Category: amides-buliding-blocks

Rydfjord, Jonas published the artcileDecarboxylative Palladium(II)-Catalyzed Synthesis of Aryl Amidines from Aryl Carboxylic Acids: Development and Mechanistic Investigation, Recommanded Product: N,N-Dibenzylcyanamide, the publication is Chemistry – A European Journal (2013), 19(41), 13803-13810, database is CAplus and MEDLINE.

A fast and convenient synthesis of aryl amidines starting from carboxylic acids and cyanamides is reported. The reaction was achieved by palladium(II) catalysis in a one-step microwave protocol using [Pd(O₂CCF₃)₂], 6-methyl-2,2′-bipyridyl, and trifluoroacetic acid (TFA) in N-methylpyrrolidinone (NMP), providing the corresponding aryl amidines in moderate to excellent yields. E.g., in this system, reaction of 2,4,6-trimethoxybenzoic acid and N-cyanopiperidine gave 96% amidine I. The protocol is very robust with regards to the cyanamide coupling partner but requires electron-rich ortho-substituted aryl carboxylic acids. Mechanistic insight was provided by a DFT investigation and direct ESI-MS studies of the reaction. The results of the DFT study correlated well with the exptl. findings and, together with the ESI-MS study, support the suggested mechanism. Furthermore, a scale-out (scale-up) was performed with a non-resonant microwave continuous-flow system, achieving a maximum throughput of 11 mmol h^-1 by using a glass reactor with an inner diameter of 3 mm at a flow rate of 1 mL min^-1.

Chemistry – A European Journal 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

Timari, Geza published the artcileA convenient synthesis of two new indoloquinoline alkaloids, HPLC of Formula: 146140-95-6, the publication is Synlett (1997), 1067-1068, database is CAplus.

A concise synthesis of cryptosanguinolentine and cryptotackieine (neocryptolepine), isolated from Cryptolepis sanguinolenta is reported. The Pd-catalyzed cross-coupling reaction of 3-bromoquinoline or 3-bromo-N-methyl-2-quinolinone with 2-(pivaloylamino)phenylboronate gave the corresponding biaryls from which the indoloquinolines could be synthesized.

Synlett 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 C7H8BBrO2, HPLC of Formula: 146140-95-6.

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

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

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

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

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

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

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