Category: piperazines

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.Electric Literature of C5H12N2 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: 109-01-3Electric 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

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. COA of Formula: 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: 109-01-3COA of Formula: 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..COA of Formula: 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.. SDS of cas: 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: 70006-24-5SDS of cas: 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.SDS of cas: 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. Quality Control of 1-Methylpiperazine 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: 109-01-3Quality 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

Archana, Sriramapura D.; Kumar, Haruvegowda Kiran; Yathirajan, Hemmige S.; Foro, Sabine; Abdelbaky, Mohammed S. M.; Garcia-Granda, Santiago published an article in 2021. The article was titled 《Crystal structure studies of 4-ethylpiperazin-1-ium 3,5-dinitrobenzoate, 4-methylpiperazin-1-ium 3,5-dinitrobenzoate and 4-methylpiperazin-1-ium 4-iodobenzoate》, and you may find the article in Acta Crystallographica, Section E: Crystallographic Communications.Application In Synthesis of 1-Methylpiperazine The information in the text is summarized as follows:

As part of our ongoing investigation on the chem. and biol. properties of piperazinium salts, we synthesized three novel compounds: 1-ethylpiperazinium 3,5-dinitrobenzoate (I), 1-methylpiperazinium 3,5-dinitrobenzoate (II) and 1-methylpiperazinium 4-iodobenzoate (III). The crystal structures of these compounds are built up of organic layers formed by the strong connection between the mols. by hydrogen bonds of type N-H···O. These layers are linked through N-H···O hydrogen bonds and C-H···O interactions or C-I···N halogen bonding, leading to the formation of a three-dimensional network. The results came from multiple reactions, including the reaction of 1-Methylpiperazine(cas: 109-01-3Application In Synthesis 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..Application In Synthesis of 1-Methylpiperazine

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

The author of 《A low-cost, passive release device for the surveillance and control of mosquitoes》 were Kwan, Michael W. C.; Bosak, Alexander; Kline, Jedidiah; Pita, Mario A.; Giel, Nicholas; Pereira, Roberto M.; Koehler, Philip G.; Kline, Daniel L.; Batich, Christopher D.; Willenberg, Bradley Jay. And the article was published in International Journal of Environmental Research and Public Health in 2019. Synthetic Route of C5H12N2 The author mentioned the following in the article:

Mosquitoes continue to be a major threat to global health, and the ability to reliably monitor, catch, and kill mosquitoes via passive traps is of great importance. Global, low-cost, and easy-to-use outdoor devices are needed to augment existing efforts in mosquito control that combat the spread of disease, such as Zika. Thus, we have developed a modular, portable, non-powered (passive), self-contained, and field-deployable device suitable for releasing volatiles with a wide range of applications such as attracting, repelling, and killing mosquitoes. This unique device relies on a novel nested wick and two-reservoir design that achieves a constant release of volatiles over several hundred hours. Devices loaded with one of either two compounds, geraniol or 1-methylpiperazine (MP), were tested in a controlled environment (32°C and 70% relative humidity), and both compounds achieved a constant release from our devices at a rate of 2.4 mg/h and 47 mg/h, resp. The liquid payload can be volatile attractants or repellents as well as mosquitocide-containing feeding solutions for capture and surveillance. This low-cost device can be utilized for both civilian and military mosquito control purposes, but it will be particularly important for protecting those in economically repressed environments, such as sub-Saharan Africa and Central and South America. After reading the article, we found that the author used 1-Methylpiperazine(cas: 109-01-3Synthetic Route 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..Synthetic Route of C5H12N2

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

The author of 《Syntheses and crystal structures of a new family of hybrid perovskites: C5H14N2·ABr3·0.5H2O (A = K, Rb, Cs)》 were Ferrandin, Sarah; Slawin, Alexandra M. Z.; Harrison, William T. A.. And the article was published in Acta Crystallographica, Section E: Crystallographic Communications in 2019. Quality Control of 1-Methylpiperazine The author mentioned the following in the article:

The syntheses and crystal structures of three hybrid perovskites, viz. poly[1-methylpiperizine-1,4-diium [tri-μ-bromido-potassium] hemihydrate], {(C5H14N2)[KBr3]·0.5H2O}n, (I), poly[1-methylpiperizine-1,4-diium [tri-μ-bromido-rubidium] hemihydrate], {(C5H14N2)[RbBr3]·0.5H2O}n, (II), and poly[1-methylpiperizine-1,4-diium [tri-μ-bromido-caesium] hemihydrate], {(C5H14N2)[CsBr3]·0.5H2O}n, (III), are described. These isostructural (space group Amm2) phases contain a three-dimensional, corner-sharing network of distorted ABr6 octahedra (A = K, Rb, Cs) with the same topol. as the classical perovskite structure. The doubly protonated C5H14N22+ cations occupy interstices bounded by eight octahedra and the water mols. lie in square sites bounded by four octahedra. N-H···Br, N-H···(Br,Br), N-H···O and O-H···Br hydrogen bonds consolidate the structures. The experimental part of the paper was very detailed, including the reaction process 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

Jakhmola, Vikas; Jawla, Sunil; Mishra, Ravinesh; Rao, N. G. Raghavendra published their research in International Journal of Pharmaceutical Sciences and Research in 2021. The article was titled 《Synthesis and in-vivo activity of novel antihypertensive agent based on pyridazine scaffold》.Related Products of 109-01-3 The article contains the following contents:

The main objective of the present research work to synthesize, characterization, and in-vivo evaluation of Pyridazine derivatives To study the different synthesized derivatives by using different anal. parameters like IR, Mass, and NMR anal. And also find out the antihypertensive activity. The studies on the hydralazine group drugs led to the synthesis of many Pyridazine derivatives with a wide activity spectrum on the cardiovascular system. Pyridazine derivatives, a class of compounds containing the N-N bond, exhibit a wide range of pharmacol. activities such as antidepressant, antihypertensive, and cardiotonic, etc. Some 6-(substituted phenyl)-2-(substituted methyl)-4,5-dihydropyridazin-3(2H)-one derivative was synthesized by reacting 6-Ph substituted 2,3,4,5-Tetrahydro pyridazin-3-one with cyclic secondary amine under Mannich reaction conditions. A total of twenty compounds (vj1-vj20) were synthesized under Mannich reaction conditions. Out of twenty compounds, around six derivatives were selected for evaluation of antihypertensive activities by a non-invasive method using the Tail Cuff method. Most of the compounds showed good antihypertensive activity. Few compounds like vj3, vj6, vj9, vj14, vj19, and vj20 were found to show a highly significant reduction in mean arterial blood pressure but at a higher dose in comparison to standard drugs like propanolol and hydralazine. The substituted pyridazine derivatives discovered in this study may provide valuable therapeutic intervention for the treatment of hypertension. After reading the article, we found that the author used 1-Methylpiperazine(cas: 109-01-3Related Products of 109-01-3)

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..Related Products of 109-01-3

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

The author of 《Determination of base dissociation constants (Pkb) of mono- and polyamines by pH metric method》 were Ahmad, Mamshad; Masohan, Asha; Sawhney, S. S.. And the article was published in International Journal of Research in Chemistry and Environment in 2019. Application In Synthesis of 1-Methylpiperazine The author mentioned the following in the article:

Dissociation constants of acids and bases (pKa and pKb) are very important criteria to define the strength of acids or bases. In organic chem. acids generally the compounds that contain -COOH group and bases are amines and their derivatives This paper presents the study of pKb of about 20 organic amines. pKb determination is done pH metrically which is a very simple method for this type of study. pKb of some of the reported amines are already determined by various researcher by using different methods. Most of the amines reported in this paper are studied fist time for pKb study. It is found that those amines which are studied for pKb value and available in the literature, give almost same result with presented corresponding values. Some of the amines (bases) are common but most of the amines are uncommon and they are used for a very specific purpose. pKa value is used in many cases to solve connecting problems. These pKb values can be used for research and other purposes. This paper presents the pKa/pKb determination of mono-(one amino group), di-(two amino group), tri-(three amino group) and tetra (four amino groups) amines, which will be a very good work for others for research purposes. The results came from multiple reactions, including the reaction of 1-Methylpiperazine(cas: 109-01-3Application In Synthesis 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..Application In Synthesis of 1-Methylpiperazine

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

《Ring substituents on substituted benzamide ligands indirectly mediate interactions with position 7.39 of transmembrane helix 7 of the D4 dopamine receptor》 was written by Ericksen, Spencer S.; Cummings, David F.; Teer, Michael E.; Amdani, Shahnawaz; Schetz, John A.. Name: Abt-724 And the article was included in Journal of Pharmacology and Experimental Therapeutics on August 31 ,2012. The article conveys some information:

In an effort to delineate how specific mol. interactions of dopamine receptor ligand classes vary between D2-like dopamine receptor subtypes, a conserved threonine in transmembrane (TM) helix 7 (Thr7.39), implicated as a key ligand interaction site with biogenic amine G protein-coupled receptors, was substituted with alanine in D2 and D4 receptors. Interrogation of different ligand chemotypes for sensitivity to this substitution revealed enhanced affinity in the D4, but not the D2 receptor, specifically for substituted benzamides (SBAs) having polar 4- (para) and/or 5- (meta) benzamide ring substituents. D4-T7.39A was fully functional, and the mutation did not alter the sodium-mediated pos. and neg. allostery observed with SBAs and agonists, resp. With the exception of the non-SBA ligand (+)-butaclamol, which, in contrast to certain SBAs, had decreased affinity for the D4-T7.39A mutant, the interactions of numerous other ligands were unaffected by this mutation. SBAs were docked into D4 models in the same mode as observed for eticlopride in the D3 crystal structure. In this mode, interactions with TM5 and TM6 residues constrain the SBA ring position that produces distal steric crowding between pyrrolidinyl/diethylamine moieties and D4-Thr7.39. Ligand-residue interaction energy profiles suggest this crowding is mitigated by substitution with a smaller alanine. The profiles indicate sites that contribute to the SBA binding interaction and site-specific energy changes imparted by the D4-T7.39A mutation. Substantial interaction energy changes are observed at only a few positions, some of which are not conserved among the dopamine receptor subtypes and thus seem to account for this D4 subtype-specific structure-activity relationship. In the experiment, the researchers used many compounds, for example, Abt-724(cas: 70006-24-5Name: Abt-724)

Abt-724(cas: 70006-24-5) belongs to piperazines. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Name: Abt-724

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