifoulants》 was written by Labriere, Christophe; Elumalai, Vijayaragavan; Staffansson, Jannie; Cervin, Gunnar; Le Norcy, Tiffany; Denardou, Hugo; Rehel, Karine; Moodie, Lindon W. K.; Hellio, Claire; Pavia, Henrik; Hansen, Joern H.; Svenson, Johan. Formula: C10H22N2O2 And the article was included in Journal of Natural Products in 2020. The article conveys some information:

Stationary and slow-moving marine organisms regularly employ a natural product chem. defense to prevent being colonized by marine micro- and macroorganisms. While these natural antifoulants can be structurally diverse, they often display highly conserved chemistries and physicochem. properties, suggesting a natural marine antifouling pharmacophore. In our current report, we investigate the marine natural product phidianidine A, which displays several chem. properties found in highly potent marine antifoulants. Phidianidine A and synthetic analogs were screened against the settlement and metamorphosis of Amphibalanus improvisus cyprids, and several of the compounds displayed inhibitory activities at low micromolar concentrations with IC50 values down to 0.7μg/mL observed The settlement study highlights that phidianidine A is a potent natural antifoulant and that the scaffold can be tuned to generate simpler and improved synthetic analogs. The bioactivity is closely linked to the size of the compound and to its basicity. The study also illustrates that active analogs can be prepared in the absence of the natural constrained 1,2,4-oxadiazole ring. A synthetic lead analog of phidianidine A was incorporated in a coating and included in antifouling field trials, where it was shown that the coating induced potent inhibition of marine bacteria and microalgae settlement. The experimental part of the paper was very detailed, including the reaction process of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Formula: 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).Formula: C10H22N2O2

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

《Formaldehyde-activated WEHI-150 induces DNA interstrand crosslinks with unique structural features》 was written by Pumuye, Paul P.; Evison, Benny J.; Konda, Shyam K.; Collins, J. Grant; Kelso, Celine; Medan, Jelena; Sleebs, Brad E.; Watson, Keith; Phillips, Don R.; Cutts, Suzanne M.. Computed Properties of C10H22N2O2 And the article was included in Bioorganic & Medicinal Chemistry in 2020. The article conveys some information:

Mitoxantrone is an anticancer anthracenedione that can be activated by formaldehyde to generate covalent drug-DNA adducts. Despite their covalent nature, these DNA lesions are relatively labile. It was recently established that analogs of mitoxantrone featuring extended side-chains terminating in primary amino groups typically yielded high levels of stable DNA adducts following their activation by formaldehyde. In this study we describe the DNA sequence-specific binding properties of the mitoxantrone analog WEHI-150 which is the first anthracenedione to form apparent DNA crosslinks mediated by formaldehyde. The utility of this compound lies in the versatility of the covalent binding modes displayed. Unlike other anthracenediones described to date, WEHI-150 can mediate covalent adducts that are independent of interactions with the N-2 of guanine and is capable of adduct formation at novel DNA sequences. Moreover, these covalent adducts incorporate more than one formaldehyde-mediated bond with DNA, thus facilitating the formation of highly lethal DNA crosslinks. The versatility of binding observed is anticipated to allow the next generation of anthracenediones to interact with a broader spectrum of nucleic acid species than previously demonstrated by the parent compounds, thus allowing for more diverse biol. activities.tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Computed Properties of C10H22N2O2) was used in this study.

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

《Fluorescent H2 Receptor Squaramide-Type Antagonists: Synthesis, Characterization, and Applications》 was written by Biselli, Sabrina; Alencastre, Ines; Tropmann, Katharina; Erdmann, Daniela; Chen, Mengya; Littmann, Timo; Maia, Andre F.; Gomez-Lazaro, Maria; Tanaka, Miho; Ozawa, Takeaki; Keller, Max; Lamghari, Meriem; Buschauer, Armin; Bernhardt, Guenther. Safety of N-Boc-1,6-Diaminohexane And the article was included in ACS Medicinal Chemistry Letters in 2020. The article conveys some information:

Fluorescence labeled ligands have been gaining importance as mol. tools, enabling receptor-ligand-binding studies by various fluorescence-based techniques. Aiming at red-emitting fluorescent ligands for the hH2R, a series of squaramides labeled with pyridinium or cyanine fluorophores (19-27) was synthesized and characterized. The highest hH2R affinities in radioligand competition binding assays were obtained in the case of pyridinium labeled antagonists 19-21 (pKi: 7.71-7.76) and cyanine labeled antagonists 23 and 25 (pKi: 7.67, 7.11). These fluorescent ligands proved to be useful tools for binding studies (saturation and competition binding as well as kinetic experiments), using confocal microscopy, flow cytometry, and high content imaging. Saturation binding experiments revealed pKd values comparable to the pKi values. The fluorescent probes 21, 23, and 25 could be used to localize H2 receptors in HEK cells and to determine the binding affinities of unlabeled compounds In the experiment, the researchers used N-Boc-1,6-Diaminohexane(cas: 51857-17-1Safety 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.Safety of N-Boc-1,6-Diaminohexane

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

Application In Synthesis of N-Boc-1,6-DiaminohexaneIn 2021 ,《Label-free detection of target proteins using peptide molecular wires as conductive supports》 was published in Sensors and Actuators, B: Chemical. The article was written by Puiu, Mihaela; Zamfir, Lucian-Gabriel; Danila, George Madalin; Papi, Francesco; Nativi, Cristina; Mirceski, Valentin; Bala, Camelia. The article contains the following contents:

We report on the electrochem. of a peptide mol. wire as a conductive support for ligand immobilization in biosensing assays. The helical 9-mer peptide, tagged at Nterminus with Methylene Blue (MB) and thiol-functionalized at Cterminus was anchored on a gold surface via gold/thiol chem. The helical peptide acts as mol. wire, mediating the two-step electron transfer (ET) from MB to the gold surface. The forward and backward square wave voltametric (SWV) components recorded in the presence of peptide wire were used to estimate the kinetic parameters of the electrode reaction. The simulated data matched the exptl. ones for the two-step sequential surface mechanism (EE), with the rate constant of the first step ksur,1 = 20 s-1 and the cathodic ET coefficient α1 = 0.55. The kinetic parameters of the second step were ksur,2 > 1000 s-1, and α2 = 0.5. Small ligands for high-mol. weight targets can be grafted on the peptide wire between the MB tag and the surface through covalent bonding. The binding of the target to the peptide-anchored ligand hampers the ET transfer from MB to the electrode surface, causing a decrease of the peak current. These findings were used further to develop an electrochem. peptide-based biosensor with signaling-off interrogation. The biosensor was tested against two relevant targets for medical diagnosis: the anti-tumor-associated carbohydrate antigen (α-Tn) antibody and the growth hormone secretagogue receptor (GHS-R1a), after ligand grafting. Both targets were detected in the nanomolar range with an overall assay time of 10 min. In the experiment, the researchers used many compounds, for example, N-Boc-1,6-Diaminohexane(cas: 51857-17-1Application In Synthesis of N-Boc-1,6-Diaminohexane)

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.Application In Synthesis of N-Boc-1,6-Diaminohexane

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

Recommanded Product: tert-Butyl (5-aminopentyl)carbamateIn 2016 ,《Structure-Activity Relationships and Kinetic Studies of Peptidic Antagonists of CBX Chromodomains》 was published in Journal of Medicinal Chemistry. The article was written by Stuckey, Jacob I.; Simpson, Catherine; Norris-Drouin, Jacqueline L.; Cholensky, Stephanie H.; Lee, Junghyun; Pasca, Ryan; Cheng, Nancy; Dickson, Bradley M.; Pearce, Kenneth H.; Frye, Stephen V.; James, Lindsey I.. The article contains the following contents:

To better understand the contribution of methyl-lysine (Kme) binding proteins to various disease states, the authors recently developed and reported the discovery of I (UNC3866), a chem. probe that targets two families of Kme binding proteins, CBX and CDY chromodomains, with selectivity for CBX4 and -7. The discovery of I was enabled in part by the use of mol. dynamics simulations performed with CBX7 and its endogenous substrate. Herein, the authors describe the design, synthesis and structure-activity relationship studies that led to the development of I and provide support for the model of CBX7-ligand recognition by examining the binding kinetics of the antagonists with CBX7 as determined by surface-plasmon resonance. The results came from multiple reactions, including the reaction of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Recommanded Product: tert-Butyl (5-aminopentyl)carbamate)

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).Recommanded Product: tert-Butyl (5-aminopentyl)carbamate

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

In 2022,Arendse, Lauren B.; Cozier, Gyles E.; Eyermann, Charles J.; Basarab, Gregory S.; Schwager, Sylva L.; Chibale, Kelly; Acharya, K. Ravi; Sturrock, Edward D. published an article in Journal of Medicinal Chemistry. The title of the article was 《Probing the Requirements for Dual Angiotensin-Converting Enzyme C-Domain Selective/Neprilysin Inhibition》.Application of 7524-52-9 The author mentioned the following in the article:

Selective inhibition of the angiotensin-converting enzyme C-domain (cACE) and neprilysin (NEP), leaving the ACE N-domain (nACE) free to degrade bradykinin and other peptides, has the potential to provide the potent antihypertensive and cardioprotective benefits observed for nonselective dual ACE/NEP inhibitors, such as omapatrilat, without the increased risk of adverse effects. We have synthesized three 1-carboxy-3-phenylpropyl dipeptide inhibitors with nanomolar potency based on the previously reported C-domain selective ACE inhibitor lisinopril-tryptophan (LisW) to probe the structural requirements for potent dual cACE/NEP inhibition. Here we report the synthesis, enzyme kinetic data, and high-resolution crystal structures of these inhibitors bound to nACE and cACE, providing valuable insight into the factors driving potency and selectivity. Overall, these results highlight the importance of the interplay between the S1′ and S2′ subsites for ACE domain selectivity, providing guidance for future chem. efforts toward the development of dual cACE/NEP inhibitors. In the part of experimental materials, we found many familiar compounds, such as H-Trp-OMe.HCl(cas: 7524-52-9Application of 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.Application of 7524-52-9

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

Maiocchi, Sophie; Ku, Jacqueline; Hawtrey, Tom; De Silvestro, Irene; Malle, Ernst; Rees, Martin; Thomas, Shane R.; Morris, Jonathan C. published an article in 2021. The article was titled 《Polyamine-Conjugated Nitroxides Are Efficacious Inhibitors of Oxidative Reactions Catalyzed by Endothelial-Localized Myeloperoxidase》, and you may find the article in Chemical Research in Toxicology.Synthetic Route of C10H22N2O2 The information in the text is summarized as follows:

The heme enzyme myeloperoxidase (MPO) is a key mediator of endothelial dysfunction and a therapeutic target in cardiovascular disease. During inflammation, MPO released by circulating leukocytes is internalized by endothelial cells and transcytosed into the subendothelial extracellular matrix of diseased vessels. At this site, MPO mediates endothelial dysfunction by catalytically consuming nitric oxide (NO) and producing reactive oxidants, hypochlorous acid (HOCl) and the nitrogen dioxide radical (•NO2). Accordingly, there is interest in developing MPO inhibitors that effectively target endothelial-localized MPO. Here the authors studied a series of piperidine nitroxides conjugated to polyamine moieties as novel endothelial-targeted MPO inhibitors. ESR anal. of cell lysates showed that polyamine conjugated nitroxides were efficiently internalized into endothelial cells in a heparan sulfate dependent manner. Nitroxides effectively inhibited the consumption of MPO’s substrate hydrogen peroxide (H2O2) and formation of HOCl catalyzed by endothelial-localized MPO, with their efficacy dependent on both nitroxide and conjugated-polyamine structure. Nitroxides also differentially inhibited protein nitration catalyzed by both purified and endothelial-localized MPO, which was dependent on •NO2 scavenging rather than MPO inhibition. Finally, nitroxides uniformly inhibited the catalytic consumption of NO by MPO in human plasma. Nitroxides effectively inhibit local oxidative reactions catalyzed by endothelial-localized MPO. Novel polyamine-conjugated nitroxides, ethylenediamine-TEMPO and putrescine-TEMPO, emerged as efficacious nitroxides uniquely exhibiting high endothelial cell uptake and efficient inhibition of MPO-catalyzed HOCl production, protein nitration, and NO oxidation Polyamine-conjugated nitroxides represent a versatile class of antioxidant drugs capable of targeting endothelial-localized MPO during vascular inflammation. In the experiment, the researchers used tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Synthetic Route 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).Synthetic Route of C10H22N2O2

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

The author of 《Development of an N-Acyl Amino Acid That Selectively Inhibits the Glycine Transporter 2 To Produce Analgesia in a Rat Model of Chronic Pain》 were Mostyn, Shannon N.; Rawling, Tristan; Mohammadi, Sarasa; Shimmon, Susan; Frangos, Zachary J.; Sarker, Subhodeep; Yousuf, Arsalan; Vetter, Irina; Ryan, Renae M.; Christie, Macdonald J.; Vandenberg, Robert J.. And the article was published in Journal of Medicinal Chemistry in 2019. Recommanded Product: 51644-96-3 The author mentioned the following in the article:

Inhibitors that target the glycine transporter 2, GlyT2, show promise as analgesics, but may be limited by their toxicity through complete or irreversible binding. Acyl-glycine inhibitors, however, are selective for GlyT2 and have been shown to provide analgesia in animal models of pain with minimal side effects, but are comparatively weak GlyT2 inhibitors. Here, we modify the simple acyl-glycine by synthesizing lipid analogs with a range of amino acid head groups in both L- and D-configurations, to produce nanomolar affinity, selective GlyT2 inhibitors. The potent inhibitor oleoyl-D-lysine (33) is also resistant to degradation in both human and rat plasma and liver microsomes, and is rapidly absorbed following an i.p. injection to rats and readily crosses the blood-brain barrier. We demonstrate that 33 provides greater analgesia at lower doses, and does not possess the severe side effects of the very slowly reversible GlyT2 inhibitor, ORG25543 (2). The results came from multiple reactions, including the reaction of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Recommanded Product: 51644-96-3)

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).Recommanded Product: 51644-96-3

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

《Electrochemical reduction of fluorinated aromatic carboxylic acids》 was published in Journal of the Chemical Society in 1972. These research results belong to Drakesmith, F. G.. Application of 4522-93-4 The article mentions the following:

Pentafluorobenzoic acid was electrochem. reduced in HClO4 to give 60% pentafluorobenzyl alc., and in aqueous Et4NBF4 to give, e.g., 40% 2,3,5,6-tetrafluorobenzoic acid (I) and 55% 2,3,5,6-tetrafluorobenzyl alc. Similar reduction of 4-chloro-, 4-amino-, and 4-methoxytetrafluorobenzoic acids, I, pentafluorobenzaldehyde, Et pentafluorobenzoate, and pentafluorobenzamide gave products dependent on the potential of the cathode, the acidity, and the type of ions in the base electrolyte. In the experiment, the researchers used many compounds, for example, Ethyl 2,3,4,5,6-pentafluorobenzoate(cas: 4522-93-4Application of 4522-93-4)

Ethyl 2,3,4,5,6-pentafluorobenzoate(cas: 4522-93-4) belongs to esters.Application of 4522-93-4 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

Romagnoli, Romeo; Prencipe, Filippo; Oliva, Paola; Baraldi, Stefania; Baraldi, Pier Giovanni; Schiaffino Ortega, Santiago; Chayah, Mariem; Kimatrai Salvador, Maria; Lopez-Cara, Luisa Carlota; Brancale, Andrea; Ferla, Salvatore; Hamel, Ernest; Ronca, Roberto; Bortolozzi, Roberta; Mariotto, Elena; Mattiuzzo, Elena; Viola, Giampietro published an article on February 14 ,2019. The article was titled 《Design, Synthesis, and Biological Evaluation of 6-Substituted Thieno[3,2-d]pyrimidine Analogues as Dual Epidermal Growth Factor Receptor Kinase and Microtubule Inhibitors》, and you may find the article in Journal of Medicinal Chemistry.HPLC of Formula: 169759-79-9 The information in the text is summarized as follows:

The clin. evidence for the success of tyrosine kinase inhibitors in combination with microtubule-targeting agents prompted us to design and develop single agents that possess both epidermal growth factor receptor (EGFR) kinase and tubulin polymerization inhibitory properties. A series of 6-aryl/heteroaryl-4-(3′,4′,5′-trimethoxyanilino)thieno[3,2-d]pyrimidine derivatives were discovered as novel dual tubulin polymerization and EGFR kinase inhibitors. The 4-(3′,4′,5′-trimethoxyanilino)-6-(p-tolyl)thieno[3,2-d]pyrimidine derivative I was the most potent compound of the series as an antiproliferative agent, with half-maximal inhibitory concentration (IC50) values in the single- or double-digit nanomolar range. Compound I bound to tubulin in the colchicine site and inhibited tubulin assembly with an IC50 value of 0.71 μM, and I inhibited EGFR activity with an IC50 value of 30 nM. Our data suggested that the excellent in vitro and in vivo profile of I may be derived from its dual inhibition of tubulin polymerization and EGFR kinase. The experimental process involved the reaction of Methyl 4-amino-[2,2′-bithiophene]-5-carboxylate(cas: 169759-79-9HPLC of Formula: 169759-79-9)

Methyl 4-amino-[2,2′-bithiophene]-5-carboxylate(cas: 169759-79-9) belongs to anime. Amine, any member of a family of nitrogen-containing organic compounds that is derived, either in principle or in practice, from ammonia (NH3). Naturally occurring amines include the alkaloids, which are present in certain plants; the catecholamine neurotransmitters (i.e., dopamine, epinephrine, and norepinephrine); and a local chemical mediator, histamine, that occurs in most animal tissues.HPLC of Formula: 169759-79-9

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