Tag: M.W=200-250

Strahlhofer-Augsten, Manuela published the artcileThe Distinct Role of the HDL Receptor SR-BI in Cholesterol Homeostasis of Human Placental Arterial and Venous Endothelial Cells, Product Details of C12H23N3S, the publication is International Journal of Molecular Sciences (2022), 23(10), 5364, database is CAplus and MEDLINE.

As opposed to adults, high-d. lipoprotein (HDL) is the main cholesterol carrying lipoprotein in fetal circulation. The major HDL receptor, scavenger receptor class B type I (SR-BI), contributes to local cholesterol homeostasis. Arterial endothelial cells (ECA) from human placenta are enriched with cholesterol compared to venous endothelial cells (ECV). Moreover, umbilical venous and arterial plasma cholesterol levels differ markedly. We tested the hypothesis that the uptake of HDL-cholesteryl esters differs between ECA and ECV because of the differential expression of SR-BI. We aimed to identify the key regulators underlying these differences and the functional consequences. Immunohistochem. was used for visualization of SR-BI in situ. ECA and ECV were isolated from the chorionic plate of human placenta and used for RT-qPCR, Western Blot, and HDL uptake assays with 3H- and 125I-labeled HDL. DNA was extracted for the methylation profiling of the SR-BI promoter. SR-BI regulation was studied by exposing ECA and ECV to differential oxygen concentrations or shear stress. Our results show elevated SR-BI expression and protein abundance in ECA compared to ECV in situ and in vitro. Immunohistochem. demonstrated that SR-BI is mainly expressed on the apical side of placental endothelial cells in situ, allowing interaction with mature HDL circulating in the fetal blood. This was functionally linked to a higher increase of selective cholesterol ester uptake from fetal HDL in ECA than in ECV, and resulted in increased cholesterol availability in ECA. SR-BI expression on ECV tended to decrease with shear stress, which, together with heterogeneous immunostaining, suggests that SR-BI expression is locally regulated in the placental vasculature. In addition, hypomethylation of several CpG sites within the SR-BI promoter region might contribute to differential expression of SR-BI between chorionic arteries and veins. Therefore, SR-BI contributes to a local cholesterol homeostasis in ECA and ECV of the human feto-placental vasculature.

International Journal of Molecular Sciences published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C6HBrF4O, Product Details of C12H23N3S.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Schaefer, Olga published the artcileInvestigation of α-amino acid N-carboxyanhydrides by X-ray diffraction for controlled ring-opening polymerization, SDS of cas: 2418-95-3, the publication is Tetrahedron Letters (2019), 60(3), 272-275, database is CAplus.

The need for a scalable synthesis of not sequence defined polypeptides as biomaterials is met by the ring-opening polymerization of α-amino acid N-carboxyanhydrides (NCAs). Even though this polymerization technique appears straight forward, it holds pitfalls in terms of reproducibility and overall control over the polymerization conditions, which depends, beside choice of solvent or initiator, significantly on reagent purity. In addition, the synthesis of monomers can lead to the formation of racemic amino acids. Thus, in this work, we describe the benefits of highly pure monomers in order to control nucleophilic ring-opening polymerization NCAs. Hereby, monomer purity is investigated by relating m.ps. of NCAs with single-crystal and powder X-ray diffraction crystallog. data, which further proves retained stereo-information of NCAs.

Tetrahedron Letters published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C11H22N2O4, SDS of cas: 2418-95-3.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Volpi, Stefano published the artcileSubmonomeric strategy with minimal protection for the synthesis of C(2)-modified peptide nucleic acids, Name: H-Lys(Boc)-OH, the publication is Organic Letters (2021), 23(3), 902-907, database is CAplus and MEDLINE.

A novel synthesis of C(2)-modified peptide nucleic acids (PNAs) is proposed, using a submonomeric strategy with minimally protected building blocks, which allowed a reduction in the required synthetic steps. N(3)-unprotected, D-Lys- and D-Arg-based backbones were used to obtain pos. charged PNAs with high optical purity, as inferred from chiral GC measurements. “Chiral-box” PNAs targeting the G12D point mutation of the KRAS gene were produced using this method, showing improved sequence selectivity for the mutated- vs wild-type DNA strand with respect to unmodified PNAs.

Organic Letters published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C5H5F3O2, Name: H-Lys(Boc)-OH.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Bakunov, Stanislav A. published the artcileModification of the Tiemann rearrangement: One-pot synthesis of N,N-disubstituted cyanamides from amidoximes, SDS of cas: 2451-91-4, the publication is Synthesis (2000), 1148-1159, database is CAplus.

Amidoximes were converted to N,N-disubstituted cyanamides in 70-92% yield in a one-pot synthetic procedure by treating the amidoximes with tosyl chloride, followed by treatment with alkyl halide under phase-transfer conditions.

Synthesis published new progress about 2451-91-4. 2451-91-4 belongs to amides-buliding-blocks, auxiliary class Nitrile,Amine,Benzene, name is N,N-Dibenzylcyanamide, and the molecular formula is C15H14N2, SDS of cas: 2451-91-4.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Yashaswini, Puttaraju Srikantamurthy published the artcileIn vivo modulation of LPS induced leukotrienes generation and oxidative stress by sesame lignans, Name: [(2-Hexylcyclopentylidene)amino]thiourea, the publication is Journal of Nutritional Biochemistry (2017), 151-157, database is CAplus and MEDLINE.

The role of inflammation and oxidative stress is critical during onset of metabolic disorders and this has been sufficiently established in literature. In the present study, we evaluated the effects of sesamol and sesamin, two important bioactive mols. present in sesame oil, on the generation of inflammatory and oxidative stress factors in LPS injected rats. Sesamol and sesamin lowered LPS induced expression of cPLA₂ (61 and 56%), 5-LOX (44 and 51%), BLT-1(32 and 35%) and LTC₄ synthase (49 and 50%), resp., in liver homogenate. The diminished serum LTB₄ (53 and 64%) and LTC₄ (67 and 44%) levels in sesamol and sesamin administered groups, resp., were found to be concurrent with the observed decrease in the expression of cPLA₂ and 5-LOX. The serum levels of TNF-α (29 and 19%), MCP-1 (44 and 57%) and IL-1β (43 and 42%) were found to be reduced in sesamol and sesamin group, resp., as given in parentheses, compared to LPS group. Sesamol and sesamin offered protection against LPS induced lipid peroxidation in both serum and liver. Sesamol, but not sesamin, significantly restored the loss of catalase and glutathione reductase activity due to LPS (P<.05). However, both sesamol and sesamin reverted SOD activities by 92 and 98%, resp. Thus, oral supplementation of sesamol and sesamin beneficially modulated the inflammatory and oxidative stress markers, as observed in the present study, in LPS injected rats. Our report further advocates the potential use of sesamol and sesamin as an adjunct therapy wherein, inflammatory and oxidative stress is of major concern.

Journal of Nutritional Biochemistry published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C14H28O5S, Name: [(2-Hexylcyclopentylidene)amino]thiourea.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Oae, Shigeru published the artcileNucleophilic substitution and elimination reactions on the nitrogen atom. Reaction of N,N-dibenzyl-O-p-nitrobenzoylhydroxylamine with various nucleophiles in dipolar aprotic solvents, Computed Properties of 2451-91-4, the publication is Chemistry Letters (1974), 621-4, database is CAplus.

The reactions of p-O2NC6H4CO2N(CH2Ph)2 (I) with NaN3, LiCl, NaBr, NaI, or NaOH in DMF or Me2SO gave Ph-CHO, PhCH2NH2, and p-O2NC6H4CO2- via an E2 mechanism. This was substantiated by kinetic isotope effects of 7.6 and 8.1for the reactions with N3- and Cl-, resp. The reaction of I with NaCN in Me2SO gave 8% PhCHO, 8% PhCH2NH2, 46% (PhCH2)2NCN, and ∼100% p-O2NC6H4CO2- in an SN2 reaction at the N atom.

Chemistry Letters published new progress about 2451-91-4. 2451-91-4 belongs to amides-buliding-blocks, auxiliary class Nitrile,Amine,Benzene, name is N,N-Dibenzylcyanamide, and the molecular formula is C15H14N2, Computed Properties of 2451-91-4.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Arbizzani, Federica published the artcileIncreasing ergosterol levels delays formin-dependent assembly of F-actin cables and disrupts division plane positioning in fission yeast, Safety of [(2-Hexylcyclopentylidene)amino]thiourea, the publication is Journal of Cell Science (2019), 132(13), jcs227447, database is CAplus and MEDLINE.

In most eukaryotes, cytokinesis is mediated by the constriction of a contractile acto-myosin ring (CR), which promotes the ingression of the cleavage furrow. Many components of the CR interact with plasma membrane lipids suggesting that lipids may regulate CR assembly and function. Although there is clear evidence that phosphoinositides play an important role in cytokinesis, much less is known about the role of sterols in this process. Here, we studied how sterols influence division plane positioning and CR assembly in fission yeast.We show that increasing ergosterol levels in the plasma membrane blocks the assembly of F-actin cables from cytokinetic precursor nodes, preventing their compaction into a ring. Abnormal F-actin cables form after a delay, leading to randomly placed septa. Since the formin Cdc12 was detected on cytokinetic precursors and the phenotype can be partially rescued by inhibiting the Arp2/3 complex, which competes with formins for F-actin nucleation, we propose that ergosterol may inhibit formin dependent assembly of F-actin cables from cytokinetic precursors.

Journal of Cell Science published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C12H23N3S, Safety of [(2-Hexylcyclopentylidene)amino]thiourea.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Kwon, Sun-Young published the artcileMediatory roles of leukotriene B₄ receptors in LPS-induced endotoxic shock, Related Products of amides-buliding-blocks, the publication is Scientific Reports (2019), 9(1), 1-8, database is CAplus and MEDLINE.

Sepsis, a systemic inflammatory response syndrome caused by infection, is the most common disease in patients treated in intensive care units. Endotoxic shock, the most critical form of sepsis, is caused by gram-neg. bacterial infection. However, the detailed mechanism of endotoxic shock remains unclear. In the present study, we observed that the production of leukotriene B₄ (LTB₄) and 12(S)-hydroxyeicosatetraenoic acid (HETE), inflammatory lipid mediators acting on LTB₄ receptors (BLT1 and BLT2), was significantly upregulated in peritoneal lavage fluid (PF) and serum from an LPS-induced endotoxic shock mouse model. Furthermore, BLT1/2-dependent signaling pathways mediated the expression of IL-17, IL-6, and IL-1β, key cytokines for the development of endotoxic shock, via NF-κB activation in the LPS-induced endotoxic shock mouse model. Addnl., inhibition of BLT1/2 significantly attenuated inflammation and tissue damage associated with endotoxic shock and enhanced the survival rate of mice with this inflammatory complication. Together, these results suggest that LTB₄ receptors play critical mediatory roles in the development of endotoxic shock. Our findings point to LTB₄ receptors as potential therapeutic targets for the treatment of endotoxic shock.

Scientific Reports published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C12H23N3S, Related Products of amides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Godard, A. published the artcileMetalation in connection with cross-coupling reactions. Coupling of hindered aryls for the synthesis of 4-phenylpyridines as part of Streptonigrin and Lavendamycin analogs, Synthetic Route of 146140-95-6, the publication is Journal of Organometallic Chemistry (1996), 517(1-2), 25-36, database is CAplus.

The synthesis of the C-D ring system of Streptonigrin and Lavendamycin alkaloid analogs by cross-coupling under Suzuki’s conditions has been studied. Steric hindrance is the main problem. It has been solved either by using strong bases or working in a sealed tube under pressure.

Journal of Organometallic Chemistry published new progress about 146140-95-6. 146140-95-6 belongs to amides-buliding-blocks, auxiliary class Boronic acid and ester,Amine,Benzene,Amide,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (2-Pivalamidophenyl)boronic acid, and the molecular formula is C11H16BNO3, Synthetic Route of 146140-95-6.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Arzel, Erwan published the artcileNew synthesis of benzo-δ-carbolines, cryptolepines, and their salts: in vitro cytotoxic, antiplasmodial, and antitrypanosomal activities of δ-carbolines, benzo-δ-carbolines, and cryptolepines, Quality Control of 146140-95-6, the publication is Journal of Medicinal Chemistry (2001), 44(6), 949-960, database is CAplus and MEDLINE.

Benzo-δ-carbolines I and cryptolepines II (R = H, Me, Et, Pr, Ph) and their salts were prepared using strategies based on the association between halogen-dance and hetero-ring cross-coupling. The syntheses are fully convergent and regioselective with overall yields of 27-70%. Thus, coupling of 3-fluoro-2-iodoquinoline with the phenylboronate 2-(Me₃CCONH)C₆H₄B(OH)₂ gave the phenylquinoline III. Treatment of III with pyridinium chloride at 215° for 30 min and then with aqueous NH₃ gave 83% I (R = H). A halogen-dance mechanism in the quinoline series was proposed. The formal synthesis of potential antimalarial compounds and the first total synthesis of 11-isopropylcryptolepine was described. Cytotoxic activity against mammalian cells and activities against Plasmodium falciparum and Trypanosoma cruzi of benzo-δ-carbolines and δ-carbolines were evaluated in vitro to study the structure-activity relationships. For benzo-δ-carbolines, methylation at N-5 increases the cytotoxic and antiparasitic activities. A further alkylation on C-11 generally increases the cytotoxic activity but not the antiparasitic activity, cryptolepine and 11-methylcryptolepine being the most active on both parasites. Taking advantage of the fluorescence of the indoloquinoline chromophore, cryptolepine was localized by fluorescence microscopy in parasite DNA-containing structures suggesting that these compounds act through interaction with parasite DNA as proposed for cryptolepine on melanoma cells. For δ-carbolines, methylation at N-1 is essential for the antimalarial activity. 1-Methyl-δ-carboline specifically accumulates in the intracellular parasite. It has weak cytotoxic activity and can be considered as a potential antimalarial compound

Journal of Medicinal Chemistry published new progress about 146140-95-6. 146140-95-6 belongs to amides-buliding-blocks, auxiliary class Boronic acid and ester,Amine,Benzene,Amide,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (2-Pivalamidophenyl)boronic acid, and the molecular formula is C11H16BNO3, Quality Control of 146140-95-6.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics