Category: 39512-49-7

On April 30, 2014, Chai, Christina L. L.; Teo, Serena L. M.; Jameson, Felicity K. M.; Lee, Serina S. C.; Likhitsup, Asawin; Chen, Chia-Lung; Rittschof, Dan published an article.Synthetic Route of 39512-49-7 The title of the article was Loperamide-based compounds as additives for biofouling management. And the article contained the following:

The com. pharmaceutical Imodium, which contains the active ingredient loperamide hydrochloride, has been shown to have biofouling control properties. However, due to concerns associated with safety and persistence of this active pharmaceutical ingredient (API) in the environment, the development of loperamide as an anti-fouling additive is not desirable. In this paper, we report our efforts directed towards the design and synthesis of small mol. anti-foulants using the loperamide parent compound as the lead compound These loperamide-based compounds can be synthesized readily and inexpensively. Several of the compounds identified are potentially useful as additives in marine antifouling coatings as they control attachment of barnacles in laboratory tests and an estimation program (BIOWIN) developed by the US Environmental Protection Agency predicts that they will degrade completely in weeks to months. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Synthetic Route of 39512-49-7

The Article related to balanus loperamide additive marine antifouling coating material, Agrochemical Bioregulators: Microbial and other aspects.Synthetic Route of 39512-49-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On April 30, 2018, Mieszkowski, Dominik; Sroka, Wiktor Dariusz; Marszall, Michat Piotr published an article.Category: piperidines The title of the article was Ionic liquids as separation enhancers of haloperidol and its two metabolites in high-performance thin-layer chromatography supported with mass spectrometry. And the article contained the following:

High-performance thin-layer chromatog. (HPTLC)-densitometric method of haloperidol (HP) and its two metabolites (reduced haloperidol [RHP], 4-(4-chlorophenyl)-4-hydroxypiperidine [CPHP]) from human plasma has been developed by use of mobile-phase additives. The influence of the type of inorganic/organic additive on the retention of the studied compounds was evaluated. The chromatog. process was carried out with traditional mobile phase modifiers and 1-alkyl-imidazolium ionic liquid as separation enhancers, in the presence of chlorpromazine as internal standard 1-Ethyl-3-methylimidazolium tetrafluoroborate ([emim][BF4]) ionic liquid offered good selectivity in comparison with traditional mobile phase additives. The studied drugs were well distributed as the RF values were 0.31 for chlorpromazine hydrochloride (CPZ), 0.38 for HP, 0.44 for CPHP, and 0.58 for RHP, resp., with no apparent broadening and overlapping of spots. The test compounds were extracted using acetonitrile as precipitation agent. The identity of the bands from human plasma was addnl. confirmed by rapid and contamination-free CAMAG thin-layer chromatog.-mass spectrometry (TLC-MS) interface. The limit of detection (LOD) values obtained by densitometry scanning were 0.1807, 0.3158, and 0.3924μg spot-1 (for HP, RHP, and CPHP), whereas the limit of quantification (LOQ) values for the presented method were 0.5476, 0.9570, and 1.1892μg spot-1 (for HP, RHP, and CPHP). Recovery values of all tested compounds were in the range from 95.43% to 99.60% (intra-day) and 96.13% to 103.18% (inter-day);%RSD did not exceed the value of 5%. The results confirm the pos. effect of ionic liquids in the separation process related to their silanol blocking properties and their suitability for use in thin-layer chromatog./mass spectrometry method. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Category: piperidines

The Article related to ionic liquid haloperidol metabolite thin layer chromatog mass spectrometry, Organic Analytical Chemistry: Other and other aspects.Category: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On August 15, 2016, Etukala, Jagan R.; Zhu, Xue Y.; Eyunni, Suresh V. K.; Onyameh, Edem K.; Ofori, Edward; Bricker, Barbara A.; Kang, Hye J.; Huang, Xi-Ping; Roth, Bryan L.; Ablordeppey, Seth Y. published an article.Computed Properties of 39512-49-7 The title of the article was Development of CNS multi-receptor ligands: Modification of known D2 pharmacophores. And the article contained the following:

Several known D2 pharmacophores have been explored as templates for identifying ligands with multiple binding affinities at dopamine and serotonin receptors considered as clin. relevant receptors in the treatment of neuropsychiatric diseases. This approach has resulted in the identification of ligands that target multiple CNS receptors while avoiding others associated with deleterious effects. Three compounds including I may have potential for further development as antipsychotic agents as they favorably interact with the clin. relevant receptors including D2R, 5-HT1AR, and 5-HT7R. The authors have also identified the pair of compounds I and II as high affinity D2R ligands with and without SERT binding affinities, resp. These differential binding profiles endow the pair with the potential for evaluating SERT contributions to antipsychotic drug activity in animal behavioral models. In addition, compound I has no significant affinity for 5-HT2CR and binds only moderately to the H1R, suggesting it may not induce weight gain or sedation when used clin. Taken together, compound I displays an interesting pharmacol. profile that necessitates the evaluation of its functional and in vivo effects in animal models which are currently ongoing. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Computed Properties of 39512-49-7

The Article related to central nervous system receptor ligand d2 pharmacophore antipsychotic, antipsychotic, cns receptor, dopamine receptor ligands, multi-receptor targeting, pharmacophore, Pharmacology: Structure-Activity and other aspects.Computed Properties of 39512-49-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On October 15, 2015, Kusumi, Kensuke; Shinozaki, Koji; Yamaura, Yoshiyuki; Hashimoto, Ai; Kurata, Haruto; Naganawa, Atsushi; Ueda, Hideyuki; Otsuki, Kazuhiro; Matsushita, Takeshi; Sekiguchi, Tetsuya; Kakuuchi, Akito; Seko, Takuya published an article.Safety of 4-(4-Chlorophenyl)piperidin-4-ol The title of the article was Discovery of novel S1P2 antagonists. Part 2: Improving the profile of a series of 1,3-bis(aryloxy)benzene derivatives. And the article contained the following:

The initial lead compound was modified to improve its metabolic stability. The resulting compound showed excellent metabolic stability in rat and human liver microsomes. The authors subsequently designed and synthesized compound N-[3-[4-(aminocarbonyl)phenoxy]-5-(4-fluorophenoxy)phenyl]-4-(4-chlorophenyl)-4-hydroxy-1-piperidinecarboxamide (I), which showed improved S1P2 antagonist activity and good metabolic stability. The subsequent introduction of a carboxylic acid moiety into I resulted in 4-[3-(4-fluorophenoxy)-5-[[[4-(4-fluorophenyl)-4-hydroxy-1-piperidinyl]carbonyl]amino]phenoxy]benzoic acid (II), which showed potent antagonist activity towards S1P2 with a much smaller species difference between human S1P2 and rat S1P2. Compound II also showed good metabolic stability and an improved safety profile compared with compound I. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Safety of 4-(4-Chlorophenyl)piperidin-4-ol

The Article related to aryloxybenzene preparation pharmacokinetics, antagonist, g protein-coupled receptors, metabolic stability, sphingosine-1-phosphate receptor 2, Pharmacology: Structure-Activity and other aspects.Safety of 4-(4-Chlorophenyl)piperidin-4-ol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On January 1, 2014, Gitto, Rosaria; De Luca, Laura; Ferro, Stefania; Scala, Angela; Ronsisvalle, Simone; Parenti, Carmela; Prezzavento, Orazio; Buemi, Maria Rosa; Chimirri, Alba published an article.Formula: C11H14ClNO The title of the article was From NMDA receptor antagonists to discovery of selective σ2 receptor ligands. And the article contained the following:

Following previous studies focused on the search for new mols. targeting GluN2B-containing NMDA, a small series of 1-(1H-indol-3-yl)-2-(4-phenylpiperidin-1-yl)ethanone derivatives has been synthesized by using Microwave Assisted Organic Synthesis (MAOS). Given that GluN2B ligands frequently exert off-target effects we also tested their affinity towards sigma receptors. Binding assay revealed that only the 1-(5-hydroxy-1H-indol-3-yl)-2-(4-phenylpiperidin-1-yl)ethanone (7a) retained GluN2B affinity. Interestingly, the 5-methoxyindoles 5a and 6a were efficient and selective ligands toward σ2 receptor (Ki values of 10 nM and 20 nM, resp.). Thus, in this case the discovery of new σ2 receptor selective ligands was an unexpected result emerging from the screening of cross-activity against other CNS receptors. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Formula: C11H14ClNO

The Article related to indole derivative preparation binding glun2b nmda receptor structure, glun2b/nmda, glutamate, ifenprodil, indoles, sigma receptor, Pharmacology: Structure-Activity and other aspects.Formula: C11H14ClNO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Punetha, Ankita; Green, Keith D.; Garzan, Atefeh; Thamban Chandrika, Nishad; Willby, Melisa J.; Pang, Allan H.; Hou, Caixia; Holbrook, Selina Y. L.; Krieger, Kyle; Posey, James E.; Parish, Tanya; Tsodikov, Oleg V.; Garneau-Tsodikova, Sylvie published an article in 2021, the title of the article was Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from Mycobacterium tuberculosis to overcome kanamycin resistance.Application In Synthesis of 4-(4-Chlorophenyl)piperidin-4-ol And the article contains the following content:

Tuberculosis (TB), caused by Mycobacterium tuberculosis (Mtb), is a deadly bacterial disease. Drug-resistant strains of Mtb make eradication of TB a daunting task. Overexpression of the enhanced intracellular survival (Eis) protein by Mtb confers resistance to the second-line antibiotic kanamycin (KAN). Eis is an acetyltransferase that acetylates KAN, inactivating its antimicrobial function. Development of Eis inhibitors as KAN adjuvant therapeutics is an attractive path to forestall and overcome KAN resistance. We discovered that an antipsychotic drug, haloperidol (HPD, 1), was a potent Eis inhibitor with IC50 = 0.39 ± 0.08 μM. We determined the crystal structure of the Eis-haloperidol (1) complex, which guided synthesis of 34 analogs. The structure-activity relationship study showed that in addition to haloperidol (1), eight analogs, some of which were smaller than 1, potently inhibited Eis (IC50 ≤ 1 μM). Crystal structures of Eis in complexes with three potent analogs and droperidol (DPD), an antiemetic and antipsychotic, were determined Three compounds partially restored KAN sensitivity of a KAN-resistant Mtb strain K204 overexpressing Eis. The Eis inhibitors generally did not exhibit cytotoxicity against mammalian cells. All tested compounds were modestly metabolically stable in human liver microsomes, exhibiting 30-60% metabolism over the course of the assay. While direct repurposing of haloperidol as an anti-TB agent is unlikely due to its neurotoxicity, this study reveals potential approaches to modifying this chem. scaffold to minimize toxicity and improve metabolic stability, while preserving potent Eis inhibition. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Application In Synthesis of 4-(4-Chlorophenyl)piperidin-4-ol

The Article related to mycobacterium tuberculosis kanamycin resistance haloperidol analog acetyltransferase eis inhibitor, Placeholder for records without volume info and other aspects.Application In Synthesis of 4-(4-Chlorophenyl)piperidin-4-ol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Kumar, Rayala Naveen; Meshram, H. M. published an article in 2016, the title of the article was ‘Claycop’ catalyzed highly efficient and chemoselective aza-Michael addition under solvent free condition.HPLC of Formula: 39512-49-7 And the article contains the following content:

A chemoselective and highly efficient addition of amines to electron deficient alkenes is described in the presence of claycop in solvent free condition. The reaction is very rapid and exhibited higher yields in comparison with slurry reaction. Claycop can be readily recovered and reused after activation. This method is suitable for a variety of amines and alkenes. Solvent free condition and recyclability of supported catalyst makes procedure more environmental friendly. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).HPLC of Formula: 39512-49-7

The Article related to electron deficient alkene amine addition claycop solvent free condition, General Organic Chemistry: Synthetic Methods and other aspects.HPLC of Formula: 39512-49-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On August 6, 2020, U. Dighe, Shashikant; Julia, Fabio; Luridiana, Alberto; Douglas, James J.; Leonori, Daniele published an article.HPLC of Formula: 39512-49-7 The title of the article was A photochemical dehydrogenative strategy for aniline synthesis. And the article contained the following:

Chem. reactions that reliably join two mol. fragments together (cross-couplings) are essential to the discovery and manufacture of pharmaceuticals and agrochems.1,2. The introduction of amines onto functionalized aromatics at specific and pre-determined positions (ortho vs. meta vs. para) is currently achievable only in transition-metal-catalyzed processes and requires halogen- or boron-containing substrates3-6. The introduction of these groups around the aromatic unit is dictated by the intrinsic reactivity profile of the method (electrophilic halogenation or C-H borylation) so selective targeting of all positions is often not possible. Here we report a non-canonical cross-coupling approach for the construction of anilines, exploiting saturated cyclohexanones as aryl electrophile surrogates. Condensation between amines and carbonyls, a process that frequently occurs in nature and is often used by (bio-)organic chemists7, enables a predetermined and site-selective carbon-nitrogen (C-N) bond formation, while a photoredox- and cobalt-based catalytic system progressively desaturates the cyclohexene ring en route to the aniline. Given that functionalized cyclohexanones are readily accessible with complete regiocontrol using the well established carbonyl reactivity, this approach bypasses some of the frequent selectivity issues of aromatic chem. We demonstrate the utility of this C-N coupling protocol by preparing com. medicines and by the late-stage amination-aromatization of natural products, steroids and terpene feedstocks. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).HPLC of Formula: 39512-49-7

The Article related to aniline preparation photochem dehydrogenative amination, General Organic Chemistry: Synthetic Methods and other aspects.HPLC of Formula: 39512-49-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On October 31, 2020, Neganova, Margarita E.; Klochkov, Sergey G.; Pukhov, Sergey A.; Afanasieva, Svetlana V.; Aleksandrova, Yulia R.; Yandulova, Ekaterina Y.; Avila-Rodriguez, Marco F.; Mikhaleva, Liudmila M.; Nikolenko, Vladimir N.; Somasundaram, Siva G.; Kirkland, Cecil E.; Aliev, Gjumrakch published an article.Related Products of 39512-49-7 The title of the article was Synthesis and Cytotoxic Activity of Azine Derivatives of 6-Hydroxyxanthanodiene. And the article contained the following:

Background: The conjugates of the sesquiterpene lactone of the eremophilane series of 6-hydroxyxanthanodiene with hydrogenated azines (piperidines and piperazines) have been synthesized and identified by NMR spectrometer. Objective: A lactone with an unusual skeleton “6-hydroxyxanthanodiene” was extracted from the plant Elecampane (Inula helenium L) and identified various species with NMR spectrometer. Methods: The cytotoxic, mitochondrial, and antioxidant activities on different tumor lines such as A549, HCT116, RD and Jurkat were investigated and determined possible mechanisms. Results: The results showed that the most potent compound was IIIi exhibiting highest cytotoxicity against RD cells (IC50 25.23 ± 0.04 μM), depolarized the mitochondrial membrane and was an effective antioxidant (IC50 inhibition of LP 10.68 ± 3.21 μM) without any toxic side effect on healthy cells. Conclusion: The conjugates of sesquiterpene lactone 6-hydroxyxanthanodiene III and hydrogenated azines may help to design potential promising anticancer drugs. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Related Products of 39512-49-7

The Article related to hydroxyxanthanodiene azine derivative cytotoxicity anticancer drug, 6-hydroxyxanthanodiene, anticancer drug, antioxidants, apoptosis, azines, cytotoxicity, mitochondria, Placeholder for records without volume info and other aspects.Related Products of 39512-49-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Rampa, Angela; Bartolini, Manuela; Pruccoli, Letizia; Naldi, Marina; Iriepa, Isabel; Moraleda, Ignacio; Belluti, Federica; Gobbi, Silvia; Tarozzi, Andrea; Bisi, Alessandra published an article in 2018, the title of the article was Exploiting the chalcone scaffold to develop multifunctional agents for Alzheimer′s disease.Reference of 4-(4-Chlorophenyl)piperidin-4-ol And the article contains the following content:

Alzheimer′s disease still represents an untreated multifaceted pathol., and drugs able to stop or reverse its progression are urgently needed. In this paper, a series of naturally inspired chalcone-based derivatives was designed as structural simplification of our previously reported benzofuran lead compound, aiming at targeting both acetyl (AChE)- and butyryl (BuChE) cholinesterases that, despite having been studied for years, still deserve considerable attention. In addition, the new compounds could also modulate different pathways involved in disease progression, due to the peculiar trans-a,β-unsaturated ketone in the chalcone framework. All mols. presented in this study were evaluated for cholinesterase inhibition on the human enzymes and for antioxidant and neuroprotective activities on a SH-SY5Y cell line. The results proved that almost all the new compounds were low micromolar inhibitors, showing different selectivity depending on the appended substituent; some of them were also effective antioxidant and neuroprotective agents. In particular, compound 4, endowed with dual AChE/BuChE inhibitory activity, was able to decrease ROS formation and increase GSH levels, resulting in enhanced antioxidant endogenous defense. Moreover, this compound also proved to counteract the neurotoxicity elicited by Aβ1-42 oligomers, showing a promising neuroprotective potential. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Reference of 4-(4-Chlorophenyl)piperidin-4-ol

The Article related to alzheimer disease chalcone scaffold cholinesterase antioxidant neuroprotective, alzheimer’s disease, antioxidants, chalcones, cholinesterase inhibitors, neuroprotection, Placeholder for records without volume info and other aspects.Reference of 4-(4-Chlorophenyl)piperidin-4-ol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem