Heterocyclic Building Blocks-piperidine

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. Reference of 5382-16-1.

Zhu, Peiyu;Zhang, Jian;Yang, Yifei;Wang, Lixun;Zhou, Jinpei;Zhang, Huibin research published 《 Design, synthesis and biological evaluation of isoxazole-containing biphenyl derivatives as small-molecule inhibitors targeting the programmed cell death-1/ programmed cell death-ligand 1 immune checkpoint》, the research content is summarized as follows. Monoclonal antibodies targeting the programmed cell death-1/ programmed cell death-ligand 1 (PD-1/PD-L1) immune checkpoint have achieved enormous success in cancer immunotherapy. But the antibody-based immunotherapies carry a number of unavoidable deficiencies such as poor pharmacokinetic properties and immunogenicity. Small-mol. PD-1/PD-L1 inhibitors offer the superiority of complementarity with monoclonal antibodies and represent an appealing alternative. A novel series of isoxazole-containing biphenyl compounds were designed, synthesized and evaluated as PD-1/PD-L1 inhibitors in this paper. The structure-activity relationship of the novel synthesized compounds indicated that the ring-closure strategy of introducing isoxazole could be employed and the 3-cyanobenzyl group was significant for the inhibitory activity against the PD-1/PD-L1 protein-protein interactions. Mol. docking studies were performed to help understand the binding mode of the small-mol. inhibitor with the PD-L1 dimer. In particular, compound II-12 was a promising anti-PD-1/PD-L1 inhibitor with the IC₅₀ value of 23.0 nM, providing valuable information for future drug development.

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., Reference 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. Application In Synthesis of 84358-13-4.

Zhu, Mei;Zhou, Huiyu;Ma, Ling;Dong, Biao;Zhou, Jinming;Zhang, Guoning;Wang, Minghua;Wang, Juxian;Cen, Shan;Wang, Yucheng research published 《 Design and evaluation of novel piperidine HIV-1 protease inhibitors with potency against DRV-resistant variants》, the research content is summarized as follows. A novel class of HIV-1 protease inhibitors with flexible piperidine as the P2 ligand was designed with the aim of improving extensive interactions with the active subsites. Many inhibitors exhibited good to excellent inhibitory effect on enzymic activity and viral infectivity. In particular, inhibitor 3a with (R)-piperidine-3-carboxamide as the P2 ligand and 4-methoxybenzenesulfonamide as the P2 ligand showed an enzyme Ki value of 29 pM and antiviral IC50 value of 0.13 nM, more than six-fold enhancement of activity compared to DRV. Furthermore, there was no significant change in potency against DRV-resistant mutations and HIV-1NL4-3 variant for 3a. Besides, inhibitor 3a exhibited potent antiviral activity against subtype C variants with low nanomole EC50 values. In addition, the mol. modeling revealed important hydrogen bonds and other favorable van der Waals interactions with the backbone atoms of the protease and provided insight for designing and optimizing more potent HIV-1 protease inhibitors.

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., Application In Synthesis of 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. 5382-16-1, formula is C5H11NO, Name is 4-Piperidinol. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol. COA of Formula: C5H11NO.

Zhu, Li;Zhao, Rui-Han;Li, Yu;Liu, Gong-Qing;Zhao, Yu research published 《 CtD strategy to construct stereochemically complex and structurally diverse compounds from griseofulvin》, the research content is summarized as follows. The Complexity to Diversity (CtD) strategy, for the synthesis of stereochem. complexes I (R = H, C(O)Me, Ph, Bn, etc; R¹ = H, Me, n-Bu, Bn, etc.), II, III (R² = OEt, benzyloxidanyl, morpholin-4-yl, etc.) and cis/trans-IV (R³ = H; R⁴ = Me, i-Pr; R³R⁴ = -(CH₂)₅-) and structurally diverse small mols. from natural products using ring-distortion reactions, was applied in the synthesis of a 47-member compounds I, II, III and cis/trans-IV collection from the natural product griseofulvin. A Tsuji-Trost allylation and oxa-Michael cyclization tandem reaction was used for the first time in the CtD strategy to generate complex ring fused cis/trans-IV .

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., COA of Formula: C5H11NO

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. 5382-16-1, formula is C5H11NO, Name is 4-Piperidinol. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol. Safety of 4-Piperidinol.

Zhu, Li;Lu, Yapeng;Li, Yu;Ling, Yong;Zhao, Yu research published 《 Synthesis and evaluation of diphyllin β-hydroxyl amino derivatives as novel V-ATPase inhibitors》, the research content is summarized as follows. Natural diphyllin glycosides were identified as potent vacuolar H+-ATPase (V-ATPase) inhibitors. A series of diphyllin β-hydroxyl amino derivatives were designed and synthesized as novel diphyllin derivatives Most of these derivatives displayed potent cytotoxicity against six cancer cell lines with IC50 values in the submicromolar to nanomolar concentration range. Compounds 2b, 2c, 2l, 2m, and 2n showed similar V-ATPase inhibitory potency to Bafilomycin A1. Compound 2l exhibited potent activity of modulation of lysosomal pH and cytoplasmic pH.

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 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. COA of Formula: C5H11NO.

Zhou, Yu;Li, Xiaoguang;Chen, Kerong;Ba, Qian;Zhang, Xu;Li, Jingquan;Wang, Jinfang;Wang, Hui;Liu, Hong research published 《 Structural optimization and biological evaluation for novel artemisinin derivatives against liver and ovarian cancers》, the research content is summarized as follows. An increasing number of artemisinin (ARS) and its derivatives have been reported for their potential therapeutic value of human cancer. However, their therapeutic potencies are limited owing to their poor pharmacokinetic profiles. Our previous studies showed that lead compound I originated from incorporating the pharmacophore of the approved chemotherapeutic agent melphalan into the basic skeleton of artemisinin with a succinic linker exhibited an excellent toxicity to human ovarian cancer cells and low cytotoxicity to normal cells. The mechanism studies demonstrated that it inhibited the growth and proliferation of ovarian cancer cells and resulted in S-phase arrest, apoptosis and inhibition of migration. Meanwhile, it exhibited excellent antitumor activities in animal models. Herein, further structure optimization for this lead compound I was performed and nineteen novel derivatives were designed and synthesized. Several compounds demonstrated powerful cytotoxic effects against human liver cancer and ovarian cancer cell lines, with their IC_50s below 0.86μM against Hep3B and A2780 cell lines, which are superior to that of I. Four compounds were selected to further evaluate their antitumor activities in in vitro and in vivo ovarian and liver cancer models; the results indicated that compound II exhibited the best therapeutic effect, not only effectively inhibiting the growth of 7404 xenograft and Huh7 xenograft, but also presenting a good dose-dependent inhibition toward the growth of A2780 xenograft. Overall, based on these pos. results, these novel chem. structures may provide a new inspiration for the discovery of novel antitumor agents originated from artemisinin scaffolds.

COA of Formula: C5H11NO, 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. COA of Formula: C5H11NO.

Zhou, Xueying;Xu, Yaling;Wang, Caihong;Wu, Ge research published 《 Cu-catalyzed vinylamination of S-alkylisothiouronium salts with maleimides and alkylamines》, the research content is summarized as follows. A copper-catalyzed vinylamination of S-alkylisothiouronium salts with maleimide and organic amines with the assistance of FeCl₃, enabling the preparation of structurally diverse aminoalkylthiolated maleimides and applying them to late-stage modification of pharmaceuticals is reported. Importantly, this strategy makes it possible to introduce the SCD₃ functional group into the maleimide skeleton by using the prepared S-trideuteromethyl isothiouronium iodide. Preliminary mechanistic investigation shows that FeCl₃ is essential to the current multi-component reaction by triggering S-alkylisothiouronium salts.

COA of Formula: C5H11NO, 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

Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst: C5H5N + 3 H2 → C5H10NH. 84358-13-4, formula is C11H19NO4, Name is 1-(tert-Butoxycarbonyl)piperidine-4-carboxylic acid. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol. Product Details of C11H19NO4.

Zhi, Zhuoer;Zhang, Wenting;Yao, Jingchun;Shang, Yanguo;Hao, Qingjing;Liu, Zhong;Ren, Yushan;Li, Jie;Zhang, Guimin;Wang, Jinxin research published 《 Discovery of Aryl Formyl Piperidine Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase Inhibitors》, the research content is summarized as follows. Most of the current MAGL inhibitors function by an irreversible mechanism of action, causing a series of side effects. Herein, starting from irreversible inhibitors, 25 compounds were synthesized and evaluated in vitro for MAGL inhibition, among which, compound I showed the most potent inhibitory activity (IC50 = 15 nM). Crucially, docking studies demonstrated that the m-chlorine-substituted aniline fragment occupied a hydrophobic sub-pocket enclosed by side chains of Val191, Tyr194, Val270, and Lys273, which creatively identify a new key anchoring point for the development of new MAGL inhibitors. Furthermore, in vivo evaluation innovatively revealed that this reversible inhibitor I significantly displayed the depressive-like behaviors induced by reserpine. To the best of our knowledge, this is the first time that reversible inhibitors of MAGL were developed to support MAGL as a potential therapeutic target for depression.

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 structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. This gave the compound its name. 2403-88-5, formula is C9H19NO, Name is 2,2,6,6-Tetramethyl-4-piperidinol. Other examples are the fire ant toxin solenopsin, the nicotine analog anabasine of tree tobacco (Nicotiana glauca), lobeline of Indian tobacco. COA of Formula: C9H19NO.

Zheng, Wentian;Liu, Yanbiao;Liu, Wen;Ji, Haodong;Li, Fang;Shen, Chensi;Fang, Xiaofeng;Li, Xiang;Duan, Xiaoguang research published 《 A novel electrocatalytic filtration system with carbon nanotube supported nanoscale zerovalent copper toward ultrafast oxidation of organic pollutants》, the research content is summarized as follows. In this study, we designed an integrated electrochem. filtration system for catalytic activation of peroxymonosulfate (PMS) and degradation of aqueous microcontaminants. Composites of carbon nanotube (CNT) and nanoscale zero valence copper (nZVC) were developed to serve as high-performance catalysts, electrode and filtration media simultaneously. We observed both radical and nonradical reaction pathways, which collectively contributed to the degradation of model pollutants. Congo red was completely removed via a single-pass through the nZVC-CNT filter (τ <2 s) at neutral pH. The rapid kinetics of Congo red degradation were maintained across a wide pH range (from 3.0-7.0), in complicated matrixes (e.g., tap water and lake water), and for the degradation of a wide array of persistent organic contaminants. The superior activity of nZVC-CNT stems from the boosted redox cycles of Cu2+/Cu+ in the presence of an external elec. field. The flow-through design remarkably outperformed the conventional batch system due to the convection-enhanced mass transport. Mechanism studies suggested that the carbonyl group and electrophilic oxygen of CNT served as electron donor and electron acceptor, resp., to activate PMS to generate •OH and 1O2via one-electron transport. The electron-deficient Cu atoms are prone to react with PMS via surface hydroxyl group to produce reactive intermediates (Cu2+-O-O-SO-3), and then 1O2 will be generated by breaking the coordination bond of the metastable intermediate. The study will provide a green strategy for the remediation of organic pollution by a highly efficient and integrated system based on catalytic oxidation, electrochem., and nano-filtration techniques.

COA of Formula: C9H19NO, 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 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. Recommanded Product: 2,2,6,6-Tetramethyl-4-piperidinol.

Zheng, Weisheng;Sun, Yue;Gu, Yingpeng research published 《 Catalysis and adsorption of Zr-doped Fe₃O₄ nanoparticles provide a new strategy for diazinon removal and phosphorus recovery from aqueous solution》, the research content is summarized as follows. As potential persistent and toxic organic contaminants, organophosphorus pesticides (OPPs) are frequently detected in various waters. However, few studies are available on removing OPPs in aqueous solution through heterogeneous catalytic activated peroxymonosulfate (PMS). Herein, Zr-doped Fe₃O₄ magnetic nanoparticles were prepared via a facile solvothermal method and employed to activate PMS for degrading diazinon. A series of characterization and performance tests revealed that Zr_(0.3)Fe₃O₄ composite played a dual role as both adsorbent and heterogeneous catalyst for removal of diazinon. Attractively, the introduction of Zr into magnetite endowed the nanoparticles with prominent adsorption capacity for released phosphate during the oxidation reaction. Combined with ESR (EPR) spectra and quenching studies, Zr_(0.3)Fe₃O₄ effectively catalyzed PMS to produce four kinds of reactive oxygen species (ROS), and ¹O₂ and O^–₂ were dominantly responsible for diazinon degradation Furthermore, the possible degradation pathways of diazinon in Zr_(0.3)Fe₃O₄/PMS system were discussed based on liquid chromatog. mass spectrometry (LC-MS) anal. In conclusion, the Zr_(0.3)Fe₃O₄ nanoparticles can not only remove diazinon by catalytic oxidation but also immobilize degraded phosphorus, hence, this work offers a novel strategy for developing versatile composites.

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., Recommanded Product: 2,2,6,6-Tetramethyl-4-piperidinol

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. Quality Control of 84358-13-4.

Zhao, Yanmei;Xu, Lei;Zhang, Jiankang;Zhang, Mengmeng;Lu, Jingyi;He, Ruoyu;Xi, Jianjun;Zhuang, Rangxiao;Li, Jia;Zhou, Yubo research published 《 Optimization of piperidine constructed peptidyl derivatives as proteasome inhibitors》, the research content is summarized as follows. A series of non-covalent piperidine-containing peptidyl derivatives with various substituents at side chains of different residues were designed, synthesized and evaluated as proteasome inhibitors. After proteasome inhibitory evaluations of all the synthesized target compounds, selected ones were tested for their anti-proliferation activities against three multiple myeloma (MM) cell lines. Eight analogs displayed more potent activities than carfilzomib, and the most promising compound 24 (I) showed IC₅₀ values of 0.8 ± 0.2 nM against 20S proteasome and 8.42 ± 0.74 nM, 7.14 ± 0.52 nM, 14.20 ± 1.08 nM for RPMI 8226, NCI-H929 and MM.1S cell lines, resp. Addnl., mechanisms of anti-cancer activity of representative compound 24 were further investigated. Apoptosis of RPMI-8226 cells were achieved through accumulating polyubiquitin and inducing the cleavage of caspase and PARP. Besides, half-life in rat plasma of compound 24 was prolonged after optimization, which would be helpful for increasing in vivo activities of this series of derivatives All the studies confirmed that piperidine-containing non-covalent proteasome inhibitors can be potential leads for anti-MM drug development.

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., Quality Control of 84358-13-4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem