Month: October 2022

On August 15, 2014, Salama, Ismail; Loeber, Stefan; Huebner, Harald; Gmeiner, Peter published an article.COA of Formula: C11H14ClNO The title of the article was Synthesis and binding profile of haloperidol-based bivalent ligands targeting dopamine D2-like receptors. And the article contained the following:

Homodimers of dopamine D2-like receptors are suggested to be of particular importance in the pathophysiol. of schizophrenia and, thus, serve as promising targets for the discovery of atypical antipsychotics. This study describes the development of a series of novel bivalent mols. with a pharmacophore derived from the dopamine receptor antagonist haloperidol. These dimers were investigated in comparison to their monomeric analogs for their D2long, D2short, D3, and D4 receptor binding and the ability to bridge two neighboring receptor protomers. Radioligand binding studies provided diagnostic insights when Hill slopes close to two for the bivalent ligand 13 incorporating 22 spacer atoms and a comparative anal. with monovalent control ligands indicated a bivalent binding mode with a simultaneous occupancy of two neighboring binding sites. 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 bivalent ligand dopamine d2 receptor antipsychotic, binding affinity, bivalent ligands, d(2) receptor, d(3) receptor, d(4) receptor, dopamine, gpcr dimers and other aspects.COA of Formula: C11H14ClNO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On September 1, 2020, Donoghue, Craig; Cubillos-Rojas, Monica; Gutierrez-Prat, Nuria; Sanchez-Zarzalejo, Carolina; Verdaguer, Xavier; Riera, Antoni; Nebreda, Angel R. published an article.Application of 1216805-11-6 The title of the article was Optimal linker length for small molecule PROTACs that selectively target p38α and p38β for degradation. And the article contained the following:

We report the design of hetero-bifunctional small mols. that selectively target p38α and p38β for degradation These proteolysis targeted chimeras (PROTACs) are based on an ATP competitive inhibitor of p38α and p38β, which is linked to thalidomide analogs to recruit the Cereblon E3 ubiquitin ligase complex. Compound synthesis was facilitated by the use of a copper catalyzed “click” reaction. We show that optimization of the linker length and composition is crucial for the degradation-inducing activity of these PROTACs. We provide evidence that these chem. compounds can induce degradation of p38α and p38β but no other related kinases at nanomolar concentrations in several mammalian cell lines. Accordingly, the PROTACs inhibit stress and cytokine-induced p38α signaling. Our compounds contribute to understanding the development of PROTACs, and provide a useful tool to investigate functions of the p38 MAPK pathway and its involvement in diseases. The experimental process involved the reaction of 2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindoline-5-carboxylic acid(cas: 1216805-11-6).Application of 1216805-11-6

The Article related to preparation protacs targeting p38 alpha beta proteolysis, azide-alkyne click reaction, cereblon, protac linker optimization, protein degradation, thalidomide derivative, p38 mapk and other aspects.Application of 1216805-11-6

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On September 21, 2018, Mowrey, Dale R.; Reif, James J.; Milkiewicz, Karen L.; Allwein, Shawn P. published an article.Related Products of 883984-95-0 The title of the article was Development of a Novel Process for the Kilogram-Scale Synthesis of Spiro[1H-pyrido[2,3-d][1,3]oxazine-4,4′-piperidine]-2-one. And the article contained the following:

The dihydrochloride of spiro[1H-pyrido[2,3-d][1,3]oxazine-4,4′-piperidine]-2-one I·2 HCl was prepared on kilogram scale by base-mediated Boc protection of 3-bromo-2-pyridinamine, metalation with i-PrMgCl and spirocyclization with 1-Boc-4-piperidinone, and Boc deprotection with aqueous HCl in isopropanol. A two-batch kilo lab campaign generated I·2 HCl in >99% HPLC area purity and in 77% overall yield. 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).Related Products of 883984-95-0

The Article related to spiropyridooxazinepiperidinone kilogram scale preparation, butoxycarbonylation bromopyridinamine metalation spirocyclization butoxycarbonylpiperidone neutralization kilogram scale and other aspects.Related Products of 883984-95-0

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

On September 8, 2017, Himmelsbach, Frank; Blum, Andreas; Peters, Stefan published a patent.Recommanded Product: tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate The title of the patent was Preparation of pyridinylmethyl carbamimidoylcarbamate derivatives as AOC3 inhibitors. And the patent contained the following:

The invention relates to new heteroaryl derivatives I [X1 = N and CH; X2 = N and CF (with the proviso that at least one of X1 and X2 is N); A = II-IV (R4 = (un)substituted azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, etc.)] or a pharmaceutically acceptable salt thereof, to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them. Over one-hundred compounds I were prepared General procedures for preparation of compounds I were provided. For example, compound I was prepared, starting from (2,3-difluoro-4-pyridyl)methanol and 3-phenylazetidine. Exemplified compounds I were tested for their pharmacol. activity in the AOC3 assay (IC50 values were given). The experimental process involved the reaction of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate(cas: 1251006-64-0).Recommanded Product: tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate

The Article related to pyridinylmethyl carbamimidoylcarbamate preparation aoc3 vascular adhesion protein 1 inhibitor, heteroaryl carbamimidoylcarbamate preparation aoc3 vascular adhesion protein 1 inhibitor and other aspects.Recommanded Product: tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate

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

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 January 14, 2021, Tong, Youzhi; Lai, Luhua published a patent.SDS of cas: 1216805-11-6 The title of the patent was C-myc protein inhibitor, and preparation method therefor and use thereof. And the patent contained the following:

Provided are a c-Myc protein inhibitor, and a preparation method therefor and use thereof. The c-Myc protein inhibitor selectively inhibits c-Myc protein. Therefore, the inhibitor can be used for prevention and treatment of diseases related to c-Myc protein disorders, such as cancers, cardiovascular and cerebrovascular diseases, diseases related to virus infection. The experimental process involved the reaction of 2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindoline-5-carboxylic acid(cas: 1216805-11-6).SDS of cas: 1216805-11-6

The Article related to amino acid boronic acid boronate derivative preparation, myc protein inhibitor amino acid boronic acid boronate derivative, antitumor activity amino acid boronic acid boronate derivative and other aspects.SDS of cas: 1216805-11-6

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On April 20, 2006, Burgey, Christopher S.; Deng, James Z.; Potteiger, Craig; Williams, Theresa M. published a patent.Recommanded Product: Benzyl 7′-chloro-2′-oxo-1′,2′-dihydrospiro[piperidine-4,4′-pyrido[2,3-d][1,3]oxazine]-1-carboxylate The title of the patent was Preparation of oxohomopiperidinyl oxospiropiperidinepyrrolopyridinecarboxamides and related compounds as calcitonin gene-related peptide (CGRP) receptor antagonists.. And the patent contained the following:

Title compounds [I; A = bond, C(R2)2, O, SOm, NR2; B = [C(R2)2]n; R1, R2 = H, (substituted) alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, heteroaryl; pairs of R2 may form rings; R3 = H, F, cyano, (substituted) alkyl, CO2R4; R4 = H, (substituted) alkyl, fluoroalkyl, cycloalkyl, aryl, heteroaryl, PhCH2; X = C, S; Y = O, (R4)2, NCN, NHSO2Me, NCONH2; or Y = O2 when X = S; J = bond, C(R6)2, O, NR6; V = bond, C(R6)2, O, SOm, NR6, NR6NR6, etc.; Q = CR7a, C(R7A)2, CO, SOm, N, NR7a; T = CR7b, C(R7b)2, CO, SOm, N, NR7b; R6 = H, halo, OR4, CO2R4, alkyl, cycloalkyl, (substituted) aryl, heteroaryl, heterocyclyl, etc.; R7a, R7b = R2; R7aR7b = atoms to form cycloalkyl, aryl, heterocyclyl, heteroaryl rings; m = 0-2; n = 0, 1], were prepared for treatment of headache (no data). Thus, (3R,6S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one (preparation given) and 4-nitrophenyl chloroformate in THF at 0° were treated with Et3N; after 60 min. spiro[piperidine-4,3′-pyrrolo[2,3-b]pyridin]-2′(1’H)-one dihydrochloride (preparation given) and Et3N in CHCl3 were added followed by warming to room temperature to give title compound (II). 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).Recommanded Product: Benzyl 7′-chloro-2′-oxo-1′,2′-dihydrospiro[piperidine-4,4′-pyrido[2,3-d][1,3]oxazine]-1-carboxylate

The Article related to oxoazepanyl oxospiropiperidinepyrrolopyridinecarboxamide preparation cgrp receptor antagonist, headache treatment oxohomopiperidinyl spiropiperidinepyrrolopyridinecarboxamide preparation and other aspects.Recommanded Product: Benzyl 7′-chloro-2′-oxo-1′,2′-dihydrospiro[piperidine-4,4′-pyrido[2,3-d][1,3]oxazine]-1-carboxylate

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