Month: December 2022

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

Schroth, Werner published the artcile1,3-Thiazine syntheses with β-diketones via enol phosphate, Related Products of amides-buliding-blocks, the publication is Synthesis (1983), 827-30, database is CAplus.

RCOCH₂COR (R = Ph; 4-MeOC₆H₄, Me) were successively treated with Na or NaOMe, then (PhO)₂P(O)Cl in C₆H₆ or Et₂O to give 58-75% RCOCH:CROP(O)(OPh)₂ which were cyclized with H₂NC(S)R¹ (R¹ = Ph, Me, CMe₃, SEt, NH₂, NMe₂, morpholino, PhCH:NNH, MeEtC:NNH, 4-MeC₆H₄SO₂NHNH, 4-MeOC₆H₄) in AcOH containing POCl₃, with dropwise addition of 70% HClO₄ to give 39-97% thiazinium perchlorates I.

Synthesis published new progress about 14294-10-1. 14294-10-1 belongs to amides-buliding-blocks, auxiliary class Morpholine,Thiourea,Amine,Amide, name is Morpholine-4-carbothioamide, and the molecular formula is C5H10N2OS, Related Products of amides-buliding-blocks.

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

Schroth, W. published the artcileSynthesis of 1,3-thiazinium salts from β-chlorovinyl ketones and thio amide functionalized compounds, Category: amides-buliding-blocks, the publication is Tetrahedron (1982), 38(7), 937-48, database is CAplus.

Thiocarbamoyl compounds reacted with β-chlorovinyl ketones to give 1,3-thiazinium salts via S-ketovinylthioimidium derivatives E.g., condensation reaction of Me₃CCSNH₂ with 4-MeC₆H₄COCH:CHCl in HClO₄ gave the intermediate 4-MeC₆H₄COCH:CHSC(:N⁺H₂)CMe₃ ClO₄^– which underwent acid-catalyzed cyclocondensation reaction to give 72% thiazinium salt I. The thiazinium salts react with nucleophilic reagents preferentially at position 6. E.g., substitution reaction of I with morpholine at -20° gave 94% thiazine II. The scope of the cyclocondensation reaction is discussed.

Tetrahedron published new progress about 14294-10-1. 14294-10-1 belongs to amides-buliding-blocks, auxiliary class Morpholine,Thiourea,Amine,Amide, name is Morpholine-4-carbothioamide, and the molecular formula is C5H10N2OS, Category: amides-buliding-blocks.

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

Lozhkina, N G published the artcile[Clinical case: early connection of valsartan/sacubitril in the treatment of hypertension]., Application of (S)-2-(N-((2′-(1H-Tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid, the publication is Kardiologiia (2022), 62(5), 72-74, database is MEDLINE.

Metabolic syndrome is a disease the World Health Organization has called a new pandemic of the 21st century. Arterial hypertension is one of the criteria for this diagnosis and a determinant of damage to major target organs. The present clinical case demonstrates an experience of treatment of arterial hypertension associated with metabolic syndrome with a valsartan/sacubitril molecular complex.

Kardiologiia published new progress about 137862-53-4. 137862-53-4 belongs to amides-buliding-blocks, auxiliary class GPCR/G Protein,Angiotensin Receptor, name is (S)-2-(N-((2′-(1H-Tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid, and the molecular formula is C24H29N5O3, Application of (S)-2-(N-((2′-(1H-Tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid.

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

Veveris, A. published the artcileIndirect potentiometric determination of N-acylated aminosaccharides, Category: amides-buliding-blocks, the publication is Zhurnal Analiticheskoi Khimii (1990), 45(6), 1229-33, database is CAplus.

The aminosaccharides (3-6 mg) were converted to oxazole derivatives by heating with 2 mL 0.03M HClO₄ in MeNO₂ to 85 ± 5° for 40-50 min; 3 mL 0.03M trialkylamine in MeNO₂ was added, and excess amine was back-titrated with the HClO₄ solution by using glass and calomel electrodes. The relative standard deviation was ≤0.015.

Zhurnal Analiticheskoi Khimii published new progress about 14086-92-1. 14086-92-1 belongs to amides-buliding-blocks, auxiliary class Sugar Units,Glu, name is (3R,4R,5S,6R)-6-(Acetoxymethyl)-3-benzamidotetrahydro-2H-pyran-2,4,5-triyl triacetate, and the molecular formula is C11H8O3, Category: amides-buliding-blocks.

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

Wilde, Felix published the artcileTractable synthesis of multipurpose screening compounds with under-represented molecular features for an open access screening platform, Recommanded Product: 2-Cyano-N-ethylacetamide, the publication is Molecular Diversity (2014), 18(3), 483-495, database is CAplus and MEDLINE.

Abstract: The layout of multipurpose screening libraries must address criteria for the compounds such as novelty, diversity potential, innovative design, and last but not least synthetic tractability. While academic compound collections are often innovative, novel, and highly divers, synthesis of analogs or larger substance quantities is often hampered by complex multistep syntheses with low overall yields. In addition, covalently binding compounds and interaction motifs designed to bind metal ions were discriminated against by the paradigm that these interaction types must almost inevitably lead to toxic effects. We would like to challenge this hypothesis. The lack of such interactions could be a reason for frequent failure in the disclosure of hits for hitherto undruggable target proteins using com. available screening collections. Thus, easily synthesizable screening candidates equipped to bind covalently to nucleophiles or to metalloenzymes by chelation are under-represented in public access screening libraries. Within this work, we present the synthesis and deposition of 88 compounds with five distinct functional classes, each of which features under-represented screening motifs, for example, metal ion complexation, reversible covalent binding, or halogen bonding. The collection includes acetohydrazides, acylhydrazones, propylene glycol ethers, 2-cyanoacetamides, and 2-cyanoacrylamides. The rational for the synthesis of most of the compounds was recently published by our group and is now supplemented by addnl. compounds reported here for the first time. The public access disposition enables academic research groups to collectively expand the druggable space and interdisciplinary collaborate within the scientific field. Graphical Abstract: [Figure not available: see fulltext.].

Molecular Diversity published new progress about 15029-36-4. 15029-36-4 belongs to amides-buliding-blocks, auxiliary class Nitrile,Amine,Aliphatic hydrocarbon chain,Amide, name is 2-Cyano-N-ethylacetamide, and the molecular formula is C4H11NO, Recommanded Product: 2-Cyano-N-ethylacetamide.

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

Gasser, Gilles published the artcileTowards the Preparation of Novel Re/^99mTc Tricarbonyl-Containing Peptide Nucleic Acid Bioconjugates, COA of Formula: C40H35N7O8, the publication is Australian Journal of Chemistry (2011), 64(3), 265-272, database is CAplus.

A novel azido derivative of the di-(2-picolyl)amide (Dpam) ligand, namely 3-azido-N,N-bis-pyridin-2-ylmethylpropionamide (3), was prepared from 3-bromo-N,N-bis(pyridin-2-ylmethyl)propanamide (2) with an excess of sodium azide in DMSO. 3 Was then reacted, by Cu(I)-catalyzed [3+2] cycloaddition (often referred to as click chem.), with the previously reported alkyne-containing peptide nucleic acid (PNA) monomer Fmoc-1-OBu-t to give the Dpam-containing PNA monomer (Fmoc-4-OBu-t) in 44% yield. It was also demonstrated that 3 could be reacted by click chem., on the solid phase, to an alkyne-containing PNA oligomer (alkyne-PNA) to yield Dpam-PNA. The attempts to complex Dpam-PNA with [NEt₄]₂[ReBr₃(CO)₃] and [^99mTc(CO)₃(H₂O)₃]⁺ are also discussed in detail.

Australian Journal of Chemistry published new progress about 186046-83-3. 186046-83-3 belongs to amides-buliding-blocks, auxiliary class Purine,Carboxylic acid,Amine,Benzene,Amide,Others,PNA,, name is 2-(N-(2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)ethyl)-2-(2-(((benzhydryloxy)carbonyl)amino)-6-oxo-5H-purin-9(6H)-yl)acetamido)acetic acid, and the molecular formula is C40H35N7O8, COA of Formula: C40H35N7O8.

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

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