Category: 498-95-3

In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Synthesis and biological evaluation of fluorescent GAT-ligands based on asymmetric substituted BODIPY dyes, published in 2020-04-30, which mentions a compound: 498-95-3, mainly applied to fluorescent GAT ligand asymmetry BODIPY dye, Recommanded Product: 498-95-3.

The present study aimed at the development of fluorescent inhibitors addressing the GABA transporters mGAT1-mGAT4 as potential tool compounds in fluorescence based biol. assays. The design of these fluorescent GAT inhibitors followed the structural motifs common for many GAT1-GAT4 inhibitors publicly known except that the lipophilic domain present in this compounds was replaced by a BODIPY moiety to serve as a fluorescent subunit. The fluorescent compounds obtained that way were tested for their inhibitory potencies and subtype selectivities at the four murine GABA transporter subtypes mGAT1-mGAT4 and for their binding affinity for mGAT1. All BODIPY derivatives displayed only low inhibitory potencies and subtype selectivities at the GABA transport proteins mGAT1-mGAT4, as well as low affinities for mGAT1. Still, compounds were found with reasonable binding affinities towards mGAT1 (pKi ∼ 5.0) and inhibitory potencies at mGAT2 and mGAT4 (pIC50 ∼ 5.0).

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Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Electric Literature of C6H11NO2. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: Piperidine-3-carboxylic acid, is researched, Molecular C6H11NO2, CAS is 498-95-3, about Synthesis and Initial Characterization of a Reversible, Selective 18F-Labeled Radiotracer for Human Butyrylcholinesterase. Author is Gentzsch, Christian; Chen, Xinyu; Spatz, Philipp; Kosak, Urban; Knez, Damijan; Nose, Naoko; Gobec, Stanislav; Higuchi, Takahiro; Decker, Michael.

A neuropathol. hallmark of Alzheimer′s disease (AD) is the presence of amyloid-β (Aβ) plaques in the brain, which are observed in a significant number of cognitively normal, older adults as well. In AD, butyrylcholinesterase (BChE) becomes associated with Aβ aggregates, making it a promising target for imaging probes to support diagnosis of AD. In this study, we present the synthesis, radiochem., in vitro and preliminary ex and in vivo investigations of a selective, reversible BChE inhibitor as PET-tracer for evaluation as an AD diagnostic. Radiolabeling of the inhibitor was achieved by fluorination of a resp. tosylated precursor using K[18F]. IC50 values of the fluorinated compound were obtained in a colorimetric assay using recombinant, human (h) BChE. Dissociation constants were determined by measuring hBChE activity in the presence of different concentrations of inhibitor. Radiofluorination of the tosylate precursor gave the desired radiotracer in an average radiochem. yield of 20 ± 3 %. Identity and > 95.5 % radiochem. purity were confirmed by HPLC and TLC autoradiog. The inhibitory potency determined in Ellman′s assay gave an IC50 value of 118.3 ± 19.6 nM. Dissociation constants measured in kinetic experiments revealed lower affinity of the inhibitor for binding to the acylated enzyme (K2 = 68.0 nM) in comparison to the free enzyme (K1 = 32.9 nM). The reversibly acting, selective radiotracer is synthetically easily accessible and retains promising activity and binding potential on hBChE. Radiosynthesis with 18F labeling of tosylates was feasible in a reasonable time frame and good radiochem. yield.

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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.Li, Yuanyuan; Zhang, Shengnan; Wang, Rong; Cui, Menghan; Liu, Wei; Yang, Qing; Kuang, Chunxiang researched the compound: Piperidine-3-carboxylic acid( cas:498-95-3 ).COA of Formula: C6H11NO2.They published the article 《Synthesis of novel tryptanthrin derivatives as dual inhibitors of indoleamine 2,3-dioxygenase 1 and tryptophan 2,3-dioxygenase》 about this compound( cas:498-95-3 ) in Bioorganic & Medicinal Chemistry Letters. Keywords: tryptanthrin derivative preparation dual inhibitor indoleamine dioxygenase tryptophan dioxygenase; IDO1 inhibitor; IDO1/TDO dual inhibitor; Novel tryptanthrin derivative; TDO inhibitor; Water solubility. We’ll tell you more about this compound (cas:498-95-3).

Indoleamine 2,3-dioxygenase 1 (IDO1) and tryptophan 2,3-dioxygenase (TDO) are promising drug development targets due to their implications in pathologies such as cancer and neurodegenerative diseases. The search for IDO1 inhibitor has been intensely pursued but there is a paucity of potent TDO and IDO1/TDO dual inhibitors. Natural product tryptanthrin (indolo[2,1-b]quinazoline-6,12-dione) has been confirmed to bear IDO1 and/or TDO inhibitory activities. Herein, twelve novel tryptanthrin derivatives were synthesized and evaluated for the IDO1 and TDO inhibitory potency. All of the compounds were found to be IDO1/TDO dual inhibitors, in particular, compound I [R = (E)-CH:CHCO2Et, (E)-CH:CHCO2H] bore IDO1 inhibitory activity similar to that of INCB024360; and compound I [R = CHO, (E)-CH:CHCO2H] had remarkable TDO inhibitory activity superior to that of the well-known TDO inhibitor LM10. This work enriches the collection of IDO1/TDO dual inhibitors and provides chem. mols. for potential development into drugs.

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The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: Piperidine-3-carboxylic acid, is researched, Molecular C6H11NO2, CAS is 498-95-3, about Synthesis, spectral characterization, and biological studies of 3,5-disubstituted-1,3,4-oxadiazole-2(3H)-thione derivatives, the main research direction is dichlorophenyl oxadiazolethione piperidine preparation antitumor antibacterial antifungal antiyeast activity; antibacterial activity; cytotoxicity; piperidine; 1,3,4-Oxadiazole.Product Details of 498-95-3.

The reaction of 3,4-dichlorophenyl-1,3,4-oxadiazole-2(3H)-thione with piperidine derivatives I (R = H, ethoxycarbonyl; R1 = H, carboxy, ethoxycarbonyl; R2 = H, OH, CN, acetyl; R3 = ethoxycarbonyl, Ph, morpholin-4-yl, etc.) via Mannich reaction was used to generate eleven novel compounds in moderate to good yields. Antimicrobial activity and cytotoxicity studies were done by disk diffusion and NCI-60 sulfordamine B assay methods. The antimicrobial test results revealed that synthesized compounds I have better activity against gram-pos. species than gram-neg. ones. A total anal. of the antibacterial, antifungal, and antiyeast activity revealed that newly synthesized compounds I were really active against Bacillus cereus, Bacillus ehimensis, and Bacillus thuringiensis species. For cytotoxicity, among three different cancer cell lines (HCT116, MCF7, HUH7) compounds I [R = R1 = H, R2 = acetyl, R3 = Ph (II); R = R1 = H, R2 = CN, R3 = Ph (III); R = R1 = R2 = H, R3 = Bn (IV); R = R1 = R2 = H, R3 = morpholin-4-yl (V); R = R1 = R2 = H, R3 = carboxy (VI); R = R1 = R2 = H, R3 = ethoxycarbonyl (VII); R = H, R1 = ethoxycarbonyl, R2 = R3 = H (VIII); and R = ethoxycarbonyl, R1 = R2 = R3 = H] were seemed especially effective on HUH7 cancer cell line via moderate to good activity. More significantly, against liver carcinoma cell line (HUH7) most of the compounds of the series (II, III, IV, V, VI, VII, and VIII) have better IC50 values (IC50 = 18.78μM) than 5-Fluorouracil (5-FU) and also compound III possessed 10.1μM value, which represents good druggable cytotoxic activity. Further, the mols. I were also screened for in silico chemoinformatic and toxicity data to gather the predicted bioavailability and safety measurements.

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The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: Piperidine-3-carboxylic acid, is researched, Molecular C6H11NO2, CAS is 498-95-3, about RASS-Enabled S/P-C and S-N Bond Formation for DEL Synthesis, the main research direction is RASS enabled bond formation DNA encoded library; DNA encoded library; nickel cross-coupling; reversible adsorption to solid support; sulfonamide; sulfone.Quality Control of Piperidine-3-carboxylic acid.

DNA encoded libraries (DEL) showed promise as a valuable technol. for democratizing the hit discovery process. Although DEL provides relatively inexpensive access to libraries of unprecedented size, their production has been hampered by the idiosyncratic needs of the encoding DNA tag relegating DEL compatible chem. to dilute aqueous environments. Recently reversible adsorption to solid support (RASS) has been demonstrated as a promising method to expand DEL reactivity using standard organic synthesis protocols. Here the authors demonstrate a suite of on-DNA chemistries to incorporate medicinally relevant and C-S, C-P and N-S linkages into DELs, which are underrepresented in the canonical methods.

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

Related Products of 498-95-3. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: Piperidine-3-carboxylic acid, is researched, Molecular C6H11NO2, CAS is 498-95-3, about A convenient catalytic silicon-assisted route towards new non-proteinogenic amino acids with methylenebisphosphonic acids moieties. Author is Prishchenko, Andrey A.; Alekseyev, Roman S.; Livantsov, Mikhail V.; Novikova, Olga P.; Livantsova, Ludmila I.; Petrosyan, Valery S..

The new non-proteinogenic amino acids with methylenebisphosphonic acids moieties are synthesized for the first time via unique reaction of tris(trimethylsilyl) phosphite and various N-formyl amino acids at the presence of effective catalyst – trimethylsilyl triflate under mild conditions. The further treatment of initially formed trimethylsilyl intermediates with the methanol excess resulted in the water-soluble non-proteinogenic amino acids with methylenebisphosphonic acids moieties in high yields. The catalytic scheme of target substances formation is proposed and discussed in detail. The structures of target functionalized amino acids and their precursors were confirmed by the 1H, 13C, 31P NMR spectra and high resolution mass spectra. The resulted compounds are of great interest as promising antiviral substances and effective ligands.

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

Downes, Thomas D.; Jones, S. Paul; Klein, Hanna F.; Wheldon, Mary C.; Atobe, Masakazu; Bond, Paul S.; Firth, James D.; Chan, Ngai S.; Waddelove, Laura; Hubbard, Roderick E.; Blakemore, David C.; De Fusco, Claudia; Roughley, Stephen D.; Vidler, Lewis R.; Whatton, Maria Ann; Woolford, Alison J.-A.; Wrigley, Gail L.; O’Brien, Peter published an article about the compound: Piperidine-3-carboxylic acid( cas:498-95-3,SMILESS:O=C(C1CNCCC1)O ).SDS of cas: 498-95-3. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:498-95-3) through the article.

Fragment screening collections were often predominantly populated with flat, 2D mols. A workflow for the design and synthesis of 56 3D disubstituted pyrrolidine and piperidine fragments that occupy under-represented areas of fragment space (as demonstrated by a principal moments of inertia (PMI) anal.) was described. A key, and unique, underpinning design feature of this fragment collection was that assessment of fragment shape and conformational diversity (by considering conformations up to 1.5 kcal mol-1 above the energy of the global min. energy conformer) was carried out prior to synthesis and was also used to select targets for synthesis. The 3D fragments were designed to contain suitable synthetic handles for future fragment elaboration. Finally, by comparing our 3D fragments with six com. libraries, it was clear that our collection was high three-dimensionality and shape diversity.

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Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Formula: 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 TDP-43 regulates GAD1 mRNA splicing and GABA signaling in Drosophila CNS. Author is Romano, Giulia; Holodkov, Nikola; Klima, Raffaella; Feiguin, Fabian.

Alterations in the function of the RNA-binding protein TDP-43 are largely associated with the pathogenesis of amyotrophic lateral sclerosis (ALS), a devastating disease of the human motor system that leads to motoneurons degeneration and reduced life expectancy by mol. mechanisms not well known. In our previous work, we found that the expression levels of the glutamic acid decarboxylase enzyme (GAD1), responsible for converting glutamate to γ-aminobutyric acid (GABA), were downregulated in TBPH-null fies and motoneurons derived from ALS patients carrying mutations in TDP-43, suggesting that defects in the regulation of GAD1 may lead to neurodegeneration by afecting neurotransmitter balance. In this study, we observed that TBPH was required for the regulation of GAD1 pre-mRNA splicing and the levels of GABA in the Drosophila central nervous system (CNS). Interestingly, we discovered that pharmacol. treatments aimed to potentiate GABA neurotransmission were able to revert locomotion defciencies in TBPH-minus fies, revealing novel mechanisms and therapeutic strategies in ALS.

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The reaction of an aromatic heterocycle with a proton is called a protonation. One of articles about this theory is 《Revised Pharmacophore Model for 5-HT2A Receptor Antagonists Derived from the Atypical Antipsychotic Agent Risperidone》. Authors are Shah, Urjita H.; Gaitonde, Supriya A.; Moreno, Jose L.; Glennon, Richard A.; Dukat, Malgorzata; Gonzalez-Maeso, Javier.The article about the compound:Piperidine-3-carboxylic acidcas:498-95-3,SMILESS:O=C(C1CNCCC1)O).Name: Piperidine-3-carboxylic acid. Through the article, more information about this compound (cas:498-95-3) is conveyed.

Pharmacophore models for 5-HT2A receptor antagonists consist of two aromatic/hydrophobic regions at a given distance from a basic amine. We have previously shown that both aromatic/hydrophobic moieties are unnecessary for binding or antagonist action. Here, we deconstructed the 5-HT2A receptor antagonist/serotonin-dopamine antipsychotic agent risperidone into smaller structural segments that were tested for 5-HT2A receptor affinity and function. We show, again, that the entire risperidone structure is unnecessary for retention of affinity or antagonist action. Replacement of the 6-fluoro-3-(4-piperidinyl)-1,2-benz[d]isoxazole moiety by isosteric tryptamines resulted in retention of affinity and antagonist action. Addnl., 3-(4-piperidinyl)-1,2-benz[d]isoxazole (10), which represents less than half the structural features of risperidone, retains both affinity and antagonist actions. 5-HT2A receptor homol. modeling/docking studies suggest that 10 binds in a manner similar to risperidone and that there is a large cavity to accept various N4-substituted analogs of 10 such as risperidone and related agents. Alterations of this “”extended”” moiety improve receptor binding and functional potency. We propose a new risperidone-based pharmacophore for 5-HT2A receptor antagonist action.

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Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: Piperidine-3-carboxylic acid, is researched, Molecular C6H11NO2, CAS is 498-95-3, about Microglial expression of GAT-1 in the cerebral cortex..Related Products of 498-95-3.

Microglial cells are the immune cells of the brain that, by sensing the microenvironment, permit a correct brain development and function. They communicate with other glial cells and with neurons, releasing and responding to a number of molecules that exert effects on surrounding cells. Among these, neurotransmitters and, in particular, gamma-aminobutyric acid (GABA) has recently gained interest in this context. We demonstrated the expression of GABA transporter 1 (GAT-1) in microglial cells both in soma and cell processes. We show that microglial cell treatment with 1,2,5,6-tetrahydro-1-[2-[[(diphenylmethylene)amino]oxy]ethyl]-3-pyridinecarboxylic acid hydrochloride (NNC-711), a potent and selective GAT-1 inhibitor, significantly reduced Na+ -dependent GABA uptake. On the other hand, GABA uptake was significantly increased by cell treatment with (S)-1-[2-[tris(4-methoxyphenyl)methoxy]ethyl]-3-piperidinecarboxylic acid (SNAP-5114), a GAT-2/3 inhibitor, and this effect was completely blocked by the botulinum toxin BoNT/C1, that specifically cleaves and inactives syntaxin 1A (STX1A). Overall, these findings show that microglial cells express GAT-1 and indicate that STX1A plays an important role in the regulation of GAT-1-dependent GABA uptake in microglia.

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