Category: 15029-36-4

Fefelova, S. R. published the artcileRegioselective Synthesis of Pyridin-2-One Derivatives Based on Ethyl(1-Phenylethylidene)Cyanoacetate and Cyanoacetamides, HPLC of Formula: 15029-36-4, the publication is Chemistry of Heterocyclic Compounds (New York, NY, United States) (2014), 50(8), 1133-1136, database is CAplus.

Et (1-phenylethylidene)cyanoacetate reacted with cyanoacetamides in an alc. solution of sodium ethoxide, forming various pyridin-2-ones. The cyclization direction of the Michael adducts was affected by the nucleophilicity of the cyanoacetamide used as a CH acid.

Chemistry of Heterocyclic Compounds (New York, NY, United States) 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

Sakauchi, Nobuki published the artcileDiscovery of 5-Chloro-1-(5-chloro-2-(methylsulfonyl)benzyl)-2-imino-1,2-dihydropyridine-3-carboxamide (TAK-259) as a Novel, Selective, and Orally Active α_1D Adrenoceptor Antagonist with Antiurinary Frequency Effects: Reducing Human Ether-a-go-go-Related Gene (hERG) Liabilities, SDS of cas: 15029-36-4, the publication is Journal of Medicinal Chemistry (2016), 59(7), 2989-3002, database is CAplus and MEDLINE.

A novel structural class of iminopyridine derivative 1 was identified as a potent and selective human α_1D adrenoceptor (α_1D adrenergic receptor; α_1D-AR) antagonist against α_1A– and α_1B-AR through screening of an inhouse compound library. From initial structure-activity relationship studies, we found lead compound 9m with hERG K⁺ channel liability. To develop analogs with reduced hERG K⁺ channel inhibition, a combination of site-directed mutagenesis and docking studies was employed. Further optimization led to the discovery of I and II, which showed antagonistic activity by a bladder strip test in rats with bladder outlet obstruction, as well as ameliorated cystitis-induced urinary frequency in rats. Ultimately, 9u was selected as a clin. candidate. This is the first study to show the utility of iminopyridine derivatives as selective α_1D-AR antagonists and evaluate their effects in vivo.

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 C5H8N2O, SDS of cas: 15029-36-4.

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

Yokoyama, Masataka published the artcileS,N double rearrangement. 3. Reaction mechanism, Product Details of C5H8N2O, the publication is Journal of Organic Chemistry (1984), 49(1), 74-8, database is CAplus.

¹³C-labeling and crossover experiments indicated that cyclizations such as that of I with BzOH to give II proceed via a thiaallylic rearrangement of the initial ring-closure product formed from the CN and SH groups and BzOH.

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 C7H7ClN2, Product Details of C5H8N2O.

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

Kuhnert, Maren published the artcileTracing Binding Modes in Hit-to-Lead Optimization: Chameleon-Like Poses of Aspartic Protease Inhibitors, Formula: C5H8N2O, the publication is Angewandte Chemie, International Edition (2015), 54(9), 2849-2853, database is CAplus and MEDLINE.

Successful lead optimization in structure-based drug discovery depends on the correct deduction and interpretation of the underlying structure-activity relationships (SAR) to facilitate efficient decision-making on the next candidates to be synthesized. Consequently, the question arises, how frequently a binding mode (re)-validation is required, to ensure not to be misled by invalid assumptions on the binding geometry. We present an example in which minor chem. modifications within one inhibitor series lead to surprisingly different binding modes. X-ray structure determination of eight inhibitors derived from one core scaffold resulted in four different binding modes in the aspartic protease endothiapepsin, a well-established surrogate for e.g. renin and β-secretase. In addition, we suggest an empirical metrics that might serve as an indicator during lead optimization to qualify compounds as candidates for structural revalidation.

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 C5H8N2O, Formula: C5H8N2O.

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

Mitsudera, Hiroyuki published the artcileStudies on nereistoxin and its related compounds. II. Synthesis and insecticidal activity of 5-dimethylamino-1,3-dithianes, Safety of 2-Cyano-N-ethylacetamide, the publication is Nippon Noyaku Gakkaishi (1991), 16(3), 397-404, database is CAplus.

Twenty-five 2-cyano-5-(dimethylamino)-2-(substituted phenyl)-1,3-dithianes I (R = H, 4-F, 4-Me, 3-CF₃, 2-MeO, 3,4-Cl₂, etc.) and 22 2-cyano-5-(dimethylamino)-2-(substituted carbamoyl)-1,3-dithianes II (R¹ = NH₂, NHMe, NHEt, NMe₂, etc.) were synthesized and tested for their insecticidal and miticidal activities toward larvae of Chilo suppressalis, Laodelphax striatellus, Henosepilachna vigintioctapinctata, and Spodoptera litura and Tetranychus urticae adults. All compounds had high activities toward insects and mites tested, I (R = 4-Br) and II (R¹ = NHC₉H₁₉) having highest activities. Conversion of I and II into 4-(dimethylamino)-1,2-dithiolane and/or its 1-oxide in the living body and the effect of electron-withdrawing groups at the 2-position on the penetration of I and II into the body were suggested.

Nippon Noyaku Gakkaishi 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

Ukhov, S. V. published the artcileSynthesis and antimicrobial activity of 2-iminocoumarin-3-carboxylic acid amides, HPLC of Formula: 15029-36-4, the publication is Pharmaceutical Chemistry Journal (Translation of Khimiko-Farmatsevticheskii Zhurnal) (2001), 35(7), 364-365, database is CAplus.

A series of 2-iminocoumarin-3-carboxylic acid amides, e.g. I, were prepared and evaluated for antimicrobial activity. It was established that all the synthesized compounds possess antimicrobial properties with respect to both St. aureus and E. coli. The most active substances significantly exceed ethacridine in the bacteriostatic effect.

Pharmaceutical Chemistry Journal (Translation of Khimiko-Farmatsevticheskii Zhurnal) 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 C10H9ClN2O, HPLC of Formula: 15029-36-4.

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

McCall, John M. published the artcileCyanoimine chemistry: new routes to pyrimidinones and (carbonylamino)iminopropanamides, Recommanded Product: 2-Cyano-N-ethylacetamide, the publication is Journal of Organic Chemistry (1979), 44(9), 1562-3, database is CAplus.

RNHCOCH₂C(NR¹₂):NCN (I; R = Et, Bu; NR¹₂ = NEt₂, morpholino, piperidino) are versatile precursors of specific N-alkylated pyrimidinones. I are readily converted via KOCMe₃ to II. I can also be hydrolyzed to RNHCOCH₂C(NR¹₂):NCONH₂.

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, Recommanded Product: 2-Cyano-N-ethylacetamide.

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

Chen, Wei published the artcileSyntheses of 3,4-dihydro-4-oxopyrimido[4,5-b]quinolines, Quality Control of 15029-36-4, the publication is Gaodeng Xuexiao Huaxue Xuebao (1990), 11(5), 532-3, database is CAplus.

Pyrimidoquinolines I (R = H, alkyl, PHCH₂, Ph; R¹, R² = H, H; R¹R² = methylenedioxy) were prepared in 81-94% yield by heating aminoquinolinecarboxamides II with HCONH₂ at 160-170°.

Gaodeng Xuexiao Huaxue Xuebao 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, Quality Control of 15029-36-4.

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

Viswanatha, Gollapalle L. published the artcileSynthesis and anti-hyperlipidemic activity of 3H-benzo[4,5]thieno[2,3-d][1,2,3]triazin-4-ones: possible mechanism of altered lipid metabolism, Related Products of amides-buliding-blocks, the publication is Oman Medical Journal (2012), 27(5), 388-395, database is CAplus and MEDLINE.

Objectives: The present study aimed to evaluate the anti-hyperlipidemic activity of newly synthesized tricyclic benzothieno[1,2,3]triazine derivatives I (R = Me, Et, 2-chlorophenyl), namely CP-1 (3-methyl-5,6,7,8-tetrahydro-3H-benzo[4,5]thieno[2,3-d][1,2,3]triazin-4-one), CP-2 (3-ethyl-5,6,7,8-tetrahydro-3H-benzo[4,5] thieno[2,3-d][1,2,3]triazin-4-one) and CP-6 [3-(2-chlorophenyl)-5,6,7,8-tetrahydro-3H-benzo[4,5]thieno[2,3-d][1,2,3]triazin-4-one] against dexamethasone and Triton WR-1339-induced hyperlipidemia in rats. Methods: Anti-hyperlipidemic activities of the test compounds were evaluated against dexamethasone (10 mg/kg, s.c. [s.c.]) and Triton WR-1339 (200 mg/kg, i.p. [i.p]) induced hyperlipidemia in rats. Results: Administration of a single dose of Triton WR-1339 (200 mg/kg i.p) and dexamethasone (10 mg/kg s.c.) for 8 consecutive days to adult wistar rats caused severe hyperlipidemia characterized by a marked increase in serum cholesterol, LDL-C, VLDL-C and triglyceride levels along with an increase in atherogenic index. Serum HDL-C levels were decreased significantly compared to a normal control. Pretreatment with Atorvastatin (10 mg/kg p.o.), CP-1 (25 and 50 mg/kg), CP-2 (25 and 50 mg/kg) and CP-6 (25 and 50 mg/kg) showed significant and dose-dependent protection against dexamethasone and Triton WR-1339-induced hyperlipidemia in rats by maintaining serum total cholesterol, LDL-C, VLDL-C and HDL-C levels within the normal range. Also, a significant decrease in the atherogenic index was observed The anti-hyperlipidemic effect of CP-6 was comparable with reference standard Atorvastatin. Furthermore, CP-6 was found to be more potent than CP-1 and CP-2. Conclusion: These findings suggest that CP-1, CP-2 and CP-6 possess significant anti-hyperlipidemic activity against exptl. animal models of hyperlipidemia.

Oman Medical Journal 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 C6H5BN2O3, Related Products of amides-buliding-blocks.

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

Kumar, Arvind published the artcileKetene dithioacetals. Part 12. Synthesis and reactions of α-oxoketene dithioacetals derived from heterocyclic ketones, Safety of 2-Cyano-N-ethylacetamide, the publication is Journal of Chemical Research, Synopses (1979), 268-9, database is CAplus.

Ten title dithioacetals I [R²R³ = C(SMe)₂](R = H, Me; R¹ = H, Me, OMe; X = O, S, NSO₂C₆H₄Me-4; n = 1, 2) were prepared (51-75%) from the corresponding benzopyranones I (R² = R³ = H) by treatment with CS₂ in the presence of NaOCMe₃ followed by methylation. I [R = R¹ = H, R²R³ = C(SMe)₂, X = S, n = 1] (II) reacted with NH₂NH₂ in EtOH in the presence and absence of morpholine to give 48% benzothiopyranopyrazole III (R = NHNH₂) and 87% III (R = SMe), resp. II reacted with H₂NC(:NH)NH₂ to give 30% benzothiopyranopyrimidine IV (R = OMe) and 9% IV (R = H) and with NCCH₂CONHR (R = H, Me, Et) in the presence of NaOCHMe₂ to give 76% benzothiopyranopyridone V and 69-74% benzothiopyranonaphthyridinedione VI (R = Me, Et), resp.

Journal of Chemical Research, Synopses 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