Day: February 22, 2023

Pre-treatment of BALB/c mice with a centrally acting serotonin antagonist (Cyproheptadine) reduces mortality from Boophone Disticha poisoning was written by Mutseura, M.;Tagwireyi, D.;Gadaga, L. L.. And the article was included in Clinical Toxicology in 2013.Related Products of 969-33-5 This article mentions the following:

Crude extracts of Boophone disticha are used in Southern African traditional medical practice for the management of various illnesses and conditions and have also been abused for their claimed euphoric and hallucinogenic effects. Unfortunately, ingestion of Boophone disticha has resulted in toxicity and death. The results of a recent acute toxicity study in a rat model insinuated that central nervous system (CNS) serotonin overdrive could be the cause of toxicity in B. disticha poisoning. The present work sought to test that hypothesis by investigating whether pre-treatment of B. disticha poisoned BALB/c mice with the CNS acting serotonin antagonist, cyproheptadine, has a dose-dependent protective effect on toxicity and mortality. A hydroethanolic extract of B. disticha was used in all the experiments Five groups each with 10 animals were constituted as follows; a neg. control group (received 10 mL/kg Normal Saline), a pos. control group (received 375 mg/kg of the B. disticha extract), and three test groups each receiving 10 mg/kg, 15 mg/kg and 20 mg/kg cyproheptadine i.p. 15 min before oral gavage administration of 375 mg/kg B. disticha extract resp. The Functional Observational Battery was used to evaluate neurobehavioral and physiol. changes resulting from toxicity of the plant extract The mice were then placed in an open field for another five minutes and the number of rearings and border crossings were counted and recorded. Gait abnormalities, involuntary motor movements, mobility, arousal and stereotypical behavior were also scored according to predefined criteria. All open field investigations were recorded electronically using a LABTEC Webcam and results were later analyzed and recorded by one of the group members. All results were entered on data collection forms. Time to death (survival time) was considered as the time period from dosage with Boophone disticha to time of death. The study follow up period was 7 days and those mice that were alive at the end of the 7 day follow-up period were considered as having survived the poisoning episode. The Kaplan Meier plot and Log-rank test were used to compare differences in mortality and median time to death for mice in the 5 treatment groups. We found that cyproheptadine pre-treatment led to a dose-dependent decrease in mortality from 80% in the group not pre-treated with cyproheptadine, to 30% in the 15 and 20 mg/kg cyproheptadine pre-treated groups (n = 10 per group, p < 0.05). There was also a dose-dependent increase in median survival times amongst the groups (p < 0.0001). Pre-treatment with cyproheptadine also resulted in a decrease of other toxic symptoms associated with Boophone disticha. We conclude that cyproheptadine has a dose-dependent protective effect on mortality and toxicity produced by exposure to Boophone disticha in our mouse model of toxicity. In the experiment, the researchers used many compounds, for example, 4-(5H-Dibenzo[a,d][7]annulen-5-ylidene)-1-methylpiperidine hydrochloride (cas: 969-33-5Related Products of 969-33-5).

4-(5H-Dibenzo[a,d][7]annulen-5-ylidene)-1-methylpiperidine hydrochloride (cas: 969-33-5) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.Related Products of 969-33-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In Vitro screening for seizure liability using microelectrode array technology was written by Bradley, Jenifer A.;Luithardt, Harry H.;Metea, Monica R.;Strock, Christopher J.. And the article was included in Toxicological Sciences in 2018.Quality Control of Thioridazine hydrochloride This article mentions the following:

Drug-induced seizure liabilities produce significant compound attrition during drug discovery. Currently available in vitro cytotoxicity assays cannot predict all toxicity mechanisms due to the failure of these assays to predict sublethal target-specific electrophysiol. liabilities. Identification of seizurogenic and other electrophysiol. effects at early stages of the drug development process is important to ensure that safe candidate compounds can be developed while chem. is taking place, long before these liabilities are discovered in costly preclin. in vivo studies. The development of a high throughput and reliable in vitro assay to screen compounds for seizure liabilities would de-risk compounds significantly earlier in the drug discovery process and with greater dependability. Here the authors describe a method for screening compounds that utilizes rat cortical neurons plated onto multiwell microelectrode array plates to identify compounds that cause neurophysiol. disruptions. Changes in 12 electrophysiol. parameters (spike train descriptors) were measured after application of known seizurogenic compounds and the response pattern was mapped relative to neg. controls, vehicle control and neurotoxic controls. Twenty chems. with a variety of therapeutic indications and targets, including GABAA antagonists, glycine receptor antagonists, ion channel blockers, muscarinic agonist, 未-opioid receptor agonist, dopaminergic D2/adrenergic receptor blocker and nonsteroidal anti-inflammatory drugs, were tested to assess this system. Sixteen of the seventeen seizurogenic/neurotoxic compounds tested pos. for seizure liability or neurotoxicity, moreover, different endpoint response patterns for firing rate, burst characteristics and synchrony that distinguished the chems. into groups relating to target and seizurogenic response emerged from the data. The neg. and vehicle control compounds had no effect on neural activity. In conclusion, the multiwell microelectrode array platform using cryopreserved rat cortical neurons is a highly effective high throughput method for reliably screening seizure liabilities within an early de-risking drug development paradigm. In the experiment, the researchers used many compounds, for example, Thioridazine hydrochloride (cas: 130-61-0Quality Control of Thioridazine hydrochloride).

Thioridazine hydrochloride (cas: 130-61-0) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. Fluorinated piperidines are also the subject of continued interest in medicinal chemistry, for example in the synthesis of selective dipeptidyl peptidase II (DPP II) inhibitors. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions.Quality Control of Thioridazine hydrochloride

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Molecular Orientation and Dynamics of a Derivative of 2,2,6,6-Tetramethyl-1-Piperidinyloxyl Radical with a Large Substituent Group Dispersed in 1D-Nanochannels of 2,4,6-Tris(4-Chlorophenoxy)-1,3,5-Triazine Crystal was written by Kobayashi, Hirokazu;Odanaka, Yuki. And the article was included in Applied Magnetic Resonance in 2020.Reference of 14691-89-5 This article mentions the following:

The mol. orientation and dynamics were examined for 4-acetamido-2,2,6,6-tetramethyl-1-piperidinyloxyl (4-acetamido-TEMPO) radicals, which have a larger substituent group than many other TEMPO radicals, dispersed in the one-dimensional (1D) nanochannel of 2,4,6-tris(4-chlorophenoxy)-1,3,5-triazine (CLPOT) with 4-substituted-2,2,6,6-tetramethylpiperidine (R-TEMP; R=OH or H). When TEMPOH (R=OH) was used as a spacer for dispersion in the CLPOT nanochannels, the mol. orientation of 4-acetamido-TEMPO in the CLPOT nanochannels was similar to that of other previously reported 4-substituted-TEMPO (4-X-TEMPO; X=OH, =O or OCH₃) radicals. However, the activation energy for the rotational diffusion of 4-acetamido-TEMPO in the CLPOT nanochannels, estimated to be 11 kJ mol^-1, was larger than that of other 4-X-TEMPO mols. (6-8 kJ mol^-1). These results indicate that the mol. dynamics of 4-X-TEMPO in the CLPOT nanochannels can be controlled by the selection of a larger substituent X at the 4-position in 4-X-TEMPO (in this study, X=NHCOCH₃), and also suggest an important concept for the design of new organic magnets. In the experiment, the researchers used many compounds, for example, 4-Acetamido-2,2,6,6-tetramethylpiperidine 1-oxyl (cas: 14691-89-5Reference of 14691-89-5).

4-Acetamido-2,2,6,6-tetramethylpiperidine 1-oxyl (cas: 14691-89-5) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. 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.Reference of 14691-89-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Discovery of novel 2,4-diarylaminopyrimidine derivatives as potent and selective epidermal growth factor receptor (EGFR) inhibitors against L858R/T790M resistance mutation was written by Yan, Qi;Chen, Yuzhe;Tang, Baiyou;Xiao, Qiang;Qu, Rong;Tong, Linjiang;Liu, Jian;Ding, Jian;Chen, Yi;Ding, Ning;Tan, Wenfu;Xie, Hua;Li, Yingxia. And the article was included in European Journal of Medicinal Chemistry in 2018.Recommanded Product: 50533-97-6 This article mentions the following:

A series of novel 2,4-diarylaminopyrimidine derivatives of AZD9291 were discovered as L858R/T790M mutant selective epidermal growth factor receptor (EGFR) inhibitors. The majority of these compounds exhibited moderate to excellent EGFR T790 M/L858R inhibitory activities and comparable anti-proliferative activities against double mutant over-expressed NCI-H1975 cells to that of AZD9291. The most promising compounds 8a (N-(2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxy-5-((4-((2-(1-methyl-1H-pyrazol-3-yl)phenyl)amino)pyrimidin-2-yl)amino)phenyl)acrylamide) displayed an IC₅₀ of 4.1 nM against EGFR L858R/T790M mutants. Compound 8a also showed excellent cytotoxic effect against NCI-H1975 cells with an IC₅₀ of 59 nM and 100-fold selectivity over wide-type EGFR over-expressed A431 cells. Compound 8a significantly inhibited tumor growth in NCI-H1975 xenograft models at a non-toxic dose. Docking study performed for 8a with ATP binding site of EGFR-TK showed the similar binding mode to that of AZD9291. All these results suggested that compound 8a was a potential mutant-selective EGFR inhibitor. In the experiment, the researchers used many compounds, for example, N,N-Dimethylpiperidin-4-amine (cas: 50533-97-6Recommanded Product: 50533-97-6).

N,N-Dimethylpiperidin-4-amine (cas: 50533-97-6) belongs to piperidine derivatives. Piperidine has a role as a reagent, a protic solvent, a base, a catalyst, a plant metabolite, a human metabolite and a non-polar solvent. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Recommanded Product: 50533-97-6

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Ammonia recovery from anaerobic digester centrate using onsite pilot scale bipolar membrane electrodialysis coupled to membrane stripping was written by Ferrari, Federico;Pijuan, Maite;Molenaar, Sam;Duinslaeger, Nick;Sleutels, Tom;Kuntke, Philipp;Radjenovic, Jelena. And the article was included in Water Research in 2022.Name: 4-Oxo-tempo This article mentions the following:

Ammonia recovery from centrate of an anaerobic digester was investigated using an onsite bipolar-electrodialysis (BP-ED) pilot scale plant coupled to two liquid/liquid membrane contactor (LLMC) modules. To investigate the process performance and robustness, the pilot plant was operated at varying current densities, load ratio (current to nitrogen loading), and in continuous and intermittent current (Donnan) mode. A higher load ratio led to higher total ammonium nitrogen (TAN, sum of ammonia and ammonium) removal efficiency, whereas the increase in the applied current did not have a significant impact the TAN removal efficiency. Continuous current application resulted in the higher TAN removal compared with the Donnan dialysis mode. The lowest specific energy consumption of 6.3 kWh kg-1N was recorded in the Donnan mode, with the load ratio of 1.4, at 200 L h-1 flowrate and c.d. of 75 A m-2. Lower energy demand observed in the Donnan mode was likely due to the lower scaling and fouling of the ion exchange membranes. Nevertheless, scaling and fouling limited the operation of the BP-ED stack in all operational modes, which had to be interrupted by the daily cleaning procedures. The LLMC module enabled a highly selective recovery of ammonia as ammonium sulfate ((NH4)2SO4), with the concentration of ammonia ranging from 19 to 33 gN L-1. However, the anal. of per- and polyfluoroalkyl substances (PFASs) in the obtained (NH4)2SO4 product revealed the presence of 212-253 ng L-1 of 6:2 fluorotelomer sulfonate (FTS), a common substitute of legacy PFAS. Given the very low concentrations of 6:2 FTS (i.e., < 2 ng L-1) encountered in the concentrated stream, 6:2 FTS was likely released from the Teflon-based components in the sulfuric acid dosage line. Thus, careful selection of the pilot plant tubing, pumps and other components is required to avoid any risks associated with the PFAS presence and ensure safe use of the final product as fertilizer. In the experiment, the researchers used many compounds, for example, 4-Oxo-tempo (cas: 2896-70-0Name: 4-Oxo-tempo).

4-Oxo-tempo (cas: 2896-70-0) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising 伪-glucosidase inhibitors. The former are analogs of DNJ with an improved 伪-glucosidase inhibitory profile than that of DNJ. Boisson et al.Name: 4-Oxo-tempo

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Ionic Liquid Stabilized 2,2,6,6-Tetramethylpiperidine 1-Oxyl Catalysis for Alcohol Oxidation was written by Li, Min;Klunder, Kevin;Blumenthal, Emmy;Prater, Matthew B.;Lee, Jack;Matthiesen, John E.;Minteer, Shelley D.. And the article was included in ACS Sustainable Chemistry & Engineering in 2020.Application of 14691-89-5 This article mentions the following:

N-Oxyl reagents, particularly 2,2,6,6-tetramethylpiperidine 1-oxyl (TEMPO), have been extensively used for alc. oxidations While TEMPO-mediated oxidations are kinetically and thermodynamically favorable in high-pH electrolytes, base-induced degradation often results in significant loss of catalytic activity. Herein, we demonstrate enhanced alk. stability of a TEMPO derivative in ionic liquids (ILs). By incorporating TEMPO in an imidazole-anchored IL, no loss of current was observed at pH 10.0 after 2.0 h during the oxidation of butanol and glycerol, while TEMPO in polycaprolactone (PCL), a patternable binder material, degraded 58.5% and 67.1%, resp. The stability enhancement was further demonstrated by analyzing the conversion of glycerol in an 800渭L electrochem. cell using bulk chem. anal. techniques. Successive cycles of glycerol oxidation indicated 14-fold stability enhancement by applying IL in a TEMPO electrode composite in comparison to PCL. The strategy demonstrated here provides an opportunity to prepare catalytic systems with enhanced stability. Further, this method provides the ability to convert what are typically homogeneous catalysts to heterogeneous systems. To improve the stability of TEMPO, used to mediate oxidations for biorenewables, an ionic liquid based catalyst was developed. In the experiment, the researchers used many compounds, for example, 4-Acetamido-2,2,6,6-tetramethylpiperidine 1-oxyl (cas: 14691-89-5Application of 14691-89-5).

4-Acetamido-2,2,6,6-tetramethylpiperidine 1-oxyl (cas: 14691-89-5) belongs to piperidine derivatives. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. 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.Application of 14691-89-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Synthesis, characterization, crystal structures, and the biological evaluation of 2-phenylthiazole derivatives as cholinesterase inhibitors was written by Shi, Da-Hua;Song, Meng-qiu;Ma, Xiao-Dong;Su, Jia-Bin;Wang, Jing;Wang, Xiu-Jun;Liu, Yu-Wei;Liu, Wei-Wei;Si, Xin-Xin. And the article was included in Journal of Chemical Research in 2021.HPLC of Formula: 1126-09-6 This article mentions the following:

Four 2-phenylthiazole derivatives I [R = 4-methylpiperazin-1-yl, 2-morpholin-4-yl-Et, 3,5-dimethylpiperidin-1-yl, etc.] were synthesized, characterized and evaluated as cholinesterase inhibitors. The structures of the 2-phenylthiazole derivatives were confirmed by ¹H and ¹³C NMR spectroscopy, single-crystal X-ray diffraction studies, and Hirshfeld surfaces anal. Hirshfeld surface anal. of the prepared compounds showed C-H路路路O intermol. interactions. The cholinesterase inhibition activities of the synthesized compounds were tested by Ellman’s method. Compound I [R = 3,5-dimethylpiperidin-1-yl] showed the best acetylcholinesterase inhibition activity with an IC₅₀ value of 8.86渭M and the best butyrylcholinesterase inhibition activity with an IC₅₀ value of 1.03渭M. A docking study demonstrated that the same compound interacted with the catalytic anionic site and peripheral anionic site of acetylcholinesterase and the catalytic anionic site of butyrylcholinesterase. In the experiment, the researchers used many compounds, for example, Ethyl piperidine-4-carboxylate (cas: 1126-09-6HPLC of Formula: 1126-09-6).

Ethyl piperidine-4-carboxylate (cas: 1126-09-6) belongs to piperidine derivatives. Piperidine and its derivatives have become increasingly popular in many synthetic schemes. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.HPLC of Formula: 1126-09-6

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Phytochemicals in Breast Cancer-Induced Osteoclastogenesis and Bone Resorption: Mechanism and Future Perspective was written by Pore, Subrata Kumar;Hahm, Eun-Ryeong. And the article was included in Current Pharmacology Reports in 2022.Electric Literature of C9H15NO5 This article mentions the following:

Most breast cancer patients develop bone metastasis and bone-related complications at the late stage of the disease irresp. of the subtypes. Breast cancer destroys bones by inducing osteoclastogenesis, a bone erosion process. Bisphosphonates and denosumab treatments are clin. approved but often with several limitations. Phytochems. have been shown to have anticancer properties against breast cancer especially as chemo-preventive agents. The highly promising phytochems. against breast cancer include cruciferous vegetable components (phenethyl isothiocyanate, benzyl isothiocyanate, and sulforaphane), food constituents (curcumin, piperine, and epigallocatechin gallate), and medicinal plant components (dihydroartemisinin, betulinic acid, silibinin, and plumbagin). A few of them, e.g., isothiocyanates from cruciferous vegetables are under clin. trials. These structurally diverse non-toxic phytochems. could also suppress breast cancer-induced osteoclastogenesis and bone destruction by regulating either breast cancer cells or osteoclast precursors. This review aims to discuss the mechanistic aspects and future perspective for clin. significance of these diverse phytochems. in breast cancer-induced osteoclastogenesis and osteolytic bone erosion. In the experiment, the researchers used many compounds, for example, (2E,4E)-5-(Benzo[d][1,3]dioxol-5-yl)-1-(piperidin-1-yl)penta-2,4-dien-1-one (cas: 94-62-2Electric Literature of C9H15NO5).

(2E,4E)-5-(Benzo[d][1,3]dioxol-5-yl)-1-(piperidin-1-yl)penta-2,4-dien-1-one (cas: 94-62-2) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.Electric Literature of C9H15NO5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Dopaminergic activity in a series of N-substituted 2-aminopyrimidines was written by Moragues, J.;Prieto, J.;Spickett, R. G. W.;Vega, A.;Salazar, W.;Roberts, D. J.. And the article was included in Farmaco, Edizione Scientifica in 1980.Category: piperidines This article mentions the following:

Twenty-four title compounds, most of the structure I (R and R¹ = H or Me; R² = H, Cl, or OMe; R³ = H, Cl, Me, or OMe; or R²R³ = OCH₂O), were synthesized and tested for pharmacol. activity associated with stimulation of central and peripheral dopamine receptors using piribedil as the reference standard Most of the new compounds had some degree of dopaminergic activity although in many cases central activity was not accompanied by peripheral activity and vice versa. Structure-activity relations were not apparent, and none of the new compounds possessed dopamine receptor blocking properties. In the experiment, the researchers used many compounds, for example, 1-(4-Methoxybenzyl)piperidin-4-amine dihydrochloride (cas: 57645-54-2Category: piperidines).

1-(4-Methoxybenzyl)piperidin-4-amine dihydrochloride (cas: 57645-54-2) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Piperidine derivatives bearing a masked aldehyde function in the 蔚-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Category: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Synthesis and biological evaluation of bufalin-3-yl nitrogen-containing-carbamate derivatives as anticancer agents was written by Lei, Min;Xiao, Zhiyong;Ma, Biao;Chen, Yijia;Liu, Miao;Liu, Junhua;Guo, De’an;Liu, Xuan;Hu, Lihong. And the article was included in Steroids in 2016.Name: N,N-Dimethylpiperidin-4-amine This article mentions the following:

A series of bufalin-3-yl nitrogen-containing-carbamate derivatives 3 were designed, synthesized, and evaluated for their proliferation inhibition activities against human cervical epithelial adenocarcinoma (HeLa) cell line. The structure-activity relationships (SARs) of this new series are described in this paper. Cytotoxicity data revealed that the C3 moiety had an important influence on cytotoxic activity. Compound 3i-HCl exhibited significant in vitro antiproliferative activity against the ten tested tumor cell lines, with IC₅₀ values ranging from 0.30 to 1.09 nM. Furthermore, 3i-HCl can significantly inhibit tumor growth by 100% at the dose 2 mg/kg by iv, or 4 mg/kg by ig. In the experiment, the researchers used many compounds, for example, N,N-Dimethylpiperidin-4-amine (cas: 50533-97-6Name: N,N-Dimethylpiperidin-4-amine).

N,N-Dimethylpiperidin-4-amine (cas: 50533-97-6) belongs to piperidine derivatives. Piperidine and its derivatives have become increasingly popular in many synthetic schemes. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N鈥揌 bond in an axial position, and the other in an equatorial position.Name: N,N-Dimethylpiperidin-4-amine

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem