Month: October 2022

In 1993,Bulletin of the Faculty of Pharmacy (Cairo University) included an article by Al-Deeb, O. A.; Al-Rashood, K. A.; Khalil, A. A.. Product Details of 34352-59-5. The article was titled 《Synthesis of new (1-phenylcyclohexyl)piperazine derivatives as potential analgesics》. The information in the text is summarized as follows:

A series of phencyclidine isostere derivatives was prepared by replacement of the piperidine ring by N-substituted piperazines. The Strecker synthesis was employed for synthesis of the intermediate carbonitriles I [R = (un)substituted Ph, Me, PhCH2; R1 = CN]. The synthesis of the target compounds I (same R; R1 = Ph) was accomplished by treatment of the carbonitrile with phenylmagnesium bromide. These compounds were tested for analgesic activity, but none were effective. The experimental part of the paper was very detailed, including the reaction process of 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

In 2016,Journal of Enzyme Inhibition and Medicinal Chemistry included an article by Gul, Halise Inci; Tugrak, Mehtap; Sakagami, Hiroshi. Recommanded Product: 1-Methylpiperazine dihydrochloride. The article was titled 《Synthesis of some acrylophenones with N-methylpiperazine and evaluation of their cytotoxicities》. The information in the text is summarized as follows:

In this study, the compounds having acrylophenone structure, 1-aryl-2-(N-methylpiperazinomethyl)-2-propen-1-one dihydrochlorides, were synthesized and their chem. structures were identified with 1H NMR, 13C NMR and HRMS spectra. The cytotoxicities of the compounds were tested towards Ca9-22 (human gingival carcinoma), HSC-2 (human oral squamous carcinoma), HSC-3 (human oral squamous carcinoma) and HSC-4 (human oral squamous carcinoma) cell lines as tumor cell lines and HGF (gingival fibroblasts), HPLF (periodontal ligament fibroblasts) and HPC (pulp cells) cell lines as non-tumor cell lines. PSE of the compound TA2 which has a Me substituent on Ph ring, pointed out the compound TA2 as a leader compound to be considered. In the part of experimental materials, we found many familiar compounds, such as 1-Methylpiperazine dihydrochloride(cas: 34352-59-5Recommanded Product: 1-Methylpiperazine dihydrochloride)

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..Recommanded Product: 1-Methylpiperazine dihydrochloride

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

Kesarkar, Dnyanadeo J.; Kashid, Bharat B.; Sukthankar, Sunil S. published an article in 2021. The article was titled 《Facile new alternative method for the synthesis of 1-(3-methyl-1-phenyl-1H-pyrazole-5-yl)piperazine from 1-methylpiperazine and 1-benzylpiperazine》, and you may find the article in Organic Preparations and Procedures International.Recommanded Product: 1-Methylpiperazine The information in the text is summarized as follows:

An alternative method for the synthesis of 1-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazine I from 1-methylpiperazine and 1-benzylpiperazine was described. This method avoided the use of labile protecting groups and thus had the potential to improve the impurity profile of key intermediate I. The method used com. available reactants and did not require the use of highly unstable, expensive or hazardous reagents. 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

Synthetic Route of C5H12N2In 2020 ,《Solvent free synthesis of three cyclotriphosphazene derivatives containing piperazine substituents using microwave irradiation. Spectral, theoretical, solution and docking studies》 was published in Phosphorus, Sulfur and Silicon and the Related Elements. The article was written by Hakimi, Mohammad; Rezaei, Homeyra; Moeini, Keyvan; Mardani, Zahra; Carpenter-Warren, Cameron. The article contains the following contents:

Three new cyclotriphosphazene-based compounds, 2,2,4,4,6,6-hexakis(4-R-piperazin-1-yl)-1,3,5,2λ5,4λ5,6λ5-cyclotriazatriphosphinine (1-3; R = Me, Et, Ph), were prepared and identified by elemental anal., FT-IR, Raman as well as 1H and 31P NMR spectroscopy. The redox properties of the compounds were investigated by cyclic voltammetry. The predicted structures and charge distribution patterns of the compounds were obtained by DFT calculations and NBO anal. The geometrical parameters in these optimized structures are in good agreement with the average values obtained for analogs from the CSD database. The theor. studies confirm presence of a strong resonance in the cyclotriphosphazene ring. Finally, the ability of the three new derivatives to interact with ten selected biomacromols. (BRAF kinase, CatB, DNA gyrase, HDAC7, rHA, RNR, TrxR, TS, Top II, B-DNA) was investigated by docking calculations and compared with that of doxorubicin. In addition to this study using 1-Methylpiperazine, there are many other studies that have used 1-Methylpiperazine(cas: 109-01-3Synthetic Route of C5H12N2) was used in this study.

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

COA of Formula: C17H19N5On November 30, 2010 ,《Transmembrane segment five serines of the D4 dopamine receptor uniquely influence the interactions of dopamine, norepinephrine, and Ro10-4548. [Erratum to document cited in CA153:164511]》 appeared in Journal of Pharmacology and Experimental Therapeutics. The author of the article were Cummings, David F.; Ericksen, Spencer S.; Goetz, Angela; Schetz, John A.. The article conveys some information:

On page 685, in Figure 1, the structure for Ro10-4548 was incorrectly given; the correct version of the structure is given. The results came from multiple reactions, including the reaction of Abt-724(cas: 70006-24-5COA of Formula: C17H19N5)

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).COA of Formula: C17H19N5

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

Recommanded Product: Abt-724On May 31, 2008, Newman-Tancredi, Adrian; Heusler, Peter; Martel, Jean-Claude; Ormiere, Anne-Marie; Leduc, Nathalie; Cussac, Didier published an article in International Journal of Neuropsychopharmacology. The article was 《Agonist and antagonist properties of antipsychotics at human dopamine D4.4 receptors: G-protein activation and K+ channel modulation in transfected cells》. The article mentions the following:

Interaction at dopamine D4 receptors may improve cognitive function, which is highly impaired in individuals with schizophrenia, but comparative studies of recent antipsychotics in cellular models of D4 receptor activation are lacking. Here, we report the in-vitro profile of over 30 ligands at recombinant hD4.4 receptors. In [35S]GTPγS binding experiments using membranes of CHO-hD4.4 cells, apomorphine, preclamol and the selective D4 agonists, ABT724, CP226269, Ro-10-5824 and PD168077, behaved as partial agonists (Emax 20-60% vs. dopamine), whereas L745870 and RBI257, displayed antagonist properties. The conventional’ antipsychotic, haloperidol and the atypicals’, clozapine and risperidone, exhibited antagonist properties, while third generation’ compounds bifeprunox, SLV313 and F15063, acted as partial agonists (10-30%). Aripiprazole and SSR181507 slightly stimulated [35S]GTPγS binding at micromolar concentrations In Xenopus laevis oocytes co-expressing hD4.4 receptors with G-protein-coupled inwardly rectifying potassium (GIRK) channels, apomorphine, preclamol, ABT724, CP226269, and PD168077 stimulated GIRK currents (Emax 70-80%). The 5-HT1A receptor ligands, WAY100635 and flibanserin, also exhibited partial agonist activity (30% and 15%, resp.). Haloperidol, clozapine, olanzapine and nemonapride did not stimulate GIRK currents, whereas aripiprazole, bifeprunox, SLV313 and F15063, but not SSR181507, exhibited partial agonism (Emax 20-35%). In-vitro responses depended on exptl. conditions: increasing NaCl concentration (30 mm to 100 mm) reduced agonist efficacy in [35S]GTPγS binding, whereas decreasing the amount of hD4.4 cRNA injected into oocytes (from 2.0 to 0.5 ng/oocyte) reduced agonist efficacy of several compounds These data indicate that, unlike conventional or atypical’ antipsychotics, several third generation’ agents display D4 receptor partial agonism that may be sufficient to influence physiol. D4 receptor activity in vivo. In the experiment, the researchers used many compounds, for example, Abt-724(cas: 70006-24-5Recommanded Product: Abt-724)

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.Recommanded Product: Abt-724

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

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

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 《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