Tag: M.W=200-250

Karatzas, Anastasis published the artcileMacromolecular Architecture and Encapsulation of the Anticancer Drug Everolimus Control the Self-Assembly of Amphiphilic Polypeptide-Containing Hybrids, Application of H-Lys(Boc)-OH, the publication is Biomacromolecules (2019), 20(12), 4546-4562, database is CAplus and MEDLINE.

Macromol. architecture plays an important role in the self-assembly process of block copolymer amphiphiles. Herein, two series of stimuli-responsive amphiphilic 3-miktoarm star hybrid terpolypeptides and their corresponding linear analogs were synthesized exhibiting the same overall composition and mol. weight but different macromol. architecture. The macromol. architecture was found to be a key parameter in defining the morphol. of the nanostructures formed in aqueous solutions as well as to alter the self-assembly behavior of the polymers independently of their composition In addition, it was found that the assemblies prepared from the star-shaped polymers showed superior tolerance against enzymic degradation due to the increased corona block d. on the outer surface of the nanoparticles. Encapsulation of the hydrophobic anticancer drug Everolimus resulted in the formation of intriguing non-spherical and non-sym. pH-responsive nanostructures, such as “stomatocytes” and “multi-compartmentalized suprapolymersomes”, while the pH-triggered release of the drug was also investigated. Owing to the similarities of the developed “stomatocytes” with red blood cells, in combination with their pH-responsiveness and superior stability over enzymic degradation, they are expected to present advanced drug delivery properties and have the ability to bypass several extra- and intracellular barriers to reach and effectively treat cancer cells.

Biomacromolecules 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, Application of H-Lys(Boc)-OH.

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

Ye, Fei published the artcileSolvent-free ruthenium trichloride-mediated [2 + 2 + 2] cycloaddition of α,ω-diynes and cyanamides: a convenient access to 2-aminopyridines, Safety of N,N-Dibenzylcyanamide, the publication is Organic Chemistry Frontiers (2017), 4(6), 1063-1068, database is CAplus.

A convenient access to functionalized 2-aminopyridines via a solventless Ru-catalyzed [2 + 2 + 2] cycloaddition reaction of α,ω-diynes and cyanamides was described. This transformation efficiently proceeded in the presence of a stable, easy to handle, and cost-effective RuCl₃·nH₂O complex, leading to various 2-aminopyridines in good to excellent yields according to an eco-friendly, straightforward approach.

Organic Chemistry Frontiers 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 C16H24BF4Ir, Safety of N,N-Dibenzylcyanamide.

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

Ye, Fei published the artcileRuthenium-Catalyzed [2 + 2 + 2] Cycloaddition Reaction Forming 2-Aminopyridine Derivatives from α,ω-Diynes and Cyanamides, Category: amides-buliding-blocks, the publication is Organic Letters (2017), 19(5), 1104-1107, database is CAplus and MEDLINE.

A novel, efficient, and mild synthetic route for the preparation of 2-aminopyridines , e. g., I, via ruthenium-mediated [2 + 2 + 2] cycloaddition of α,ω-diynes and cyanamides has been developed. This atom-economical catalytic process demonstrated remarkable regioselectivities to access pyridine derivatives of high synthetic utility.

Organic 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 C16H24BF4Ir, Category: amides-buliding-blocks.

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

Csanyi, D. published the artcileSynthesis of two new heteroaromatic β-carboline-fused pentacycles. observation of a new intercalating agent, Product Details of C11H16BNO3, the publication is Bioorganic & Medicinal Chemistry Letters (2000), 10(15), 1767-1769, database is CAplus and MEDLINE.

Five-step synthetic routes of two new polyfused heterocycles: indazolo[3,2-a]-ss-carboline (3) and benzo[4′,5′][1,2,3]triazino[6,1-a]-ss-carbolinium salt (10) applying Pd(0)-catalyzed cross-coupling reaction were elaborated.

Bioorganic & Medicinal Chemistry Letters 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, Product Details of C11H16BNO3.

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

Li, Bin published the artcileSubstance P-regulated leukotriene B4 production promotes acute pancreatitis-associated lung injury through neutrophil reverse migration, Recommanded Product: [(2-Hexylcyclopentylidene)amino]thiourea, the publication is International Immunopharmacology (2018), 147-156, database is CAplus and MEDLINE.

Leukotriene B4 (LTB4) is a potent chemoattractant and inflammatory mediator involved in multiple inflammatory diseases. Substance P (SP) has been reported to promote production of LTB4 in itch-associated response in vivo and in some immune cells in vitro. Here, we investigated the role of LTB4 in acute pancreatitis (AP), AP-associated acute lung injury (ALI) and the related mechanisms of LTB4 production in AP. In vivo, murine AP model was induced by caerulein and lipopolysaccharide or L-arginine. The levels of LTB4 and its specific receptor BLT1 were markedly upregulated in both AP models. Blockade of BLT1 by LY293111 attenuated the severity of AP, decreased neutrophil reverse transendothelial cell migration (rTEM) into the circulation and alleviated the severity of ALI. In vitro, treatment of pancreatic acinar cells with SP increased LTB4 production Furthermore, SP treatment increased phosphorylation of protein kinase C (PKC) α and mitogen activated protein kinases (MAPKs), including extracellular signal-regulated kinase (ERK), p-38 MAPK and c-Jun NH2-terminal kinase (JNK). Finally, blockade of neurokinin-1 receptor by CP96345 significantly attenuated the severity of AP and decreased the level of LTB4 when compared to AP group. In summary, these results show that SP regulates the production of LTB4 via PKC α/MAPK pathway, which further promotes AP-associated ALI through neutrophil rTEM.

International Immunopharmacology 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, Recommanded Product: [(2-Hexylcyclopentylidene)amino]thiourea.

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

Duchamp, Edouard published the artcileCyanide-Free Synthesis of Air Stable N-Substituted Li and K Cyanamide Salts from Tetrazoles. Applications toward the Synthesis of Primary and Secondary Cyanamides as Precursors to Amidines, Recommanded Product: N,N-Dibenzylcyanamide, the publication is Organic Letters (2020), 22(21), 8487-8491, database is CAplus and MEDLINE.

A practical two-step synthesis of N,N’-disubstituted cyanamides such as N-allyl-N-benzylcyanamide consists in the low-temperature metalation of N-substituted 5H-tetrazoles such as 1-allyl-1H-tetrazole that undergo spontaneous cycloreversion at 0°C releasing dinitrogen, and forming N-metalated cyanamides that can be reacted in situ with a variety of electrophiles. Remarkably, N-substituted Li and K cyanamides such as lithium N-benzylcyanamide are air stable white solids at room temperature Addition of lithium organometallics to the N,N’-disubstituted cyanamides provides a new method for accessing N,N’-disubstituted amidines.

Organic 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, Recommanded Product: N,N-Dibenzylcyanamide.

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

Charifson, Paul S. published the artcileNovel Dual-Targeting Benzimidazole Urea Inhibitors of DNA Gyrase and Topoisomerase IV Possessing Potent Antibacterial Activity: Intelligent Design and Evolution through the Judicious Use of Structure-Guided Design and Structure-Activity Relationships, COA of Formula: C11H16BNO3, the publication is Journal of Medicinal Chemistry (2008), 51(17), 5243-5263, database is CAplus and MEDLINE.

The discovery of new antibacterial agents with novel mechanisms of action is necessary to overcome the problem of bacterial resistance that affects all currently used classes of antibiotics. Bacterial DNA gyrase and topoisomerase IV are well-characterized clin. validated targets of the fluoroquinolone antibiotics which exert their antibacterial activity through inhibition of the catalytic subunits. Inhibition of these targets through interaction with their ATP sites has been less clin. successful. The discovery and characterization of a new class of low mol. weight, synthetic inhibitors of gyrase and topoisomerase IV that bind to the ATP sites are presented. The benzimidazole ureas are dual targeting inhibitors of both enzymes and possess potent antibacterial activity against a wide spectrum of relevant pathogens responsible for hospital- and community-acquired infections. The discovery and optimization of this novel class of antibacterials by the use of structure-guided design, modeling, and structure-activity relationships are described. Data are presented for enzyme inhibition, antibacterial activity, and in vivo efficacy by oral and i.v. administration in two rodent infection models.

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, COA of Formula: C11H16BNO3.

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

Zahariev, Sotir published the artcileSolvent-free synthesis of azole carboximidamides, Product Details of C15H14N2, the publication is Tetrahedron Letters (2004), 45(51), 9423-9426, database is CAplus.

A one-pot procedure is described for the preparation of 1H-pyrazole-carboximidamides, 1H-benzotriazole-carboximidamides and guanidinylation of amines with 1H-benzotriazole-carboximidamides. The X-ray crystal structure of N,N-dimethyl-1H-benzotriazole-1-carboximidamide (I), has been determined The reaction of 1H-benzotriazole hydrochloride with N,N-dimethylcyanamide to give I (in situ) was followed by addition of N²-[(phenylmethoxy)carbonyl]-L-ornithine (II) under microwave irradiation conditions. This reaction yielded the corresponding guanidine derivative, i.e., N²-tert-butoxycarbonyl-N^G,N^G-dimethyl-L-arginine (III).

Tetrahedron 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 0, Product Details of C15H14N2.

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

Hao, Qi published the artcileMesenchymal stem cell-derived extracellular vesicles decrease lung injury in mice, Safety of [(2-Hexylcyclopentylidene)amino]thiourea, the publication is Journal of Immunology (2019), 203(7), 1961-1975, database is CAplus and MEDLINE.

Human mesenchymal stem cell (MSC) extracellular vesicles (EV) can reduce the severity of bacterial pneumonia, but little is known about the mechanisms underlying their antimicrobial activity. In the current study, we found that bacterial clearance induced by MSC EV in Escherichia coli pneumonia in C57BL/6 mice was associated with high levels of leukotriene (LT) B₄ in the injured alveolus. More importantly, the antimicrobial effect of MSC EV was abrogated by cotreatment with a LTB₄ BLT1 antagonist. To determine the role of MSC EV on LT metabolism, we measured the effect of MSC EV on a known ATP-binding cassette transporter, multidrug resistance-associated protein 1 (MRP1), and found that MSC EV suppressed MRP1 mRNA, protein, and pump function in LPS-stimulated Raw264.7 cells in vitro. The synthesis of LTB₄ and LTC₄ from LTA₄ are competitive, and MRP1 is the efflux pump for LTC₄. Inhibition of MRP1 will increase LTB₄ production In addition, administration of a nonspecific MRP1 inhibitor (MK-571) reduced LTC₄ and subsequently increased LTB₄ levels in C57BL/6 mice with acute lung injury, increasing overall antimicrobial activity. We previously found that the biol. effects of MSC EV were through the transfer of its content, such as mRNA, microRNA, and proteins, to target cells. In the current study, miR-145 knockdown abolished the effect of MSC EV on the inhibition of MRP1 in vitro and the antimicrobial effect in vivo. In summary, MSC EV suppressed MRP1 activity through transfer of miR-145, thereby resulting in enhanced LTB₄ production and antimicrobial activity through LTB₄/BLT1 signaling.

Journal of Immunology 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

Kabes, Connor Q. published the artcileSyntheses of enantiopure 1,2-ethylenediamines with tethered secondary amines of the formula H₂NCH₂CH[(CH₂)_nNHMe]NH₂ (n = 1 – 4) from α-amino acids: New agents for asymmetric catalysis, Category: amides-buliding-blocks, the publication is Synthesis (2020), 52(21), 3277-3285, database is CAplus.

Tris(hydrochloride) adducts of the title compounds are prepared from the inexpensive α-amino acids H₂N(C:O)CH₂CH(NH₂)CO₂H, HO(C:O)(CH₂)_nCH(NH ₂)CO ₂H (n = 1, 2), and H₂N(CH₂)₄CH(NH₂)CO₂H, resp. (steps/overall yield = 5/32%, 7/30%, 7/33%, 5/38%). The NH₂ group that is remote from the secondary amine is installed via BH₃ reduction of an amide [(C=O)NR₂] derived from an α-amino carboxylic acid. The MeNHCH₂ units are introduced by BH₃ reductions of alkyl carbamate [RO(C:O)NHCH₂; R = Et, t-Bu] or amide [MeHN(C:O)] moieties.

Synthesis 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, Category: amides-buliding-blocks.

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