Category: piperazines

Evrard, Deborah A.; Zhou, Ping; Yi, Soo Y.; Zhou, Dahui; Smith, Deborah L.; Sullivan, Kelly M.; Hornby, Geoffrey A.; Schechter, Lee E.; Andree, Terrance H.; Mewshaw, Richard E. published an article on February 15 ,2005. The article was titled 《Studies towards the next generation of antidepressants. Part 4: Derivatives of 4-(5-fluoro-1H-indol-3-yl)cyclohexylamine with affinity for the serotonin transporter and the 5-HT1A receptor》, and you may find the article in Bioorganic & Medicinal Chemistry Letters.Category: piperazines The information in the text is summarized as follows:

Derivatives of the serotonin reuptake inhibitor 4-(5-fluoro-1H-indol-3-yl)cyclohexylamine, in which serotonin 1A (5-HT1A) receptor pharmacophoric elements are incorporated, are reported. Analogs exhibiting affinity for both the serotonin transporter and the 5-HT1A receptor are described. Compounds containing 1-(4-indolyl)piperazine and 2-(1H-indol-4-yloxy)ethylamine are promising leads for further SAR studies. In the experimental materials used by the author, we found 4-(Piperazin-1-yl)-1H-indole(cas: 84807-09-0Category: piperazines)

4-(Piperazin-1-yl)-1H-indole(cas: 84807-09-0) belongs to piperazines. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines.Category: piperazines

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

Product Details of 34352-59-5On October 20, 2015 ,《(2-Arylethenyl)-1,3,5-triazin-2-amines as a novel histamine H4 receptor ligands》 was published in European Journal of Medicinal Chemistry. The article was written by Kaminska, Katarzyna; Ziemba, Julia; Ner, Joanna; Schwed, Johannes Stephan; Lazewska, Dorota; Wiecek, Malgorzata; Karcz, Tadeusz; Olejarz, Agnieszka; Latacz, Gniewomir; Kuder, Kamil; Kottke, Tim; Zygmunt, Malgorzata; Sapa, Jacek; Karolak-Wojciechowska, Janina; Stark, Holger; Kiec-Kononowicz, Katarzyna. The article contains the following contents:

Within the constantly growing number of histamine H4 (H4R) receptor ligands there is a large group of azine derivatives A series of novel compounds in the group of 4-methylpiperazinyl-1,3,5-triazin-2-amines were designed and obtained. Structures were modified at the triazine 6-position by introduction of variously substituted arylethenyl moieties. Their affinities to histamine H4 receptors were evaluated in radioligand binding assays with use of Sf9 cells, transiently expressing human H4R. Pharmacol. studies identified 4-[(E)-2-(3-chlorophenyl)ethenyl]-6-(4-methylpiperazin-1-yl)-1,3,5-triazin-2-amine (Ki = 253 nM) as the most potent compound in the present series. In the experiment, the researchers used many compounds, for example, 1-Methylpiperazine dihydrochloride(cas: 34352-59-5Product Details of 34352-59-5)

1-Methylpiperazine dihydrochloride(cas: 34352-59-5) is used in the preparation of 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), 1-methylpiperazine-1,4-diium tetrachloridozincate hemihydrate, 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), an antimicrotubular drug..Product Details of 34352-59-5

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

《Dopamine D4 receptor involvement in the discriminative stimulus effects in rats of LSD, but not the phenethylamine hallucinogen DOI》 was written by Marona-Lewicka, Danuta; Chemel, Benjamin R.; Nichols, David E.. COA of Formula: C17H19N5 And the article was included in Psychopharmacology (Berlin, Germany) on April 30 ,2009. The article conveys some information:

Rationale: Lysergic acid diethylamide (LSD) differs from other types of hallucinogens in that it possesses direct dopaminergic effects. The exact nature of this component has not been elucidated. Objective: The present study sought to characterize the effects of several dopamine D4 agonists and antagonists on the discriminative stimulus effect of LSD at two pretreatment times and 2,5-dimethoxy-4-iodoamphetamine (DOI), a selective 5-HT2A/2C agonist. Materials and methods: Male Sprague-Dawley rats were trained in a two-lever, fixed ratio (FR) 50, food-reinforced task with LSD-30 (0.08 mg/kg, i.p., 30-min pretreatment time), LSD-90 (0.16 mg/kg, i.p., 90-min pretreatment time), and DOI (0.4 mg/kg, i.p., 30-min pretreatment time) as discriminative stimuli. Substitution and combination tests with the dopamine D4 agonists, ABT-724 and WAY 100635, were performed in all groups. Combination tests were run using the dopamine D4 antagonists A-381393 and L-745,870 and two antipsychotic drugs, clozapine and olanzapine. Results: WAY 100635 produced full substitution in LSD-90 rats, partial substitution in LSD-30 rats, and saline appropriate responding in DOI-trained rats. ABT-724 partially mimicked the LSD-90 and LSD-30 cues, but produced no substitution in DOI-trained rats. In combination tests, both agonists shifted the dose-response curve of LSD leftward, most potently for the LSD-90 cue. The D4 antagonists significantly attenuated both the LSD-90 and LSD-30 cue, but had no effect on the DOI cue. Conclusion: Dopamine D4 receptor activation plays a significant modulatory role in the discriminative stimulus effects in LSD-90-trained rats, most markedly for the later temporal phase of LSD, but has no effect on the cue produced by DOI.Abt-724(cas: 70006-24-5COA of Formula: C17H19N5) was used in this study.

Abt-724(cas: 70006-24-5) belongs to piperazines. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines.COA of Formula: C17H19N5

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

Onder, Ferah Comert; Sahin, Kader; Senturk, Murat; Durdagi, Serdar; Ay, Mehmet published an article in 2022. The article was titled 《Identifying highly effective coumarin-based novel cholinesterase inhibitors by in silico and in vitro studies》, and you may find the article in Journal of Molecular Graphics & Modelling.Recommanded Product: 1-Methylpiperazine The information in the text is summarized as follows:

Inhibition of high cholinesterase levels including acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), is one of the most important strategies for the treatment of Alzheime′s disease (AD). Clin. limited drugs are used in the treatment of AD, so there is a need to find new effective inhibitors today. Therefore, in this study, synthesized six coumarin carboxamides (A1, A2, B1-B4) were evaluated against AChE and BChE by combined in silico and in vitro studies. The in vitro assessment of studied compounds revealed that A1, A2, B3, and B4 showed highest inhibition potential against AChE and BChE. As demonstrated with our structure activity relationship (SAR) study, the promising inhibition result of AChE at nanomolar concentrations was obtained with heterocyclic amines including pyrrolidine and N-Me piperazine moieties for tertiary amide substituted coumarin compounds B3 and B4, displaying KI values of 9.78 nM and 8.07 nM, resp. Thus, compounds B3 and B4 had around 5.7- and 6.9-fold more potency compared to the reference mol., neostigmine. Moreover, coumarin-3-carboxamide derivative A1 bearing benzylmorpholine moiety on coumarin scaffold at position 3 displayed stronger inhibition potential against BChE. Furthermore, in order to better understand their mol. mechanisms in these targets, we conducted mol. docking and MD simulations. Our promising preclin. results show that the lead compounds A1, A2, B3 and B4 have high potential as effective inhibitors for the treatment of AD. The experimental process involved the reaction of 1-Methylpiperazine(cas: 109-01-3Recommanded Product: 1-Methylpiperazine)

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Recommanded Product: 1-Methylpiperazine

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

Pullagurla, Manik; Siripurapu, Uma; Kolanos, Renata; Bondarev, Mikhail L.; Dukat, Malgorzata; Setola, V.; Roth, B. L.; Glennon, Richard A. published their research in Bioorganic & Medicinal Chemistry Letters on December 1 ,2005. The article was titled 《Binding of amine-substituted N 1-benzenesulfonylindoles at human 5-HT6 serotonin receptors》.Reference of 4-(Piperazin-1-yl)-1H-indole The article contains the following contents:

An examination of several amine-substituted analogs of N1-benzenesulfonylindoles reveals that although they bind at human 5-HT6 serotonin receptors with high affinity, they are likely to bind in a dissimilar manner. The experimental part of the paper was very detailed, including the reaction process of 4-(Piperazin-1-yl)-1H-indole(cas: 84807-09-0Reference of 4-(Piperazin-1-yl)-1H-indole)

4-(Piperazin-1-yl)-1H-indole(cas: 84807-09-0) belongs to piperazines. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines.Reference of 4-(Piperazin-1-yl)-1H-indole

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

Electric Literature of C22H25ClN6O2On November 1, 2017 ,《Design, synthesis and biological evaluation of WZ4002 analogues as EGFR inhibitors》 appeared in Bioorganic & Medicinal Chemistry Letters. The author of the article were Romu, Aireen A.; Lei, Zining; Zhou, Bin; Chen, Zhe-Sheng; Korlipara, Vijaya. The article conveys some information:

A series of thirty two anilinopyrimidines derived from WZ4002 has been synthesized and evaluated for percentage inhibition of six different EGFR kinases using LanthaScreen binding assay method (EGFR d746 – 750) or Z’LYTE assay method (EGFR-WT, EGFR d746 – 750, EGFR T790M, EGFR T790M L858R, EGFR C797S and EGFR T790M L858R C797S). Ortho-hydroxyacetamide I (R = 2′-NHCOCH2OH) exhibited complete inhibition of all the six kinases at 10 μM. Against the triple mutant, EGFR T790M C797S L858R, compounds I [R = 2′-NHCOCH2OCH2Ph, 2′-NHCOCH2OH, 2′-NHCO(CH2)2OCH2Ph, 2′-NHCO(CH2)2OH] exhibited complete inhibition at 10 μM and nearly complete inhibition at 1 μM. The target compounds were also evaluated using the MTT assay to determine their cytotoxic activity against human non-small cell lung cancer cells (PC9, PC9GR and H460) and mouse leukemic cells (Ba/F3 WT and Ba/F3T 3151). Overall, I [R = 2′-N3, 2′-NHCOCH2OCH2Ph, 2′-NHCOCH2OH, 2′-NHCO(CH2)2OCH2Ph, 2′-NHCO(CH2)2OH, 4′-NHCOCH2OCH2Ph, 4′-NHCOCH2OH] were found to be the most potent compounds across all five cell lines. In the experiment, the researchers used many compounds, for example, 4-(3-Aminophenoxy)-5-chloro-N-(2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)pyrimidin-2-amine(cas: 1213269-26-1Electric Literature of C22H25ClN6O2)

4-(3-Aminophenoxy)-5-chloro-N-(2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)pyrimidin-2-amine(cas: 1213269-26-1) is a member of pyrimidine. Pyrimidine derivatives are an important class of N-heterocycles. They are well-known for their wide spectrum of promising biological activities such as antitumors, bactericidals, and fungicidal.Electric Literature of C22H25ClN6O2

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

Ayad, Magda Mohamed; Hosny, Mervat Mohamed; Metias, Youstina Mekhail published an article in 2022. The article was titled 《Green micellar liquid chromatographic analysis of alfuzosin hydrochloride and sildenafil citrate in a binary mixture compared to classical RPLC with stability indicating studies》, and you may find the article in Drug Development and Industrial Pharmacy.Quality Control of 1-Methylpiperazine The information in the text is summarized as follows:

Two simple and validated chromatog. studies were performed for simultaneous estimation of sildenafil citrate (SIL) and alfuzosin hydrochloride (ALF) in bulk, pharmaceuticals, and in the presence of their main degradation products. Two systems of mobile phase were applied isocratically for their first chromatog. separation using conventional and micellar mobile phases. Methanol, acetonitrile, and 0.02 M potassium dihydrogen phosphate (43:14:43 volume/volume; pH 4.66) were pumped at 1.3 mL/min in method I. Meanwhile, method II was based on less hazardous micellar mobile phase of nonionic surfactant (0.005 M Brij-35 in water; pH 2.5 adjusted with 0.1% orthophosphoric acid) with a flow rate of 1 mL/min. Both methods were carried on C18 column and coupled with UV detection at 225 nm at ambient temperature The first method was rectilinear over the concentration range of 5-62.5 μg/mL for both drugs, while the second method showed higher linearity ranges of 0.5-40, 2.5-62.5 μg/mL for ALF and (SIL), resp. The developed methods successfully enabled the quantification of the studied binary mixture in their tablets dosage form and evaluation their stabilities. Validation of the proposed methods according to ICH guidelines and system suitability were ascertained. Moreover, the applied methods were evaluated and compared from the perspective of green anal. chem., employing the National Environmental Methods Index, anal. Eco-Scale score, and Green Anal. Procedure Index, as three assessment tools. The results came from multiple reactions, including the reaction of 1-Methylpiperazine(cas: 109-01-3Quality Control of 1-Methylpiperazine)

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Quality Control of 1-Methylpiperazine

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

In 2019,Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry included an article by Manouchehrizadeh, Elham; Mostoufi, Azar; Tahanpesar, Elham; Fereidoonnezhad, Masood. Electric Literature of C5H12N2. The article was titled 《Design, synthesis, molecular docking and cytotoxic activity evaluations of novel piperidine and piperazine derivatives of dichloroacetate as potential anticancer agents》. The information in the text is summarized as follows:

A series of novel dichloro(piperidinyl/piperazinyl)-ethanone derivatives I [X = CH2, NH, NPh, etc.] of dichloroacetate was designed and subjected to mol. docking studies. Based on the docking results, compounds with the lowest binding energy and better interaction with PDKs isoenzymes were selected and synthesized. The cytotoxic activity of the synthesized compounds was evaluated against HT-29 and MCF7 human cancer cell lines. These compounds showed moderate potencies with much higher anticancer activity than DCA. The most active of the series, I [X = NH], showed IC50 value of 7.79μM against HT-29 cell line. In the experimental materials used by the author, we found 1-Methylpiperazine(cas: 109-01-3Electric Literature of C5H12N2)

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Electric Literature of C5H12N2

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

《Activation of dopamine D4 receptors by ABT-724 induces penile erection in rats》 was written by Brioni, Jorge D.; Moreland, Robert B.; Cowart, Marlon; Hsieh, Gin C.; Stewart, Andrew O.; Hedlund, Petter; Donnelly-Roberts, Diana L.; Nakane, Masaki; Lynch, James J. III; Kolasa, Teodozyi; Polakowski, James S.; Osinski, Mark A.; Marsh, Kennan; Andersson, Karl-Erik; Sullivan, James P.. Related Products of 70006-24-5 And the article was included in Proceedings of the National Academy of Sciences of the United States of America on April 27 ,2004. The article conveys some information:

Apomorphine, a nonselective dopamine receptor agonist, facilitates penile erection and is effective in patients suffering from erectile dysfunction. The specific dopamine receptor subtype(s) responsible for its erectogenic effect is not known. Here we report that the dopamine D4 receptor plays a role in the regulation of penile function. ABT-724 is a selective dopamine D4 receptor agonist that activates human dopamine D4 receptors with an EC50 of 12.4 nM and 61% efficacy, with no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 dose-dependently facilitates penile erection when given s.c. to conscious rats, an effect that is blocked by haloperidol and clozapine but not by domperidone. A proerectile effect is observed after intracerebroventricular but not intrathecal administration, suggesting a supraspinal site of action. S.c. injections of ABT-724 increase intracavernosal pressure in awake freely moving rats. In the presence of sildenafil, a potentiation of the proerectile effect of ABT-724 is observed in conscious rats. The ability of ABT-724 to facilitate penile erection together with the favorable side-effect profile indicates that ABT-724 could be useful for the treatment of erectile dysfunction. In the experiment, the researchers used Abt-724(cas: 70006-24-5Related Products of 70006-24-5)

Abt-724(cas: 70006-24-5) belongs to piperazines. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines.Related Products of 70006-24-5

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

The author of 《PET imaging of microglia by targeting macrophage colony-stimulating factor 1 receptor (CSF1R)》 were Horti, Andrew G.; Naik, Ravi; Foss, Catherine A.; Minn, Il; Misheneva, Varia; Du, Yong; Wang, Yuchuan; Mathews, William B.; Wu, Yunkou; Hall, Andrew; La Course, Catherine; Ahn, Hye-Hyun; Nam, Hwanhee; Lesniak, Wojciech G.; Valentine, Heather; Pletnikova, Olga; Troncoso, Juan C.; Smith, Matthew D.; Calabresi, Peter A.; Savonenko, Alena V.; Dannals, Robert F.; Pletnikov, Mikhail V.; Pomper, Martin G.. And the article was published in Proceedings of the National Academy of Sciences of the United States of America in 2019. Category: piperazines The author mentioned the following in the article:

While neuroinflammation is an evolving concept and the cells involved and their functions are being defined, microglia are understood to be a key cellular mediator of brain injury and repair. The ability to measure microglial activity specifically and noninvasively would be a boon to the study of neuroinflammation, which is involved in a wide variety of neuropsychiatric disorders including traumatic brain injury, demyelinating disease, Alzheimer disease (AD), and Parkinson disease, among others. We have developed [11C]CPPC [5-cyano-N-(4-(4-[11C]methylpiperazin-1-yl)-2-(piperidin-1-yl)phenyl)furan-2-carboxamide], a positron-emitting, high-affinity ligand that is specific for the macrophage colony-stimulating factor 1 receptor (CSF1R), the expression of which is essentially restricted to microglia within brain. [11C]CPPC demonstrates high and specific brain uptake in a murine and nonhuman primate lipopolysaccharide model of neuroinflammation. It also shows specific and elevated uptake in a murine model of AD, exptl. allergic encephalomyelitis murine model of demyelination and in postmortem brain tissue of patients with AD. Radiation dosimetry in mice indicated [11C]CPPC to be safe for future human studies. [11C]CPPC can be synthesized in sufficient radiochem. yield, purity, and specific radioactivity and possesses binding specificity in relevant models that indicate potential for human PET imaging of CSF1R and the microglial component of neuroinflammation. The results came from multiple reactions, including the reaction of 1-Methylpiperazine(cas: 109-01-3Category: piperazines)

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Category: piperazines

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