Category: piperazines

Nitroaldol reactions catalyzed by amine-MCM-41 hybrids was written by Wang, Qingqing;Shantz, Daniel F.. And the article was included in Journal of Catalysis in 2010.Product Details of 21867-64-1 This article mentions the following:

The catalytic properties of several amine-functionalized MCM-41 materials in a nitroaldol (Henry) reaction are reported. The work investigated the effects of organoamine type (primary, secondary, tertiary), amine d., and the presence of silanol groups on the catalytic activity and product selectivity. High selectivity to the nitro alc. product was achieved by introducing secondary and tertiary amine groups on the MCM-41 surface, while the nitroalkene is the dominant product for primary amines. Steric effects appear to be significant in determining the overall reactivity as the least sterically hindered amines are the most active. The capping of silanols with trimethylsilyl groups resulted in a reduction in catalytic activity for nearly all samples, indicating the importance of surface silanols and/or the surface polarity in the reaction. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Product Details of 21867-64-1).

1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Although many piperazine derivatives occur naturally, piperazine itself can be synthesized by reacting alcoholic ammonia with 1,2-dichloroethane, by the action of sodium and ethylene glycol on ethylene diamine hydrochloride, or by reduction of pyrazine with sodium in ethanol.Product Details of 21867-64-1

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

New Heterocyclic Hepatitis C Virus (HCV) Inhibitors Containing A 2-Aminomethyl-1H-Indole Fragment was written by Ivachtchenko, A. V.;Yamanushkin, P. M.;Mit’kin, O. D.;Ezhova, E. V.;Korzinov, O. M.;Bulanova, E. A.;Bichko, V. V.;Ivashchenko, A. A.. And the article was included in Pharmaceutical Chemistry Journal in 2015.SDS of cas: 21867-64-1 This article mentions the following:

A focused library of heterocyclic compounds including a 2-aminomethyl-1H-benzimidazole, 2-aminomethylindole, benzofuran-2-ylmethylamine, or 2-piperazin-1-ylmethylbenzoxazole fragment was screened for the ability to inhibit in vitro hepatitis C virus (HCV). The synthetic methods were described. The antiviral activity and cytotoxicity data were presented. Most of the compounds carrying a benzoxazol-2-ylmethylamine fragment inhibited Huh7.3 human hepatoma cells infected in vitro with HCV with nanomolar potency but were inactive against the HCV RNA-replicon. The only exception was 9-methyl-N(6)-(3-nitrophenyl)-2,3,4,9-tetrahydro-1H-carbazole-1,6-diamine, which demonstrated nanomolar potency against HCV in both models. The most active and selective compounds were (piperazin-1-yl)-[(1H-indol-2-ylmethyl)piperidin-4-yl]-ketones (EC₅₀ 0.31-2.2 μM, CC₅₀ 10.2-110 μM) and 2-(1,2,3a,4,5,6-hexahydropyrazino[3,2,1-jk]carbazol-3-yl)acetamide (EC₅₀ 1.69±0.5 μM, CC₅₀ 114±42 μM). The two most selective inhibitors I (TI₅₀ = 52) and II (TI₅₀ = 68) were selected for further preclin. trials. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1SDS of cas: 21867-64-1).

1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.SDS of cas: 21867-64-1

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

Synthesis and hypoglycemic activity of 7,8-dihydro-6H-thiopyrano[3,2-d]pyrimidine derivatives and related compounds was written by Ohno, Sachio;Mizukoshi, Kiyoshi;Komatsu, Osamu;Kuno, Yasuo;Nakamura, Yoshiki;Kato, Eiichi;Nagasaka, Mitsuaki. And the article was included in Chemical & Pharmaceutical Bulletin in 1986.Related Products of 21867-64-1 This article mentions the following:

Apparatus 80 amino piperazino derivatives of the title system were prepared and tested for hypoglycemic activity for potential use as antidiabetics. The most promising were I and II. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Related Products of 21867-64-1).

1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 °C and boils at 125–130 °C. Piperazine is an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines.Related Products of 21867-64-1

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

Discovery of 3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-[4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl]benzamide (AP24534), a Potent, Orally Active Pan-Inhibitor of Breakpoint Cluster Region-Abelson (BCR-ABL) Kinase Including the T315I Gatekeeper Mutant was written by Huang, Wei-Sheng;Metcalf, Chester A.;Sundaramoorthi, Raji;Wang, Yihan;Zou, Dong;Thomas, R. Mathew;Zhu, Xiaotian;Cai, Lisi;Wen, David;Liu, Shuangying;Romero, Jan;Qi, Jiwei;Chen, Ingrid;Banda, Geetha;Lentini, Scott P.;Das, Sasmita;Xu, Qihong;Keats, Jeff;Wang, Frank;Wardwell, Scott;Ning, Yaoyu;Snodgrass, Joseph T.;Broudy, Marc I.;Russian, Karin;Zhou, Tianjun;Commodore, Lois;Narasimhan, Narayana I.;Mohemmad, Qurish K.;Iuliucci, John;Rivera, Victor M.;Dalgarno, David C.;Sawyer, Tomi K.;Clackson, Tim;Shakespeare, William C.. And the article was included in Journal of Medicinal Chemistry in 2010.Recommanded Product: 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline This article mentions the following:

In the treatment of chronic myeloid leukemia (CML) with BCR-ABL kinase inhibitors, the T315I gatekeeper mutant has emerged as resistant to all currently approved agents. This report describes the structure-guided design of a novel series of potent pan-inhibitors of BCR-ABL, including the T315I mutation. A key structural feature is the carbon-carbon triple bond linker which skirts the increased bulk of Ile315 side chain. Extensive SAR studies led to the discovery of development candidate benzamide I (AP24534), which inhibited the kinase activity of both native BCR-ABL and the T315I mutant with low nM IC₅₀s, and potently inhibited proliferation of corresponding Ba/F3-derived cell lines. Daily oral administration of I significantly prolonged survival of mice injected i.v. with BCR-ABL^T315I expressing Ba/F3 cells. These data, coupled with a favorable ADME profile, support the potential of I to be an effective treatment for CML, including patients refractory to all currently approved therapies. In the experiment, the researchers used many compounds, for example, 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6Recommanded Product: 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline).

4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. Recommanded Product: 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline

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

Synthesis, and antitumor activity of some N1-(7-coumarinyl)amidrazones and related congeners was written by Mustafa, Mohammad S.;El-Abadelah, Mustafa M.;Zihlif, Malek A.;Naffa, Randa G.;Mubarak, Mohammad S.. And the article was included in Molecules in 2011.Category: piperazines This article mentions the following:

Piperazine coumarin amidrazone derivatives and related congeners were designed, the synthesis of the target compounds was achieved using 2-oxo-N-(2-oxo-4-methyl-2H-1-benzopyran-7-yl)propanehydrazonoyl chloride and piperazine derivatives, piperidine, morpholine, thiomorpholine, 1-[2-ethyl-4-nitro-1-(phenylmethyl)-1H-imidazol-5-yl]piperazine, etc., as reactants and the products thus obtained [i.e., 1-(1-piperazinyl)-1,2-propanedione 1-[2-(3-methyl-2-oxo-2H-1-benzopyran-7-yl)hydrazone] derivatives, amidrazones] were confirmed by elemental analyses, ¹H-NMR, ¹³C-NMR, and ESI-HRMS spectral data. The title compounds were evaluated against the cell line MCF-7 (human mammary adenocarcinoma cell line), cell line K562 (human chronic myelogenous leukemia cell line), cell line HL60 (human promyelocytic leukemia cell line) and cell line ZR-75-1 (human mammary tumor, breast carcinoma cell line) it was discovered that they displayed activity as antitumor agents. Among all the compounds tested, 7-[2-[1-[4-(1-benzyl-2-ethyl-4-nitro-1H-imidazol-5-yl)-1-piperazinyl]-2-(oxo)propylidene]hydrazinyl]-4-methyl-2-chromenone was the most potent against MCF-7 and K562 cells, with IC₅₀ values of 20.2 and 9.3 μM, resp. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Category: piperazines).

1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 °C and boils at 125–130 °C. Piperazine is an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines.Category: piperazines

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

A Highly Regioselective Amination of 6-Aryl-2,4-dichloropyrimidine was written by Peng, Zhi-Hui;Journet, Michel;Humphrey, Guy. And the article was included in Organic Letters in 2006.Category: piperazines This article mentions the following:

A highly regioselective amination of 6-aryl-2,4-dichloropyrimidines with aliphatic secondary amines and aromatic amines which strongly favors the formation of the C4-substituted product has been developed. The reactions with aliphatic amines are carried out using LiHMDS as the base and are catalyzed by Pd, while the aromatic amines require no catalyst. In the experiment, the researchers used many compounds, for example, (R)-1-Cbz-3-methylpiperazine (cas: 623586-00-5Category: piperazines).

(R)-1-Cbz-3-methylpiperazine (cas: 623586-00-5) belongs to piperazine derivatives. The piperazine scaffold is often found in biologically active compounds in different therapeutic areas. These therapeutic areas include antifungals, antidepressants, antivirals, and serotonin receptor (5-HT) antagonists/agonists. 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).Category: piperazines

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

Synthesis, biological evaluation, X-ray molecular structure and molecular docking studies of RGD mimetics containing 6-amino-2,3-dihydroisoindolin-1-one fragment as ligands of integrin α_IIbβ₃ was written by Krysko, Andrei A.;Samoylenko, Georgiy V.;Polishchuk, Pavel G.;Fonari, Marina S.;Kravtsov, Victor Ch.;Andronati, Sergei A.;Kabanova, Tatyana A.;Lipkowski, Janusz;Khristova, Tetiana M.;Kuz’min, Victor E.;Kabanov, Vladimir M.;Krysko, Olga L.;Varnek, Alexandre A.. And the article was included in Bioorganic & Medicinal Chemistry in 2013.Synthetic Route of C16H22N2O4 This article mentions the following:

Acylaminooxoisoindolealkanoic acid RGD mimetics such as tetrahydroisoquinolinecarbonylamino oxoisoindolylpropanoic acid I•HCl were prepared as integrin α_IIbβ₃ ligands for inhibiting platelet aggregation for potential use as antithrombotic agents. The inhibition of platelet aggregation by the oxoisoindolealkanoic acids was determined, and for some compounds, the inhibition of fluorescein-labeled fibrinogen binding to human platelets (and thus to integrin α_IIbβ₃) was also determined; for example, I•HCl inhibited platelet aggregation with an IC₅₀ value of 1.1 μM and inhibited the binding of fluorescein-labeled fibrinogen to platelets with an IC₅₀ value of 6.5 nM. Mol. docking calculations of eight of the prepared compounds bound to integrin α_IIbβ₃ were performed, indicating the key interactions present; correlations between docking scores and binding affinities were also found. Of the motifs tried, the use of an N-terminal tetrahydroisoquinolinecarbonyl group and a C-terminal β-alanine moiety provided the most effective platelet aggregation inhibitors. The structures for a Me aminooxoisoindolebutanoate, a tetrahydroisoquinolinedicarboxylic acid mono-tert-Bu ester, and solvates, salts, or free bases of five of the oxoisoindolealkanoic acids prepared including I•H₂O were determined by X-ray crystallog. In the experiment, the researchers used many compounds, for example, 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid (cas: 162046-66-4Synthetic Route of C16H22N2O4).

4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid (cas: 162046-66-4) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Although many piperazine derivatives occur naturally, piperazine itself can be synthesized by reacting alcoholic ammonia with 1,2-dichloroethane, by the action of sodium and ethylene glycol on ethylene diamine hydrochloride, or by reduction of pyrazine with sodium in ethanol.Synthetic Route of C16H22N2O4

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

Multistep Continuous-Flow Synthesis in Medicinal Chemistry: Discovery and Preliminary Structure-Activity Relationships of CCR8 Ligands was written by Petersen, Trine P.;Mirsharghi, Sahar;Rummel, Pia C.;Thiele, Stefanie;Rosenkilde, Mette M.;Ritzen, Andreas;Ulven, Trond. And the article was included in Chemistry – A European Journal in 2013.Recommanded Product: 623586-00-5 This article mentions the following:

A three-step continuous-flow synthesis system and its application to the assembly of a new series of chemokine receptor ligands directly from com. building blocks is reported. No scavenger columns or solvent switches are necessary to recover the desired test compounds, which were obtained in overall yields of 49-94%. The system is modular and flexible, and the individual steps of the sequence can be interchanged with similar outcome, extending the scope of the chem. Biol. evaluation confirmed activity on the chemokine CCR8 receptor and provided initial structure-activity-relationship (SAR) information for this new ligand series, with the most potent member displaying full agonist activity with single-digit nanomolar potency. To the best of the knowledge, this represents the first published example of efficient use of multistep flow synthesis combined with biol. testing and SAR studies in medicinal chem. In the experiment, the researchers used many compounds, for example, (R)-1-Cbz-3-methylpiperazine (cas: 623586-00-5Recommanded Product: 623586-00-5).

(R)-1-Cbz-3-methylpiperazine (cas: 623586-00-5) belongs to piperazine derivatives. The piperazine scaffold is often found in biologically active compounds in different therapeutic areas. These therapeutic areas include antifungals, antidepressants, antivirals, and serotonin receptor (5-HT) antagonists/agonists. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.Recommanded Product: 623586-00-5

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

Tetrahydroquinoline sulfonamides as γ-secretase inhibitors was written by Asberom, Theodros;Bara, Thomas A.;Clader, John W.;Greenlee, William J.;Guzik, Henry S.;Josien, Hubert B.;Li, Wei;Parker, Eric M.;Pissarnitski, Dmitri A.;Song, Lixin;Zhang, Lili;Zhao, Zhiqiang. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2007.Synthetic Route of C7H16N2 This article mentions the following:

The development of a novel series of tetrahydroquinoline-derived γ-secretase inhibitors for the potential treatment of Alzheimer’s disease is described. Incorporation of a fluorine substituent at position 7 resulted in the most potent compound I. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Synthetic Route of C7H16N2).

1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Synthetic Route of C7H16N2

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

Chemotherapeutically active anthraquinones. II. Aminomethylanthraquinones was written by Winkelmann, E.;Raether, W.. And the article was included in Arzneimittel-Forschung in 1986.SDS of cas: 21867-64-1 This article mentions the following:

Anthraquinones [I, R = OAc, S₂CNEt₂, Sc(:NH)NH₂, NH₂, dialkylamino, heterocyclic, S(CH₂)₂NEt₂, OC₆H₄NH₂, R¹ = H, XR, R² = H, XR, Me, R³ = R⁵ = H, OH, heterocyclic, R⁴ = H, OH] were prepared and tested in vitro and in vivo (in hamster) against Entamoeba histolytica and interferon-inducing property in mice. Activity against Trichomonas foetus (in mice) was also tested. Most of the compounds showed chemotherapeutic activities in these tests. Structure-activity relations are discussed. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1SDS of cas: 21867-64-1).

1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Although many piperazine derivatives occur naturally, piperazine itself can be synthesized by reacting alcoholic ammonia with 1,2-dichloroethane, by the action of sodium and ethylene glycol on ethylene diamine hydrochloride, or by reduction of pyrazine with sodium in ethanol.SDS of cas: 21867-64-1

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