Tag: 100-200

Bryan, Marian C.; Drobnick, Joy; Gobbi, Alberto; Kolesnikov, Aleksandr; Chen, Yongsheng; Rajapaksa, Naomi; Ndubaku, Chudi; Feng, Jianwen; Chang, Willy; Francis, Ross; Yu, Christine; Choo, Edna F.; DeMent, Kevin; Ran, Yingqing; An, Le; Emson, Claire; Huang, Zhiyu; Sujatha-Bhaskar, Swathi; Brightbill, Hans; DiPasquale, Antonio; Maher, Jonathan; Wai, John; McKenzie, Brent S.; Lupardus, Patrick J.; Zarrin, Ali A.; Kiefer, James R. published an article in Journal of Medicinal Chemistry. The title of the article was 《Development of Potent and Selective Pyrazolopyrimidine IRAK4 Inhibitors》.Related Products of 39546-32-2 The author mentioned the following in the article:

A series of pyrazolopyrimidine inhibitors of IRAK4 were developed from a high-throughput screen (HTS). Modification of an HTS hit led to a series of bicyclic heterocycles with improved potency and kinase selectivity but lacking sufficient solubility to progress in vivo. Structure-based drug design, informed by cocrystal structures with the protein and small-mol. crystal structures, yielded a series of dihydrobenzofurans. This semisatd. bicycle provided superior druglike properties while maintaining excellent potency and selectivity. Improved physicochem. properties allowed for progression into in vivo experiments, where lead mols. exhibited low clearance and showed target-based inhibition of IRAK4 signaling in an inflammation-mediated PK/PD mouse model. In the experiment, the researchers used many compounds, for example, Piperidine-4-carboxamide(cas: 39546-32-2Related Products of 39546-32-2)

Piperidine-4-carboxamide(cas: 39546-32-2) belongs to anime. Examples of direct uses of amines and their salts are as corrosion inhibitors in boilers and in lubricating oils (morpholine), as antioxidants for rubber and roofing asphalt (diarylamines), as stabilizers for cellulose nitrate explosives (diphenylamine), as protectants against damage from gamma radiation (diarylamines), as developers in photography (aromatic diamines), as flotation agents in mining, as anticling and waterproofing agents for textiles, as fabric softeners, in paper coating, and for solubilizing herbicides.Related Products of 39546-32-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Recommanded Product: TriacetonamineOn September 5, 2020 ,《Diatomite supported hierarchical 2D CoNi3O4 nanoribbons as highly efficient peroxymonosulfate catalyst for atrazine degradation》 was published in Applied Catalysis, B: Environmental. The article was written by Dong, Xiongbo; Ren, Bangxing; Zhang, Xiangwei; Liu, Xiaorui; Sun, Zhiming; Li, Chunquan; Tan, Ye; Yang, Shanshan; Zheng, Shuilin; Dionysiou, Dionysios D.. The article contains the following contents:

Reactive oxygen radicals generated by peroxymonosulfate (PMS) activation exhibit great potential to treat refractory pollutants of emerging concern; however, mass production of efficient, cost-effective catalysts for PMS activation is a long-term goal for its widespread practical application. A CoNi3O4/diatomite hybrid was prepared via vertically oriented growth of two dimensional (2D) CoNi3O4 nanoribbons of at. layer-thickness on a cost-effective diatomite template. Distinct from stacked CoNi3O4, the CoNi3O4/diatomite composite has abundant exposed edges, sharp corners, and open diffusion channels. Abundant exposed edges and sharp corners create more open space and active sites for PMS activation. Open diffusion channels accelerate PMS and pollutants migration. Such properties provide CoNi3O4/diatomite hybrid excellent PMS activation efficiency. Sulfate radical played the dominant role in atrazine degradation, and superoxide radical contributed to reversible redox cycle of Co2+/Co3+ and Ni2+/Ni3+. This work provided a strategy for cost-effective mass production of Fenton-like 2D catalysts. In the experiment, the researchers used Triacetonamine(cas: 826-36-8Recommanded Product: Triacetonamine)

Triacetonamine(cas: 826-36-8) is a member of piperidine. Piperidine is ubiquitous structural motif widely occurred in diverse synthetically and naturally occurring bioactive molecules. Piperidines are an immensely important class of compounds medicinally: the piperidine ring is the most common heterocyclic subunit among FDA approved drugs.Recommanded Product: Triacetonamine

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

HPLC of Formula: 826-36-8On March 15, 2021, Ye, Jian; Dai, Jiangdong; Wang, Lulu; Li, Chunxiang; Yan, Yongsheng; Yang, Guoyu published an article in Journal of Colloid and Interface Science. The article was 《Investigation of catalytic self-cleaning process of multiple active species decorated macroporous PVDF membranes through peroxymonosulfate activation》. The article mentions the following:

Currently, carbon-based catalysts integrated with macroporous catalytic membrane have aroused considerable attention for environmental remediation because of its practicability and high efficiency. Herein, nitrogen doped carbon nanotube hybrids (Fe-Co@NC-CNTs) decorated with multiple active species (Fe3Co7/CoFe2O4@Fe/Co-N-C) were designed through N-mol. assisted pyrolysis of bimetallic (Fe/Co) metal-organic frameworks, and then immobilized on poly(vinylidene fluoride) (PVDF) membrane to construct macroporous Fe-Co@NC-CNTs/PVDF catalytic membrane via directional freezing technique, where active sites were efficiently exposed for oxidants and target pollutants. As expected, Fe-Co@NC-CNTs/PVDF membrane successfully achieved almost 100% bisphenol A (BPA) degradation after 40 min via PMS activation, which was significantly overperformed the majority of conventional carbon-based catalysts. Besides, we found that Fe-Co@NC-CNTs/PVDF membrane not only exhibited ideal catalytic and self-cleaning property in humic acid (HA)-BPA coexistence system, but also maintained the excellent reusability and ultrahigh water flux (10464.45 L m-2 h-1) even after 5 cycles. Notably, in EPR anal. and quenching experiments, it was found that sulfate radicals (SO4·- and ·OH) and singlet oxygen (1O2) participated the degradation process while 1O2 made a major contribution. More significantly, this study is very meaningful for the development of novel catalytic self-cleaning membranes with PMS activation. The experimental part of the paper was very detailed, including the reaction process of Triacetonamine(cas: 826-36-8HPLC of Formula: 826-36-8)

Triacetonamine(cas: 826-36-8) is a member of piperidine. Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Hence, continuous efforts have been made to develop convenient methods to prepare piperidine derivatives.HPLC of Formula: 826-36-8

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

HPLC of Formula: 39546-32-2On March 1, 2021, Mizukawa, Yuki; Ikegami-Kawai, Mayumi; Horiuchi, Masako; Kaiser, Marcel; Kojima, Masayoshi; Sakanoue, Seiki; Miyagi, Seiya; Nanga Chick, Christian; Togashi, Hiroyuki; Tsubuki, Masayoshi; Ihara, Masataka; Usuki, Toyonobu; Itoh, Isamu published an article in Bioorganic & Medicinal Chemistry. The article was 《Quest for a potent antimalarial drug lead: Synthesis and evaluation of 6,7-dimethoxyquinazoline-2,4-diamines》. The article mentions the following:

Quinazolines have long been known to exert varied pharmacol. activities that make them suitable for use in treating hypertension, viral infections, tumors, and malaria. Since 2014, author’s have synthesized approx. 150 different 6,7-dimethoxyquinazoline-2,4-diamines and evaluated their antimalarial activity via structure-activity relationship studies. Here, author’s summarize the results and report the discovery of 6,7-dimethoxy-N4-(1-phenylethyl)-2-(pyrrolidin-1-yl)quinazolin-4-amine, which exhibits high antimalarial activity as a promising antimalarial drug lead. The results came from multiple reactions, including the reaction of Piperidine-4-carboxamide(cas: 39546-32-2HPLC of Formula: 39546-32-2)

Piperidine-4-carboxamide(cas: 39546-32-2) belongs to anime. The reaction of alkyl halides, R―X, where X is a halogen, or analogous reagents with ammonia (or amines) is useful with certain compounds. Not all alkyl halides are effective reagents; the reaction is sluggish with secondary alkyl groups and fails with tertiary ones. Its usefulness is largely confined to primary alkyl halides (those having two hydrogen atoms on the reacting site).HPLC of Formula: 39546-32-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Related Products of 1690-72-8On October 31, 1990 ,《Synthesis and biological activity of 1,2,4-oxadiazole derivatives: highly potent and efficacious agonists for cortical muscarinic receptors》 appeared in Journal of Medicinal Chemistry. The author of the article were Street, Leslie J.; Baker, Raymond; Book, Tracey; Kneen, Clare O.; MacLeod, Angus M.; Merchant, Kevin J.; Showell, Graham A.; Saunders, John; Herbert, Richard H.. The article conveys some information:

The synthesis and biochem. evaluation of novel 1,2,4-oxadiazole-based muscarinic agonists which can readily penetrate into the CNS is reported. Efficacy and binding of these compounds are markedly influenced by the structure and physicochem. properties of the cationic head group. In a series of azabicyclic ligands efficacy and affinity are influenced by the size of the surface area presented to the receptor at the active site, and the degree of conformational flexibility. The exo-1-azanorbornane I represents the optimum arrangement, and this compound is one of the most efficacious and potent muscarinic agonists known. In a series of isoquinuclidine-based muscarinic agonists efficacy and affinity are influenced by the geometry between the cationic head group and H-bond acceptor pharmacophore and steric bulk in the vicinity of the base. The anti configuration represented by II is optimal for muscarinic activity. Ligands with pKa <6.5 show poor binding to the muscarinic receptor as exemplified by the diazabicyclic derivative III. In the experiment, the researchers used Methyl 1-methylpiperidine-3-carboxylate(cas: 1690-72-8Related Products of 1690-72-8)

Methyl 1-methylpiperidine-3-carboxylate(cas: 1690-72-8) is a member of piperidine. Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Hence, continuous efforts have been made to develop convenient methods to prepare piperidine derivatives.Related Products of 1690-72-8

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Design, synthesis and biological evaluation of imidazo[1,5-a]pyrazin-8(7H)-one derivatives as BRD9 inhibitors》 was written by Zheng, Peiyuan; Zhang, Jian; Ma, Hui; Yuan, Xinrui; Chen, Pan; Zhou, Jinpei; Zhang, Huibin. HPLC of Formula: 39546-32-2 And the article was included in Bioorganic & Medicinal Chemistry on April 1 ,2019. The article conveys some information:

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. In the experimental materials used by the author, we found Piperidine-4-carboxamide(cas: 39546-32-2HPLC of Formula: 39546-32-2)

Piperidine-4-carboxamide(cas: 39546-32-2) belongs to anime. Examples of direct uses of amines and their salts are as corrosion inhibitors in boilers and in lubricating oils (morpholine), as antioxidants for rubber and roofing asphalt (diarylamines), as stabilizers for cellulose nitrate explosives (diphenylamine), as protectants against damage from gamma radiation (diarylamines), as developers in photography (aromatic diamines), as flotation agents in mining, as anticling and waterproofing agents for textiles, as fabric softeners, in paper coating, and for solubilizing herbicides.HPLC of Formula: 39546-32-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Safety of 2-(Piperidin-4-yl)ethanolIn 2012 ,《Investigations of primary and secondary amine carbamate stability by 1H NMR spectroscopy for post combustion capture of carbon dioxide》 appeared in Journal of Chemical Thermodynamics. The author of the article were Fernandes, Debra; Conway, William; Burns, Robert; Lawrance, Geoffrey; Maeder, Marcel; Puxty, Graeme. The article conveys some information:

Carbamate formation is one of the major chem. reactions that can occur in solution in the capture of CO2 by amine-based solvents, and carbamate formation makes a significant enthalpy contribution to the absorption-desorption of CO2 that occurs in the absorber/stripper columns of the PCC process. Consequently, the formation of carbamates of selected series of primary and secondary amines over the temperature range (288 to 318) K has been investigated by equilibrium 1H NMR studies, and the stability constants (K 9) for the equilibrium:RNH2+HCO3-⇄K9RNHCOO-+H2Oare reported. van’t Hoff analyses have resulted in standard molar enthalpies, ΔHmo, and entropies, ΔSmo, of carbamate formation. A ΔHmo-ΔSmo plot generates a linear correlation for carbamate formation (providing a mean standard molar free energy, ΔGmo, for carbamate formation of about -7 kJ · mol-1), and this relationship helps provide a guide to the selection of an amine(s) solvent for CO2 capture, in terms of enthalpy considerations. A linear ΔHmo-ΔSmo plot also occurs for carbamate protonation. The formation of the carbamates has been correlated with systematic changes in composition and structure, and steric effects have been identified by comparing mol. geometries obtained using d. functional B3LYP/6-311++G(d,p) calculations Trends in steric effects have been identified in the series of compounds monoethanolamine (MEA), 1-amino-2-propanol, 2-amino-1-propanol (AP) and 2-amino-2-methyl-1-propanol (AMP). In the case of 2-piperidinemethanol, 2-piperidineethanol and 3-piperidinemethanol, strong intramol. hydrogen bonding is shown to be the likely cause for lack of carbamate formation, and in the ring systems of pyrrolidine, morpholine, piperidine and thiomorpholine trends in carbamate formation (as given by K 9) have been correlated with the internal ring angle at the amine nitrogen, as well as the planarity of the environment around the nitrogen atom. In the part of experimental materials, we found many familiar compounds, such as 2-(Piperidin-4-yl)ethanol(cas: 622-26-4Safety of 2-(Piperidin-4-yl)ethanol)

2-(Piperidin-4-yl)ethanol(cas: 622-26-4) have been used as an intermediate in the synthetic preparation of cellular-active allosteric inhibitors of FAKSafety of 2-(Piperidin-4-yl)ethanol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2022,Wang, Chang; Qu, Lunjun; Chen, Xiaohong; Zhou, Qian; Yang, Yan; Zheng, Yan; Zheng, Xian; Gao, Liang; Hao, Jinqiu; Zhu, Lingyun; Pi, Bingxue; Yang, Chaolong published an article in Advanced Materials (Weinheim, Germany). The title of the article was 《Poly(arylene piperidine) Quaternary Ammonium Salts Promoting Stable Long-Lived Room-Temperature Phosphorescence in Aqueous Environment》.SDS of cas: 1445-73-4 The author mentioned the following in the article:

Room-temperature phosphorescence (RTP) materials have garnered considerable research attention owing to their excellent luminescence properties and potential application prospects in anti-counterfeiting, information storage, and optoelectronics. However, several RTP systems are extremely sensitive to humidity, and consequently, the realization of long-lived RTP in water remains a formidable challenge. Herein, a feasible and effective strategy is presented to achieve long-lived polymeric RTP systems, even in an aqueous environment, through doping of synthesized polymeric phosphor PBHDB into a poly(Me methacrylate) (PMMA) matrix. Compared to the precursor polymer PBN and organic mol. HDBP, a more rigid polymer microenvironment and electrostatic interaction are formed between the PMMA matrix and polymer PBHDB, which effectively reduce the nonradiative decay rate of triplet excitons and dramatically increase the phosphorescence intensity. Specifically, the phosphorescence lifetime of the PBHDB@PMMA film (1258.62 ms) is much longer than those of PBN@PMMA (674.20 ms) and HDBP@PMMA (1.06 ms). Most importantly, a bright-green afterglow can be observed after soaking the PBHDB@PMMA film in water for more than a month. The excellent water resistance and reversible response properties endow these systems with promising potential for dynamic information encryption even in water.1-Methyl-4-piperidone(cas: 1445-73-4SDS of cas: 1445-73-4) was used in this study.

1-Methyl-4-piperidone(cas: 1445-73-4) is a member of piperidine. Piperidine is ubiquitous structural motif widely occurred in diverse synthetically and naturally occurring bioactive molecules. Piperidines are an immensely important class of compounds medicinally: the piperidine ring is the most common heterocyclic subunit among FDA approved drugs.SDS of cas: 1445-73-4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Misal Castro, Luis C.; Sultan, Ibrahim; Nishi, Kohei; Tsurugi, Hayato; Mashima, Kazushi published their research in Journal of Organic Chemistry in 2021. The article was titled 《Direct Synthesis of Indoles from Azoarenes and Ketones with Bis(neopentylglycolato)diboron Using 4,4′-Bipyridyl as an Organocatalyst》.Safety of 1-Methyl-4-piperidone The article contains the following contents:

Multifunctionalized indole derivatives were prepared by reducing azoarenes in the presence of ketones and bis(neopentylglycolato)diboron (B2nep2) with a catalytic amount of 4,4′-bipyridyl under neutral reaction conditions, where 4,4′-bipyridyl acted as an organocatalyst to activate the B-B bond of B2nep2 and form N,N’-diboryl-1,2-diarylhydrazines as a key intermediate. Further reaction of N,N’-diboryl-1,2-diarylhydrazines with ketones afforded N-vinyl-1,2-diarylhydrazines, which rearranged to the corresponding indoles via the Fischer indole mechanism. This organocatalytic system was applied to diverse alkyl cyclic ketones, dialkyl, and alkyl/aryl ketones, including heteroatoms. Me alkyl ketones gave the corresponding 2-methyl-3-substituted indoles in a regioselective manner. This protocol allowed us to expand the preparation of indoles having high compatibility with not only electron-donating and electron-withdrawing groups but also N- and O-protecting functional groups. In the part of experimental materials, we found many familiar compounds, such as 1-Methyl-4-piperidone(cas: 1445-73-4Safety of 1-Methyl-4-piperidone)

1-Methyl-4-piperidone(cas: 1445-73-4) is a member of piperidine. Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Hence, continuous efforts have been made to develop convenient methods to prepare piperidine derivatives.Safety of 1-Methyl-4-piperidone

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Design, synthesis and biological activities of piperidine-spirooxadiazole derivatives as α7 nicotinic receptor antagonists》 was published in European Journal of Medicinal Chemistry in 2020. These research results belong to Zhang, Han; He, Xiaomeng; Wang, Xintong; Yu, Bo; Zhao, Siqi; Jiao, Peili; Jin, Hongwei; Liu, Zhenming; Wang, KeWei; Zhang, Liangren; Zhang, Lihe. Category: piperidines The article mentions the following:

7 Nicotinic acetylcholine receptors (nAChRs) expressed in the nervous and immune systems was suggested to play important roles in the control of inflammation. However, the lack of antagonist tools specifically inhibiting α7 nAChR impedes the validation of the channel as therapeutic target. To discover a selective α7 antagonist, a pharmacophore-based virtual screening and identified a piperidine-spirooxadiazole derivative T761-0184 that acts as a α7 antagonist. A series of novel piperidine-spirooxadiazole derivatives were subsequently synthesized and evaluated using two-electrode voltage clamp (TEVC) assay in Xenopus oocytes. Lead compounds from two series inhibited α7 with their IC50 values ranging from 3.3μM to 13.7μM. Compound 3-(4-Bromophenyl)-8-methyl-1-oxa-2,4,8-triazaspiro[4.5]dec-2-ene exhibited α7 selectivity over other α4β2 and α3β4 nAChR subtypes. The anal. of structure-activity relationship (SAR) provides valuable insights for further development of selective α7 nAChR antagonists. In the experiment, the researchers used 1-Methyl-4-piperidone(cas: 1445-73-4Category: piperidines)

1-Methyl-4-piperidone(cas: 1445-73-4) is a member of piperidine. Piperidine is ubiquitous structural motif widely occurred in diverse synthetically and naturally occurring bioactive molecules. Piperidines are an immensely important class of compounds medicinally: the piperidine ring is the most common heterocyclic subunit among FDA approved drugs.Category: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem