Heterocyclic Building Blocks-piperazine

Fischer, Wolfgang; Franke, Heike; Kruegel, Ute; Mueller, Heiko; Dinkel, Klaus; Lord, Brian; Letavic, Michael A.; Henshall, David C.; Engel, Tobias published an article in 2016, the title of the article was Critical evaluation of p2x7 receptor antagonists in selected seizure models.Electric Literature of 1428327-31-4 And the article contains the following content:

The ATP-gated P2X7 receptor (P2X7R) is a non-selective cation channel which senses high extracellular ATP concentrations and has been suggested as a target for the treatment of neuroinflammation and neurodegenerative diseases. The use of P2X7R antagonists may therefore be a viable approach for treating CNS pathologies, including epileptic disorders. Recent studies showed anticonvulsant potential of P2X7R antagonists in certain animal models. To extend this work, we tested three CNS-permeable P2X7R blocker (Brilliant Blue G, AFC-5128, JNJ-47965567) and a natural compound derivative (tanshinone IIA sulfonate) in four well-characterized animal seizure models. In the maximal electroshock seizure threshold test and the pentylenetetrazol (PTZ) seizure threshold test in mice, none of the four compounds demonstrated anticonvulsant effects when given alone. Notably, in combination with carbamazepine, both AFC-5128 and JNJ-47965567 increased the threshold in the maximal electroshock seizure test. In the PTZ-kindling model in rats, useful for testing antiepileptogenic activities, Brilliant Blue G and tanshinone exhibited a moderate retarding effect, whereas the potent P2X7R blocker AFC-5128 and JNJ-47965567 showed a significant and long-lasting delay in kindling development. In fully kindled rats, the investigated compounds revealed modest effects to reduce the mean seizure stage. Furthermore, AFC- 5128- and JNJ-47965567-treated animals displayed strongly reduced Iba 1 and GFAP immunoreactivity in the hippocampal CA3 region. In summary, our results show that P2X7R antagonists possess no remarkable anticonvulsant effects in the used acute screening tests, but can attenuate chem.-induced kindling. Further studies would be of interest to support the concept that P2X7R signalling plays a crucial role in the pathogenesis of epileptic disorders. The experimental process involved the reaction of N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide(cas: 1428327-31-4).Electric Literature of 1428327-31-4

The Article related to seizure p2x7 receptor antagonist afc5128 jnj47965567, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Electric Literature of 1428327-31-4

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

On April 28, 2022, Rome, Zachary; Derby, Michael published a patent.Recommanded Product: N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide The title of the patent was Administration of antipurinergic compositions for treating nervous system disorders. And the patent contained the following:

The present invention provides methods and compositions for treating nervous system disorders such as cognitive, social, or behavioral disabilities, and neurodevelopmental disorders. More specifically, the present invention demonstrates that administration of antipurinergic agents such as berberine, emodin, suramin, tangeretin, A-438079, A-839977, A-804598, JNJ-47965567, and KN-62 are effective to ameliorate or provide an improvement in one or more of the symptoms or manifestations associated with these disabilities and disorders. The experimental process involved the reaction of N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide(cas: 1428327-31-4).Recommanded Product: N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide

The Article related to antipurinergic agent nervous system disorder treatment, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Recommanded Product: N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide

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

On December 26, 2019, Goldman, Steven A.; Osipovitch, Mikhail published a patent.Category: piperazines The title of the patent was Methods of treating or inhibiting onset of Huntington’s disease with gene modulatory compounds. And the patent contained the following:

The disclosure herein relates generally to a method of treating or inhibiting onset of Huntington’s disease. This method involves selecting a subject having or at risk of having Huntington’s disease and administering to the subject one or modulators of one or more genes as described herein, or proteins encoded therefrom, under conditions effective to treat or inhibit onset of Huntington’s disease in the subject. The exemplary compounds of the invention include e.g. 2-amino-4-(3,4-(methylenedioxy)benzylamino)-6-(3-methoxyphenyl)pyrimidine (2-AMBMP), curcumin, simvastatin, opicinumab, GSK-249320, sodium lauryl sulfate, repaglinide, altiratinib. The experimental process involved the reaction of N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide(cas: 1428327-31-4).Category: piperazines

The Article related to neuroprotectant antihuntington drug huntington disease treatment, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Category: piperazines

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

On April 22, 2021, Hopper, Allen T.; Juhl, Martin; Hornberg, Jorrit; Badolo, Lassina; Kilburn, John Paul; Thougaard, Annemette; Smagin, Gennady; Song, Dekun; Calice, Londye; Menon, Veena; Dale, Elena; Zhang, Hong; Cajina, Manuel; Nattini, Megan E.; Gandhi, Adarsh; Grenon, Michel; Jones, Ken; Khayrullina, Tanzilya; Chandrasena, Gamini; Thomsen, Christian; Zorn, Stevin H.; Brodbeck, Robb; Poda, Suresh Babu; Staal, Roland; Moller, Thomas published an article.Related Products of 1428327-31-4 The title of the article was Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139. And the article contained the following:

There remains an insufficient number of P2X7 receptor antagonists with adequate rodent potency, CNS permeability, and pharmacokinetic properties from which to evaluate CNS disease hypotheses preclinically. Herein, we describe the mol. pharmacol., safety, pharmacokinetics, and functional CNS target engagement of Lu AF27139, a novel rodent-active and CNS-penetrant P2X7 receptor antagonist. Lu AF27139 is highly selective and potent against rat, mouse, and human forms of the receptors. The rat pharmacokinetic profile is favorable with high oral bioavailability, modest clearance (0.79 L/(h kg)), and good CNS permeability. In vivo mouse CNS microdialysis studies of lipopolysaccharide (LPS)-primed and 2′(3′)-O-(benzoylbenzoyl)adenosine-5′-triphosphate (BzATP)-induced IL-1β release demonstrate functional CNS target engagement. Importantly, Lu AF27139 was without effect in standard in vitro and in vivo toxicity studies. Based on these properties, we believe Lu AF27139 will be a valuable tool for probing the role of the P2X7 receptor in rodent models of CNS diseases. The experimental process involved the reaction of N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide(cas: 1428327-31-4).Related Products of 1428327-31-4

The Article related to orally bioavailable cns penetrant p2x7 receptor antagonist probe, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Related Products of 1428327-31-4

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

Dong, Ze-Xi; Shi, Zhi-Hao; Li, Nian-Guang; Zhang, Wei; Gu, Ting; Zhang, Peng-Xuan; Wu, Wen-Yu; Tang, Yu-Ping; Fang, Fang; Xue, Xin; Li, He-Min; Cheng, Hai-Bo; Yang, Jian-Ping; Duan, Jin-Ao published an article in 2016, the title of the article was Design, Synthesis, and Biological Evaluation of Scutellarein Derivatives Based on Scutellarin Metabolic Mechanism In Vivo.Synthetic Route of 53788-12-8 And the article contains the following content:

Three series of scutellarein derivatives have been designed and synthesized based on metabolic mechanism of scutellarin (1) in vivo. Their thrombin inhibition activities were tested through the analyzation of prothrombin time (PT), activated partial thromboplastin time (APTT), thrombin time (TT), and fibrinogen (FIB). The antioxidant activities of these target products were assessed by 1,1-diphenyl-2-picrylhydrazyl radical (DPPH) assay and the ability to protect PC12 cells against H2O2-induced cytotoxicity, and their solubilities were evaluated by UV spectrophotometer. The results showed that the two iso-Pr groups substituted derivative (18c) demonstrated stronger anticoagulant activity, better water solubility, and good antioxidant activity compared with scutellarein (2), which warrants further development of 18c as a promising agent for ischemic cerebrovascular disease treatment. The experimental process involved the reaction of 4-Ethyl-piperazine-1-carbonyl chloride(cas: 53788-12-8).Synthetic Route of 53788-12-8

The Article related to scutellarein derivative neuroprotectant antioxidant, antioxidant, scutellarein, scutellarin, solubility, thrombin, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Synthetic Route of 53788-12-8

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

On August 31, 2008, Chen, Yonghao; Long, Shengjing published an article.Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was Synthesis of ketoconazole by phase-transfer catalysis. And the article contained the following:

Antifungal drug ketoconazole was synthesized by utilization of phase-transfer catalysis from [2-bromomethyl-2-(2,4-dichlorophenyl)-1,3-dioxolan-4-yl]methanol via acylation, N-alkylation with imidazole and hydrolysis, formation the active ester with methanesulfonyl chloride, and then condensation with the side chain 1-acetyl-4-(4-hydroxyphenyl)piperazine. The overall yield was about 30%. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

The Article related to ketoconazole synthesis antifungal drug bromomethyldichlorophenyl dioxolanylmethanol, Industrial Organic Chemicals, Leather, Fats, and Waxes: Manufacture Of Industrial Organic Chemicals and other aspects.Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

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

On April 30, 1997, Huang, Liang-Fu; Kim, Jang-Woo; Bauer, Ludwig; Doss, George published an article.Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was Synthesis of 1,2,4-triazole and thiazole analogs of ketoconazole. And the article contained the following:

The synthesis of 1,2,4-triazole and thiazole analogs of ketoconazole is described in which one of the α azole ring carbons is linked to C-2 of the ketal by means of a three methylene tether. Lithiation of 1-methyl-1,2,4-triazole and thiazole and subsequent alkylation with 2-(2,4-dichlorophenyl)-2-(3-iodopropyl)-1,3-dioxolane produced, after an aqueous acidic workup, 2,4-dichlorophenyl 3-[5-(1-methyl-1,2,4-triazolyl) and 2-thiazolyl]propyl ketones, resp. Ketalization with glycerol furnished the corresponding diastereomeric pairs of cis- and trans-1,3-dioxolanes. The reaction of 2,4-dichlorophenyl 3-[5-(1-methyl-1,2,4-triazolyl)]propyl ketone with 3-mercapto-1,2-propanediol produced the corresponding diastereomeric cis- and trans-hydroxymethyl-1,3-oxathiolanes. The diastereomeric racemates were separated by column chromatog. and their stereochem. established by NOE NMR experiments Some of these racmic cis ketal alcs. were converted by benzyl bromide to the corresponding benzyl ethers. Several of these racemic cis-ketals were reacted, first with methanesulfonyl chloride, then with 1-acetyl-4-(4-hydroxyphenyl)piperazine, to furnish the title compounds 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 ketoconazole triazole thiazole analog preparation, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

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

On August 31, 2007, He, Qiuqin; Liu, Chaomei; Li, Ke; Cao, Yongbing; Zhao, Lihua; Tang, Wenya published an article.Reference of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was Synthesis and antifungal activities of 1-(1H-1,2,4-triazol-1-yl)-2-(tert-butyl)-3-(O-substituted)-2-propanol derivatives. And the article contained the following:

A method for the synthesis of the title compounds [i.e., α-(1,1-dimethylethyl)-α-[[4-(1-piperazinyl)phenoxy]methyl]-1H-1,2,4-Triazole-1-ethanol derivatives] is reported here. The antifungal activity of triazole derivatives bearing a tert-Bu group was studied and their antifungal activity was compared with those of the control drugs (fluconazole and itraconazole). Twelve target compounds were designed by the replacement of a 2,4-difluorophenyl group with a tert-Bu group. The target compounds were determined by NMR, IR. The MICs80 of these title compounds were determined by a method recommended by the National Committee for Clin. Laboratory Standards (NCCLS) using an RPMI 1640 test medium. The results of the preliminary antifungal test showed that all the target compounds exhibited potent antifungal activity. Other hydrophobic moieties besides a 2,4-difluorophenyl group can be introduced to design triazole compounds The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Reference of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

The Article related to triazoleethanol dimethylethyl piperazinyl phenoxy preparation antifungal agent, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Reference of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

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

Heeres, J.; Backx, L. J. J.; Van Cutsem, J. published an article in 1984, the title of the article was Antimycotic azoles. 7. Synthesis and antifungal properties of a series of novel triazol-3-ones.Computed Properties of 67914-60-7 And the article contains the following content:

The antifungal triazolone derivatives I [R = H, Me, Q (X = N, CH); R1 = H, alkyl; R2 = H, Me) were prepared by a multistep sequence from 1-(p-methoxyphenyl)piperazine or MeSO3Q via piperazines III (R3 = H, Bz) and cyclization of III [R3 = C(:NH)NH2] with R2C(:NH)NH2. In vitro and in vivo antifungal properties of I are reported. Compound I [R = Q (X = N), R1 = MeEtCH, R2 = H], which displays a pronounced oral activity against vaginal candidosis in rats and against microsporosis in guinea pigs, was selected for clin. evaluation. 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 triazolone phenylpiperazinophenyl preparation fungicide, fungicide phenylpiperazinophenyltriazolone, piperazinophenyltriazolone phenyl, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Computed Properties of 67914-60-7

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

Yang, Jiqiu; Liu, Lilin; Wang, Xiaoyan; Lu, Jiaguo; Sun, Changsheng; Zhang, Huanxiang; Zhou, Youjun; Zhang, Zhong published an article in 1984, the title of the article was Synthesis of an antifungal drug ketoconazole.Formula: C12H16N2O2 And the article contains the following content:

The title compound [I, R = p-(4-acetylpiperazin-1-yl)phenyl] was prepared by condensation of I (R = MeSO2) with piperazine II which was prepared starting from piperazine. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Formula: C12H16N2O2

The Article related to ketoconazole, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Formula: C12H16N2O2

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