Category: 15029-36-4

Tauber, Carolin published the artcileChemical Evolution of Antivirals Against Enterovirus D68 through Protein-Templated Knoevenagel Reactions, Related Products of amides-buliding-blocks, the publication is Angewandte Chemie, International Edition (2021), 60(24), 13294-13301, database is CAplus and MEDLINE.

The generation of bioactive mols. from inactive precursors is a crucial step in the chem. evolution of life, however, mechanistic insights into this aspect of abiogenesis are scarce. Here, we investigate the protein-catalyzed formation of antivirals by the 3C-protease of enterovirus D68. The enzyme induces aldol condensations yielding inhibitors with antiviral activity in cells. Kinetic and thermodn. analyses reveal that the bioactivity emerges from a dynamic reaction system including inhibitor formation, alkylation of the protein target by the inhibitors, and competitive addition of non-protein nucleophiles to the inhibitors. The most active antivirals are slowly reversible inhibitors with elongated target residence times. The study reveals first examples for the chem. evolution of bio-actives through protein-catalyzed, non-enzymic C-C couplings. The discovered mechanism works under physiol. conditions and might constitute a native process of drug development.

Angewandte Chemie, International Edition 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 C6H9NO3, Related Products of amides-buliding-blocks.

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

Semichenko, E. S. published the artcileZeolites in the synthesis of 1-alkyl-2-oxonicotinonitriles, Product Details of C5H8N2O, the publication is Russian Journal of Organic Chemistry (2005), 41(2), 313-314, database is CAplus.

Cyclocondensation of acetylacetone with cyanoacetamide or N-alkylcyanoacetamides (alkyl = Me, Et) in the presence of NaA zeolite afforded 4,6-dimethyl-2-oxonicotinonitrile or 1-alkyl-4,6-dimethyl-2-oxonicotinonitriles, resp. The condensation of 3-hydroxyiminopenta-2,4-dione with cyanoacetamide in the same manner furnished 4,6-dimethyl-5-nitroso-2-oxonicotinonitrile.

Russian Journal of Organic Chemistry 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 C13H10O2, Product Details of C5H8N2O.

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

Unterhalt, B. published the artcileNitramines; IX. Acylnitramines, SDS of cas: 15029-36-4, the publication is Synthesis (1976), 241-2, database is CAplus.

Acylnitramines RCONMeNO2 (R = Me, Ph, PhCH2, 4-O2NC6H4, etc.) were prepared in 39-64% yield by the reaction of O2NNNaMe with RCOCl in anhydrous MeCN containing K2CO3. RCONR1NO2 [R = H, Me, NCCH2, O2NC6H4, (O2N)2C6H3, etc.; R1 = Me, Et) were prepared in 36-96% yield by the nitration of RCONHR1 with N2O5 in anhydrous HCCl3 at -60°.

Synthesis 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 C27H39ClN2, SDS of cas: 15029-36-4.

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

Doshi, Hiren published the artcile6-Tosyl-4,5,6,7-Tetrahydrothieno[2,3-c]Pyridine-3-Carboxamide Analogues: Synthesis, Characterization, MO Calculation, and Antibacterial Activity, Category: amides-buliding-blocks, the publication is Applied Biochemistry and Biotechnology (2015), 175(3), 1700-1709, database is CAplus and MEDLINE.

A series of 6-tosyl-4,5,6,7-tetrahydrothieno[2,3-c]pyridine-3-carboxamide I (R¹ = H, OH; R² = R³ = H, Cl, OCH₃; R⁴ = H, Cl, OCH₃, OH) analogs are synthesized. These are tested for their antibacterial activity against Bacillus subtilis (abbreviated as BS), Staphylococcus aureus (abbreviated as SA), and Escherichia coli (abbreviated as EC). The synthesized compounds are able to inhibit the growth of the SA and EC. None of the compounds are effective against BS. All valence MO (abbreviated as MO) calculations with PM⁶ have been carried out for the mols. for which bioactivity data are available. Ciprofloxacin is taken as the standard antibiotics to compare activity with the mols. synthesized. It has been attempted to correlate the activity of the mols. with their electronic structure.

Applied Biochemistry and Biotechnology 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 C5H8N2O, Category: amides-buliding-blocks.

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

McCall, J. M. published the artcileNew approach to triaminopyrimidine N-oxides, HPLC of Formula: 15029-36-4, the publication is Journal of Organic Chemistry (1975), 40(22), 3304-6, database is CAplus and MEDLINE.

2,4,Diamino-6-(substituted amino)pyrimidine 3-oxides (I, R = H, R2 = Me, Et, Bu, n-C10H21, cyclohexyl; R = R1 = Bu, cyclohexyl; NRR1 = piperidine, 1-pyrrolidinyl) are prepared from amides NCCH2CONRR1 which are O-methylated to NCCH:C(OMe)NRR2, the products reacted with H2NCN to give NCCH2C(NRR1):NCN, and these treated in situ with NH2OH to give I. The sequential generation of the heterocycle from smaller fragments unequivocally establishes the position of the amine and N-oxide functionalities and allows ready variation of the 6-amino substituent. The three-step process proceeds in good yield and is easily performed.

Journal of Organic Chemistry 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 C5H8N2O, HPLC of Formula: 15029-36-4.

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

Zhou, Linna published the artcileA Class of 5-Nitro-2-furancarboxylamides with Potent Trypanocidal Activity against Trypanosoma brucei in Vitro, Recommanded Product: 2-Cyano-N-ethylacetamide, the publication is Journal of Medicinal Chemistry (2013), 56(3), 796-806, database is CAplus and MEDLINE.

Recently, the World Health Organization approved the nifurtimox-eflornithine combination therapy for the treatment of human African trypanosomiasis, renewing interest in nitroheterocycle therapies for this and associated diseases. In this study, we have synthesized a series of novel 5-nitro-2-furancarboxylamides that show potent trypanocidal activity, ∼1000-fold more potent than nifurtimox against in vitro Trypanosoma brucei with very low cytotoxicity against human HeLa cells. More importantly, the most potent analog showed very limited cross-resistance to nifurtimox-resistant cells and vice versa. This implies that our novel, relatively easy to synthesize and therefore cheap, 5-nitro-2-furancarboxylamides are targeting a different, but still essential, biochem. process to those targeted by nifurtimox or its metabolites in the parasites. The significant increase in potency (smaller dose probably required) has the potential for greatly reducing unwanted side effects and also reducing the likelihood of drug resistance. Collectively, these findings have important implications for the future therapeutic treatment of African sleeping sickness.

Journal of Medicinal Chemistry 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 C15H24S, Recommanded Product: 2-Cyano-N-ethylacetamide.

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

Zhang, Zhichao published the artcileNovel soluble myeloid cell leukemia sequence 1 (Mcl-1) inhibitor (E,E)-2-(benzylaminocarbonyl)-3-styrylacrylonitrile (4g) developed using a fragment-based approach, HPLC of Formula: 15029-36-4, the publication is European Journal of Medicinal Chemistry (2013), 141-149, database is CAplus and MEDLINE.

Based on a known nanomolar Bcl-2 homol. domain 3 (BH3) mimetic 3-thiomorpholin-8-oxo-8H-acenaphtho[1,2-b] pyrrole-9-carbonitrile (I, MW: 331), we applied a fragment-based approach to obtain BH3 mimetics with improved affinity and improved solubility in a water-ethanol (9:1) cosolvent. After the deconstruction of I, we obtained fragment cyanoacetamide (II), which was determined to be a ligand efficiency (LE) hot part. After a rational optimization through fragment evolution beginning with fragment II, a smaller Mcl-1 inhibitor (E,E)-2-(benzylaminocarbonyl)-3-styrylacrylonitrile (III, MW: 288) with a 6-fold increase in affinity compared to I was obtained, as predicted by our optimization curve and identified by Mcl-1 protein NMR (NMR).

European Journal of Medicinal Chemistry 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 C9H7NO2, HPLC of Formula: 15029-36-4.

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

Ramesh, Pattipati published the artcileDesign, synthesis and biological evaluation of some novel 3-substituted acrylamide quinoline derivatives, Safety of 2-Cyano-N-ethylacetamide, the publication is International Journal of ChemTech Research (2017), 10(3), 259-270, database is CAplus.

A new series of (2,8-dichloroquinolin-3-yl)acrylamide derivatives I (R¹ = Me, c-Pr, Ph, etc.; R² = H; -R¹R²– = -(CH₂)₄-, -(CH₂)O(CH₂)-) were designed by incorporating simple chem. methods. Here different N-substituted cyanoacetamide derivatives were used as the pharmacophore entities to link with the parent quinoline moiety. Antimicrobial activity of synthesized compounds was screened, which has revealed that the few of the compounds were more potent than the corresponding standard drugs.

International Journal of ChemTech Research 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 C5H8N2O, Safety of 2-Cyano-N-ethylacetamide.

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

Devani, M. B. published the artcileSynthesis of 2-aminothiophenes and thieno[2,3-d]pyrimidines, Safety of 2-Cyano-N-ethylacetamide, the publication is Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry (1976), 14B(5), 357-60, database is CAplus.

The thienopyrimidinones I [R = Me, R1 = CO2Et, R2 = H; RR1 = (CH2)4, R2 = Ph] were prepared by treating the aminothiophenes II (R = CO2Et, CONHPh) with HCONH2 or (EtO)3CH, whereas cyclization of II [R = Me, R1 = EtO2C, R3 = cyano; RR1 = (CH2)4, R3 = cyano] with HCONH2 gave the corresponding aminothienopyrimidines III. Furthermore, the spiro[benzothienopyrimidine-2,1′-cyclohexane] IV was prepared by cyclization of NCCH2CONHNHPh with cyclohexanone in the presence of S. IV had antiinflammatory and anticonvulsant activities and II had only antiinflammatory activity.

Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry 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 C5H8N2O, Safety of 2-Cyano-N-ethylacetamide.

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