Day: September 15, 2022

Piperidine is an organic compound with the molecular formula (CH2)5NH. This heterocyclic amine consists of a six-membered ring containing five methylene bridges (–CH2–) and one amine bridge (–NH–). 2403-88-5, formula is C9H19NO, Name is 2,2,6,6-Tetramethyl-4-piperidinol. It is a colorless liquid with an odor described as objectionable, and typical of amines. Safety of 2,2,6,6-Tetramethyl-4-piperidinol.

Asif, Abdul Hannan;Rafique, Nasir;Hirani, Rajan Arjan Kalyan;Wu, Hong;Shi, Lei;Sun, Hongqi research published 《 Heterogeneous activation of peroxymonosulfate by Co-doped Fe₂O₃ nanospheres for degradation of p-hydroxybenzoic acid》, the research content is summarized as follows. Environmental remediation has become more effective when using nanotechnologies. In this study, iron oxide (α-Fe₂O₃) nanospheres with different cobalt doping levels (xCo-Fe₂O₃) were synthesized and applied in the heterogeneous activation of peroxymonosulfate (PMS) for the degradation of p-hydroxybenzoic acid (p-HBA). The catalyst (3Co-Fe₂O₃) with 3% Co doping exhibits the best performance for PMS activation, possibly because of the larger sp. surface area and the tailored catalyst surface as confirmed by XPS. Reaction parameters were investigated to optimize the degradation efficiency. The metal ions leaching tests confirmed the higher stability of the catalyst, thanks to the leaching suppression by the doping of Co²⁺. The main contribution of free radicals (SO•^–₄ and •OH) was confirmed by ESR (EPR) spectra, whereas partial contribution of oxygen anions and singlet oxygen (O•^–₂, ¹O₂) was observed during the quenching tests. Finally, a radical based degradation mechanism was proposed for the removal of p-HBA. It is expected to open up a novel perspective for the application of iron oxide as a potential catalyst for the removal of emerging contaminants.

Safety of 2,2,6,6-Tetramethyl-4-piperidinol, 2,2,6,6-Tetramethyl-4-piperidinol(TEMPO) is a useful research compound. Its molecular formula is C9H19NO and its molecular weight is 157.25 g/mol. The purity is usually 95%.
TEMPO is an intermediate used in the preparation of Piperidinyloxy free radical derivatives.
TEMPO is an organic compound that acts as a radical scavenger. It is stable in the presence of water and air and can be used for the inhibition of bacterial growth. TEMPO reacts with reactive intermediates to form non-reactive substances and terminate chain reactions. This process is optimal at temperatures between 0°C and 40°C and pH values between 3.5 and 7.5. TEMPO has been shown to inhibit the growth of bacteria by reacting with reactive molecules such as amines, chlorides, or low energy radicals in aqueous solution. TEMPO also has genotoxic activity that inhibits DNA synthesis in bacterial cells through oxidation of guanine residues on DNA molecules., 2403-88-5.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Piperidine the name comes from the genus name Piper, which is the Latin word for pepper. 5382-16-1, formula is C5H11NO, Name is 4-Piperidinol. Although piperidine is a common organic compound, it is best known as a representative structure element within many pharmaceuticals and alkaloids, such as natural-occurring solenopsins. Quality Control of 5382-16-1.

Armani, Elisabetta;Capaldi, Carmelida;Bagnacani, Valentina;Saccani, Francesca;Aquino, Giancarlo;Puccini, Paola;Facchinetti, Fabrizio;Martucci, Cataldo;Moretto, Nadia;Villetti, Gino;Patacchini, Riccardo;Civelli, Maurizio;Hurley, Chris;Jennings, Andrew;Alcaraz, Lilian;Bloomfield, Dawn;Briggs, Michael;Daly, Stephen;Panchal, Terry;Russell, Vince;Wicks, Sharon;Finch, Harry;Fitzgerald, Mary;Fox, Craig;Delcanale, Maurizio research published 《 Design, Synthesis, and Biological Characterization of Inhaled p38α/β MAPK Inhibitors for the Treatment of Lung Inflammatory Diseases》, the research content is summarized as follows. The identification of novel inhaled p38α/β mitogen-activated protein kinases (MAPK) (MAPK14/11) inhibitors suitable for the treatment of pulmonary inflammatory conditions has been described. A rational drug design approach started from the identification of a novel tetrahydronaphthalene series, characterized by nanomolar inhibition of p38α with selectivity over p38γ and p38δ isoforms. SAR optimization of 1c is outlined, where improvements in potency against p38α and ligand-enzyme dissociation kinetics led to several compounds showing pronounced anti-inflammatory effects in vitro (inhibition of TNFα release). Targeting of the defined physicochem. properties allowed the identification of compounds 3h, 4e, and 4f, which showed, upon intratracheal instillation, low plasma levels, prolonged lung retention, and anti-inflammatory effects in a rat acute model of a bacterial endotoxin-induced pulmonary inflammation. Compound 4e (I), in particular, displayed remarkable efficacy and duration of action and was selected for progression in disease models of asthma and chronic obstructive pulmonary disease (COPD).

5382-16-1, 4-Hydroxypiperidine is a molecule with a carbonyl group. It is the most active and selective CCR5 receptor antagonist that has been studied to date. 4-Hydroxypiperidine inhibits HIV infection by preventing the binding of HIV to its receptor on the surface of white blood cells, thereby preventing it from entering these cells. 4-Hydroxypiperidine also acts as an anti-inflammatory agent in chronic bronchitis patients, due to its ability to inhibit prostaglandin synthesis. The chemical ionization mass spectra of this molecule show peaks for methyl ethyl, malic acid, and hydroxyl groups. These properties make 4-hydroxypiperidine a useful candidate for drug development against inflammatory diseases and several cancers.
The molecular structure, vibrational spectra, NBO and UV-spectral analysis of 4-Hydroxypiperidine have been studied. The compounds with a substituted 4-piperidinol core have been found to be potent antagonists of the human H receptor., Quality Control of 5382-16-1

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Piperidine was first reported in 1850 by the Scottish chemist Thomas Anderson and again, independently, in 1852 by the French chemist 84358-13-4, formula is C11H19NO4, Name is 1-(tert-Butoxycarbonyl)piperidine-4-carboxylic acid. Auguste Cahours, who named it. Both of them obtained piperidine by reacting piperine with nitric acid. Product Details of C11H19NO4.

Alverez, Celeste N.;Park, Jung-Eun;Toti, Kiran S.;Xia, Yangliu;Krausz, Kristopher W.;Rai, Ganesha;Bang, Jeong K.;Gonzalez, Frank J.;Jacobson, Kenneth A.;Lee, Kyung S. research published 《 Identification of a New Heterocyclic Scaffold for Inhibitors of the Polo-Box Domain of Polo-like Kinase 1》, the research content is summarized as follows. As a mitotic-specific target widely deregulated in various human cancers, polo-like kinase 1 (Plk1) has been extensively explored for anticancer activity and drug discovery. Although multiple catalytic domain inhibitors were tested in preclin. and clin. studies, their efficacies are limited by dose-limiting cytotoxicity, mainly from off-target cross reactivity. The C-terminal noncatalytic polo-box domain (PBD) of Plk1 has emerged as an attractive target for generating new protein-protein interaction inhibitors. Here, we identified a 1-thioxo-2,4-dihydro-[1,2,4]triazolo[4,3-a]quinazolin-5(1H)-one scaffold that efficiently inhibits Plk1 PBD but not its related Plk2 and Plk3 PBDs. Structure-activity relationship studies led to multiple inhibitors having ≥10-fold higher inhibitory activity than the previously characterized Plk1 PBD-specific phosphopeptide, PLHSpT (K_d ~450 nM). In addition, S-Me prodrugs effectively inhibited mitotic progression and cell proliferation and their metabolic stability was determined These data describe a novel class of small-mol. inhibitors that offer a promising avenue for future drug discovery against Plk1-addicted cancers.

Product Details of C11H19NO4, N-BOC-piperidine-4-carboxylic acid, also known asN-Boc-isonipecotic acid , is a useful research compound. Its molecular formula is C11H19NO4 and its molecular weight is 229,28 g/mole. The purity is usually 95%.

N-Boc-isonipecotic acid is a potent antitumor agent that has been clinically shown to be effective against leukemia and lymphoma. It has potent antibacterial activity against Gram-positive bacteria such as Staphylococcus aureus and Streptococcus pyogenes. N-Boc-isonipecotic acid binds to the gyrase enzyme, which is used by these bacteria to maintain the integrity of their DNA, inhibiting protein synthesis and cell division. This drug also has anti-inflammatory properties. N-Boc-isonipecotic acid inhibits prostaglandin synthesis in cells, which may be due to its ability to inhibit the production of tumor necrosis factor α (TNFα) in macrophages., 84358-13-4.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst: C5H5N + 3 H2 → C5H10NH. 2403-88-5, formula is C9H19NO, Name is 2,2,6,6-Tetramethyl-4-piperidinol. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol. COA of Formula: C9H19NO.

Alvarez-Martin, Alba;George, John;Kaplan, Emily;Osmond, Lauren;Bright, Leah;Newsome, G. Asher;Kaczkowski, Rebecca;Vanmeert, Frederik;Kavich, Gwenaelle;Heald, Susan research published 《 Identifying VOCs in exhibition cases and efflorescence on museum objects exhibited at Smithsonian’s National Museum of the American Indian-New York》, the research content is summarized as follows. Abstract: Two mass spectrometry (MS) methods, solid-phase microextraction gas chromatog. (SPME-GC-MS) and direct anal. in real time (DART-MS), have been explored to investigate widespread efflorescence observed on exhibited objects at the Smithsonian’s National Museum of the American Indian in New York (NMAI-NY). Both methods show great potential, in terms of speed of anal. and level of information, for identifying the organic component of the efflorescence as 2,2,6,6-tetramethyl-4-piperidinol (TMP-ol) emitted by the structural adhesive (Terostat MS 937) used for exhibit case construction. The utility of DART-MS was proven by detecting the presence of TMP-ol in construction materials in a fraction of the time and effort required for SPME-GC-MS anal. In parallel, an unobtrusive SPME sampling strategy was used to detect volatile organic compounds (VOCs) accumulated in the exhibition cases. This sampling technique can be performed by collections and conservation staff at the museum and shipped to an off-site laboratory for anal. This broadens the accessibility of MS techniques to museums without access to instrumentation or inhouse anal. capabilities.

2403-88-5, 2,2,6,6-Tetramethyl-4-piperidinol(TEMPO) is a useful research compound. Its molecular formula is C9H19NO and its molecular weight is 157.25 g/mol. The purity is usually 95%.
TEMPO is an intermediate used in the preparation of Piperidinyloxy free radical derivatives.
TEMPO is an organic compound that acts as a radical scavenger. It is stable in the presence of water and air and can be used for the inhibition of bacterial growth. TEMPO reacts with reactive intermediates to form non-reactive substances and terminate chain reactions. This process is optimal at temperatures between 0°C and 40°C and pH values between 3.5 and 7.5. TEMPO has been shown to inhibit the growth of bacteria by reacting with reactive molecules such as amines, chlorides, or low energy radicals in aqueous solution. TEMPO also has genotoxic activity that inhibits DNA synthesis in bacterial cells through oxidation of guanine residues on DNA molecules., COA of Formula: C9H19NO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Piperidine is an organic compound with the molecular formula (CH2)5NH. This heterocyclic amine consists of a six-membered ring containing five methylene bridges (–CH2–) and one amine bridge (–NH–). 84358-13-4, formula is C11H19NO4, Name is 1-(tert-Butoxycarbonyl)piperidine-4-carboxylic acid. It is a colorless liquid with an odor described as objectionable, and typical of amines. Reference of 84358-13-4.

AlNajjar, Yasmeen T.;Gabr, Moustafa;ElHady, Ahmed K.;Salah, Mohamed;Wilms, Gerrit;Abadi, Ashraf H.;Becker, Walter;Abdel-Halim, Mohammad;Engel, Matthias research published 《 Discovery of novel 6-hydroxybenzothiazole urea derivatives as dual Dyrk1A/α-synuclein aggregation inhibitors with neuroprotective effects》, the research content is summarized as follows. A role of Dyrk1A in the progression of Down syndrome-related Alzheimer’s disease (AD) is well supported. However, the involvement of Dyrk1A in the pathogenesis of Parkinson’s disease (PD) was much less studied, and it is not clear whether it would be promising to test Dyrk1A inhibitors in relevant PD models. Herein, we modified our previously published 1-(6-hydroxybenzo[d]thiazol-2-yl)-3-phenylurea scaffold of Dyrk1A inhibitors to obtain a new series of analogs with higher selectivity for Dyrk1A on the one hand, but also with a novel, addnl. activity as inhibitors of α-synuclein (α-syn) aggregation, a major pathogenic hallmark of PD. The Ph acetamide derivative b27 displayed the highest potency against Dyrk1A with an IC₅₀ of 20 nM and high selectivity over closely related kinases. Furthermore, b27 was shown to successfully target intracellular Dyrk1A and to inhibit SF3B1 phosphorylation in HeLa cells with an IC₅₀ of 690 nM. In addition, two compounds among the Dyrk1A inhibitors, b1 and b20, also suppressed the aggregation of α-synuclein (α-syn) oligomers (with IC₅₀ values of 10.5μM and 7.8μM, resp.). Both compounds but not the Dyrk1A reference inhibitor harmine protected SH-SY5Y neuroblastoma cells against α-syn-induced cytotoxicity, with b20 exhibiting a higher neuroprotective effect. Compound b1 and harmine were more efficient in protecting SH-SY5Y cells against 6-hydroxydopamine-induced cell death, an effect that was previously correlated to Dyrk1A inactivation in cells but not yet verified using chem. inhibitors. The presented dual inhibitors exhibited a novel activity profile encouraging for further testing in neurodegenerative disease models.

Reference of 84358-13-4, N-BOC-piperidine-4-carboxylic acid, also known asN-Boc-isonipecotic acid , is a useful research compound. Its molecular formula is C11H19NO4 and its molecular weight is 229,28 g/mole. The purity is usually 95%.

N-Boc-isonipecotic acid is a potent antitumor agent that has been clinically shown to be effective against leukemia and lymphoma. It has potent antibacterial activity against Gram-positive bacteria such as Staphylococcus aureus and Streptococcus pyogenes. N-Boc-isonipecotic acid binds to the gyrase enzyme, which is used by these bacteria to maintain the integrity of their DNA, inhibiting protein synthesis and cell division. This drug also has anti-inflammatory properties. N-Boc-isonipecotic acid inhibits prostaglandin synthesis in cells, which may be due to its ability to inhibit the production of tumor necrosis factor α (TNFα) in macrophages., 84358-13-4.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Piperidine is an organic compound with the molecular formula (CH2)5NH. This heterocyclic amine consists of a six-membered ring containing five methylene bridges (–CH2–) and one amine bridge (–NH–). 2403-88-5, formula is C9H19NO, Name is 2,2,6,6-Tetramethyl-4-piperidinol. It is a colorless liquid with an odor described as objectionable, and typical of amines. Application In Synthesis of 2403-88-5.

Aiba, Motohiro;Koizumi, Take-aki;Futamura, Michinari;Okamoto, Kazuaki;Yamanaka, Motoshi;Ishigaki, Yuzo;Oda, Mitsuo;Ooka, Chihiro;Tsuruoka, Ayuko;Takahashi, Akira;Otsuka, Hideyuki research published 《 Use of Bis(2,2,6,6-tetramethylpiperidin-1-yl)trisulfide as a Dynamic Covalent Bond for Thermally Healable Cross-Linked Polymer Networks》, the research content is summarized as follows. Dynamic covalent bonds (DCBs), which can undergo reversible cleavage and reformation upon exposure to readily useable stimuli, have attracted dramatic attention, but the library of such bonds still remains to be developed. Herein, we report mol. structures, dynamic behaviors, and healability of bis(2,2,6,6-tetramethylpiperidin-1-yl)trisulfide (BITEMPS-S3) to compare with its disulfide analog (BITEMPS-S2) exchanged at moderate temperature Unsym. cleavage of trisulfide linkage induced relatively rapid disproportionation to di- and tetrasulfide derivatives In the bulk, poly(hexyl methacrylate) networks partially containing the BITEMPS-S3 moiety as a crosslinking point afforded nearly quant. damage healability only by simple hot pressing at 110°C under mild pressure. A slightly higher healability of BITEMPS-S2 compared to that of BITEMPS-S3 would be due to the differences in the chain-transfer reaction for the trisulfide linkage during free-radical polymerization rather than thermal exchangeability of the BITEMPS-S3 moiety. Therefore, not only BITEMPS-S2 but also BITEMPS-S3 should be regarded as one of DCBs triggered upon exposure to mild external stimuli.

2403-88-5, 2,2,6,6-Tetramethyl-4-piperidinol(TEMPO) is a useful research compound. Its molecular formula is C9H19NO and its molecular weight is 157.25 g/mol. The purity is usually 95%.
TEMPO is an intermediate used in the preparation of Piperidinyloxy free radical derivatives.
TEMPO is an organic compound that acts as a radical scavenger. It is stable in the presence of water and air and can be used for the inhibition of bacterial growth. TEMPO reacts with reactive intermediates to form non-reactive substances and terminate chain reactions. This process is optimal at temperatures between 0°C and 40°C and pH values between 3.5 and 7.5. TEMPO has been shown to inhibit the growth of bacteria by reacting with reactive molecules such as amines, chlorides, or low energy radicals in aqueous solution. TEMPO also has genotoxic activity that inhibits DNA synthesis in bacterial cells through oxidation of guanine residues on DNA molecules., Application In Synthesis of 2403-88-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Piperidine was first reported in 1850 by the Scottish chemist Thomas Anderson and again, independently, in 1852 by the French chemist 84358-13-4, formula is C11H19NO4, Name is 1-(tert-Butoxycarbonyl)piperidine-4-carboxylic acid. Auguste Cahours, who named it. Both of them obtained piperidine by reacting piperine with nitric acid. Product Details of C11H19NO4.

Adu-Ampratwum, Daniel;Pan, Yuhan;Koneru, Pratibha C.;Antwi, Janet;Hoyte, Ashley C.;Kessl, Jacques;Griffin, Patrick R.;Kvaratskhelia, Mamuka;Fuchs, James R.;Larue, Ross C. research published 《 Identification and Optimization of a Novel HIV-1 Integrase Inhibitor》, the research content is summarized as follows. Human immunodeficiency virus-1 (HIV-1) is the causative agent of acquired immunodeficiency syndrome (AIDS). HIV-1, like all retroviruses, stably integrates its vDNA copy into host chromatin, a process allowing for permanent infection. This essential step for HIV-1 replication is catalyzed by viral integrase (IN) and aided by cellular protein LEDGF/p75. In addition, IN is also crucial for proper virion maturation as it interacts with the viral RNA genome to ensure encapsulation of ribonucleoprotein complexes within the protective capsid core. These key functions make IN an attractive target for the development of inhibitors with various mechanisms of action. We conducted a high-throughput screen (HTS) of ~370,000 compounds using a homogeneous time-resolved fluorescence-based assay capable of capturing diverse inhibitors targeting multifunctional IN. Our approach revealed chem. scaffolds containing diketo acid moieties similar to IN strand transfer inhibitors (INSTIs) as well as novel compounds distinct from all current IN inhibitors including INSTIs and allosteric integrase inhibitors (ALLINIs). Specifically, our HTS resulted in the discovery of compound I, with a novel IN inhibitor scaffold amenable for chem. modification. Its more potent derivative II similarly inhibited catalytic activities of WT and mutant INs containing archetypical INSTI- and ALLINI-derived resistant substitutions. Further SAR-based optimization resulted in compound III with an antiviral EC₅₀ of ~58μM and a selectivity index of >8500. Thus, our studies identified a novel small-mol. scaffold for inhibiting HIV-1 IN, which provides a promising platform for future development of potent antiviral agents to complement current HIV-1 therapies.

Product Details of C11H19NO4, N-BOC-piperidine-4-carboxylic acid, also known asN-Boc-isonipecotic acid , is a useful research compound. Its molecular formula is C11H19NO4 and its molecular weight is 229,28 g/mole. The purity is usually 95%.

N-Boc-isonipecotic acid is a potent antitumor agent that has been clinically shown to be effective against leukemia and lymphoma. It has potent antibacterial activity against Gram-positive bacteria such as Staphylococcus aureus and Streptococcus pyogenes. N-Boc-isonipecotic acid binds to the gyrase enzyme, which is used by these bacteria to maintain the integrity of their DNA, inhibiting protein synthesis and cell division. This drug also has anti-inflammatory properties. N-Boc-isonipecotic acid inhibits prostaglandin synthesis in cells, which may be due to its ability to inhibit the production of tumor necrosis factor α (TNFα) in macrophages., 84358-13-4.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Piperidine is an organic compound with the molecular formula (CH2)5NH. This heterocyclic amine consists of a six-membered ring containing five methylene bridges (–CH2–) and one amine bridge (–NH–). 2403-88-5, formula is C9H19NO, Name is 2,2,6,6-Tetramethyl-4-piperidinol. It is a colorless liquid with an odor described as objectionable, and typical of amines. Synthetic Route of 2403-88-5.

Adil, Sawaira;Kim, Woong Sub;Kim, Tae Hyeong;Lee, Seunghyun;Hong, Seok Won;Kim, Eun-Ju research published 《 Defective, oxygen-functionalized multi-walled carbon nanotubes as an efficient peroxymonosulfate activator for degradation of organic pollutants》, the research content is summarized as follows. Defects and surface O functionalities of multi-walled C nanotubes (MWCNT) prepared by a solid state reaction were demonstrated as effective to activate peroxymonosulfate (PMS) for organic pollutant degradation The catalytic activity of defective, O-functionalized CNT (dCNT) was much better than bare CNT, due to many CNT surface active sites, including structural defects and carbonyl functional groups, and excellent elec. conductivity The effect of several operational factors and water conditions on the degradation rate of targeted pollutants and material stability were comprehensively evaluated for the practical application of the dCNT/PMS integrated process. The dCNT underlying catalytic mechanism is expected to occur by a non-radical pathway and radical-induced oxidation, where surface-bound radicals play a more dominant role than free radicals. A defect and O functional group tuning strategy provided an effective method to develop advanced C catalysts for Fenton-like reactions.

2403-88-5, 2,2,6,6-Tetramethyl-4-piperidinol(TEMPO) is a useful research compound. Its molecular formula is C9H19NO and its molecular weight is 157.25 g/mol. The purity is usually 95%.
TEMPO is an intermediate used in the preparation of Piperidinyloxy free radical derivatives.
TEMPO is an organic compound that acts as a radical scavenger. It is stable in the presence of water and air and can be used for the inhibition of bacterial growth. TEMPO reacts with reactive intermediates to form non-reactive substances and terminate chain reactions. This process is optimal at temperatures between 0°C and 40°C and pH values between 3.5 and 7.5. TEMPO has been shown to inhibit the growth of bacteria by reacting with reactive molecules such as amines, chlorides, or low energy radicals in aqueous solution. TEMPO also has genotoxic activity that inhibits DNA synthesis in bacterial cells through oxidation of guanine residues on DNA molecules., Synthetic Route of 2403-88-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Piperidine the name comes from the genus name Piper, which is the Latin word for pepper. 5382-16-1, formula is C5H11NO, Name is 4-Piperidinol. Although piperidine is a common organic compound, it is best known as a representative structure element within many pharmaceuticals and alkaloids, such as natural-occurring solenopsins. Name: 4-Piperidinol.

Lei, Hongrui;Wang, Xinyu;Zhao, Guolong;Li, Tong;Cui, Youbao;Wu, Huinan;Yang, Jing;Jiang, Nan;Zhai, Xin research published 《 Design, synthesis and promising anti-tumor efficacy of novel imidazo[1,2-a]pyridine derivatives as potent autotaxin allosteric inhibitors》, the research content is summarized as follows. Aiming to track the potential antitumor effect of novel allosteric autotaxin (ATX) inhibitors, a hybrid strategy was utilized by merging ATX inhibitors PF-8380 and GLPG1690, while the piperazinyl group in GLPG1690 was replaced with benzene ring to furnish imidazo[1,2-a]pyridine derivatives I [R¹ = 3,5-diCl, 4-CF₃, 3,4-di-F; R² = L-Prolinol, 4-hydroxyethylpiperazinyl, morpholine, etc.; R³ = CH₂, C(O); X = O, N]. Based on ATX enzymic assay, further changed the substituents within benzyl carbamate moiety and tuned the carbamate linker to urea group. Delightfully, compound I [R¹ = 3,5-diCl, R² = 4-hydroxyethylpiperazinyl] was identified as the optimal ATX inhibitor with an IC₅₀ value of 3.4 nM. Compound I [R¹ = 3,5-diCl, R² = 4-hydroxyethylpiperazinyl] exerted the most impressive antitumor effects, especially on Hep3B (0.58μM) and RAW264.7 (0.63μM) cell lines highly expressing ATX mRNA. Moreover, compound I [R¹ = 3,5-diCl, R² = 4-hydroxyethylpiperazinyl] could dose-dependently suppress the RAW264.7 cell migration rate in wound healing assay and significantly inhibit RAW264.7 cell colony formation. Meanwhile, compound I [R¹ = 3,5-diCl, R² = 4-hydroxyethylpiperazinyl] was capable of inducing weak to moderate apoptosis and achieved notable G2 phase arrest on RAW264.7 cells. Compound I [R¹ = 3,5-diCl, R² = 4-hydroxyethylpiperazinyl] may serve as a novel lead to probe possible role of ATX allosteric inhibitors in tumor diseases.

Name: 4-Piperidinol, 4-Hydroxypiperidine is a molecule with a carbonyl group. It is the most active and selective CCR5 receptor antagonist that has been studied to date. 4-Hydroxypiperidine inhibits HIV infection by preventing the binding of HIV to its receptor on the surface of white blood cells, thereby preventing it from entering these cells. 4-Hydroxypiperidine also acts as an anti-inflammatory agent in chronic bronchitis patients, due to its ability to inhibit prostaglandin synthesis. The chemical ionization mass spectra of this molecule show peaks for methyl ethyl, malic acid, and hydroxyl groups. These properties make 4-hydroxypiperidine a useful candidate for drug development against inflammatory diseases and several cancers.
The molecular structure, vibrational spectra, NBO and UV-spectral analysis of 4-Hydroxypiperidine have been studied. The compounds with a substituted 4-piperidinol core have been found to be potent antagonists of the human H receptor., 5382-16-1.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Piperidine is an organic compound with the molecular formula (CH2)5NH. This heterocyclic amine consists of a six-membered ring containing five methylene bridges (–CH2–) and one amine bridge (–NH–). 5382-16-1, formula is C5H11NO, Name is 4-Piperidinol. It is a colorless liquid with an odor described as objectionable, and typical of amines. Safety of 4-Piperidinol.

Lei, Hongrui;Cao, Zhi;Wu, Huinan;Li, Tong;Wang, Xinyu;Chen, Yuxiang;Ma, Enlong;Sun, Lixin;Zhai, Xin research published 《 Structural and PK-guided identification of indole-based non-acidic autotaxin (ATX) inhibitors exhibiting high in vivo anti-fibrosis efficacy in rodent model》, the research content is summarized as follows. In recent decades, pharmacol. targeting of the autotaxin (ATX)/lysophosphatidic acid (LPA) axis accounted for excellent disease management benefits. Herein, to extend the scope of structure-activity relationships (SARs), fifteen indole-based carbamate derivatives I [R = 4-Me, 3,4-difluoro, 2,3-dichloro; R¹ = pyrrolidin-1-yl, (4-methyl-1-piperidyl), (4-methylpiperazin-1-yl); R² = H, CH₃, etc] were prepared to evaluate the ATX inhibitory potency. Among them, compound I [R = 3,5-dichloro; R¹ = morpholino; R² = H] bearing morpholine moiety was identified as the optimal ATX inhibitor (0.41 nM), superior to the pos. control GLPG1690 (2.90 nM). To resolve the intractable issue of poor pharmacokinetic (PK) property, urea moiety was introduced as a surrogate of carbamate which furnished compounds II [R³ = morpholino, (4-hydroxy-1-piperidyl), [2-(hydroxymethyl)pyrrolidin-1-yl]; R⁴ = H, 4-Cl, 4-F, etc]. The dedicated modification identified the diethanolamine entity II [R³ = [bis(2-hydroxyethyl)amino]; R⁴ = (3-chloro-4-methoxy-phenyl)] with satisfactory water solubility and PK profiles with a min. sacrifice of ATX inhibition (2.17 nM). The most promising candidate II [R³ = [bis(2-hydroxyethyl)amino]; R⁴ = (3-chloro-4-methoxy-phenyl)] was evaluated for anti-fibrosis effect in a bleomycin challenged mice lung fibrosis model. Upon treatment with II [R³ = [bis(2-hydroxyethyl)amino]; R⁴ = (3-chloro-4-methoxy-phenyl)], the in vivo ATX activity in both lung homogenate and broncheoalveolar fluid (BALF) sample was significantly down-regulated. Furthermore, the gene expression of pro-fibrotic cytokines transforming growth factor-β (TGF-β), interleukin- 6 (IL-6) and tumor necrosis factor-α (TNF-α) in lung tissue was reduced to normal level. Collectively, the promising biol. effects may advocate potential application of II [R³ = [bis(2-hydroxyethyl)amino]; R⁴ = (3-chloro-4-methoxy-phenyl)] in fibrosis relevant diseases.

Safety of 4-Piperidinol, 4-Hydroxypiperidine is a molecule with a carbonyl group. It is the most active and selective CCR5 receptor antagonist that has been studied to date. 4-Hydroxypiperidine inhibits HIV infection by preventing the binding of HIV to its receptor on the surface of white blood cells, thereby preventing it from entering these cells. 4-Hydroxypiperidine also acts as an anti-inflammatory agent in chronic bronchitis patients, due to its ability to inhibit prostaglandin synthesis. The chemical ionization mass spectra of this molecule show peaks for methyl ethyl, malic acid, and hydroxyl groups. These properties make 4-hydroxypiperidine a useful candidate for drug development against inflammatory diseases and several cancers.
The molecular structure, vibrational spectra, NBO and UV-spectral analysis of 4-Hydroxypiperidine have been studied. The compounds with a substituted 4-piperidinol core have been found to be potent antagonists of the human H receptor., 5382-16-1.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem