Category: 39512-49-7

On October 1, 2017, Schwalbe, Tobias; Kaindl, Jonas; Huebner, Harald; Gmeiner, Peter published an article.COA of Formula: C11H14ClNO The title of the article was Potent haloperidol derivatives covalently binding to the dopamine D2 receptor. And the article contained the following:

The dopamine D2 receptor (D2R) is a common drug target for the treatment of a variety of neurol. disorders including schizophrenia. Structure based design of subtype selective D2R antagonists requires high resolution crystal structures of the receptor and pharmacol. tools promoting a better understanding of the protein-ligand interactions. Recently, we reported the development of a chem. activated dopamine derivative (FAUC150) designed to covalently bind the L94C mutant of the dopamine D2 receptor. Using FAUC150 as a template, we elaborated the design and synthesis of irreversible analogs of the potent antipsychotic drug haloperidol forming covalent D2R-ligand complexes. The disulfide- and Michael acceptor-functionalized compounds showed significant receptor affinity and an irreversible binding profile in radioligand depletion experiments The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).COA of Formula: C11H14ClNO

The Article related to preparation haloperidol derivative covalently binding dopamine d2 receptor, chemical probe, covalent ligand, disulfide tethering, dopamine d(2) receptor, g protein-coupled receptor, haloperidol and other aspects.COA of Formula: C11H14ClNO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Wakulik, Karolina; Wiatrak, Benita; Szczukowski, Lukasz; Bodetko, Dorota; Szandruk-Bender, Marta; Dobosz, Agnieszka; Swiatek, Piotr; Gasiorowski, Kazimierz published an article in 2020, the title of the article was Effect of novel pyrrolo[3,4-d]pyridazinone derivatives on lipopolysaccharide-induced neuroinflammation.COA of Formula: C11H14ClNO And the article contains the following content:

Neuroinflammation is considered to be one of the potential causes for the development of neurodegenerative diseases, including Alzheimer’s disease. In this study, we evaluated the effect of four newly synthesized pyrrolo[3,4-d]pyridazinone derivatives on the neuron-like PC12 cells under simulated inflammation conditions by preincubation with lipopolysaccharide (LPS). Our novel derivatives are selective cyclooxygenase-2 (COX-2) inhibitors and have similar effects to nonsteroidal anti-inflammatory drugs (NSAIDs). We assessed viability (LDH assay), metabolic activity (MTT assay), DNA damage (number of double-strand breaks measured by fast halo assay), and the neuronal features of cells (average neurite length and neurite outgrowth measured spectrofluorimetrically). DCF-DA and Griess assays were also performed, which allowed determining the impact of the tested compounds on the level of oxygen free radicals and nitrites. LPS administration significantly neg. affected the results in all tests performed, and treatment with the tested derivatives in most cases significantly reduced this neg. impact. Multiple-criteria decision anal. indicated that overall, the best results were observed for compounds 2a and 2b at a concentration of 10μM. The new derivatives showed intense activity against free oxygen radicals and nitrites. Reduced reactive oxygen species level also correlated with a decrease in the number of DNA damage. The compounds improved neuronal features, such as neurite length and outgrowth, and they also increased cell viability and mitochondrial activity. Our results suggest that derivatives 2a and 2b may also act addnl. on mechanisms other than 3a and 3b. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).COA of Formula: C11H14ClNO

The Article related to pyrrolo pyridazinone derivative neuroregenerative neuroinflammation dna damage, alzheimer’s disease, lps, nsaid, cyclooxygenase inhibitor, lipopolysaccharide, neuroinflammation, pyridazinone and other aspects.COA of Formula: C11H14ClNO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Kaneria, A. A.; Thumar, N. M.; Ladva, K. D.; Vadodaria, M. S. published an article in 2017, the title of the article was Synthesis, characterization and antimicrobial activity studies of some new N-substituted piperidine derivatives of 2-(4-chloro-4-(4-chlorophenyl))piperidine.Recommanded Product: 4-(4-Chlorophenyl)piperidin-4-ol And the article contains the following content:

Two series of N-substituted piperidine derivatives containing oxadiazoles I [R = H, 4-MeOC6H4, 4-BrC6H4, etc.] and acetohydrazides II were synthesized via reaction of 2-(2-chlorophenyl)-2-(4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl)acetohydrazide with aromatic carboxylic acids and aryl aldehydes resp. Compounds I and II were screened for their antimicrobial activities against various strains of bacteria and fungi. Compounds I [R = Ph, 4-FC6H4, 4-MeOC6H4, 4-O2NC6H4] and II [R = Ph, 4-OH-3-MeOC6H3, 2,4,5-FC6H2] and pyridyl derivative exhibited excellent activity against Gram pos. bacteria, Gram neg. bacteria and fungi. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Recommanded Product: 4-(4-Chlorophenyl)piperidin-4-ol

The Article related to chloro piperidinyl chlorophenylmethyl aryl oxadiazole preparation antibacterial antifungal, arylidene hydroxypiperidinyl chlorophenyl acetohydrazide preparation antibacterial antifungal and other aspects.Recommanded Product: 4-(4-Chlorophenyl)piperidin-4-ol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On August 25, 2016, Boudhar, Aicha; Ng, Xiao Wei; Loh, Chiew Yee; Chia, Wan Ni; Tan, Zhi Ming; Nosten, Francois; Dymock, Brian W.; Tan, Kevin S. W. published an article.Safety of 4-(4-Chlorophenyl)piperidin-4-ol The title of the article was Overcoming chloroquine resistance in malaria: Design, synthesis and structure-activity relationships of novel chemoreversal agents. And the article contained the following:

Malaria remains a significant infectious disease with even artemisinin-based therapies now facing resistance in the field. Development of new therapies is urgently needed, either by finding new compounds with unique modes of action, or by reversing resistance towards known drugs with ‘chemosensitizers’ or ‘chemoreversal’ agents (CRA). Concerning the latter, we have focused on the resistance mechanisms developed against chloroquine (CQ). We have synthesized a series of compounds related to previously identified CRAs, and found promising novel compounds These compounds show encouraging results in a coumarin labeled chloroquine uptake assay, exhibiting a dose response in resensitizing parasites to the antimalarial effects of chloroquine. Selected compounds show consistent potency across a panel of chloroquine and artemisinin sensitive and resistant parasites, and a wide therapeutic window. This data supports further study of CRAs in the treatment of malaria and, ultimately, their use in chloroquine-based combination therapies. 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 structure malaria antimalarial chemoreversal preparation chloroquine resistance, antimalarial, artemisinin-resistant, chemoreversal, chemosensitiser, chloroquine, chloroquine-resistant and other aspects.Safety of 4-(4-Chlorophenyl)piperidin-4-ol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On May 8, 2020, Ji, Changjin; Liu, Na; Tu, Jie; Li, Zhuang; Han, Guiyan; Li, Jian; Sheng, Chunquan published an article.Quality Control of 4-(4-Chlorophenyl)piperidin-4-ol The title of the article was Drug Repurposing of Haloperidol: Discovery of New Benzocyclane Derivatives as Potent Antifungal Agents against Cryptococcosis and Candidiasis. And the article contained the following:

Despite the high morbidity and mortality of invasive fungal infections (IFIs), effective and safe antifungal agents are rather limited. Starting from antifungal lead compound haloperidol that was identified by drug repurposing, a series of novel benzocyclane derivatives were designed, synthesized, and assayed. Several compounds showed improved antifungal potency and broader antifungal spectra. Particularly, compound B10 showed good inhibitory activities against a variety of fungal pathogens and was proven to be an inhibitor of several virulence factors important for drug resistance. In the in vivo cryptococcosis and candidiasis models, compound B10 could effectively reduce the brain fungal burden of Cryptococcus neoformans and synergize with fluconazole to treat resistant Candida albicans infections. Preliminary antifungal mechanism studies revealed that compound B10 regained cell membrane damage and down-regulated the overexpression of ERG11 and MDR1 genes when used in combination with fluconazole. Taken together, haloperidol derivative B10 represents a promising lead compound for the development of a new generation of antifungal agents. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Quality Control of 4-(4-Chlorophenyl)piperidin-4-ol

The Article related to antifungal haloperidol drug repurposing cryptococcus drug resistance candida, candida albicans, cryptococcus neoformans, antifungal, drug repurposing, drug resistance, haloperidol and other aspects.Quality Control of 4-(4-Chlorophenyl)piperidin-4-ol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Aguilar Troyano, Francisco Jose; Ballaschk, Frederic; Jaschinski, Marcel; Oezkaya, Yasemin; Gomez-Suarez, Adrian published an article in 2019, the title of the article was Light-Mediated Formal Radical Deoxyfluorination of Tertiary Alcohols through Selective Single-Electron Oxidation with TEDA2+..Name: 4-(4-Chlorophenyl)piperidin-4-ol And the article contains the following content:

The synthesis of tertiary alkyl fluorides through a formal radical deoxyfluorination process was described. This light-mediated, catalyst-free methodol. was fast and broadly applicable allowing for the preparation of C-F bonds from (hetero)benzylic, propargylic and non-activated tertiary alc. derivatives Preliminary mechanistic studies supported that the key step of the reaction is the single-electron oxidation of cesium oxalates-which are readily available from the corresponding tertiary alcs.-with in situ generated TEDA2+ (TEDA: N-(chloromethyl)triethylenediamine), a radical cation derived from Selectfluor. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Name: 4-(4-Chlorophenyl)piperidin-4-ol

The Article related to alc tertiary selectfluor photochem radical deoxyfluorination, tertiary alkyl fluoride preparation, fluorination, mechanistic studies, organic synthesis, photochemistry, radicals and other aspects.Name: 4-(4-Chlorophenyl)piperidin-4-ol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On March 12, 2021, Yang, Wanzhen; Tu, Jie; Ji, Changjin; Li, Zhuang; Han, Guiyan; Liu, Na; Li, Jian; Sheng, Chunquan published an article.Application In Synthesis of 4-(4-Chlorophenyl)piperidin-4-ol The title of the article was Discovery of Piperidol Derivatives for Combinational Treatment of Azole-Resistant Candidiasis. And the article contained the following:

Effective strategies are needed to deal with invasive fungal infections caused by drug-resistant fungi. Previously, we designed a series of antifungal benzocyclane derivatives based on the drug repurposing of haloperidol. Herein, further structural optimization and antifungal mechanism studies were performed, leading to the discovery of new piperidol derivative B2 (I) with improved synergistic antifungal potency, selectivity, and water solubility In particular, the combination of compound B2 and fluconazole showed potent in vitro and in vivo antifungal activity against azole-resistant Candida albicans. Compound B2 inhibited important virulence factors by regulating virulence-associated genes and improved the efficacy of fluconazole by down-regulating the CYP51-coding gene and efflux pump gene. Taken together, the piperidol derivative B2 represents a promising lead compound for the combinational treatment of azole-resistant candidiasis. 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 antifungal candida drug resistance virulence factor candidiasis piperidol derivative, candida albicans, antifungal, drug resistance, piperidol derivatives, virulence factors and other aspects.Application In Synthesis of 4-(4-Chlorophenyl)piperidin-4-ol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On June 30, 2013, Razavi, Seyyede Faeze; Khoobi, Mehdi; Nadri, Hamid; Sakhteman, Amirhossein; Moradi, Alireza; Emami, Saeed; Foroumadi, Alireza; Shafiee, Abbas published an article.HPLC of Formula: 39512-49-7 The title of the article was Synthesis and evaluation of 4-substituted coumarins as novel acetylcholinesterase inhibitors. And the article contained the following:

A series of 4-hydroxycoumarin derivatives were designed and synthesized as new acetylcholinesterase (AChE) inhibitors which could be considered for Alzheimer’s disease therapeutics. Among the 19 coumarin-derived compounds tested toward Electrophorus electricus acetylcholinesterase (eelAChE) and horse serum butyrylcholinesterase (eqBChE), N-(1-benzylpiperidin-4-yl)acetamide derivative I displayed highest AChE inhibitory activity (IC50 = 1.2 μM) and good selectivity (37 times). The docking study of the most potent compound I, indicated that Phe330 is responsible for ligand recognition and trafficking by forming π-cation interaction with benzylpiperidine moiety. Furthermore, the formation of an addnl. π-π interaction between coumarin moiety and Trp279 of peripheral anionic site could stabilize the ligand in the active site resulting in more potent inhibition of the enzyme. 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 coumarin preparation acetylcholinesterase inhibitor, Heterocyclic Compounds (One Hetero Atom): Benzopyrans (Including Coumarins, Isocoumarins, Chromones, Benzopyrones, Dibenzopyrans, and Other Arenopyrans) and other aspects.HPLC of Formula: 39512-49-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On September 2, 2016, Zhang, Wen; Wang, Fei; McCann, Scott D.; Wang, Dinghai; Chen, Pinhong; Stahl, Shannon S.; Liu, Guosheng published an article.Electric Literature of 39512-49-7 The title of the article was Enantioselective cyanation of benzylic C-H bonds via copper-catalyzed radical relay. And the article contained the following:

Direct methods for stereoselective functionalization of sp3-hybridized carbon-hydrogen [C(sp3)-H] bonds in complex organic mols. could facilitate much more efficient preparation of therapeutics and agrochems. Here, we report a copper-catalyzed radical relay pathway for enantioselective conversion of benzylic C-H bonds into benzylic nitriles. Hydrogen-atom abstraction affords an achiral benzylic radical that undergoes asym. C(sp3)-CN bond formation upon reaction with a chiral copper catalyst. The reactions proceed efficiently at room temperature with the benzylic substrate as limiting reagent, exhibit broad substrate scope with high enantioselectivity (typically 90 to 99% enantiomeric excess), and afford products that are key precursors to important bioactive mols. Mechanistic studies provide evidence for diffusible organic radicals and highlight the difference between these reactions and C-H oxidations mediated by enzymes and other catalysts that operate via radical rebound pathways. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Electric Literature of 39512-49-7

The Article related to enantioselective cyanation benzylic carbon copper catalyzed radical relay, Physical Organic Chemistry: Stereochemistry and Stereochemical Relationships, Including Conformational Inversions and Rotational Isomerization and other aspects.Electric Literature of 39512-49-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On May 31, 2017, Dalwadi, Dhwanil A.; Kim, Seongcheol; Schetz, John A. published an article.Name: 4-(4-Chlorophenyl)piperidin-4-ol The title of the article was Activation of the sigma-1 receptor by haloperidol metabolites facilitates brain-derived neurotrophic factor secretion from human astroglia. And the article contained the following:

Glial cells play a critical role in neuronal support which includes the production and release of the neurotrophin brain-derived neurotrophic factor (BDNF). Activation of the sigma-1 receptor (S1R) has been shown to attenuate inflammatory stress-mediated brain injuries, and there is emerging evidence that this may involve a BDNF-dependent mechanism. In this report we studied S1R-mediated BDNF release from human astrocytic glial cells. Astrocytes express the S1R, which mediates BDNF release when stimulated with the prototypical S1R agonists 4-PPBP and (+)-SKF10047. This effect could be antagonized by a selective concentration of the S1R antagonist BD1063. Haloperidol is known to have high affinity interactions with the S1R, yet it was unable to facilitate BDNF release. Remarkably, however, two metabolites of haloperidol, haloperidol I and haloperidol II (reduced haloperidol), were discovered to facilitate BDNF secretion and this effect was antagonized by BD1063. Neither 4-PPBP, nor either of the haloperidol metabolites affected the level of BDNF mRNA as assessed by qPCR. These results demonstrate for the first time that haloperidol metabolites I and II facilitate the secretion of BDNF from astrocytes by acting as functionally selective S1R agonists. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Name: 4-(4-Chlorophenyl)piperidin-4-ol

The Article related to human astroglia haloperidol metabolite brain neurotrophic factor sigma receptor, (+)-skf10047, 4-ppbp, astrocytes, bd1063, bdnf, haloperidol (pubchem cid: 3559), haloperidol metabolite i, haloperidol metabolite iii, in situ elisa, ne-100, neurotrophin, pf-04418948, pge2, reduced haloperidol, sigma receptor and other aspects.Name: 4-(4-Chlorophenyl)piperidin-4-ol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem