Tag: M.W=200-250

Timari, Geza published the artcileSynthesis of novel ellipticine analogs and their inhibition of Moloney leukemia reverse transcriptase, Product Details of C11H16BNO3, the publication is Bioorganic & Medicinal Chemistry Letters (1996), 6(23), 2831-2836, database is CAplus.

Two new ellipticine analogs I [R = H, Cl] were synthesized as potential non-nucleoside inhibitors of reverse transcriptase and were tested on Moloney leukemia virus reverse transcriptase in vitro. Both I showed considerable inhibitory effect with ID₅₀ of 2.8 to 4.5 × 10^-5 M.

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 C7H8BBrO3, Product Details of C11H16BNO3.

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

Zoccal, Karina F. published the artcileOpposing roles of LTB₄ and PGE₂ in regulating the inflammasome-dependent scorpion venom-induced mortality, Application In Synthesis of 321673-30-7, the publication is Nature Communications (2016), 10760, database is CAplus and MEDLINE.

Tityus serrulatus sting causes thousands of deaths annually worldwide. T. serrulatus-envenomed victims exhibit local or systemic reaction that culminates in pulmonary edema, potentially leading to death. However, the mol. mechanisms underlying T. serrulatus venom (TsV) activity remain unknown. Here we show that TsV triggers NLRP3 inflammasome activation via K⁺ efflux. Mechanistically, TsV triggers lung-resident cells to release PGE₂, which induces IL-1β production via E prostanoid receptor 2/4-cAMP-PKA-NFκB-dependent mechanisms. IL-1β/IL-1R actions account for edema and neutrophil recruitment to the lungs, leading to TsV-induced mortality. Inflammasome activation triggers LTB₄ production and further PGE₂ via IL-1β/IL-1R signalling. Activation of LTB₄-BLT1/2 pathway decreases cAMP generation, controlling TsV-induced inflammation. Exogenous administration confirms LTB₄ anti-inflammatory activity and abrogates TsV-induced mortality. These results suggest that the balance between LTB₄ and PGE₂ determines the amount of IL-1β inflammasome-dependent release and the outcome of envenomation. We suggest COX1/2 inhibition as an effective therapeutic intervention for scorpion envenomation.

Nature Communications 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 C12H17BO4S, Application In Synthesis of 321673-30-7.

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

Trindade, Bruno Caetano published the artcileLeukotrienes are upregulated and associated with human T-lymphotropic virus type 1 (HTLV-1)-associated neuroinflammatory disease, Formula: C12H23N3S, the publication is PLoS One (2012), 7(12), e51873, database is CAplus and MEDLINE.

Leukotrienes (LTs) are lipid mediators involved in several inflammatory disorders. We investigated the LT pathway in human T-lymphotropic virus type 1 (HTLV-1) infection by evaluating LT levels in HTLV-1-infected patients classified according to the clin. status as asymptomatic carriers (HACs) and HTLV-1-associated myelopathy/tropical spastic paraparesis (HAM/TSP) patients. Bioactive LTB₄ and CysLTs were both increased in the plasma and in the supernatant of peripheral blood mononuclear cell cultures of HTLV-1-infected when compared to non-infected. Interestingly, CysLT concentrations were increased in HAM/TSP patients. Also, the concentration of plasma LTB₄ and LTC₄ pos. correlated with the HTLV-1 proviral load in HTLV-1-infected individuals. The gene expression levels of LT receptors were differentially modulated in CD4⁺ and CD8⁺ T cells of HTLV-1-infected patients. Anal. of the overall plasma signature of immune mediators demonstrated that LT and chemokine amounts were elevated during HTLV-1 infection. Importantly, in addition to CysLTs, IP-10 was also identified as a biomarker for HAM/TSP activity. These data suggest that LTs are likely to be associated with HTLV-1 infection and HAM/TSP development, suggesting their putative use for clin. monitoring.

PLoS One 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 C7H11Br, Formula: C12H23N3S.

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

Zhong, Yao published the artcile3,5-Disubstituted 2-Aminopyridines via Nickel-Catalyzed Cycloaddition of Terminal Alkynes and Cyanamides, SDS of cas: 2451-91-4, the publication is Synlett (2015), 26(3), 307-312, database is CAplus.

The regioselectivity of the Ni/SIPr [SIPr = 1,3-bis(2,6-diisopropylphenyl)imidazolidene] -catalyzed cycloaddition of terminal alkynes and cyanamides was explored. In general, 3,5-disubstituted 2-aminopyridines were formed as the major product.

Synlett 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 C14H14, SDS of cas: 2451-91-4.

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

Arbour, Christine A. published the artcileSequence Diversification by Divergent C-Terminal Elongation of Peptides, Recommanded Product: H-Lys(Boc)-OH, the publication is Journal of Organic Chemistry (2018), 83(4), 1797-1803, database is CAplus and MEDLINE.

Sequence diversification at the C terminus is traditionally limited by significant epimerization of the C-terminal residue during its activation toward nucleophilic attack, thus mandating repetition of the peptide synthesis for each targeted variation. Here, we accomplish divergent C-terminal elongation of a single peptide substrate with concomitant resin cleavage via displacement of an N-acyl urea moiety. Sterically hindered amino acids such as Ile and Pro are well-tolerated in this approach, which proceeds reasonable conversion and no detectable epimerization of the starting peptide’s C-terminal amino acid.

Journal of Organic 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, Recommanded Product: H-Lys(Boc)-OH.

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

Galindo Casas, Meritxell published the artcileDecoupling Protein Production from Cell Growth Enhances the Site-Specific Incorporation of Noncanonical Amino Acids in E. coli, Computed Properties of 2418-95-3, the publication is ACS Synthetic Biology (2020), 9(11), 3052-3066, database is CAplus and MEDLINE.

The site-specific incorporation of noncanonical amino acids (ncAAs) into proteins by amber stop codon suppression has become a routine method in academic laboratories This approach requires an amber suppressor tRNA_CUA to read the amber codon and an aminoacyl-tRNA synthetase to charge the tRNA_CUA with the ncAA. However, a major drawback is the low yield of the mutant protein in comparison to the wild type. This effect primarily results from the competition of release factor 1 with the charged suppressor tRNA_CUA for the amber codon at the A-site of the ribosome. A number of laboratories have attempted to improve the incorporation efficiency of ncAAs with moderate results. The authors aimed at increasing the efficiency to produce high yields of ncAA-functionalized proteins in a scalable setting for industrial application. To do this, the authors inserted an ncAA into the enhanced green fluorescent protein and an antibody mimetic mol. using an industrial E. coli strain, which produces recombinant proteins independent of cell growth. The controlled decoupling of recombinant protein production from cell growth considerably increased the incorporation of the ncAA, producing substantially higher protein yields vs. the reference E. coli strain BL21(DE3). The target proteins were expressed at high levels, and the ncAA was efficiently incorporated with excellent fidelity while the protein function was preserved.

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 C11H22N2O4, Computed Properties of 2418-95-3.

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

Heald, Robert A. published the artcileAntitumor polycyclic acridines. Palladium(0)-mediated syntheses of quino[4,3,2-kl]acridines bearing peripheral substituents as potential telomere maintenance inhibitors, Application of (2-Pivalamidophenyl)boronic acid, the publication is Organic & Biomolecular Chemistry (2003), 1(19), 3377-3389, database is CAplus and MEDLINE.

Pd(0)-mediated Suzuki coupling between substituted 2-(pivaloylamino)benzeneboronic acids and 10-methylacridones I (R¹ = H, HO, MeO; R² = H, Cl; R³ = Br, F₃CSO₂O) yielded intermediate 1-arylacridones which were further cyclized to 8-methylquino[4,3,2-kl]acridines II (R¹ = H, HO, MeO; R² = H, Cl; R⁴ = H, Cl) with phosphorus oxychloride or 6M HCl in EtOH. Subsequent Heck reactions between chloro- or triflate-substituted substrates II and acrylic acid derivatives afforded quinoacridines with unsaturated side-chains. Alkylboranes, prepared by interaction of 9-borabicyclo[3,3,1]nonane and allyl acetate or N-allyltrifluoroacetamide, participated in Suzuki-Miyaura reactions with chloro-substituted 8-methylquinoacridines II (R² = H, R⁴ = Cl; R² = Cl, R⁴ = H; R¹ = F₃CSO₂O) to form derivatives bearing functionalized Pr groups in the 6- and 10-positions. Representative 8-methylquinoacridines were methylated with Me iodide to yield telomerase-inhibiting 8,13-dimethylquinoacridinium iodides.

Organic & Biomolecular 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, Application of (2-Pivalamidophenyl)boronic acid.

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

Monty, Olivier B. C. published the artcileSolution-phase fmoc-based peptide synthesis for DNA-encoded chemical libraries: Reaction conditions, protecting group strategies, and pitfalls, Recommanded Product: H-Lys(Boc)-OH, the publication is ACS Combinatorial Science (2020), 22(12), 833-843, database is CAplus and MEDLINE.

Peptide drug discovery has shown a resurgence since 2000, bringing 28 non-insulin therapeutics to the market compared to 56 since its first peptide drug, insulin, in 1923. While the main method of discovery has been biol. display-phage, mRNA, and ribosome-the synthetic limitations of biol. systems has restricted the depth of exploration of peptide chem. space. In contrast, DNA-encoded chem. offers the synergy of large numbers and ribosome-independent synthetic flexibility for the fast and deeper exploration of the same space. Hence, as a bridge to building DNA-encoded chem. libraries (DECLs) of peptides, we have developed substrate-tolerant amide coupling reaction conditions for amino acid monomers, performed a coupling screen to illustrate such tolerance, developed protecting group strategies for relevant amino acids and reported the limitations thereof, developed a strategy for the coupling of α,α-disubstituted alkenyl amino acids relevant to all-hydrocarbon stapled peptide drug discovery, developed reaction conditions for the coupling of tripeptides likely to be used in DECL builds, and synthesized a fully deprotected DNA-decamer conjugate to illustrate the potency of the developed methodol. for on-DNA peptide synthesis.

ACS Combinatorial Science 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, Recommanded Product: H-Lys(Boc)-OH.

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

Rydfjord, Jonas published the artcileRoute to 3-Amidino Indoles via Pd(II)-Catalyzed C-H Bond Activation, Quality Control of 2451-91-4, the publication is Organic Letters (2017), 19(15), 4066-4069, database is CAplus and MEDLINE.

We report a facile synthesis of 3-amidino indoles from indoles and cyanamides. The reaction is Pd(II)-catalyzed and proceeds via C-H bond activation of the indole in its 3-position followed by a 1,2-addition of the resulting indole-palladium σ-complex to a cyanamide, which provides the corresponding amidine. The preference for 4,5-diazafluoren-9-one (DAF) as the ligand is investigated using DFT calculations, and a plausible reaction pathway is presented.

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, Quality Control of 2451-91-4.

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

Melekhova, Anna A. published the artcileCopper(I)-Catalyzed 1,3-Dipolar Cycloaddition of Ketonitrones to Dialkylcyanamides: A Step toward Sustainable Generation of 2,3-Dihydro-1,2,4-oxadiazoles, HPLC of Formula: 2451-91-4, the publication is ACS Omega (2017), 2(4), 1380-1391, database is CAplus and MEDLINE.

Cu^I -catalyzed cycloaddition of the ketonitrones Ph₂C=N⁺ (R’)O^– (R’ = Me, CH₂Ph) to the disubstituted cyanamides NCNR₂ (R = Me₂ , Et₂ , (CH₂)₄ , (CH₂)₅ , (CH₂)₄O, C₉H₁₀, (CH₂Ph)₂ , Ph(Me)) gives corresponding 5-aminosubstituted 2,3-dihydro- 1,2,4-oxadiazoles (16 examples) in good to moderate yields. The reaction proceeds under mild conditions (CH₂Cl₂ , RT or 45 °C) and requires 10 mol% of [Cu(NCMe)₄](BF₄) as the catalyst. Somehow reduced yields are due to the individual properties of 2,3- dihydro-1,2,4-oxadiazoles, which easily undergo ring-opening via the N-O bond splitting. Results of the DFT calculations reveal that the cycloaddition of ketonitrones to Cu^I -bound cyanamides is a concerted process and the copper-catalyzed reaction is controlled by the predominant contribution of HOMO_dipole-LUMO_{dipolarophile} interaction (group I by the Sustmann’s classification). Metal-involving process is much more asynchronous and profitable from both kinetic and thermodn. viewpoints than the hypothetical metal-free reaction.

ACS Omega 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, HPLC of Formula: 2451-91-4.

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