Tag: 300-400

Soluble Epoxide Hydrolase Inhibition Attenuates MPTP-Induced Neurotoxicity in the Nigrostriatal Dopaminergic System: Involvement of α-Synuclein Aggregation and ER Stress was written by Huang, Hui-Ju;Wang, Yi-Ting;Lin, Hui-Ching;Lee, Yi-Hsuan;Lin, Anya Maan-Yuh. And the article was included in Molecular Neurobiology in 2018.Application of 1222780-33-7 The following contents are mentioned in the article:

Soluble epoxide hydrolase (sEH) is widely expressed in the mammalian brain and possesses dual enzymic activities, including C-terminal epoxide hydrolase (C-EH) which degrades epoxyeicosatrienoic acid (EET), a beneficial arachidonic acid metabolite. In the present study, the neuroprotective effect of sEH inhibition on 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced neurodegeneration of nigrostriatal dopaminergic system was investigated using genetic and pharmacol. approaches. MPTP (15 mg/kg) was i.p. injected in sEH knockout (KO) mice and C57BL/6J mice as wild-type (WT) mice. Compared with the MPTP-treated WT mice, MPTP-induced reductions in striatal dopamine content and nigral tyrosine hydroxylase level (TH, a biomarker of dopaminergic neurons) were less significant in the treated sEH mice. Furthermore, MPTP-induced HO-1 elevation (a redox-regulated protein), α-synuclein aggregation, and caspase 12 activation (a hallmark of ER stress) were less prominent in sEH KO mice than in WT mice. These data indicate that sEH KO mice are more resistant to MPTP-induced neurotoxicity. The pharmacol. effect of N-[1-(1-oxopropyl)-4-piperidinyl]-N0-[4-(trifluoromethoxy)phenyl]-urea (TPPU, an sEH inhibitor) on MPTP-induced neurotoxicity was investigated in WT mice. TPPU (1 mg/kg, i.p.) attenuated MPTP-induced reduction in striatal dopamine content, TH-pos. cell numbers, TH, and pro-caspase 9 protein levels (an initiator caspase of apoptosis) in mouse SN. Moreover, TPPU reduced MPTP-induced HO-1 elevation, α-synuclein aggregation and caspase 12 activation, indicating that TPPU is effective in attenuating MPTP-induced oxidative stress, apoptosis, protein aggregation, and ER stress. In conclusion, our study suggests that sEH is a potential target for developing therapies for parkinsonism. Furthermore, sEH inhibitors may be of clin. significance for treating CNS neurodegenerative diseases. This study involved multiple reactions and reactants, such as 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7Application of 1222780-33-7).

1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N–H bond in an axial position, and the other in an equatorial position.Application of 1222780-33-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Anti-inflammatory treatment with a soluble epoxide hydrolase inhibitor attenuates seizures and epilepsy-associated depression in the LiCl-pilocarpine post-status epilepticus rat model was written by Shen, Yijun;Peng, Weifeng;Chen, Qinglan;Hammock, Bruce D.;Liu, Junyan;Li, Dongyang;Yang, Jun;Ding, Jing;Wang, Xin. And the article was included in Brain, Behavior, and Immunity in 2019.Recommanded Product: 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea The following contents are mentioned in the article:

This study aimed to investigate whether 1-trifluoromethoxyphenyl-3-(1-propionylpiperidin-4-yl) urea (TPPU), a soluble epoxide hydrolase inhibitor with anti-inflammatory effects, could alleviate spontaneous recurrent seizures (SRS) and epilepsy-associated depressive behaviors in the lithium chloride (LiCl)-pilocarpine-induced post-status epilepticus (SE) rat model. The rats were i.p. (IP) injected with LiCl (127 mg/kg) and pilocarpine (40 mg/kg) to induce SE. A video surveillance system was used to monitor SRS in the post-SE model for 6 wk (from the onset of the 2nd week to the end of the 7th week after SE induction). TPPU (0.1 mg/kg/d) was intragastrically given for 4 wk from the 21st day after SE induction in the SRS + 0.1 TPPU group. The SRS + PEG 400 group was given the vehicle (40% polyethylene glycol 400) instead, and the control group was given LiCl and PEG 400 but not pilocarpine. The sucrose preference test (SPT) and forced swim test (FST) were conducted to evaluate the depression-like behaviors of rats. Immunofluorescent staining, ELISA, and western blot anal. were performed to measure astrocytic and microglial gliosis, neuronal loss, and levels of soluble epoxide hydrolase (sEH), cytokines [tumor necrosis factor alpha (TNF-α), interleukin (IL)-1β, and IL-6], and cyclic adenosine monophosphate (cAMP)-response element binding protein (CREB). The frequency of SRS was significantly decreased at 6 wk and 7 wk after SE induction in the 0.1TPP U group compared with the SRS + PEG 400 group. The immobility time (IMT) evaluated by FST was significantly decreased, whereas the climbing time (CMT) was increased, and the sucrose preference rate (SPR) evaluated by SPT was in an increasing trend. The levels of sEH, TNF-α, IL-1β, and IL-6 in the hippocampus (Hip) and prefrontal cortex (PFC) were all significantly increased in the SRS + PEG 400 group compared with the control group; neuronal loss, astrogliosis, and microglial activation were also observed The astrocytic and microglial activation and levels of the pro-inflammatory cytokines in the Hip and PFC were significantly attenuated in the TPPU group compared with the SRS + PEG 400 group; moreover, neuronal loss and the decreased CREB expression were significantly alleviated as well. TPPU treatment after SE attenuates SRS and epilepsy-associated depressive behaviors in the LiCl-pilocarpine induced post-SE rat model, and it also exerts anti-inflammatory effects in the brain. Our findings suggest a new therapeutic approach for epilepsy and its comorbidities, especially depression. This study involved multiple reactions and reactants, such as 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7Recommanded Product: 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea).

1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7) belongs to piperidine derivatives. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising α-glucosidase inhibitors. The former are analogs of DNJ with an improved α-glucosidase inhibitory profile than that of DNJ. Boisson et al.Recommanded Product: 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Inhibition of soluble epoxide hydrolase offers protection against fructose-induced diabetes and related metabolic complications in rats was written by Shah, S. Ali;Mehmood, M. H.;Khan, M.;Bukhari, I. Ali;Alorainey, B. I.;Vohra, F.. And the article was included in Journal of Physiology and Pharmacology in 2020.Name: 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea The following contents are mentioned in the article:

Stabilization of epoxyeicosatrienoic acids (EETs) levels via soluble epoxide hydrolase (sEH) deletion or its pharmacol. inhibition have been shown to have beneficial effects on inflammation, ischemia, hypertension and diabetes. Owing to the diverse role of EETs, current study was designed to evaluate the therapeutic potential of 1-trifluoromethoxyphenyl-3-(1-propionylpiperidine-4-yl) urea (TPPU), a novel sEHI against fructose-induced diabetes and related complications in rats. Sprague-Dawley rats (200 – 230 g) were divided into four different groups, each containing 10 animals. One group served as a normal control and received standard diet and drinking water. The second group served as a diseased control and received standard diet, 25% fructose in drinking water and was treated with vehicle only. The third and fourth groups received standard diet, 25% fructose in drinking water and TPPU (2 mg/kg) or metformin (150 mg/kg), resp. All treatments were given orally for 12 wk. At the end of the study, blood samples were collected to measure serum insulin levels and other biochem. parameters. Animals were dissected to collect tissue specimens for histol. and immunohistochem. anal. Animals fed on fructose and treated with vehicle demonstrated elevated blood insulin and glucose levels as well as high levels (P < 0.001) of triglycerides (TGs), cholesterol, low-d. lipoprotein (LDL) and homeostatic model assessment of insulin resistance (HOMA-IR) compared to naive rats. Similarly, the levels of alk. phosphatase (ALP), alanine aminotransferase (ALT), urea and uric acid were significantly (P < 0.001) increased in vehicle treated fructose fed animals. TPPU (2 mg/kg p.o.) and simultaneously fed on fructose for 12 wk substantially decreased HOMA-IR levels, lowered blood glucose, serum cholesterol, LDLs and TGs while high-d. lipoproteins (HDL) levels were increased compared to untreated animals. Metformin, a standard reference drug showed similar results. Microscopic studies of liver and pancreatic sections of TPPU treated animals showed marked improvement in cellular architecture compared to untreated animals. Current study demonstrated profound therapeutic potential of TPPU against fructose induced-diabetes and related metabolic complications which was evident by its attenuating effect fructose-induced hyperglycemia, hyperlipidemia and impaired renal and hepatic serum markers. This study involved multiple reactions and reactants, such as 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7Name: 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea).

1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising α-glucosidase inhibitors. The former are analogs of DNJ with an improved α-glucosidase inhibitory profile than that of DNJ. Boisson et al.Name: 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Tip-enhanced Raman spectroscopy of bradykinin and its B₂ receptor antagonists adsorbed onto colloidal suspended Ag nanowires was written by Swiech, D.;Tanabe, I.;Vantasin, S.;Sobolewski, D.;Ozaki, Y.;Prahl, A.;Mackowski, S.;Proniewicz, E.. And the article was included in Physical Chemistry Chemical Physics in 2015.Computed Properties of C21H21NO4 The following contents are mentioned in the article:

The tip-enhanced Raman scattering (TERS) spectra of bradykinin (BK) and its potent B₂ BK receptor antagonists, [D-Arg⁰,Hyp³,Thi^5,8,L-Pip⁷]BK and [D-Arg⁰,Hyp³,Thi⁵,D-Phe⁷,L-Pip⁸]BK, approx. with a size of about 40 nm, adsorbed onto colloidal suspended Ag nanowires with diameter in the range of 350-500 nm and length of 2-50 μm were recorded. The metal surface plasmon resonance and morphol. of the Ag nanowires were studied by UV-visible (UV-Vis) spectroscopy and SEM (SEM). Briefly, it was shown that two C-terminal amino acids of BK and [D-Arg⁰,Hyp³,Thi^5,8,L-Pip⁷]BK are involved in the interaction with the colloidal suspended Ag nanowire surface, whereas three last amino acids of the [D-Arg⁰,Hyp³,Thi⁵,D-Phe⁷,L-Pip⁸]BK sequence attached the Ag surface. Thus, BK adsorbs on the colloidal suspended Ag nanowires mainly through the Phe^5/8 ring (tilted orientation) and the one oxygen atom of the carboxylate group and the H₂N-C-NH-CH₂– fragment of Arg⁹. In the case of [D-Arg⁰,Hyp³,Thi^5,8,L-Pip⁷]BK, the Thi⁸ ring (through the lone electron pair on the sulfur atom) and the both oxygen atoms of the carboxylate group and the amine group of Arg⁹ mainly participated in the interaction with the Ag nanowire surface. For [D-Arg⁰,Hyp³,Thi⁵,D-Phe⁷,L-Pip⁸]BK, the D-Phe⁷ ring, the Pip⁸ ring, and the Arg⁹ side-chain assisted in the peptide interaction with the Ag surface. The obtained results emphasize the importance of the C-terminal part of these peptides in the adsorption process onto the colloidal suspended Ag nanowires. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Computed Properties of C21H21NO4).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. Several piperidine alkaloids isolated from natural herbs, were found to exhibit antiproliferation and antimetastatic effects on various types of cancers both in vitro and in vivo for example Piperine, Evodiamine, Matrine, Berberine and Tetrandine.Computed Properties of C21H21NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Tip-enhanced Raman spectroscopy of bradykinin and its B₂ receptor antagonists adsorbed onto colloidal suspended Ag nanowires was written by Swiech, D.;Tanabe, I.;Vantasin, S.;Sobolewski, D.;Ozaki, Y.;Prahl, A.;Mackowski, S.;Proniewicz, E.. And the article was included in Physical Chemistry Chemical Physics in 2015.HPLC of Formula: 86069-86-5 The following contents are mentioned in the article:

The tip-enhanced Raman scattering (TERS) spectra of bradykinin (BK) and its potent B₂ BK receptor antagonists, [D-Arg⁰,Hyp³,Thi^5,8,L-Pip⁷]BK and [D-Arg⁰,Hyp³,Thi⁵,D-Phe⁷,L-Pip⁸]BK, approx. with a size of about 40 nm, adsorbed onto colloidal suspended Ag nanowires with diameter in the range of 350-500 nm and length of 2-50 μm were recorded. The metal surface plasmon resonance and morphol. of the Ag nanowires were studied by UV-visible (UV-Vis) spectroscopy and SEM (SEM). Briefly, it was shown that two C-terminal amino acids of BK and [D-Arg⁰,Hyp³,Thi^5,8,L-Pip⁷]BK are involved in the interaction with the colloidal suspended Ag nanowire surface, whereas three last amino acids of the [D-Arg⁰,Hyp³,Thi⁵,D-Phe⁷,L-Pip⁸]BK sequence attached the Ag surface. Thus, BK adsorbs on the colloidal suspended Ag nanowires mainly through the Phe^5/8 ring (tilted orientation) and the one oxygen atom of the carboxylate group and the H₂N-C-NH-CH₂– fragment of Arg⁹. In the case of [D-Arg⁰,Hyp³,Thi^5,8,L-Pip⁷]BK, the Thi⁸ ring (through the lone electron pair on the sulfur atom) and the both oxygen atoms of the carboxylate group and the amine group of Arg⁹ mainly participated in the interaction with the Ag nanowire surface. For [D-Arg⁰,Hyp³,Thi⁵,D-Phe⁷,L-Pip⁸]BK, the D-Phe⁷ ring, the Pip⁸ ring, and the Arg⁹ side-chain assisted in the peptide interaction with the Ag surface. The obtained results emphasize the importance of the C-terminal part of these peptides in the adsorption process onto the colloidal suspended Ag nanowires. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5HPLC of Formula: 86069-86-5).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.HPLC of Formula: 86069-86-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Unbiased Molecular Dynamics of 11 min Timescale Drug Unbinding Reveals Transition State Stabilizing Interactions was written by Lotz, Samuel D.;Dickson, Alex. And the article was included in Journal of the American Chemical Society in 2018.Electric Literature of C16H20F3N3O3 The following contents are mentioned in the article:

Ligand (un)binding kinetics is being recognized as a determinant of drug specificity and efficacy in an increasing number of systems. However, the calculation of kinetics and the simulation of drug unbinding is more difficult than computing thermodn. quantities, such as binding free energies. Here we present the first full simulations of an unbinding process at pharmacol. relevant time scales (11 min), without the use of biasing forces, detailed prior knowledge, or specialized processors using the weighted ensemble based algorithm, WExplore. These simulations show the inhibitor TPPU unbinding from its enzyme target soluble epoxide hydrolase, which is a clin. relevant target that has attracted interest in kinetics optimization in order to increase efficacy. We make use of conformation space networks that allow us to conceptualize unbinding not just as a linear process, but as a network of interconnected states that connect the bound and unbound states. This allows us to visualize patterns in hydrogen-bonding, solvation, and nonequilibrium free energies, without projection onto progress coordinates. The topol. and layout of the network reveal multiple unbinding pathways, and other rare events, such as the reversal of ligand orientation within the binding site. Furthermore, we make a prediction of the transition state ensemble, using transition path theory, and identify protein-ligand interactions which are stabilizing to the transition state. Addnl., we uncover trends in ligand and binding site solvation that corroborate exptl. evidence from more classical structure kinetics relationships and generate new questions as to the role of drug modifications in kinetics optimization. Finally, from only 6 μs of simulation time we observed 75 unbinding events from which we calculate a residence time of 42 s, and a standard error range of 23 to 280 s. This nearly encompasses the exptl. residence time 11 min (660 s). In addition to the insights to sEH inhibitor unbinding, this study shows that simulations of complex processes on timescales as long as minutes are becoming feasible for more researchers to perform. This study involved multiple reactions and reactants, such as 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7Electric Literature of C16H20F3N3O3).

1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. Piperidine derivatives are being utilized in different ways as anticancer, antiviral, antimalarial, antimicrobial, antifungal, antihypertension, analgesic, anti-inflammatory, anti-Alzheimer, antipsychotic and/or anticoagulant agents.Electric Literature of C16H20F3N3O3

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On November 15, 2009, Burgey, Christopher S.; Potteiger, Craig M.; Deng, James Z.; Mosser, Scott D.; Salvatore, Christopher A.; Yu, Sean; Roller, Shane; Kane, Stefanie A.; Vacca, Joseph P.; Williams, Theresa M. published an article.Formula: C19H18ClN3O4 The title of the article was Optimization of azepanone calcitonin gene-related peptide (CGRP) receptor antagonists: Development of novel spiropiperidines. And the article contained the following:

Several novel spiropiperidine-based CGRP receptor antagonists have been developed that maintain good potency and have reduced potential for metabolism The experimental process involved the reaction of Benzyl 7′-chloro-2′-oxo-1′,2′-dihydrospiro[piperidine-4,4′-pyrido[2,3-d][1,3]oxazine]-1-carboxylate(cas: 883984-95-0).Formula: C19H18ClN3O4

The Article related to spiropiperidine cgrp receptor antagonist preparation migraine, Pharmacology: Structure-Activity and other aspects.Formula: C19H18ClN3O4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On March 16, 2018, Ishoey, Mette; Chorn, Someth; Singh, Natesh; Jaeger, Martin G.; Brand, Matthias; Paulk, Joshiawa; Bauer, Sophie; Erb, Michael A.; Parapatics, Katja; Muller, Andre C.; Bennett, Keiryn L.; Ecker, Gerhard F.; Bradner, James E.; Winter, Georg E. published an article.COA of Formula: C14H10N2O6 The title of the article was Translation Termination Factor GSPT1 Is a Phenotypically Relevant Off-Target of Heterobifunctional Phthalimide Degraders. And the article contained the following:

Protein degradation is an emerging therapeutic strategy with a unique mol. pharmacol. that enables the disruption of all functions associated with a target. This is particularly relevant for proteins depending on mol. scaffolding, such as transcription factors or receptor tyrosine kinases (RTKs). To address tractability of multiple RTKs for chem. degradation by the E3 ligase CUL4-RBX1-DDB1-CRBN (CRL4CRBN), we synthesized a series of phthalimide degraders based on the promiscuous kinase inhibitors sunitinib and PHA665752. While both series failed to induce degradation of their consensus targets, individual mols. displayed pronounced efficacy in leukemia cell lines. Orthogonal target identification supported by mol. docking led us to identify the translation termination factor G1 to S phase transition 1 (GSPT1) as a converging off-target, resulting from inadvertent E3 ligase modulation. This research highlights the importance of monitoring degradation events that are independent of the resp. targeting ligand as a unique feature of small-mol. degraders. The experimental process involved the reaction of 2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindoline-5-carboxylic acid(cas: 1216805-11-6).COA of Formula: C14H10N2O6

The Article related to sunitinib pha665752 phthalimide synthesis antitumor translation termination factor gspt1, Pharmacology: Structure-Activity and other aspects.COA of Formula: C14H10N2O6

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On September 21, 2018, Steinebach, Christian; Lindner, Stefanie; Udeshi, Namrata D.; Mani, Deepak C.; Kehm, Hannes; Koepff, Simon; Carr, Steven A.; Guetschow, Michael; Kroenke, Jan published an article.Computed Properties of 1216805-11-6 The title of the article was Homo-PROTACs for the Chemical Knockdown of Cereblon. And the article contained the following:

The immunomodulatory drugs (IMiDs) thalidomide, lenalidomide, and pomalidomide, all approved for the treatment of multiple myeloma, induce targeted ubiquitination and degradation of Ikaros (IKZF1) and Aiolos (IKZF3) via the cereblon (CRBN) E3 ubiquitin ligase. IMiD-based proteolysis-targeting chimeras (PROTACs) can efficiently recruit CRBN to a protein of interest, leading to its ubiquitination and proteasomal degradation By linking two pomalidomide mols., we designed homobifunctional, so-called homo-PROTACs and investigated their ability to induce self-directed ubiquitination and degradation The homodimerized compound I was characterized as a highly potent and efficient CRBN degrader with only minimal effects on IKZF1 and IKZF3. The cellular selectivity of I for CRBN degradation was confirmed at the proteome level by quant. mass spectrometry. Inactivation by compound I did not affect proliferation of different cell lines, prevented pomalidomide-induced degradation of IKZF1 and IKZF3, and antagonized the effects of pomalidomide on multiple myeloma cells. Homobifunctional CRBN degraders will be useful tools for future biomedical investigations of CRBN-related signaling and may help to further elucidate the mol. mechanism of thalidomide analogs. The experimental process involved the reaction of 2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindoline-5-carboxylic acid(cas: 1216805-11-6).Computed Properties of 1216805-11-6

The Article related to phthalimido glutarimide synthesis antitumor cereblon ikzf1 ikzf3 multiple myeloma, Pharmacology: Structure-Activity and other aspects.Computed Properties of 1216805-11-6

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On January 15, 2010, Stewart, Scott G.; Braun, Carlos J.; Ng, Sze-Ling; Polomska, Marta E.; Karimi, Mahdad; Abraham, Lawrence J. published an article.Electric Literature of 1216805-11-6 The title of the article was New thalidomide analogues derived through Sonogashira or Suzuki reactions and their TNF expression inhibition profiles. And the article contained the following:

A library of new thalidomide C4/5 analogs containing either a Ph or alkyne tether were synthesized using Sonogashira or Suzuki cross coupling reactions from their aryl halogenated precursors. All thalidomide analogs were tested for their ability to inhibit the expression of the proinflammatory cytokine Tumor Necrosis Factor (TNF). More explicitly the use of a novel reporter system utilizing the promoter region of the TNF gene in a human T-cell line provided a rapid and effective measure of NFκB transcriptional activity. Several compounds either containing either an aryl-iso-Bu or aryl-isopropoxy group were the most effective in inhibiting TNF expression, and were several times more active than thalidomide itself. Five of the more active derivatives indicated an apoptotic response while one of these compounds, containing an aldehyde tether, showed possible influence of cell cycling effects. The experimental process involved the reaction of 2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindoline-5-carboxylic acid(cas: 1216805-11-6).Electric Literature of 1216805-11-6

The Article related to structure thalidomide analog preparation tnf inhibition cancer, Pharmacology: Structure-Activity and other aspects.Electric Literature of 1216805-11-6

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem