Author: Jessica.F

《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

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

Safety of N-(Pyridin-4-yl)isonicotinamideOn March 5, 2015, O’Donovan, Megan E.; LaDuca, Robert L. published an article in Journal of Molecular Structure. The article was 《Zinc coordination polymers containing substituted isophthalate ligands and fragments from in situ hydrolysis of 4-pyridylisonicotinamide》. The article mentions the following:

Hydrothermal treatment of Zn nitrate, a 5-substituted isophthalic acid, and 4-pyridylisonicotinamide (4-pina) resulted in crystalline coordination polymers that incorporated different fragments formed by in situ hydrolysis of the 4-pina precursor. These materials were characterized by single crystal x-ray diffraction. In the case of {[4-ampyrH]2[Zn(hip)2]·H2O}n (1, 4-ampyrH = 4-aminopyridinium, hip = 5-hydroxyisophthalate), anionic [Zn(hip)2]n2n- (4,4) grid layers co-crystallize with protonated 4-ampyr cations. Using 5-nitroisophthalic acid (H2nip), [Zn7(isonic)4(OH)6(nip)2]n (2, isonic = isonicotinate) was formed. This material manifests [Zn7(OH)6]n cationic inorganic chain motifs linked by isonic and nip ligands into a noninterpenetrated 3-dimensional coordination polymer network with pcu topol. Luminescent behavior is attributed to intra-ligand MO transitions. The results came from multiple reactions, including the reaction of N-(Pyridin-4-yl)isonicotinamide(cas: 64479-78-3Safety of N-(Pyridin-4-yl)isonicotinamide)

N-(Pyridin-4-yl)isonicotinamide(cas: 64479-78-3) belongs to amides.Safety of N-(Pyridin-4-yl)isonicotinamideAmides 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

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

Name: (S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamideOn March 31, 2012, Mallik, Shyam Kumar; Li, Da Yu; Cui, Minghua; Song, Hyun-Ok; Park, Hyun; Kim, Hak Sung published an article in Archives of Pharmacal Research. The article was 《Synthesis and evaluation of peptidyl α,β-unsaturated carbonyl derivatives as anti-malarial calpain inhibitors》. The article mentions the following:

Malarial calpain is a cysteine protease believed to be a central mediator essential for parasitic activities. N-Acetyl-L-leucyl-L-leucyl-L-norleucinal (ALLN), a calpain inhibitor, showed an excellent inhibitory effect on the erythrocytic stages of Plasmodium falciparum. However the aldehyde group of ALLN makes it susceptible to metabolism Therefore, we designed α,β-unsaturated carbonyl peptides that could serve as electrophiles for cysteine residues in calpain. Among the synthetic analogs based on the structure of ALLN, peptidyl esters (I) (R1 = i-Bu, R2 = Boc, Cbz; R1 = Ph, R2 = Cbz; Boc = tert-butoxycarbonyl, Cbz = benzyloxycarbonyl) showed the most potent anti-malarial effects, with the same IC50 values of 5.0 μM. Also they showed the high selective toxicity for the malaria vs. Hela cell with 40.6, 69.2 and 24.3 fold for I (R1 = i-Bu, R2 = Boc, Cbz; R1 = Ph, R2 = Cbz) resp. Dipeptidyl α,β-unsaturated carbonyl derivatives consisting of two amino acids gave better anti-malarial effects than those consisting with one amino acid. The fluctuation in anti-malarial activity with small changes in chem. structure indicates the possibilities of improving synthetic analogs. In the experiment, the researchers used many compounds, for example, (S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide(cas: 87694-50-6Name: (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. Because of the greater electronegativity of oxygen, the carbonyl (C=O) is a stronger dipole than the N–C dipole.Name: (S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide 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

SDS of cas: 87694-50-6On November 15, 2021 ,《Structure-activity relationship study of hydroxyethylamine isostere and P1′ site structure of peptide mimetic BACE1 inhibitors》 appeared in Bioorganic & Medicinal Chemistry. The author of the article were Kobayashi, Kazuya; Otani, Takuya; Ijiri, Saki; Kawasaki, Yuki; Matsubara, Hiroki; Miyagi, Takahiro; Kitajima, Taishi; Iseki, Risa; Ishizawa, Katsuyasu; Shindo, Naoka; Okawa, Kouta; Ueda, Kouta; Ando, Syun; Kawakita, Momoka; Hattori, Yasunao; Akaji, Kenichi. The article conveys some information:

An aromatic substituent has been introduced into a known hydroxyethylamine (HEA)-type BACE1 inhibitor containing the superior substrate sequence to enhance inhibitory activity. The HEA-type isosteres bearing different hydroxyl group and Me group configurations were prepared through a branched synthesis approach using intra- and inter-mol. epoxide opening reactions. The effect of their configuration was evaluated, showing that an R-configuration improved the inhibitory activity, while introduction of a Me group on the isostere decreased the activity. Based on the non-substituted isostere with an R-configuration, 21 derivatives containing various substituents at the P1′ site were synthesized. Our evaluation of the derivatives showed that the structure of the P1′ site had a clear effect on activity, and highly potent inhibitor 40g, which showed sub-micromolar activity against recombinant BACE1 (rBACE1), was identified. The docking simulation of 40g with rBACE1 suggested that a carboxymethyl group at the para-position of the P1′ benzene ring interacted with Lys285 in the S1′ pocket. The results came from multiple reactions, including the reaction of (S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide(cas: 87694-50-6SDS of cas: 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.SDS of cas: 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

Recommanded Product: 87694-50-6On September 12, 2018 ,《Defining the Determinants of Specificity of Plasmodium Proteasome Inhibitors》 was published in Journal of the American Chemical Society. The article was written by Yoo, Euna; Stokes, Barbara H.; de Jong, Hanna; Vanaerschot, Manu; Kumar, T. R. S.; Lawrence, Nina; Njoroge, Mathew; Garcia, Arnold; Van der Westhuyzen, Renier; Momper, Jeremiah D.; Ng, Caroline L.; Fidock, David A.; Bogyo, Matthew. The article contains the following contents:

The Plasmodium proteasome is an emerging antimalarial target due to its essential role in all the major life cycle stages of the parasite and its contribution to the establishment of resistance to artemisinin (ART)-based therapies. However, because of a similarly essential role for the host proteasome, the key property of any antiproteasome therapeutic is selectivity. Several parasite-specific proteasome inhibitors have recently been reported, however, their selectivity must be improved to enable clin. development. Here we describe screening of diverse libraries of non-natural synthetic fluorogenic substrates to identify determinants at multiple positions on the substrate that produce enhanced selectivity. We find that selection of an optimal electrophilic “”warhead”” is essential to enable high selectivity that is driven by the peptide binding elements on the inhibitor. We also find that host cell toxicity is dictated by the extent of coinhibition of the human β2 and β5 subunits. Using this information, we identify compounds with over 3 orders of magnitude selectivity for the parasite enzyme. Optimization of the pharmacol. properties resulted in mols. that retained high potency and selectivity, were soluble, sufficiently metabolically stable and orally bioavailable. These mols. are highly synergistic with ART and can clear parasites in a mouse model of infection, making them promising leads as antimalarial drugs.(S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide(cas: 87694-50-6Recommanded Product: 87694-50-6) was used in this study.

(S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide(cas: 87694-50-6) belongs to amides. 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.Recommanded Product: 87694-50-6

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

Fu, Yiqiu; Xu, Bo; Zou, Xiaomin; Ma, Chao; Yang, Xiaoming; Ke, Mou; Fu, Gang; Yang, Lue; Xu, Ping published an article on February 15 ,2007. The article was titled 《Design and synthesis of a novel class of furan-based molecules as potential 20S proteasome inhibitors》, and you may find the article in Bioorganic & Medicinal Chemistry Letters.Electric Literature of C13H26N2O4 The information in the text is summarized as follows:

A class of furan-based compounds as potential 20S proteasome inhibitors have been designed and synthesized, among which nine compounds are peptide derivatives and six mols. are statine peptidomimetics. The C-terminal furanyl moiety was introduced to target mols. as furan-based amino acids. All the compounds were obtained steadily with moderate to high yield. Compound I was a selective moderate potent proteasome peptidomimetic inhibitor. It inhibited HepG2 and HL-60 proliferation effectively. In the experiment, the researchers used many compounds, for example, (S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide(cas: 87694-50-6Electric Literature of C13H26N2O4)

(S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide(cas: 87694-50-6) belongs to amides.Electric Literature of C13H26N2O4 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

In 2011,Angewandte Chemie, International Edition included an article by Zhang, Min; Imm, Sebastian; Baehn, Sebastian; Neumann, Helfried; Beller, Matthias. Recommanded Product: 2-Hydroxy-N-phenylacetamide. The article was titled 《Synthesis of α-amino acid amides: ruthenium-catalyzed amination of α-hydroxy amides》. The information in the text is summarized as follows:

An efficient ruthenium-catalyzed amination of α-hydroxy acid derivatives is reported. Using a variety of amines, including anilines, primary and secondary aliphatic amines, and ammonia, a wide range of amino acid amides was obtained from α-hydroxy amides or esters. Combination of Ru3(CO)12 and 1,2-bis(dicyclohexylphosphino)ethane was the best catalyst system. In the experiment, the researchers used many compounds, for example, 2-Hydroxy-N-phenylacetamide(cas: 4746-61-6Recommanded Product: 2-Hydroxy-N-phenylacetamide)

2-Hydroxy-N-phenylacetamide(cas: 4746-61-6) 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.Recommanded Product: 2-Hydroxy-N-phenylacetamide 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

Lawson, Edward C.; Santulli, Rosemary J.; Dyatkin, Alexey B.; Ballentine, Scott A.; Abraham, William M.; Rudman, Sandra; Page, Clive P.; de Garavilla, Lawrence; Damiano, Bruce P.; Kinney, William A.; Maryanoff, Bruce E. published an article in Bioorganic & Medicinal Chemistry. The title of the article was 《Selection of a 2-azabicyclo[2.2.2]octane-based α4β1 integrin antagonist as an inhaled anti-asthmatic agent》.Category: amides-buliding-blocks The author mentioned the following in the article:

The α4β1 integrin, expressed on eosinophils and neutrophils, induces inflammation in the lung by facilitating cellular infiltration and activation. From a number of potent α4β1 antagonists that the authors evaluated for safety and efficacy, compound (I) was selected as a lead candidate for antiasthma therapy by the inhalation route. The authors devised an optimized stereoselective synthesis to facilitate the preparation of a sufficiently large quantity of I for assessment in vivo. Administration of I to allergen-sensitive sheep by inhalation blocked the late-phase response of asthma and abolished airway hyper-responsiveness at 24 h following the antigen challenge. Addnl., the recruitment of inflammatory cells into the lungs was inhibited. Administration of I to ovalbumin-sensitized guinea pigs i.p. blocked airway resistance and inhibited the recruitment of inflammatory cells. The experimental part of the paper was very detailed, including the reaction process of 2,6-Dichloroisonicotinamide(cas: 89281-13-0Category: amides-buliding-blocks)

2,6-Dichloroisonicotinamide(cas: 89281-13-0) belongs to anime. Acylation is one of the most important reactions of primary and secondary amines; a hydrogen atom is replaced by an acyl group (a group derived from an acid, such as RCOOH or RSO3H, by removal of ―OH, such as RC(=O)―, RS(O)2―, and so on). Reagents may be acid chlorides (RCOC1, RSO2C1), anhydrides ((RCO)2O), or even esters (RCOOR′); the products are amides of the corresponding acids.Category: amides-buliding-blocks

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