Tag: 200-300

Related Products of 87694-50-6On March 4, 2020, Schwartz, Brett D.; Zhang, Meng Yao; Attard, Riley H.; Gardiner, Michael G.; Malins, Lara R. published an article in Chemistry – A European Journal. The article was 《Structurally Diverse Acyl Bicyclobutanes: Valuable Strained Electrophiles》. The article mentions the following:

This work reported two efficient pathways for the rapid preparation of over 20 structurally diverse bicyclo[1.1.0]butane (BCB) ketones, such as I [R = cuban-1-yl, BOCHNCH2, 4-MeOC6H4, etc.] encompassing simple alkyl and aryl derivatives, as well as unprecedented amino acid, dipeptide, bioisostere, and bifunctional linchpin reagents currently inaccessible using literature methods. Analogs were readily forged in two steps and in high yields from simple carboxylic acids or through unsym. ketone synthesis beginning with a convenient carbonyl dication equivalent The utility of this novel toolbox of strained electrophiles for selective modification of proteinogenic nucleophiles was highlighted. The results came from multiple reactions, including the reaction of (S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide(cas: 87694-50-6Related Products of 87694-50-6)

(S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide(cas: 87694-50-6) belongs to amides. Because of the greater electronegativity of oxygen, the carbonyl (C=O) is a stronger dipole than the N–C dipole.Related Products of 87694-50-6 The presence of a C=O dipole and, to a lesser extent a N–C dipole, allows amides to act as H-bond acceptors. In primary and secondary amides, the presence of N–H dipoles allows amides to function as H-bond donors as well.

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

In 2017,Lin, Tse-Hsueh; Lin, Cin-Hao; Liu, Ying-Jie; Huang, Chun Yi; Lin, Yen-Cheng; Wang, Sheng-Kai published 《Controlling Ligand Spacing on Surface: Polyproline-Based Fluorous Microarray as a Tool in Spatial Specificity Analysis and Inhibitor Development for Carbohydrate-Protein Interactions》.ACS Applied Materials & Interfaces published the findings.Safety of tert-Butyl N,N’-diisopropylcarbamimidate The information in the text is summarized as follows:

Multivalent carbohydrate-protein interactions are essential for many biol. processes. Convenient characterization for multivalent binding property of proteins will aid the development of mols. to manipulate these processes. The authors exploited the polyproline helix II (PPII) structure as mol. scaffolds to adjust the distances between glycan ligand attachment sites at 9, 18, and 27 Å on a peptide scaffold. Optimized fluorous groups were also introduced to the peptide scaffold for immobilization to the microarray surface through fluorous interaction to control the orientation of the helical scaffolds. Using lectin LecA and antibody 2G12 as model proteins, the binding preference to the 27 Å glycopeptide scaffold, matched the distance of 26 Å between its two galactose binding sites on LecA and 31 Å spacing between oligomannose binding sites on 2G12, resp. The authors further demonstrate this microarray system can aid the development of inhibitors by transforming the selected surface-bound scaffold into multivalent ligands in solution This strategy can be extended to analyze proteins that lacking structural information to speed up the design of potent and selective multivalent ligands.tert-Butyl N,N’-diisopropylcarbamimidate(cas: 71432-55-8Safety of tert-Butyl N,N’-diisopropylcarbamimidate) was used in this study.

tert-Butyl N,N’-diisopropylcarbamimidate(cas: 71432-55-8) belongs to anime. Nitrous acid converts secondary amines (aliphatic or aromatic) to N-nitroso compounds (nitrosamines): R2NH + HNO2 → R2N―NO. Some nitrosamines are potent cancer-inducing substances, and their possible formation is a serious consideration when nitrites, which are salts of nitrous acid, are present in foods or pharmaceutical preparations. Tertiary amines give rise to nitrosamines more slowly; an alkyl group is eliminated as an aldehyde or ketone, along with nitrous oxide, N2O.Safety of tert-Butyl N,N’-diisopropylcarbamimidate

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

In 2014,Huerta, Elisa; van Genabeek, Bas; Stals, Patrick J. M.; Meijer, E. W.; Palmans, Anja R. A. published 《A Modular Approach to Introduce Function into Single-Chain Polymeric Nanoparticles》.Macromolecular Rapid Communications published the findings.Application of 71432-55-8 The information in the text is summarized as follows:

Here, a modular approach is reported to introduce a specific function into single-chain polymeric nanoparticles (SCPNs). Hereto, an amphiphilic polymer with pendant benzene-1,3,5-tricarboxamide (BTA) units is mixed with a “”free”” BTA that contains a functional group, either a fluorescent naphthalimide or a catalytically active l-proline. Taking advantage of hydrophobic interactions and self-recognition properties of the BTA units, the “”free”” BTAs are captured into the interior of the SCPN in water as evidenced by fluorescence studies. To illustrate that function can be readily introduced using a modular approach, l-proline-based BTAs are incorporated to procure a catalytically active SCPN in water. The aldol reaction between p-nitrobenzaldehyde and cyclohexanone shows good conversions at low catalyst loadings and substrate concentrations, and high stereoselectivities are obtained (de = 91% and ee = 98%). The experimental process involved the reaction of tert-Butyl N,N’-diisopropylcarbamimidate(cas: 71432-55-8Application of 71432-55-8)

tert-Butyl N,N’-diisopropylcarbamimidate(cas: 71432-55-8) belongs to anime. Many important products require amines as part of their syntheses. Methylamine is utilized in the production of the analgesic meperidine (trade name Demerol) and the photographic developer Metol (trademark), and dimethylamine is used in the synthesis of the antihistamine diphenhydramine (trade name Benadryl), the solvent dimethylformamide (DMF), and the rocket propellant 1,1-dimethylhydrazine. The synthesis of the insect repellent N,N-diethyl-m-toluamide (DEET) incorporates diethylamine while that of the synthetic fibre Kevlar requires aromatic amines.Application of 71432-55-8

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

Sin, Ny; Kim, Kyung Bo; Elofsson, Mikael; Meng, Lihao; Auth, Hak; Kwok, Benjamin H. B.; Crews, Craig M. published their research in Bioorganic & Medicinal Chemistry Letters on August 2 ,1999. The article was titled 《Total synthesis of the potent proteasome inhibitor epoxomicin: a useful tool for understanding proteasome biology》.Formula: C13H26N2O4 The article contains the following contents:

Epoxomicin (I), a peptide α’,β’-epoxy-ketone isolated from the actinomycete strain NumberQ996-17, possesses potent in vivo anti-tumor and anti-inflammatory activities. The authors report the first syntheses of I, [3H]-I , and a biotinylated I analog as well as the absolute configuration of the epoxide stereo-center. The natural product and derivatives have permitted the first identification of the proteasome as the specific cellular target of I. In the experimental materials used by the author, we found (S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide(cas: 87694-50-6Formula: C13H26N2O4)

(S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide(cas: 87694-50-6) belongs to amides.Formula: C13H26N2O4Amides are pervasive in nature and technology. Proteins and important plastics like Nylons, Aramid, Twaron, and Kevlar are polymers whose units are connected by amide groups (polyamides); these linkages are easily formed, confer structural rigidity, and resist hydrolysis.

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

Okada, Yoshio; Taguchi, Hiroaki; Yokoi, Toshio published their research in Chemical & Pharmaceutical Bulletin on December 31 ,1996. The article was titled 《Amino acids and peptides. XLVII. Facile synthesis of flavacol, deoxymuta-aspergillic acid and optically active deoxyaspergillic acid from dipeptidyl aldehydes》.HPLC of Formula: 87694-50-6 The article contains the following contents:

2(1H)-pyrazinone ring-containing natural products, flavacol, deoxymuta-aspergillic acid and optically active deoxyaspergillic acid, were easily synthesized by a newly developed procedure for preparation of 2(1H)-pyrazinone derivatives from dipeptidyl substrates BocNHCH(R2)CONHCH(R1)CON(Me)OMe (R1 = iso-Bu, iso-Pr, sec-Bu(S), sec-Bu(R); R2 = Bzl, iso-Bu). The absolute configuration of natural deoxyaspergillic acid was synthetically determined as S. After reading the article, we found that the author used (S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide(cas: 87694-50-6HPLC of Formula: 87694-50-6)

(S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide(cas: 87694-50-6) belongs to amides. Because of the greater electronegativity of oxygen, the carbonyl (C=O) is a stronger dipole than the N–C dipole.HPLC of Formula: 87694-50-6 The presence of a C=O dipole and, to a lesser extent a N–C dipole, allows amides to act as H-bond acceptors. In primary and secondary amides, the presence of N–H dipoles allows amides to function as H-bond donors as well.

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

Mokotoff, Michael; Ren, Kaijun; Wong, Lan K.; LeFever, Ann V.; Lee, Ping C. published their research in Journal of Medicinal Chemistry on December 11 ,1992. The article was titled 《Synthesis and biological evaluation of novel potent antagonists of the bombesin/gastrin releasing peptide receptor》.Synthetic Route of C13H26N2O4 The article contains the following contents:

The solid-phase synthesis and antagonist activity of 20 C-terminal analogs of gastrin releasing peptide (GRP) are reported.. The ability of each analog to inhibit bombesin (BN)-stimulated amylase release from rat pancreatic acini was determined, and those showing antagonist activity were further evaluated for their ability to inhibit BN stimulated [3H]-thymidine uptake in serum-starved 3T3 cells. The assays also included two known peptide antagonists, ([Leu14,ψ13,14]BN) (I) and (N-pivaloyl-GRP20-25-(R)-2-methyl-4-nonylamide) (II), as pos. controls. On the basis of these assays we suggest that a des-Met27,Leu26-ψ[CH2NHCOCH3]GRP C-terminal octapeptide imparts antagonist activity. The two most active compounds are peptides [D-Phe19,Leu26-ψ(CH2NHCOCH3)]GRP19-26 (III) and [D-Phe19,Gln20,Leu26-ψ(CH2NHCOCH3)]GRP19-26 (IV). In their ability to inhibition BN stimulated [3H]-thymidine uptake, the IC50 of peptides I, II, III, and IV were 43, 31, 3, and 33 nM, resp. In conclusion, the novel C-terminal ψ[CH2NHCOCH3] bond promises to be a useful peptide backbone modification for imparting antagonism in GRP/BN analogs. The experimental part of the paper was very detailed, including the reaction process of (S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide(cas: 87694-50-6Synthetic Route of C13H26N2O4)

(S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide(cas: 87694-50-6) belongs to amides.Synthetic Route of C13H26N2O4 The solubilities of amides and esters are roughly comparable. Typically amides are less soluble than comparable amines and carboxylic acids since these compounds can both donate and accept hydrogen bonds.

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

Recommanded Product: (S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamideOn June 1, 2014, Zhang, Jiankang; Cao, Jiayi; Xu, Lei; Zhou, Yubo; Liu, Tao; Li, Jia; Hu, Yongzhou published an article in Bioorganic & Medicinal Chemistry. The article was 《Design, synthesis and biological evaluation of novel tripeptidyl epoxyketone derivatives constructed from β-amino acid as proteasome inhibitors》. The article mentions the following:

A series of novel tripeptidyl epoxyketone derivatives constructed from β-amino acid were designed, synthesized and evaluated as proteasome inhibitors. All target compounds were tested for their proteasome inhibitory activities and selected compounds were tested for their anti-proliferation activities against two multiple myeloma (MM) cell lines RPMI 8226 and NCI-H929. Among them, eleven compounds exhibited proteasome inhibitory rates of more than 50% at the concentration of 1 μg/mL and nine compounds showed anti-proliferation activities with IC50 values at low micromolar level. Compound I displayed the most potent proteasome inhibitory activities (IC50 = 0.11 ± 0.01 μM) and anti-proliferation activities with IC50 = 0.23 ± 0.01 and 0.17 ± 0.02 μM against two tested cell lines. Addnl., the poly-ubiquitin accumulation in the western blot anal. supported that proteasome inhibition in a cellular system was induced by compound I. All these exptl. results confirmed that β-amino acid can be introduced as a building block for the development of proteasome inhibitors. The experimental process involved the reaction of (S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide(cas: 87694-50-6Recommanded Product: (S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide)

(S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide(cas: 87694-50-6) belongs to amides.Recommanded Product: (S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide Amides include many other important biological compounds, as well as many drugs like paracetamol, penicillin and LSD. Low-molecular-weight amides, such as dimethylformamide, are common solvents.

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

HPLC of Formula: 87694-50-6On October 1, 2014 ,《Semi-synthesis of biologically active nisin hybrids composed of the native lanthionine ABC-fragment and a cross-stapled synthetic DE-fragment》 was published in Bioorganic & Medicinal Chemistry. The article was written by Slootweg, Jack C.; Peters, Nienke; Quarles van Ufford, H. C.; Breukink, Eefjan; Liskamp, Rob M. J.; Rijkers, Dirk T. S.. The article contains the following contents:

The antimicrobial peptide nisin is a promising template for designing novel peptide-based antibiotics to improve its drug-like properties. First steps in that direction represent the synthesis of hybrid nisin derivatives that contain a native nisin ABC-part and synthesized cross-stapled DE-ring fragments and are described here. The biol. activity of the newly synthesized nisin derivatives was evaluated in order to compare the bioactivity of the synthetic DE-ring containing mimic and native lanthionine-bridged DE-ring containing nisin. The native nisin ABC-ring system was obtained via chymotrypsin digestion of full-length nisin, and was subsequently functionalized at the C-terminal carboxylate with two different amino alkyne moieties. Next, nisin hybrids were successfully prepared using Cu(I)-catalyzed azide alkyne cycloaddition ‘click’ chem. by chemo-selective ligation of the ABC-alkyne with the N-terminal azido functionalized dicarba-DE ring mimic. The newly synthesized compounds were active as potent lipid II binders and retained antimicrobial activity in a growth inhibition assay. However, pore formation was not observed, possibly either due to the different character of the ‘staples’ as compared to the parent sulfides, or due to the triazole moiety as a sub-optimal amide bond isostere. In the experiment, the researchers used many compounds, for example, (S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide(cas: 87694-50-6HPLC of Formula: 87694-50-6)

(S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide(cas: 87694-50-6) belongs to amides.HPLC of Formula: 87694-50-6Amides are pervasive in nature and technology. Proteins and important plastics like Nylons, Aramid, Twaron, and Kevlar are polymers whose units are connected by amide groups (polyamides); these linkages are easily formed, confer structural rigidity, and resist hydrolysis.

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

Product Details of 2418-95-3On September 8, 2021 ,《Nickel-Catalyzed Multicomponent Coupling: Synthesis of α-Chiral Ketones by Reductive Hydrocarbonylation of Alkenes》 was published in Journal of the American Chemical Society. The article was written by Chen, Jian; Zhu, Shaolin. The article contains the following contents:

A nickel-catalyzed, multicomponent regio- and enantioselective coupling via sequential hydroformylation and carbonylation from readily available starting materials has been developed. This modular multicomponent hydrofunctionalization strategy enables the straightforward reductive hydrocarbonylation of a broad range of unactivated alkenes to produce a wide variety of unsym. dialkyl ketones bearing a functionalized α-stereocenter, including enantioenriched chiral α-aryl ketones and α-amino ketones. It uses chiral bisoxazoline as a ligand, silane as a reductant, chloroformate as a safe CO source, and a racemic secondary benzyl chloride or an N-hydroxyphthalimide (NHP) ester of a protected α-amino acid as the alkylation reagent. The benign nature of this process renders this method suitable for late-stage functionalization of complex mols. The experimental process involved the reaction of H-Lys(Boc)-OH(cas: 2418-95-3Product Details of 2418-95-3)

H-Lys(Boc)-OH(cas: 2418-95-3) belongs to amino acids. These amino acids may be present in low concentrations and play a vital part as an intermediate in a biosynthetic pathway, e.g., ornithine, homoserine, or cystathionine. In contrast they may act as a major storage form of nitrogen, e.g., canavanine in the seed of Canavalia ensiformis, or may be formed in high amounts in response to an external stress, e.g., γ-aminobutyrate.Product Details of 2418-95-3 It is possible that some of these nonprotein amino acids may serve as insecticidal or fungicidal agents.

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

《Protein tyrosine kinases regulate agonist-stimulated prostacyclin release but not von Willebrand factor secretion from human umbilical vein endothelial cells》 was written by Wheeler-Jones, Caroline P. D.; May, Michael J.; Morgan, Anthony J.; Pearson, Jeremy D.. HPLC of Formula: 106392-48-7 And the article was included in Biochemical Journal on April 15 ,1996. The article conveys some information:

The rapid synthesis and release of prostacyclin (PGI2) and the exocytotic secretion of von Willebrand Factor (vWF) elicited by activation of G-protein-coupled receptors on endothelium occur via signaling mechanisms which are incompletely defined. Activation of protein tyrosine kinases (PTKs) and modulation of the tyrosine-phosphorylation state of endogenous proteins have been implicated in several cellular processes including arachidonate release and exocytosis. In the present study we have examined the regulatory role of PTKs in agonist-stimulated release of PGI2 and vWF from human umbilical vein endothelial cells (HUVECs) using two chem. and mechanistically dissimilar PTK inhibitors (genistein and ST271). Genistein, but not the less active analog daidzein, dose-dependently attenuated PGI2 release in response to thrombin and histamine (IC50approx. 20 μM), and to the thrombin-receptor-activating peptide. A more potent inhibition of thrombin- and histamine-induced PGI2 synthesis was observed in cells exposed to ST271. In contrast, neither genistein nor ST271 modulated agonist-drive vWF secretion. At concentrations that abolished PGI2 release, genistein blocked thrombin- or histamine-evoked tyrosine phosphorylation of a 42 kDa protein. Ca2+ ionophore-induced PGI2 generation, but not vWF secretion, was also inhibited by both genistein and ST271, suggesting that these agents modulate PGI2 synthesis by acting at, or distal to, agonist-induced changes in intracellular Ca2+ ([Ca2+]i). In fura-2-loaded HUVECs genistein partially reduced the histamine-induced peak [Ca2+]i but had no effect on the thrombin response. Ca2+-induced PGI2 release from elec. permeabilized HUVECs was abolished in the presence of ST271 or genistein, but not daidzein. The generation of PGI2 in response to exogenous arachidonic acid was not modulated by genistein or ST271, suggesting that PTK inhibitors do not directly inhibit cyclo-oxygenase activity. Taken together, these results suggest that PTKs regulate PGI2 synthesis and release in HUVECs by modulating, directly or indirectly, a Ca2+-sensitive step upstream of cyclo-oxygenase.2-Cyano-3-(4-hydroxy-3,5-diisopropylphenyl)acrylamide(cas: 106392-48-7HPLC of Formula: 106392-48-7) was used in this study.

2-Cyano-3-(4-hydroxy-3,5-diisopropylphenyl)acrylamide(cas: 106392-48-7) belongs to amides. Because of the greater electronegativity of oxygen, the carbonyl (C=O) is a stronger dipole than the N–C dipole. The presence of a C=O dipole and, to a lesser extent a N–C dipole, allows amides to act as H-bond acceptors.“,” In primary and secondary amides, the presence of N–H dipoles allows amides to function as H-bond donors as well. HPLC of Formula: 106392-48-7

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