Tag: 100-200

《Synthesis, characterization and carbonic anhydrase I and II inhibitory evaluation of new sulfonamide derivatives bearing dithiocarbamate》 was published in European Journal of Medicinal Chemistry in 2020. These research results belong to Saglik, Begum Nurpelin; Osmaniye, Derya; Cevik, Ulviye Acar; Levent, Serkan; Cavusoglu, Betul Kaya; Buyukemir, Oya; Nezir, Deniz; Karaduman, Abdullah Burak; Ozkay, Yusuf; Koparal, Ali Savas; Beydemir, Sukru; Kaplancikli, Zafer Asim. Quality Control of 1-Methylpiperazine The article mentions the following:

In this study, novel dithiocarbamate-sulfonamide derivatives I [R = Me, cyclohexyl, 4-O2NC6H4, etc.] were synthesized to investigate their inhibitory activity on purified human carbonic anhydrase (hCA) I and II. The IC50 and Ki values of the compounds were calculated to compare their inhibition profiles on hCA I and II isoenzymes. Acetazolamide was used as the standard inhibitor in the enzyme inhibition assay. Compounds I [R = Me, 4-MeC6H4CH2, CH2CH2NMe2, CH2CH2CH2NMe2, 2-pyridinyl, 2-pyrimidinyl] showed notable inhibitory effects against hCA I and II. Among these compounds, compound I [R = CH2CH2CH2NMe2] was found to be the most active derivate against both the hCA I and II enzymes with Ki values of 0.032 ± 0.001μM and 0.013 ± 0.0005μM, resp. The cytotoxicity of compounds I [R = Me, 4-MeC6H4CH2, CH2CH2NMe2, CH2CH2CH2NMe2, 2-pyridinyl, 2-pyrimidinyl] toward NIH/3T3 (mouse embryonic fibroblast cell line) was observed and the compounds were found to be non-cytotoxic. Furthermore, mol. docking studies were performed to investigate the interaction types between compound I [R = CH2CH2CH2NMe2] and the hCA I and II enzymes. As a result of this study a novel and potent class of CA inhibitors with good activity potential were identified. 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

Synthetic Route of C5H14Cl2N2On 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: 34352-59-5Synthetic Route of C5H14Cl2N2)

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..Synthetic Route of C5H14Cl2N2

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.Computed Properties of C5H12N2 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: 109-01-3Computed Properties 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..Computed Properties of C5H12N2

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.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

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