Category: 5382-16-1

Piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. This gave the compound its name. 5382-16-1, formula is C5H11NO, Name is 4-Piperidinol. Other examples are the fire ant toxin solenopsin, the nicotine analog anabasine of tree tobacco (Nicotiana glauca), lobeline of Indian tobacco. Safety of 4-Piperidinol.

Dai, Xinyan;Wang, Ke;Chen, Hao;Huang, Xupeng;Feng, Zhiqiang research published 《 Design, synthesis, and biological evaluation of 1-methyl-1H-pyrazolo[4,3-b]pyridine derivatives as novel small-molecule inhibitors targeting the PD-1/PD-L1 interaction》, the research content is summarized as follows. Blockade of the programmed cell death-1 (PD-1)/programmed cell death-ligand 1 (PD-L1) signalling pathway is a promising tumor immunotherapeutic approach, and small mol. drugs have more advantages than monoclonal antibody macromols. in clin. applications. Therefore, a series of 1-methyl-1H-pyrazolo[4,3-b]pyridine derivatives as PD-1/PD-L1 interaction novel small-mol. inhibitors were designed employing a ring fusion strategy. The inhibitory activity of compounds was evaluated by the HTRF assay, among which I was identified as the most potent PD-1/PD-L1 interaction inhibitor with an IC₅₀ value of 9.6 nM. Furthermore, I exhibited prominent inhibitory activity against the PD-1/PD-L1 interaction with an EC₅₀ value of 1.61μM in a coculture model of PD-L1/TCR activator-expressing CHO cells and PD-1-expressing Jurkat cells. In addition, the preliminary structure-activity relationships (SARs) of compounds were elucidated, and the binding mode of I with the PD-L1 dimer was analyzed by mol. docking. Overall, I could be employed as a prospective lead compound of PD-1/PD-L1 interaction inhibitors for further development.

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

Piperidine was first reported in 1850 by the Scottish chemist Thomas Anderson and again, independently, in 1852 by the French chemist 5382-16-1, formula is C5H11NO, Name is 4-Piperidinol. Auguste Cahours, who named it. Both of them obtained piperidine by reacting piperine with nitric acid. Category: piperidines.

Di Porzio, Anna;Galli, Ubaldina;Amato, Jussara;Zizza, Pasquale;Iachettini, Sara;Iaccarino, Nunzia;Marzano, Simona;Santoro, Federica;Brancaccio, Diego;Carotenuto, Alfonso;De Tito, Stefano;Biroccio, Annamaria;Pagano, Bruno;Tron, Gian Cesare;Randazzo, Antonio research published 《 Synthesis and Characterization of Bis-Triazolyl-Pyridine Derivatives as Noncanonical DNA-Interacting Compounds》, the research content is summarized as follows. Besides the well-known double-helical conformation, DNA is capable of folding into various noncanonical arrangements, such as G-quadruplexes (G4s) and i-motifs (iMs), whose occurrence in gene promoters, replication origins, and telomeres highlights the breadth of biol. processes that they might regulate. Particularly, previous studies have reported that G4 and iM structures may play different roles in controlling gene transcription. Anyway, mol. tools able to simultaneously stabilize/destabilize those structures are still needed to shed light on what happens at the biol. level. Herein, a multicomponent reaction and a click chem. functionalization were combined to generate a set of 31 bis-triazolyl-pyridine derivatives which were initially screened by CD for their ability to interact with different G4 and/or iM DNAs and to affect the thermal stability of these structures. All the compounds were then clustered through multivariate data anal., based on such capability. The most promising compounds were subjected to a further biophys. and biol. characterization, leading to the identification of two mols. simultaneously able to stabilize G4s and destabilize iMs, both in vitro and in living cells.

Category: piperidines, 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 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. Recommanded Product: 4-Piperidinol.

Elbadawi, Mostafa M.;Eldehna, Wagdy M.;Wang, Wenjie;Agama, Keli K.;Pommier, Yves;Abe, Manabu research published 《 Discovery of 4-alkoxy-2-aryl-6,7-dimethoxyquinolines as a new class of topoisomerase I inhibitors endowed with potent in vitro anticancer activity》, the research content is summarized as follows. Two novel series of 4-alkoxy-2-arylquinolines I (n = 1, 2; R = pyrrolidino, 4-hydroxypiperidino, piperidino, morpholino; X = Cl, CF₃) were designed and synthesized based on SARs of the reported TOP1 inhibitors and structural features required for stabilization of TOP1-DNA cleavage complexes (TOP1ccs). The in vitro anticancer activity of these two series of compounds was evaluated at one dose level using NCI-60 cancer cell lines panel. Compounds with p-substituted Ph at C2 and Pr linker at C4, were the most potent and were selected for assay at five doses level in which they exhibited potent anticancer activity at sub-micromolar level against diverse cancer cell lines. Compound I (Ar = 4-F₃CC₆H₄, 2-furyl, 2-thienyl, etc.; n = 2; R = pyrrolidino) was the most potent with full panel GI₅₀ MG-MID 1.26μM and the most sensitive cancers were colon cancer, leukemia and melanoma. Melanoma (LOX IMVI) was the most sensitive cell line to all tested compounds displaying GI₅₀ and LC₅₀ at sub-micromolar concentration against almost of the tested compounds Few compounds were assayed using TOP1-mediated DNA cleavage assay to evaluate their ability to stabilize TOP1ccs resulting in cancer cell death. The morpholino analogs I (n = 2; R = morpholino; X = Cl, CF₃) exhibited moderate TOP1 inhibitory activity compared to 1μM camptothecin suggesting their use as lead compounds that can be optimized for the development of more potent anticancer agents with potential TOP1 inhibitory activity.

Recommanded Product: 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. Reference of 5382-16-1.

Eliwa, Essam M.;Frese, Marcel;Halawa, Ahmed H.;Soltan, Maha M.;Ponomareva, Larissa V.;Thorson, Jon S.;Shaaban, Khaled A.;Shaaban, Mohamed;El-Agrody, Ahmed M.;Sewald, Norbert research published 《 Metal-free domino amination-Knoevenagel condensation approach to access new coumarins as potent nanomolar inhibitors of VEGFR-2 and EGFR》, the research content is summarized as follows. A metal-free, atom-economy and simple work-up domino amination-Knoevenagel condensation approach to construct new coumarin analogous I [R¹ = pyrrolidin-1-yl, morpholino, (4-hydroxy-1-piperidyl), etc.; R² = cyano, methoxycarbonyl, (1-amino-2,2-dicyano-vinyl)] were described. Further, new formyl and nitro coumarin derivatives II [R¹ = methoxy, pyrrolidin-1-yl, morpholino, etc.; R³ = formyl, nitro] were synthesized via C-N coupling reaction of various cyclic secondary amines and 4-chloro-3-(formyl-/nitro)coumarins resp. The confirmed compounds were screened for their in vitro anti-proliferative activity against KB-3-1, A549 and PC3 human cancer cell lines using resazurin cellular-based assay. Among them, coumarin derivatives I [R¹ = (4-piperidylmethylamino); R² = cyano, methoxycarbonyl] displayed the best anti-cervical cancer potency (KB-3-1) with IC₅₀ values of 15.5 ± 3.54 and 21 ± 4.24μM, resp. Also, I [R¹ = (4-piperidylmethylamino); R² = methoxycarbonyl] showed the most promising cytotoxicity toward A549 with IC₅₀ value of 12.94 ± 1.51μM. As well, II [R¹ = morpholino; R³ = nitro]presented a more significant impact of potency against PC3 with IC₅₀ 7.31 ± 0.48μM. Moreover, I [R¹ = morpholino; R² = cyano] manifested selectivity against PC3 (IC₅₀ = 20.16 ± 0.07μM), while I [R¹ = (4-piperidylmethylamino); R² = cyano] was selective toward KB-3-1 cell line (IC₅₀ = 21 ± 4.24μM). Matching with docking profile, the enzymic assay divulged that I [R¹ = (4-piperidylmethylamino); R² = cyano] was a dual potent single-digit nanomolar inhibitor of VEGFR-2 and EGFR with IC₅₀ values of 24.67 nM and 31.6 nM that were almost equipotent to sorafenib (31.08 nM) and erlotinib (26.79 nM), resp.

Reference of 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., 5382-16-1.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. This gave the compound its name. 5382-16-1, formula is C5H11NO, Name is 4-Piperidinol. Other examples are the fire ant toxin solenopsin, the nicotine analog anabasine of tree tobacco (Nicotiana glauca), lobeline of Indian tobacco. Quality Control of 5382-16-1.

Bata, Nicole;Chaikuad, Apirat;Bakas, Nicole A.;Limpert, Allison S.;Lambert, Lester J.;Sheffler, Douglas J.;Berger, Lena M.;Liu, Guoxiong;Yuan, Cunxiang;Wang, Li;Peng, Yi;Dong, Jing;Celeridad, Maria;Layng, Fabiana;Knapp, Stefan;Cosford, Nicholas D. P. research published 《 Inhibitors of the Hippo Pathway Kinases STK3/MST2 and STK4/MST1 Have Utility for the Treatment of Acute Myeloid Leukemia》, the research content is summarized as follows. Serine/threonine-protein kinases 3 and 4 (STK3 and STK4, resp.) are key components of the Hippo signaling pathway, which regulates cell proliferation and death and provides a potential therapeutic target for acute myeloid leukemia (AML). Herein, we report the structure-based design of a series of pyrrolopyrimidine derivatives as STK3 and STK4 inhibitors. In an initial screen, the compounds exhibited low nanomolar potency against both STK3 and STK4. Crystallization of compound 6 with STK4 revealed two-point hinge binding in the ATP-binding pocket. Further characterization and anal. demonstrated that compound 20 (SBP-3264) specifically inhibited the Hippo signaling pathway in cultured mammalian cells and possessed favorable pharmacokinetic and pharmacodynamic properties in mice. We show that genetic knockdown and pharmacol. inhibition of STK3 and STK4 suppress the proliferation of AML cells in vitro. Thus, SBP-3264 is a valuable chem. probe for understanding the roles of STK3 and STK4 in AML and is a promising candidate for further advancement as a potential therapy.

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 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. Application In Synthesis of 5382-16-1.

Bai, Jixiang;Wang, Tianxin;Dai, Botao;Liu, Qingchao;Yu, Peiyuan;Jia, Tiezheng research published 《 Radical Anion Promoted Chemoselective Cleavage of Csp²-S Bond Enables Formal Cross-Coupling of Aryl Methyl Sulfones with Alcohols》, the research content is summarized as follows. A novel formal cross-coupling of aryl Me sulfones and alcs. affording alkyl aryl ethers ROR¹ [R = n-Bu, Bn, (CH₂)₂cyclohexyl, etc.; R¹ = Ph, 1-naphthyl, 2-pyridyl, etc.] via an SRN¹ pathway was developed. Two marketed antitubercular drugs were efficiently prepared employing this approach as the key step. A dimsyl-anion initiated radical chain process was revealed as the major pathway. DFT calculations indicate that the formation of a radical anion via nucleophilic addition of alkoxide to the aryl radical was the key step in determining the observed chemoselectivity.

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., Application In Synthesis of 5382-16-1

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 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

5382-16-1, 4-Piperidinol is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(d) A solution containing 4-piperidinol (5 g) and triethylamine (7 ml) in dichloromethane (50 ml) was treated with benzyl chloroformate (7.5 ml), added dropwise, and the resulting mixture was allowed to stand for 2 hours. The mixture was diluted with dichloromethane (50 ml) and washed with water (2*50 ml) and with saturated brine (50 ml). The organic solution was dried (MgSO4) and concentrated. The residue was purified by column chromatography, eluding with ether/hexane (50%, then 75%) followed by ether, to give 1-(benzyloxycarbonyl)piperidin-4-ol (7.5 g) as a colourless oil; NMR Spectrum 1.2-1.4 (2H, m); 1.6-1.8 (2H, m); 3.0-3.2 (2H, m); 3.6-3.8 (3H, m); 4.7 (1H, d); 5.05 (2H, s); 7.3-7.4 (5H, m).

5382-16-1, As the paragraph descriping shows that 5382-16-1 is playing an increasingly important role.

Reference£º
Patent; Zeneca Limited; US5612373; (1997); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem