Tag: 200-300

On January 17, 2022, Lodha, Kamlesh K.; Wavhal, Deepak S.; Bhalekar, Sujit B.; Meshram, Rohan J.; Shinde, Vaishali S. published an article.Computed Properties of 67914-60-7 The title of the article was Exploring new tetrahydrothienopyridine derivatives as platelet agglutination inhibitors: synthesis, biological evaluation and In silico study. And the article contained the following:

The P2Y12 receptor is the major target for antithrombic drugs which plays a key role in platelet activation. New derivatives of 4,5,6,7-tetrahydrothieno[3,2-c]pyridine (THP) were designed targeting P2Y12 receptor. An efficient route was developed for synthesis of THP derivatives and subsequently evaluated for their antiplatelet agglutination activity. Amongst the synthesized THP derivatives (4 a-4 g), the compounds 4 a and 4 g displayed significant activity (with 88.25 and 70.17 % inhibition) as compared to other analogs and comparable with that of the reference drugs, aspirin and prasugrel. Data extracted from computational chem. techniques such as mol. docking, provided the structural rationale for the observed platelet agglutination inhibition by the newly synthesized tetrahydrothienopyridine analogs. We proposed the involvement of residues such as Cys-194 in the formation of the covalent adduct with the active metabolite of tetrahydrothienopyridine derivatives This study also put forward the possibility of the existence of an alternate pathway for metabolizing the tetrahydrothienopyridine compounds The structural data presented in this study is expected to accelerate the research on developing a tetrahydrothienopyridine scaffold as an effective antithrombotic therapeutic modality. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Computed Properties of 67914-60-7

The Article related to platelet agglutination tetrahydrothienopyridine screening antiplatelet, Placeholder for records without volume info and other aspects.Computed Properties of 67914-60-7

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Dong, Kui; Zhao, Chuang-Yuan; Wang, Xiao-Ju; Wu, Li-Zhu; Liu, Qiang published an article in , the title of the article was Bioinspired Selective Synthesis of Heterodimer 8-5′ or 8-O-4′ Neolignan Analogs.Safety of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone And the article contains the following content:

The bioinspired synthesis of heterodimer neolignan analogs is reported by single-electron oxidation of both alkenyl phenols and phenols individually, followed by a combination of the resultant radicals. This oxidative radical cross-coupling strategy can afford heterodimer 8-5′ or 8-O-4′ neolignan analogs selectively with the use of air as the terminal oxidant and copper acetate as the catalyst at room temperature The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Safety of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

The Article related to neolignan heterodimer preparation oxidative radical cross coupling, Placeholder for records without volume info and other aspects.Safety of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On February 28, 2018, Kamata, Ryo; Nakajima, Daisuke; Shiraishi, Fujio published an article.HPLC of Formula: 67914-60-7 The title of the article was Agonistic effects of diverse xenobiotics on the constitutive androstane receptor as detected in a recombinant yeast-cell assay. And the article contained the following:

The constitutive androstane receptor (CAR) is a nuclear receptor and transcription factor regulating proteins involved in xenobiotic metabolism Agonist activation of the CAR can trigger metabolic activation and toxification as well as detoxification and clearance; accordingly, xenobiotic substances acting as CAR ligands may pose a threat to human and animal health. The authors used yeast cells transduced with the human CAR and the response pathway to measure the CAR-agonistic activities of 549 synthetic or natural compounds: 216 of the tested compounds exhibited CAR-agonistic effects. Eighty-four percent of CAR-activating compounds were aromatic compounds, and >65% of these active compounds were aromatic hydrocarbons, bisphenols, monoalkyl phenols, phthalates, styrene dimers, di-Ph ethers, organochlorines, and organophosphates. The ten most potent compounds were 4-tert-octylphenol (4tOP; reference substance), 4-nonylphenol, diethylstilbestrol, benzyl Bu phthalate, 2-(4-hydroxyphenyl)-2,4,4-trimethylchroman, o,p’-DDT, methoxychlor, di-Pr phthalate, hexestrol, and octachlorostyrene. The activities of these nine non-reference compounds exceeded 10% of the 4tOP activity. Anal. of para-monoalkyl phenols suggests that branching of the alkyl group and chlorination at the ortho position raises potency. This study provides critical information for identifying the potential of CAR-mediated toxic hazards and for understanding the relevant mechanism. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).HPLC of Formula: 67914-60-7

The Article related to xenobiotic constitutive androstane receptor, alkyl phenol, bisphenol, constitutive androstane receptor, organochlorine, recombinant yeast, styrene dimer, Toxicology: Methods (Including Analysis) and other aspects.HPLC of Formula: 67914-60-7

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On June 15, 2014, Nirantar, Saurabh R.; Li, Xiang; Siau, Jia Wei; Ghadessy, Farid J. published an article.COA of Formula: C12H16N2O2 The title of the article was Rapid screening of protein-protein interaction inhibitors using the protease exclusion assay. And the article contained the following:

We have previously developed a sensitive and modular homogenous biosensor system using peptides to detect target ligands. By transposing the basic mechanistic principle of the nuclease protection assay into this biosensor framework, we have developed the protease exclusion (PE) assay which can discern antagonists of protein-protein interactions in a rapid, single-step format. We demonstrate the concept with multiple protein-peptide pairs and validate the method by successfully screening a small mol. library for compounds capable of inhibiting the therapeutically relevant p53-Mdm2 interaction. The Protease Exclusion method adds to the compendium of assays available for rapid analyte detection and is particularly suited for drug screening applications. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).COA of Formula: C12H16N2O2

The Article related to protease small mol screening biosensor p53 mdm2 protein, biosensor, high throughput screening, p53–mdm2 interaction, protein–protein interaction, Pharmacology: Structure-Activity and other aspects.COA of Formula: C12H16N2O2

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Kuriyama, Masami; Kujirada, Shota; Tsukuda, Kotaro; Onomura, Osamu published an article in 2017, the title of the article was Nickel-Catalyzed Deoxygenative Deuteration of Aryl Sulfamates.Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone And the article contains the following content:

The nickel-catalyzed deoxygenative deuteration of aryl/heteroaryl sulfamates was developed, and the effective incorporation of deuterium into a variety of aromatic compounds was achieved with sufficient catalytic efficiency and high deuteration degree. This process tolerated reducible functional moieties and heterocyclic structures. Addnl., a double introduction of deuterium also successfully gave a desired product with a high yield and deuterium content. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

The Article related to aryl sulfamate deoxygenative deuteration nickel catalyst, General Organic Chemistry: Synthetic Methods and other aspects.Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Kuriyama, Masami; Kujirada, Shota; Tsukuda, Kotaro; Onomura, Osamu published an article in 2017, the title of the article was Nickel-Catalyzed Deoxygenative Deuteration of Aryl Sulfamates.Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone And the article contains the following content:

The nickel-catalyzed deoxygenative deuteration of aryl/heteroaryl sulfamates was developed, and the effective incorporation of deuterium into a variety of aromatic compounds was achieved with sufficient catalytic efficiency and high deuteration degree. This process tolerated reducible functional moieties and heterocyclic structures. Addnl., a double introduction of deuterium also successfully gave a desired product with a high yield and deuterium content. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

The Article related to aryl sulfamate deoxygenative deuteration nickel catalyst, General Organic Chemistry: Synthetic Methods and other aspects.Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Deka, Nabajyoti; Bajare, Swapnil; Anthony, Jessy; Nair, Amrutha; Damre, Anagha; Patel, Dharmeshkumar; B.-Rao, Chandrika; Sivaramakrishnan, H.; Mutt, Shivaprakash Jagalur; Wilankar, Chandan; Marita, Rosalind published an article in 2013, the title of the article was Synthesis of N-(6-(4-(piperazin-1-yl)phenoxy)pyridin-3-yl)benzenesulfonamide derivatives for the treatment of metabolic syndrome.Recommanded Product: 67914-60-7 And the article contains the following content:

Metabolic syndrome is a widely prevalent multifactorial disorder associated with an increased risk of cardiovascular disease and type 2 diabetes mellitus. High plasma levels of insulin and glucose due to insulin resistance are a major component of the metabolic disorder. Thiazolidinediones (TZDs) are potent PPARγ ligands and used as insulin sensitizers in the treatment of type 2 diabetes mellitus. They are potent insulin-sensitizing agents but due to adverse effects like hepatotoxicity, a safer alternative of TZDs is highly demanded. The synthesis of N-(6-(4-(piperazin-1-yl)phenoxy)pyridin-3-yl)benzenesulfonamide derivatives I (R = 2,4-Cl2C6H3, 2,5-(OCH3)2C6H3, 2-thienyl, etc.) an alternate remedy for insulin resistance is reported. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Recommanded Product: 67914-60-7

The Article related to piperazinyl pyridinyl benzenesulfonamide preparation metabolic syndrome, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Recommanded Product: 67914-60-7

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On January 27, 2022, Lee, Song Hee; Ryu, Je Ho; Ahn, Jung Min; Choi, Yu Ri; Lee, Ho Hyun; Jang, Mi Young; Woo, Yae Jin; Kim, Hanwool; Kim, Ji Young; Park, Ji Youn published a patent.Related Products of 1211568-27-2 The title of the patent was Amide compound for androgen receptor degradation, and pharmaceutical use thereof. And the patent contained the following:

The present invention provides a compound I [R1 = H, alkyl, halogen, etc.; R2 = H, alkyl, halogen, etc.; X1, X3, X4 and X5 = independently CH or N; X2 = CR3 or N; R3 = H, alkyl, halogen, etc.; n = 0, 1, or 2; m = 0 or 1; L = -(CH2)q1-A1-(CH2)q2-B1-(CH2)q3-A2-(CH2)q4-B2-(CH2)q5-A3-(CH2)q6-B3-; A1, A2 and A3 = independently direct bond, -O-, -N(R4)-, etc.; R4 = H, alkyl or haloalkyl; B1, B2 and B3 = independently direct bond, cycloalkyl, heterocycle, etc.; q1-q6 = independently 0-6; E = Q1 or Q2; X6, X7, X8 and X9 = independently CH or N; Y = -C(R6)2-, -C(O)-, -C(R6)2-C(R6′)2-, etc.; Z = direct bond, -C(R6)2-, -O-, etc.; R5 and R5′ = independently H, alkyl, halogen, etc.; R6 and R6′ = independently H, alkyl, halogen, etc.] of a specific chem. structure, having androgen receptor (AR) degradation activity, or a pharmaceutically acceptable salt thereof. The present invention also provides a composition containing the compound or a pharmaceutically acceptable salt thereof. According to present invention, provided is a pharmaceutical use of the compound, the salt thereof, and the composition containing same for treating or preventing AR-related diseases. According to the present invention, further provided is a method for treating or preventing AR-related diseases, the method comprising administering, to a subject in need of treatment, an effective amount of the compound, the salt thereof, or the composition containing same. For example, compound II (preparation given) was coupled with compound III (preparation given) to provide compound IV. The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).Related Products of 1211568-27-2

The Article related to amide compound preparation androgen receptor degradation activity, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Related Products of 1211568-27-2

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On August 11, 1998, De Laszlo, Stephen E.; Liverton, Nigel J.; Ponticello, Gerald S.; Selnick, Harold G.; Mantlo, Nathan B. published a patent.Electric Literature of 890092-19-0 The title of the patent was Preparation of arylpyrroles as cytokine inhibitors. And the patent contained the following:

Title compounds [I; R1 = H, alkyl, heterocyclyl, aryl, etc.; R2 = alk(en)yl, alkynyl, heterocyclyl, etc.; R3 = H, halo, alkyl, heterocyclyl, etc.; R4 = (un)substituted heteroaryl; R5 = ZR; R = 1-3 of halo, alkyl, acyl, (hetero)aryl, etc.; Z = (hetero)arylene] were prepared Thus, R5COCH2R4 (R4 = 4-pyridyl, R5 = 4-FC6H4) was α-alkylated by ClCH2COR2 (R2 = 1-benzyloxycarbonyl-4-piperidinyl)(preparation each given) and the product cyclocondensed with NH4Ac to give, after reduction, I (R1 = R3 = H, R2 = 1-methyl-4-piperidinyl, R4 = 4-pyridyl, R5 = 4-FC6H4). Data for biol. activity of I were given. The experimental process involved the reaction of 4-(4-Acetylpiperazin-1-yl)benzaldehyde(cas: 890092-19-0).Electric Literature of 890092-19-0

The Article related to arylpyrrole preparation cytokine inhibitor, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Electric Literature of 890092-19-0

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On March 16, 1986, Orjales Venero, Aurelio; Toledo Avello, Antonio published a patent.Synthetic Route of 59695-29-3 The title of the patent was Process for the preparation of amide derivatives of 4-amino-1,2,3,4,4a,9b-hexahydro-8,9b-dimethyldibenzofuran-3-one. And the patent contained the following:

The title amides I (R = alkyl; n = 1-4), known to be useful as analgesics and antitussives, are prepared by amidation of the title amine (II) with the corresponding (alkylpiperazinyl)alkanoic acids III in an anhydrous organic solvent and in the presence of a dehydrating agent. Thus, a solution of II.HCl in DMF was neutralized with K2CO3, filtered, and added to a solution of III.2HCl (R = Me, n = 2) and DCC in DMF, followed by workup and acidification, to give 50% I.2HCl (R = Me, n = 2). The experimental process involved the reaction of 3-(4-Methylpiperazin-1-yl)propanoic acid dihydrochloride(cas: 59695-29-3).Synthetic Route of 59695-29-3

The Article related to dibenzofuranone piperazinylalkanoylamino preparation analgesic antitussive, piperazinylalkanoylaminodibenzofuranone preparation analgesic antitussive, Heterocyclic Compounds (One Hetero Atom): Furans and other aspects.Synthetic Route of 59695-29-3

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics