Tag: M.W=200-250

Van Raad, Damian published the artcileIn Vitro Protein Synthesis in Semipermeable Artificial Cells, Quality Control of 2418-95-3, the publication is ACS Synthetic Biology (2021), 10(5), 1237-1244, database is CAplus and MEDLINE.

A novel cell free protein synthesis (CFPS) system utilizing layer-by-layer (LbL) polymer assembly was developed to reduce the operational cost of conventional CFPS. This yielded an encapsulated cell system, dubbed “eCells”, that successfully performs in vitro CFPS and allows cost-effective incorporation of noncanonical amino acids into proteins. The use of eCells in CFPS circumvents the need for traditional cell lysate preparation and purification of amino acyl-tRNA synthetases (aaRS) while still retaining the small scale of an in vitro reaction. eCells were found to be 55% as productive as standard dialysis CFPS at 13% of the cost. The reaction was shown to be scalable over a large range of reaction volumes, and the crowding environment in eCells confers a stabilizing effect on marginally stable proteins, such as the pyrrolysl tRNA synthetase (PylRS), providing a means for their application in in vitro protein expression. Photocaged-cysteine (PCC) and N_ε-(tert-butoxycarbonyl)-L-lysine (Boc-lysine) were incorporated into Peptidyl-prolyl cis-trans isomerase B (PpiB) using small amounts of ncAA with an adequate yield of protein. Fluorescent activated cell sorting (FACS) was used to demonstrate the partition of the lysate within the eCells in contrast to standard one pot cell lysate-based methods.

ACS Synthetic Biology 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 C10H14O, Quality Control of 2418-95-3.

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

Zhang, Mengyuan published the artcilePlaque-hyaluronidase-responsive high-densitylipoprotein-mimetic nanoparticles for multistage intimal-macrophage-targeted drug delivery and enhanced anti-atherosclerotic therapy, Recommanded Product: [(2-Hexylcyclopentylidene)amino]thiourea, the publication is International Journal of Nanomedicine (2017), 533-558, database is CAplus and MEDLINE.

Increasing evidence has highlighted the pivotal role that intimal macrophage (iMΦ) plays in the pathophysiol. of atherosclerotic plaques, which represents an attractive target for atherosclerosis treatment. In this work, to address the insufficient specificity of conventional reconstituted high-d. lipoprotein (rHDL) for iMΦ and its limited cholesterol efflux ability, we designed a hyaluronan (HA)-anchored core-shell rHDL. This nanoparticle achieved efficient iMΦ-targeted drug delivery via a multistage-targeting approach, and excellent cellular cholesterol removal. It contained a biodegradable poly (lactic-co-glycolic acid) (PLGA) core within a lipid bilayer, and apolipoprotein A-I (apoA-I) absorbing on the lipid bilayer was covalently decorated with HA. The covalent HA coating with superior stability and greater shielding was favorable for not only minimizing the liver uptake but also facilitating the accumulation of nanoparticles at leaky endothelium overexpressing CD44 receptors in atherosclerotic plaques. The ultimate iMΦ homing was achieved via apoA-I after HA coating degraded by hyaluronidase (HAase) (abundant in atherosclerotic plaque). The multistage-targeting mechanism was revealed on the established injured endothelium-macrophage co-culture dynamic system. Upon treatment with HAase in vitro, the nanoparticle HA-(C)-PLGA-rHDL exhibited a greater cholesterol efflux capacity compared with conventional rHDL (2.43-fold). Better targeting efficiency toward iMΦ and attenuated liver accumulation were further proved by results from ex vivo imaging and iMΦ-specific fluorescence localization. Ultimately, HA-(C)-PLGA-rHDL loaded with simvastatin realized the most potent anti-atherogenic efficacies in model animals over other preparations Thus, the HAase-responsive HDL-mimetic nanoparticle was shown in this study to be a promising nanocarrier for anti-atherogenic therapy, in the light of efficient iMΦ-targeted drug delivery and excellent function of mediating cellular cholesterol efflux.

International Journal of Nanomedicine 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 C8H8O3, Recommanded Product: [(2-Hexylcyclopentylidene)amino]thiourea.

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

Filgueiras, Luciano Ribeiro published the artcileLeukotriene B4 as a potential therapeutic target for the treatment of metabolic disorders, Name: [(2-Hexylcyclopentylidene)amino]thiourea, the publication is Frontiers in Immunology (2015), 515/1-515/4, database is CAplus and MEDLINE.

A review discusses the role of leukotriene B4 role in metabolic dysfunctions. By increasing MyD88 expression, LTB₄ enhances macrophage response to TLR/IL1 receptor agonists potentiating the sterile inflammation, a central event in metabolic disease progression. Furthermore, LTB₄ can amplify tissue injury by increasing reactive oxygen and nitrogen species that are known to mediate β-cell destruction, impairing insulin production Although further studies are required, inhibition of the LTB4/BLT1 axis is a promising therapeutic strategy for the treatment of metabolic disorders. It also discusses about the development of 5-LO inhibitor that is already approved to treat asthma, and BLT1 antagonists and reduction in LTB₄ production or activity may reduce sterile inflammation and decrease disease severity.

Frontiers in 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, Name: [(2-Hexylcyclopentylidene)amino]thiourea.

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

Garbrecht, William L. published the artcileThe synthesis of certain 5-aminotetrazole derivatives. I. The action of hydrazoic acid on some dialkylcyanamides, Name: N,N-Dibenzylcyanamide, the publication is Journal of Organic Chemistry (1953), 1003-13, database is CAplus.

A number of 5-dialkylaminotetrazoles, HN.N:N.N:C-NR₂ (I), are prepared to be tested for their pharmacol. activity by the interaction of R₂NCN and HN₃ in polar and non-polar solvents. R₂NCN are prepared by 2 methods: (A) 12 cc. Br in 40 cc. Skellysolve B is added dropwise to 32 g. Am₂NH and 59 g. KCN in 60 cc. H₂O with vigorous stirring at 0°, giving 88% Am₂NCN, b₁₂ 154-8°, n²⁰_D 1.4422; (B) 53 g. BrCN in ether is added (2 h.) to 71 g. pyrrolidine in ether with cooling and stirring, giving 58% 1-cyanopyrrolidine, b₁₇ 107-10°, n²³_D 1.4670. Other R₂NCN prepared are: R = Bu, b₃₅ 147-51°, n²⁰_D 1.4382; iso-Bu, b₂₅ 123°, n²⁰_D 1.4346; iso-Am, b₁₄ 134°, n²⁰_D 1.4405; PhCH₂, b₁₀ 145-8°, m. 54°; Me, PhCH₂, b₁₂ 139-42°, n²⁰_D 1.5297; Et, PhCH₂, b₁₂ 160°, n²⁰_D 1.5223; 1-cyanopiperidine, b₁₁ 102°, n²⁵_D 1.4678; 4-cyanomorpholine, b₁₅ 117-19°, n²⁵_D 1.4708. Adding (1.5 h.) 250 cc. concentrated H₂SO₄ to 520 g. NaN₃ in 500 cc. H₂O and 1.5 l. C₆H₆ with stirring and cooling, and drying the C₆H₆ layer with Na₂SO₄ give a stock solution containing 15-17 g. HN₃/100 cc. Adding HN₃ from 33 g. NaN₃ in 100 cc. H₂O to 39 g. Bu₂NCN in 200 cc. 95% EtOH gives 85% I (R = Bu), fine needles, m. 132.5-3.5°. Refluxing 80 g. Me(PhCH₂)NCN in 200 cc. xylene containing 32 g. HN₃ 5 h., adding another 100 cc. HN₃ solution, and refluxing another 18 h. give 89% I (R = Me and PhCH₂), fine needles, m. 135.5-6.5° [HCl salt, needles, decompose 179° (sealed tube)]. Refluxing 10 g. (iso-Am)₂NCN with 35 cc. xylene containing 4.5 g. HN₃ 22 h. and, after addition of another 35 cc., another 67 h. gives 9.8 g. I (R = iso-Am), needles, m. 100-1°. Refluxing 6.3 g. Pr₂NCN and 4.2 g. NH₃ in 100 cc. EtOH and 50 cc. H₂O 65 h. gives 39% I (R = iso-Pr), existing in 2 forms, m. 162.5-3.5° and 184° (decomposition). The following addnl. I are prepared [R, solvent used, time (hrs.), % yield, and m.p. in the order given]: Me (II), aqueous EtOH, 5.5, 78, 235-6°; Et, aqueous EtOH, 6, 43, 124-5°; allyl, aqueous EtOH, 17.5, 36 (EtOAc, 20, 58), 96-7°; Bu, aqueous EtOH, 15, 85, 132.5-3.5° (HCl salt, plates, decompose 183°); iso-Bu, aqueous EtOH, 14, 91, 190-1°; Am, aqueous EtOH, 24, 87, 91.5-2.5°; PhCH₂, aqueous EtOH, 46, 91, 158-9°; Et and PhCH₂, xylene, 57, 88, 134.5-5°; piperidino, aqueous EtOH, 43, 79 (C₆H₆, 25, 85), 199-9.5°; morpholino, C₆H₆, 23, 78, 180.5-1°; 1-pyrrolidinyl, aqueous EtOH, 26, 54 (C₆H₆, 23, 86), 231° (decomposition). The Ag salts are prepared by treating I in EtOH with aqueous AgNO₃ solution The apparent dissociation constants and equivalent weights of I in 50% MeOH were determined and the UV absorption curves of I (R = H), II, and some related compounds are described.

Journal of Organic Chemistry 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, Name: N,N-Dibenzylcyanamide.

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

Nagatake, Takahiro published the artcileBLT1 mediates commensal bacteria-dependent innate immune signals to enhance antigen-specific intestinal IgA responses, Synthetic Route of 321673-30-7, the publication is Mucosal Immunology (2019), 12(5), 1082-1091, database is CAplus and MEDLINE.

Leukotriene B₄ receptor 1 (BLT1) triggers the migration of granulocytes and activated T cells; however, its role in B-cell function remains unclear. Here we report that BLT1 is required to induce the production of antigen-specific IgA against oral vaccine through mediating innate immune signals from commensal bacteria. B cells acquire BLT1 expression during their differentiation to IgA⁺ B cells and plasma cells in Peyer’s patches and the small intestinal lamina propria, resp. BLT1 KO mice exhibited impaired production of antigen-specific fecal IgA to oral vaccine despite normal IgG responses to systemically immunized antigen. Expression of MyD88 was decreased in BLT1 KO gut B cells and consequently led to diminished proliferation of commensal bacteria-dependent plasma cells. These results indicate that BLT1 enhances the proliferation of commensal bacteria-dependent IgA⁺ plasma cells through the induction of MyD88 and thereby plays a key role in the production of antigen-specific intestinal IgA.

Mucosal 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, Synthetic Route of 321673-30-7.

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

Darguzyte, Milita published the artcileInfluence of Riboflavin Targeting on Tumor Accumulation and Internalization of Peptostar Based Drug Delivery Systems, Product Details of C11H22N2O4, the publication is Bioconjugate Chemistry (2020), 31(12), 2691-2696, database is CAplus and MEDLINE.

Riboflavin carrier protein (RCP) and riboflavin transporters (RFVTs) have been reported to be highly overexpressed in various cancer cells. Hence, targeting RCP and RFVTs using riboflavin may enhance tumor accumulation and internalization of drug delivery systems. To test this hypothesis, butyl-based 3-arm peptostar polymers were synthesized consisting of a lysine core (10 units per arm) and a sarcosine shell (100 units per arm). The end groups of the arms and the core were successfully modified with riboflavin and the Cy5.5 fluorescent dye, resp. While in phosphate buffered saline the functionalized peptostars showed a bimodal behavior and formed supramol. structures over time, they were stable in the serum maintaining their hydrodynamic diameter of 12 nm. Moreover, the polymers were biocompatible and the uptake of riboflavin targeted peptostars in A431 and PC3 cells was higher than in nontargeted controls and could be blocked competitively. In vivo, the polymers showed a moderate passive tumor accumulation, which was not significantly different between targeted and nontargeted peptostars. Nonetheless, at the histol. level, internalization into tumor cells was strongly enhanced for the riboflavin-targeted peptostars. Based on these results, we conclude that passive accumulation is dominating the accumulation of peptostars, while tumor cell internalization is strongly promoted by riboflavin targeting.

Bioconjugate Chemistry 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, Product Details of C11H22N2O4.

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

Sawada, Yu published the artcileResolvin E1 attenuates murine psoriatic dermatitis, Category: amides-buliding-blocks, the publication is Scientific Reports (2018), 8(1), 1-9, database is CAplus and MEDLINE.

The potential of omega-3 poly-unsaturated fatty acids (PUFAs) as a therapeutic target for psoriasis, a chronic inflammatory skin disease of IL-23/IL-17 axis, is a long-disputed question, since various epidemiol. studies have suggested the association between high-intake of omega-3 PUFAs and the reduced frequency and severity of psoriasis. However, their actual significance and the mol. mechanisms remain largely unknown. To address these issues, we focused on resolvin E1 (RvE1), an omega-3 PUFAs-derived metabolite, and examined its effects on psoriatic dermatitis, using an imiquimod-induced mouse psoriasis model. RvE1 potently suppressed the inflammatory cell infiltration and epidermal hyperplasia in the psoriatic skin. RvE1 decreased the mRNA expression of IL-23 in the skin. Consistently, RvE1 inhibited IL-23 production by dendritic cells (DCs) in vitro. Furthermore, RvE1 exerted inhibitory effects on migration of cutaneous DCs and γδ T cells, a major IL-17-producing cell population in mouse, both in vivo and in vitro. These suppressive effects of RvE1 were mediated by its antagonistic function on BLT1, a receptor of leukotriene B4, and were also observed in human DCs, Th17 and Tc17 cells. Our results indicate a novel mechanism of omega-3 PUFA-mediated amelioration of psoriasis, and suggest a potential of RvE1 as a therapeutic target for psoriasis.

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, Category: amides-buliding-blocks.

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

Keil, Dietmar published the artcilePreparation and characterization of N,N-disubstituted 2-amino-selenazoles, Recommanded Product: N,N-Dibenzylcyanamide, the publication is Phosphorus, Sulfur and Silicon and the Related Elements (1999), 169-184, database is CAplus.

As a result of checking suited methods for preparing N,N-disubstituted 2-amino-selenazoles, e.g. I, as a nearly unknown class of highly reactive selenazoles a simple route starting from N,N-disubstituted selenoureas has been elaborated and used for the synthesis of a series of these compounds The necessary selenium-containing starting compounds N,N-disubstituted selenoureas are available from N,N-disubstituted cyanamides and hydrogen selenide.

Phosphorus, Sulfur and Silicon and the Related Elements 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

Keil, Dietmar published the artcileA simple route to N,N-disubstituted selenoureas from N,N-disubstituted cyanamides, Application In Synthesis of 2451-91-4, the publication is Synthesis (2004), 15-16, database is CAplus.

N,N-Disubstituted selenoureas I [R¹ = R² = Me, Et, Bn; R¹R² = O(CH₂CH₂)₂, (CH₂)₅, (CH₂)₄] can be obtained in good yields by addition of an acid to a mixture of freshly prepared sodium selenide and N,N-disubstituted cyanamides II.

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, Application In Synthesis of 2451-91-4.

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

Grimes, Kimberly D. published the artcileCopper(II)-catalyzed conversion of aryl/heteroaryl boronic acids, boronates, and trifluoroborates into the corresponding azides: substrate scope and limitations, Safety of (2-Pivalamidophenyl)boronic acid, the publication is Synthesis (2010), 1441-1448, database is CAplus and MEDLINE.

We report the copper(II)-catalyzed conversion of organoboron compounds into the corresponding azide derivatives A systematic series of phenylboronic acid derivatives is evaluated to examine the importance of steric and electronic effects of the substituents on reaction yield as well as functional group compatibility. Heterocyclic substrates are also shown to participate in this mild reaction while compounds incorporating B-C(sp³) bonds are unreactive under the reaction conditions. The copper(II)-catalyzed boronic acid-azide coupling reaction is further extended to both boronate esters and potassium organotrifluoroborate salts. The method described herein complements existing procedures for the preparation of aryl azides from the resp. amino, triazene, and halide derivatives and we expect that it will greatly facilitate copper- and ruthenium-catalyzed azide-alkyne cycloaddition reactions for the preparation of diversely functionalized 1-aryl- or 1-heteroaryl-1,2,3-triazoles derivatives

Synthesis 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, Safety of (2-Pivalamidophenyl)boronic acid.

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