Category: 498-95-3

Safety of Piperidine-3-carboxylic acid. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: Piperidine-3-carboxylic acid, is researched, Molecular C6H11NO2, CAS is 498-95-3, about Design, synthesis, and structure-activity relationship of programmed cell death-1/programmed cell death-ligand 1 interaction inhibitors bearing a benzo[d]isothiazole scaffold. Author is Chen, Hao; Wang, Ke; Yang, Yang; Huang, Xupeng; Dai, Xinyan; Feng, Zhiqiang.

A novel series of compounds such as I [R = CH2NHCHCO2HCH2OH, CH2(N-piperidin-3-ol), CH2(N-pyrrolidin-3-ol), etc.] bearing a benzo[d]isothiazole scaffold were developed, among which compound I [R = CH2NHCHCO2HCH2OH] exhibited promising activity, with an IC50 value of 8.5 nM. Further cell-based PD-1/PD-L1 blockade bioassays indicated that compound I [R = CH2NHCHCO2HCH2OH] could inhibit the PD-1/PD-L1 interaction at the cellular level, with an EC50 value of 5.6μM compound I [R = CH2NHCHCO2HCH2OH] could had better potency in restoring the activity of effector cells, as the maximal luminescence values (RLUmax) of compound I [R = CH2NHCHCO2HCH2OH] were equivalent to those of PD-L1 mAbs. The docking anal. of compound I [R = CH2NHCHCO2HCH2OH] with the PD-L1 dimer complex (PDB ID: 6R3K) confirmed that I [R = CH2NHCHCO2HCH2OH] was a promising lead compound for the development of inhibitors of the PD-1/PD-L1 interaction. The preliminary structure-activity relationship was investigated in this paper, with the aim of future drug development.

Different reactions of this compound(Piperidine-3-carboxylic acid)Safety of Piperidine-3-carboxylic acid require different conditions, so the reaction conditions are very important.

Reference:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Safety of Piperidine-3-carboxylic acid. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: Piperidine-3-carboxylic acid, is researched, Molecular C6H11NO2, CAS is 498-95-3, about Design, synthesis, and structure-activity relationship of programmed cell death-1/programmed cell death-ligand 1 interaction inhibitors bearing a benzo[d]isothiazole scaffold. Author is Chen, Hao; Wang, Ke; Yang, Yang; Huang, Xupeng; Dai, Xinyan; Feng, Zhiqiang.

A novel series of compounds such as I [R = CH2NHCHCO2HCH2OH, CH2(N-piperidin-3-ol), CH2(N-pyrrolidin-3-ol), etc.] bearing a benzo[d]isothiazole scaffold were developed, among which compound I [R = CH2NHCHCO2HCH2OH] exhibited promising activity, with an IC50 value of 8.5 nM. Further cell-based PD-1/PD-L1 blockade bioassays indicated that compound I [R = CH2NHCHCO2HCH2OH] could inhibit the PD-1/PD-L1 interaction at the cellular level, with an EC50 value of 5.6μM compound I [R = CH2NHCHCO2HCH2OH] could had better potency in restoring the activity of effector cells, as the maximal luminescence values (RLUmax) of compound I [R = CH2NHCHCO2HCH2OH] were equivalent to those of PD-L1 mAbs. The docking anal. of compound I [R = CH2NHCHCO2HCH2OH] with the PD-L1 dimer complex (PDB ID: 6R3K) confirmed that I [R = CH2NHCHCO2HCH2OH] was a promising lead compound for the development of inhibitors of the PD-1/PD-L1 interaction. The preliminary structure-activity relationship was investigated in this paper, with the aim of future drug development.

Different reactions of this compound(Piperidine-3-carboxylic acid)Safety of Piperidine-3-carboxylic acid require different conditions, so the reaction conditions are very important.

Reference:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

HPLC of Formula: 498-95-3. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: Piperidine-3-carboxylic acid, is researched, Molecular C6H11NO2, CAS is 498-95-3, about Blockade Of γ-Aminobutyric Acid Transporters In Brain Synapses Protects Against Hyperbaric Oxygen-Induced Convulsions. Author is Moskvin, A. N.; Platonova, T. Ph.; Zhilyaev, S. Yu.; Alekseeva, O. S.; Nikitina, E. R.; Demchenko, I. T..

Respiration of hyperbaric oxygen (HBO2) suppresses the synthesis of γ-aminobutyric acid (GABA) in the brain, leading to weakening of inhibitory GABAergic neurotransmission and the development of convulsive syndrome of the epileptic seizure type. We report here our testing of the hypothesis that inhibition of GABA transporters might compensate for insuffi ciency of inhibitory transmitter synthesis, strengthen GABAergic transmission, and weaken or prevent the development of oxygen-induced convulsions. The development of convulsions was studied in conscious rats in a barochamber containing oxygen at a pressure of 5 atm (absolute atmospheres) after prior intracerebroventricular administration of drugs inhibiting selective neuronal (NO-711) or nonselective neuronal/glial GABA transporters (nipecotic acid). Studies in a sep. group of rats measured GABA in the striatum by microdialysis with liquid chromatog. These experiments showed that inhibition of neuronal and glial GABA transporters increases the level of GABA in the brain and weakens the development of oxygen-induced convulsions. A more effective anticonvulsant effect was seen after intracerebroventricular administration of the nonselective inhibitor of GABA transporters. These data provide evidence that blockade of the functions of neuronal and glial GABA transporters increases the GABA level in the brain and weakens the development of convulsive syndrome in HBO2. The anticonvulsant effects of the inhibitors used here appear to result from strengthening of GABA-mediated synaptic and extrasynaptic neurotransmission by hyperbaric hyperoxia. Inhibition of GABA transporters may constitute a potential direction for the development of effective methods of preventing oxygen-induced convulsions.

The article 《Blockade Of γ-Aminobutyric Acid Transporters In Brain Synapses Protects Against Hyperbaric Oxygen-Induced Convulsions》 also mentions many details about this compound(498-95-3)HPLC of Formula: 498-95-3, you can pay attention to it, because details determine success or failure

Reference:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

SDS of cas: 498-95-3. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: Piperidine-3-carboxylic acid, is researched, Molecular C6H11NO2, CAS is 498-95-3, about Synthesis, characterization, in-silico and in-vitro evaluations of symmetrical 1,3-diketones. Author is Porchezhiyan, V.; Kalaivani, D.; Shobana, J.; Noorjahan, S. E..

The new sym. 1,3-diketones bearing L-proline, 2-methyl-5-iodobenzoic acid, piperidine-3-carboxylic acid and naphthalene-1-acetic acid moieties I, II [R = 5-iodo-2-methyl-Ph, 1-naphthylmethyl], III were synthesized by coupling reaction of appropriate ketone with N-acyl triazole in the presence of MgBr2·Et2O and DIPEA. The chem. structure of the compounds were confirmed from the spectral data such as 1H, 13C-NMR, FT-IR and HRMS. Mol. docking studies were carried out for all the compounds with tumor associated protein tyrosine kinase-6 (PTK6) and inflammatory protein cyclooxygenase-2 (COX2). The in-vitro evaluation was carried out using breast cancer cell lines (MTT assay) and HRBC stabilization assays. During in-silico studies, the ki values obtained against PTK6 and COX2 for I, II [R = 5-iodo-2-methyl-Ph, 1-naphthylmethyl], III compounds were in the range (-7.5 to -10.6) and (-7.6 to -9.8) kcal/mol, resp. The compound II [R = 1-naphthylmethyl] was selected for MTT assay, since it exhibited the highest binding affinity (-10.6 kcal/mol) against PTK6 and gave IC50 – 2.4μg/mL against breast cancer cell lines. The HRBC stabilization of all the compounds I, II [R = 5-iodo-2-methyl-Ph, 1-naphthylmethyl], III were in the range (59.28-93.4) %, with highest stabilization value by compound II [R = 1-naphthylmethyl], which also displayed higher binding affinity with -7.6 kcal/mol towards COX2. Thus, the synthesized sym. 1,3-diketones I, II [R = 5-iodo-2-methyl-Ph, 1-naphthylmethyl], III with suitable functionality can be both anticancer and anti-inflammatory agents.

The article 《Synthesis, characterization, in-silico and in-vitro evaluations of symmetrical 1,3-diketones》 also mentions many details about this compound(498-95-3)SDS of cas: 498-95-3, you can pay attention to it, because details determine success or failure

Reference:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Synthesis and biological evaluation of α- and β-hydroxy substituted amino acid derivatives as potential mGAT1-4 inhibitors, published in 2020-08-31, which mentions a compound: 498-95-3, Name is Piperidine-3-carboxylic acid, Molecular C6H11NO2, Name: Piperidine-3-carboxylic acid.

Abstract: In this study, we report the synthesis and biol. evaluation of a variety of α- and β-hydroxy substituted amino acid derivatives as potential amino acid subunits in inhibitors of GABA uptake transporters (GATs). In order to ensure that the test compounds adopt a binding pose similar to that presumed for related larger GAT inhibitors, lipophilic residues were introduced either at the amino nitrogen atom or at the alc. function. Several of the synthesized compounds were found to exhibit similar inhibitory activity at the GAT subtypes mGAT2, mGAT3, and mGAT4, resp., as compared with the reference N-butylnipecotic acid. Hence, these compounds might serve as starting point for future developments of more complex GAT inhibitors.

The article 《Synthesis and biological evaluation of α- and β-hydroxy substituted amino acid derivatives as potential mGAT1-4 inhibitors》 also mentions many details about this compound(498-95-3)Name: Piperidine-3-carboxylic acid, you can pay attention to it, because details determine success or failure

Reference:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Electrochemical [4+2] Annulation-Rearrangement-Aromatization of Styrenes: Synthesis of Naphthalene Derivatives, published in 2019, which mentions a compound: 498-95-3, Name is Piperidine-3-carboxylic acid, Molecular C6H11NO2, Synthetic Route of C6H11NO2.

We report the first electrochem. strategy to synthesize functionalized naphthalene derivatives through [4+2] annulation-rearrangement-aromatization from styrenes under mild conditions [e.g., 4-methoxy-α-methylstyrene → 7-methoxy-2-(4-methoxyphenyl)-1,4-dimethylnaphthalene (67%)]. The electrolysis does not require metals, oxidants and high valence substrates, indicating the atom and step-economy ideals. The dehydrodimer produced through [4+2] cycloaddition of 4-methoxy-α-methylstyrene is isolated and proved to be the key intermediate for the following oxydehydrogenation to form carbon cation, which undergoes rearrangement-aromatization to afford the final products. This reaction represents a powerful access to construct multi-substituted naphthalene blocks in a single step.

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Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Computed Properties of C6H11NO2. The protonation of heteroatoms in aromatic heterocycles can be divided into two categories: lone pairs of electrons are in the aromatic ring conjugated system; and lone pairs of electrons do not participate. Compound: Piperidine-3-carboxylic acid, is researched, Molecular C6H11NO2, CAS is 498-95-3, about Discovery of CYR715: A novel carboxylic acid-containing soluble guanylate cyclase stimulator. Author is Rennie, Glen R.; Barden, Timothy C.; Bernier, Sylvie G.; Carvalho, Andrew; Deming, Renee; Germano, Peter; Hudson, Colleen; Im, G-Yoon J.; Iyengar, Rajesh R.; Jia, Lei; Jung, Joon; Kim, Elise; Lee, Thomas W.-H.; Mermerian, Ara; Moore, Joel; Nakai, Takashi; Perl, Nicholas R.; Tobin, Jenny; Zimmer, Daniel P.; Renhowe, Paul A..

Soluble guanylate cyclase (sGC) is a clin. validated therapeutic target in the treatment of pulmonary hypertension. Modulators of sGC have the potential to treat diseases that are affected by dysregulation of the NO-sGC-cGMP signal transduction pathway. This letter describes the SAR efforts that led to the discovery of CYR715, a novel carboxylic acid-containing sGC stimulator, with an improved metabolic profile relative to our previously described stimulator, IWP-051. CYR715 addressed potential idiosyncratic drug toxicity (IDT) liabilities associated with the formation of reactive, migrating acyl glucuronides (AG) found in related carboxylic acid-containing analogs and demonstrated high oral bioavailability in rat and dose-dependent hemodynamic pharmacol. in normotensive Sprague-Dawley rats.

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Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: Piperidine-3-carboxylic acid(SMILESS: O=C(C1CNCCC1)O,cas:498-95-3) is researched.Formula: C8H12I2Pt. The article 《Midazolam Exposure Impedes Oligodendrocyte Development via the Translocator Protein and Impairs Myelination in Larval Zebrafish》 in relation to this compound, is published in Molecular Neurobiology. Let’s take a look at the latest research on this compound (cas:498-95-3).

Anesthetics are commonly used in various medical procedures. Accumulating evidence suggests that early-life anesthetics exposure in infants and children affects brain development, causing psychiatric and neurol. disorders. However, the underlying mechanisms are poorly understood. Using zebrafish larvae as a model, we found that the proliferation and migration of oligodendrocyte progenitor cells (OPCs) were severely impaired by the exposure of midazolam (MDZ), an anesthetic widely used in pediatric surgery and intensive care medicine, leading to a reduction of oligodendroglial lineage cell in the dorsal spinal cord. This defect was mimicked by the bath application of translocator protein (TSPO) agonists and partially rescued by genetic downregulation of TSPO. Cell transplantation experiments showed that requirement of TSPO for MDZ-induced oligodendroglial lineage cell defects is cell-autonomous. Furthermore, transmission electron microscopy and in vivo electrophysiol. recording experiments demonstrated that MDZ exposure caused axon hypomyelination and action potential propagation retardation, resulting in delayed behavior initiation. Thus, our findings reveal that MDZ affects oligodendroglial lineage cell development and myelination in young animals, raising the care about its clinic use in infants and children.

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Reference:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Dhanawat, Meenakshi; Gupta, Sumeet; Mehta, Dinesh Kumar; Das, Rina researched the compound: Piperidine-3-carboxylic acid( cas:498-95-3 ).Recommanded Product: 498-95-3.They published the article 《Design, Synthesis and Enhanced BBB Penetration Studies of L-serine-Tethered Nipecotic Acid-Prodrug》 about this compound( cas:498-95-3 ) in Drug Research (Stuttgart, Germany). Keywords: pentylenetetrazole serine nipecotic acid blood brain barrier. We’ll tell you more about this compound (cas:498-95-3).

Nipecotic acid is considered to be one of the most potent inhibitors of neuronal and glial-aminobutyric acid (GABA) uptake in vitro. Due to its hydrophilic nature, nipecotic acid does not readily cross the blood-brain barrier (BBB). Large neutral amino acids (LAT1)-knotted nipecotic acid prodrug was designed and synthesized with the aim to enhance the BBB permeation by the use of carrier-mediated transport. The synthesized prodrug was tested in animal models of Pentylenetetrazole (PTZ)-induced convulsions in mice. Further pain studies were carried out followed by neurotoxicity estimation by writhing and rota-rod test resp. HPLC data suggests that the synthesized prodrug has improved penetration through BBB. Nipecotic acid-L-serine ester prodrug with considerable anti-epileptic activity, and the ability to permeate the BBB has been successfully synthesized.

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Reference:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

SDS of cas: 498-95-3. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: Piperidine-3-carboxylic acid, is researched, Molecular C6H11NO2, CAS is 498-95-3, about Synthesis and Biological Evaluation of Nipecotic Acid and Guvacine Derived 1,3-Disubstituted Allenes as Inhibitors of Murine GABA Transporter mGAT1. Author is Schaarschmidt, Maren; Hoefner, Georg; Wanner, Klaus T..

A new class of nipecotic acid I [R = Ph, 2-fluorophenyl, 4-biphenyl, etc.] and guvacine derivatives II [R1 = 2,4-difluoropheny, 2,4-dichlorophenyl, 2-phenylphenyl] were synthesized and characterized for their inhibitory potency at mGAT1-4 and binding affinity for mGAT1. Compounds I and II were defined by a four-carbon-atom allenyl spacer connecting the nitrogen atom of the nipecotic acid or guvacine head with an aromatic residue. Among the compounds investigated, the mixture of nipecotic acid derivatives I [R = terphenyl] possessing an o-terphenyl residue, was identified as highly selective and the most potent mGAT1 inhibitor in this study. For the (R)-nipecotic acid derived from of compound I [R = terphenyl], the inhibitory potency in [3H]GABA uptake assays was determined as pIC50=6.78±0.08, and the binding affinity in MS Binding Assays as pKi=7.10±0.12. The synthesis of the designed compounds I and II was carried out by a two-step procedure, generating the allene moiety via allenylation of terminal alkynes which allowed broad variation of the terminal Ph and biphenyl subunit.

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Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics