Tag: M.W=100-150

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

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

Fier, Patrick S. published the artcileA Multifunctional Reagent Designed for the Site-Selective Amination of Pyridines, Computed Properties of 1453-82-3, the publication is Journal of the American Chemical Society (2020), 142(19), 8614-8618, database is CAplus and MEDLINE.

The development of a multifunctional reagent for the direct conversion of pyridines to Boc-protected 2-aminopyridines such as I [R = H, 3-Br, 4-Ph, etc.] with exquisite site selectivity and chemoselectivity was reported. The novel reagent was prepared on 200g scale in a single step, reacted in title reaction under mild conditions without precautions toward air or moisture, and is tolerant of nearly all common functionality. Exptl. and in situ spectroscopic monitoring techniques provided detailed insights and unexpected findings for the unique reaction mechanism.

Journal of the American Chemical Society published new progress about 1453-82-3. 1453-82-3 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is Isonicotinamide, and the molecular formula is C6H6N2O, Computed Properties of 1453-82-3.

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

Katritzky, Alan R. published the artcileSynthesis of mono- and N,N-disubstituted thioureas and N-acylthioureas, SDS of cas: 14294-10-1, the publication is Synthesis (2004), 1799-1805, database is CAplus.

1-Benzotriazole-1-carbothioamide, prepared from 1-cyanobenzotriazole and hydrogen sulfide, reacts with amines to give thioureas R¹NR²CSNH₂ (R¹ = MeOC₆H₄, Bn, pyrrolidinyl, Ph, PhNH; R² = H, Bn). Reactions of (benzotriazol-1-yl)carboximidamides and acyl- or arylaminocarbonyl(benzotriazol-1-yl)carboximidamides with hydrogen sulfide give the corresponding thioureas, N-acylthioureas, or N-carbamoylthioureas.

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, SDS of cas: 14294-10-1.

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

Solankee, Anjani published the artcile2-Substituted phenyl-5-(ω-methoxycarbonyl propyl/pentyl)-Δ²-thiazolin-4-one. Part IV, HPLC of Formula: 14294-10-1, the publication is Journal of the Institution of Chemists (India) (1994), 66(3), 91-2, database is CAplus.

The title compounds I (R = substituted Ph, 3-pyridyl, morpholino, n = 3, 5) were prepared by treatment of 2-bromoadipic and 2-bromosuberic acid with thioamides followed by esterification of the corresponding acids. with MeOH and thionyl chloride.

Journal of the Institution of Chemists (India) 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 C9H8F2O2, HPLC of Formula: 14294-10-1.

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

Keshari, Twinkle published the artcileCarbon tetrabromide mediated oxidative cyclocondensation of ketones and thioureas: an easy access to 2-aminothiazoles, COA of Formula: C5H10N2OS, the publication is Tetrahedron Letters (2015), 56(41), 5623-5627, database is CAplus.

A simple, mild, and efficient one-pot method for the synthesis of substituted 2-aminothiazoles has been reported. The reaction involves the formation of sulfenyl bromide as an umpolung intermediate of nucleophilic sulfur, which is responsible for C-S bond formation leading to oxidative cyclization of ketones and thioureas to furnish the desired products. Carbon tetrabromide was used as a convenient and mild brominating reagent under basic condition at room temperature to give 2-aminothiazoles in good to excellent yields.

Tetrahedron Letters 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, COA of Formula: C5H10N2OS.

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

Jagia, Moksh published the artcileNovel Co-crystals and Eutectics of Febuxostat: Characterization, Mechanism of Formation, and Improved Dissolution, Application In Synthesis of 1453-82-3, the publication is AAPS PharmSciTech (2022), 23(1), 43, database is CAplus and MEDLINE.

Co-crystallization studies were undertaken to improve the solubility of a highly water-insoluble drug febuxostat (FXT), used in the treatment of gout and hyperuricemia. The selection of co-crystal former (CCF) mols. such as 1-hydroxy 2-naphthoic acid (1H-2NPH), 4-hydroxy benzoic acid (4-HBA), salicylic acid (SAC), 5-nitro isophthalic acid (5-NPH), isonicotinamide (ISNCT), and picolinamide (PICO) was based on the presence of complementary functional groups capable of forming hydrogen bond and the ΔpKa difference between FXT and CCF. A liquid-assisted grinding (LAG) method was successfully employed for the rapid screening of various pharmaceutical adducts. These adducts were characterized based on their unique thermal (differential scanning calorimetry) and spectroscopic (Fourier transform IR and Raman spectroscopy) profiles. Binary phase diagrams (BPD) were plotted to establish a relationship between the thermal events and adduct formed. Powder X-ray diffraction (PXRD) studies were carried out to confirm the formation of eutectic/co-crystal. Thermogravimetric anal. (TGA) was also performed for the novel co-crystals obtained. The propensity for strong homo-synthons over weak hetero-synthons and strong hetero-synthons over weak homo-synthons during supramol. growth resulted in the formation of eutectics and co-crystals resp. FXT:1H-2NPH (1), FXT:4-HBA (1), FXT:SAC (1, 2), and FXT:5-NPH (2-1) gave rise to pure eutectic systems, while FXT:ISNCT (2-1) and FXT:PICO (1) gave rise to novel co-crystals with characteristic DSC heating curves and PXRD pattern. Addnl., the impact of microenvironmental pH and microspeciation profile on the improved dissolution profile of the co-crystals was discussed.

AAPS PharmSciTech published new progress about 1453-82-3. 1453-82-3 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is Isonicotinamide, and the molecular formula is C6H6N2O, Application In Synthesis of 1453-82-3.

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