Category: 39546-32-2

Asif, Kanwal published the artcileSolid phase syntheses of peptoid like arylureido compounds and sequencing of isobars without molecular encoding, Computed Properties of 39546-32-2, the publication is Organic & Biomolecular Chemistry (2019), 17(17), 4204-4207, database is CAplus and MEDLINE.

Arylureido-backbone containing peptoid-like trimers were prepared using the one-bead-one-compound approach. Isobaric mols. were synthesized from isocyanate precursors that contain alkyl halide handles at the ortho and para-positions in the Ph ring. After chain extension with a primary amine, the piperazine-capped mols. were sequenced using tandem mass spectrometry and successfully identified based on their fragmentation pattern without a need for internal mol. encoding.

Organic & Biomolecular Chemistry published new progress about 39546-32-2. 39546-32-2 belongs to piperidines, auxiliary class Piperidine,Amine,Amide, name is Piperidine-4-carboxamide, and the molecular formula is C6H12N2O, Computed Properties of 39546-32-2.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Blazenovic, Ivana published the artcileEffects of Gut Bacteria Depletion and High-Na⁺ and Low-K⁺ Intake on Circulating Levels of Biogenic Amines, Name: Piperidine-4-carboxamide, the publication is Molecular Nutrition & Food Research (2019), 63(4), n/a, database is CAplus and MEDLINE.

Scope : High-sodium and low-potassium (HNaLK) content in Western diets increases the risk of hypertension and cardiovascular disease (CVD). It is investigated if the dietary minerals interact with gut bacteria to modulate circulating levels of biogenic amines, which are implicated in various pathologies, including hypertension and CVD. Methods and results : Using a metabolomic approach to target biogenic amines, the effects of gut bacteria depletion and HNaLK intake on circulating levels of biogenic amines in rats are examined Forty-five metabolites whose plasma levels are significantly altered by gut bacteria depletion (p < 0.05) are found, indicating their regulation by gut bacteria. Many of them are not previously linked to gut bacteria; therefore, these data provide novel insights into physiol. or pathol. roles of gut bacteria. A number of plasma metabolites that are altered both by gut bacteria and HNaLK intake are also found, suggesting possible interactions of the diet and gut bacteria in the modulation of these metabolites. The diet effects are observed with significant changes in the gut bacterial taxa Porphyromonadaceae and Prevotellaceae (p < 0.05). Conclusion : The dietary minerals may regulate abundances of certain gut bacteria to alter circulating levels of biogenic amines, which may be linked to host physiol. or pathol.

Molecular Nutrition & Food Research published new progress about 39546-32-2. 39546-32-2 belongs to piperidines, auxiliary class Piperidine,Amine,Amide, name is Piperidine-4-carboxamide, and the molecular formula is C6H12N2O, Name: Piperidine-4-carboxamide.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Akiyama, Yoshikatsu published the artcileSynthesis of Temperature-Responsive Polymers Containing Piperidine Carboxamide and N,N-diethylcarbamoly Piperidine Moiety via RAFT Polymerization, Product Details of C6H12N2O, the publication is Macromolecular Rapid Communications (2021), 42(15), 2100208, database is CAplus and MEDLINE.

In this study, poly(N-acryloylnipecotamide) (PNANAm), poly(N-acryloylisonipecotamide) (PNAiNAm), and poly(N-acryloyl-N,N-diethylnipecotamide) (PNADNAm) are synthesized as temperature-responsive polymers using reversible addition-fragmentation chain-transfer polymerization Aqueous solutions of the three polymers are examined via temperature-dependent optical transmittance measurements. The PNANAm sample with a hydrophilic terminal group shows an upper critical solution temperature (UCST) in phosphate-buffered saline (PBS) when its mol. weight (M_n) is �7600, whereas PNANAm (M_n < 7600) is soluble The UCST is influenced by mol. weight and polymer concentration In contrast, PNANAm sample with nonionic terminal group shows UCST, when M_n is < 7600, suggesting that the terminal nonionic group possibly increases UCST of PNANAm. The urea addition experiment suggests that the driving force for expression of UCST of PNANAm is the formation of inter- and intramol. hydrogen bonds among the polymer chains. PNAiNAm is soluble in PBS but exhibits an UCST in an appropriate concentration of ammonium sulfate. In contrast, PNADNAm exhibits a lower critical solution temperature Comparing the chem. structure of these polymers and their phase transition behaviors suggests that the carboxamide group position in the piperidine ring could determine the UCST expression. The results could help design temperature-responsive polymers with a desired cloud point temperature

Macromolecular Rapid Communications published new progress about 39546-32-2. 39546-32-2 belongs to piperidines, auxiliary class Piperidine,Amine,Amide, name is Piperidine-4-carboxamide, and the molecular formula is C6H12N2O, Product Details of C6H12N2O.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Manap, Sevda published the artcileSynthesis and in vitro antioxidant and antimicrobial activities of novel 3-alkyl(aryl)-4-[3-methoxy-4-(2-furylcarbonyloxy)-benzylidenamino]-4,5-dihydro-1H-1,2,4-triazol-5-ones, and their N-acetyl, N-Mannich base derivatives, COA of Formula: C6H12N2O, the publication is Journal of the Iranian Chemical Society (2022), 19(4), 1347-1368, database is CAplus.

The reactions of 3-alkyl(aryl)-4-amino-4,5-dihydro-1H-1,2,4-triazol-5-ones I (R = Me, Ph, Bn, etc.) with 3-methoxy-4-(2-furylcarbonyloxy)-benzaldehyde formed 3-alkyl(aryl)-4-[3-methoxy-4-(2-furylcarbonyloxy)-benzylidenamino]-4,5-dihydro-1H-1,2,4-triazol-5-ones II (R¹ = H). Moreover, their five N-acetyl derivatives II (R¹ = acetyl) were synthesized. Besides, compounds II (R¹ = morpholin-4-yl-methyl)/II (R¹ = N-methylpiperazinyl)/II (R¹ = (4-carbamoylpiperidin-1-yl)methyl)/III were obtained by Mannich reaction between compounds II (R¹ = H) and morpholine/N-methylpiperazine/piperidine-4-carboxyamide/piperazine in the presence of formaldehyde. Also, these compounds were evaluated for their in vitro antioxidant activity. Furthermore, in vitro antibacterial activity of the compounds was screened against six bacteria.

Journal of the Iranian Chemical Society published new progress about 39546-32-2. 39546-32-2 belongs to piperidines, auxiliary class Piperidine,Amine,Amide, name is Piperidine-4-carboxamide, and the molecular formula is C6H12N2O, COA of Formula: C6H12N2O.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Zheng, Peiyuan published the artcileDesign, synthesis and biological evaluation of imidazo[1,5-a]pyrazin-8(7H)-one derivatives as BRD9 inhibitors, Category: piperidines, the publication is Bioorganic & Medicinal Chemistry (2019), 27(7), 1391-1404, database is CAplus and MEDLINE.

BRD9 is the subunit of mammalian SWI/SNF chromatin remodeling complex (BAF). SWI/SNF complex mutations were found in nearly 20% of human cancers. The biol. role played by BRD9 bromodomain remains poorly understood, and it is therefore imperative to identify potent and highly selective inhibitors to effectively explore the biol. of individual bromodomain proteins. In this paper, we synthesized a series of imidazo[1,5-a]pyrazin-8(7H)-one derivatives as potent BRD9 inhibitors and evaluated their BRD9 inhibitory activity in vitro and anti-proliferation effects against tumor cells. Gratifyingly, compound 27(I) and 29(II) exhibited robust potency of BRD9 inhibition with IC₅₀ values of 35 and 103 nM resp. Docking studies were performed to explain the structure-activity relationship. Furthermore, I potently inhibited cell proliferation in cell lines A549 and EOL-1 with an IC₅₀ value of 6.12 μM and 1.76 μM resp. The chem. probe, I, was identified that should prove to be useful in further exploring BRD9 bromodomain biol. in both in vitro and in vivo settings.

Bioorganic & Medicinal Chemistry published new progress about 39546-32-2. 39546-32-2 belongs to piperidines, auxiliary class Piperidine,Amine,Amide, name is Piperidine-4-carboxamide, and the molecular formula is C7H16Cl2Si, Category: piperidines.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Cheng, Yarui published the artcileNew insights into the function of the proteins IsiC and IsiD from Synechocystis sp. PCC 6803 under iron limitation, Quality Control of 39546-32-2, the publication is Applied Microbiology and Biotechnology (2021), 105(11), 4693-4707, database is CAplus and MEDLINE.

Iron is a common cofactor in biol. processes such as respiration, photosynthesis, and nitrogen fixation. The genes isiC and isiD encode unknown proteins, and the growth of ΔisiC and ΔisiD mutants is inhibited under iron-deficient conditions. To study the regulatory mechanisms of IsiC and IsiD during iron starvation, we carried out transcriptome and metabolome sequencing. The Kyoto Encyclopedia of Genes and Genomes (KEGG) anal. showed that the photosynthesis, nitrogen metabolism, and ABC transporter pathways play a vital role in regulating iron deficiency. Upon iron repletion, IsiC and IsiD also have a regulatory effect on these pathways. Addnl., KEGG anal. of the differential metabolites of wild type (WT) and mutants showed that they were all enriched in starch and sucrose metabolism after iron limitation. Weighted gene co-expression network anal. (WGCNA) constructed a co-expression network of differentially expressed genes with phenotypes and metabolites, and finally identified five modules. The turquoise module was pos. correlated with iron deficiency. In contrast, the WT and blue module exhibited a neg. correlation, and the mutants ΔisiC and ΔisiD were pos. correlated with the gray and brown modules, resp. WGCNA also analyzed the relationship between metabolites and phenotypes, and the green module was related to iron starvation. The co-expression network determined the hub genes and metabolites of each module. This study lays a foundation for a better understanding of cyanobacteria in response to iron deficiency.

Applied Microbiology and Biotechnology published new progress about 39546-32-2. 39546-32-2 belongs to piperidines, auxiliary class Piperidine,Amine,Amide, name is Piperidine-4-carboxamide, and the molecular formula is C6H12N2O, Quality Control of 39546-32-2.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Cai, Dong published the artcileExploring new structural features of the 18β-glycyrrhetinic acid scaffold for the inhibition of anaplastic lymphoma kinase, Application of Piperidine-4-carboxamide, the publication is Molecules (2019), 24(19), 3631pp., database is CAplus and MEDLINE.

Novel 18β-glycyrrhetinic acid derivatives possessing a carbamate moiety I [R = 4-ClC₆H₄, 3,4-di-ClC₆H₃, 4-Cl-3-CF₃C₆H₃, etc.; R¹ = OH, morpholino] and structurally similar ester derivatives II [R² = 4-ClC₆H₄CH₂, (4-methylpiperazin-1-yl)methyl, (4-formyl-1-piperidyl)methyl, etc.] were developed and evaluated for their efficacy as antitumor inhibitors. In the cellular assays, most of the N-substituted carbamate derivatives I at the C3-position exhibited potent activities. The results of SAR investigation revealed that the introduction of the morpholine group at the C30-COOH led to a significant loss of the inhibitory potency. Among the ester derivatives, the ester group at C3-position also determined a noticeable reduction in the efficacy. Compound I [R = 3-CF₃C₆H₄; R¹ = OH] exhibited the most prominent antiproliferative activity against six human cancer cells (A549, HT29, HepG2, MCF-7, PC-3, and Karpas299). Furthermore, compound I [R = 3-CF₃C₆H₄; R¹ = OH] exerted a moderate inhibiting effect on the ALK. The results of mol. docking analyses suggested that it could bind well to the active site of the receptor ALK, which was consistent with the biol. data. These results might inspire further structural optimization of 18β-glycyrrhetinic acid aiming at the development of potent antitumor agents. The structures I [R = 4-ClC₆H₄, 4-BrC₆H₄, 4-FC₆H₄, 3-CF₃C₆H₄, 4-CF₃OC₆H₄; R¹ = morpholino] were studied by X-ray crystallog. analyses.

Molecules published new progress about 39546-32-2. 39546-32-2 belongs to piperidines, auxiliary class Piperidine,Amine,Amide, name is Piperidine-4-carboxamide, and the molecular formula is C6H12N2O, Application of Piperidine-4-carboxamide.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Wu, Qifan published the artcileDiscovery of Novel Piperidinylthiazole Derivatives As Broad-Spectrum Fungicidal Candidates, Category: piperidines, the publication is Journal of Agricultural and Food Chemistry (2019), 67(5), 1360-1370, database is CAplus and MEDLINE.

Oxathiapiprolin is one of the best active fungicides discovered for oomycetes control. To develop a fungicide candidate with a broad spectrum of activity, 22 new piperidinylthiazole derivatives were designed and synthesized. Compound (I) showed the best activity against Pseudoperonospora cubensis (Berk. et Curt.) Rostov and Phytophthora infestans in vivo with 100% and 80% of inhibition, resp., at 1 mg/L, and 72.87% of field efficacy against P. cubensis at 1 g ai/667 m² validated these results. Compound (II) exhibited a broad spectrum of excellent activity against Sclerotinia sclerotiorum with EC₅₀ = 0.30 mg/L (>10 times more active than oxathiapiprolin and azoxystrobin in vitro), good activity against Botrytis cinerea, Cercospora arachidicola, and Gibberella zeae with EC₅₀ of 14.54, 5.57, and 14.03 mg/L in vitro and against P. cubensis and P. infestans with 60% and 30% inhibition rates, resp., at 1 mg/L in vivo. Mode of action studies by RNA sequencing anal. discovered oxysterol-binding protein (OSBP), chitin synthase (CHS1), and (1,3)-β-glucan synthase (FKS2) as the potent target of II against S. sclerotiorum. Quenching studies validated that OSBP was the same target of both II and oxathiapiprolin; it was quenched by both of them. Our studies discovered isothiazole-containing piperidinylthiazole as an OSBP target-based novel lead for fungicide development.

Journal of Agricultural and Food Chemistry published new progress about 39546-32-2. 39546-32-2 belongs to piperidines, auxiliary class Piperidine,Amine,Amide, name is Piperidine-4-carboxamide, and the molecular formula is C11H8O3, Category: piperidines.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Wu, Qi-Fan published the artcileDesign, synthesis and fungicidal activity of isothiazole-thiazole derivatives, Related Products of piperidines, the publication is RSC Advances (2018), 8(69), 39593-39601, database is CAplus and MEDLINE.

3,4-Dichloroisothiazoles can induce systemic acquired resistance (SAR) to enhance plant resistance against a subsequent pathogen attack, and oxathiapiprolin exhibits excellent anti-fungal activity against oomycetes targeting at the oxysterol-binding protein. To discover novel chems. with systemic acquired resistance and fungicidal activity, 21 novel isothiazole-thiazole derivatives were designed, synthesized and characterized according to the active compound derivatization method. Compound 6u, with EC₅₀ values of 0.046 mg L^-1 and 0.20 mg L^-1 against Pseudoperonospora cubensis (Berk. et Curt.) Rostov and Phytophthora infestans in vivo, might act at the same target as oxysterol binding protein (PcORP1) of oxathiapiprolin; this result was validated by cross-resistance and mol. docking studies. The expression of the systemic acquired resistance gene pr1 was significantly up-regulated after treating with compound 6u for 24 h (43-fold) and 48 h (122-fold). These results can help the development of isothiazole-thiazole-based novel fungicides.

RSC Advances published new progress about 39546-32-2. 39546-32-2 belongs to piperidines, auxiliary class Piperidine,Amine,Amide, name is Piperidine-4-carboxamide, and the molecular formula is C19H22BNO5, Related Products of piperidines.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Tang, Kai published the artcileStructure-based design, synthesis and biological evaluation of aminopyrazines as highly potent, selective, and cellularly active allosteric SHP2 inhibitors, Computed Properties of 39546-32-2, the publication is European Journal of Medicinal Chemistry (2022), 114106, database is CAplus and MEDLINE.

Src homol.-2-containing protein tyrosine phosphatase 2 (SHP2) encoded by the proto-oncogene PTPN11 is the first identified non-receptor protein tyrosine phosphatase. SHP2 dysregulation contributes to the pathogenesis of different cancers, making SHP2 a promising therapeutic target for cancer therapy. In this article, authors report the structure-guided design based on the well-characterized SHP2 inhibitor SHP099, extensive structure-activity relationship studies (SARs) of aminopyrazines, biochem. characterization and cellular potency. These medicinal chem. efforts lead to the discovery of the lead compound TK-453 I, which potently inhibits SHP2 (SHP2WT IC₅₀ = 0.023μM, ΔTm = 7.01°C) in a reversible and noncompetitive manner. Compound I exhibits high selectivity over SHP2PTP, SHP1 and PTP1B, and may bind at the “tunnel” allosteric site of SHP2 as SHP099. As the key pharmacophore, the aminopyrazine scaffold not only reorganizes the cationic-π stacking interaction with R111 via the novel hydrogen bond interaction between the S atom of thioether linker and T219, but also mediates a hydrogen bond with E250. In vitro studies indicate that I inhibits proliferation of HeLa, KYSE-70 and THP-1 cells moderately and induces apoptosis of Hela cells. Further mechanistic studies suggest that I can decrease the phosphorylation levels of AKT and Erk1/2 in HeLa and KYSE-70 cells.

European Journal of Medicinal Chemistry published new progress about 39546-32-2. 39546-32-2 belongs to piperidines, auxiliary class Piperidine,Amine,Amide, name is Piperidine-4-carboxamide, and the molecular formula is C7H13BN2O2, Computed Properties of 39546-32-2.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem