Category: piperazines

Novel 4-substituted 2-piperazinylquinazolines as potent anticonvulsive and antihypoxic agents was written by Hori, Manabu;Iemura, Ryuichi;Hara, Hideaki;Ozaki, Akio;Sukamoto, Takayuki;Ohtaka, Hiroshi. And the article was included in Chemical & Pharmaceutical Bulletin in 1990.Synthetic Route of C7H16N2 This article mentions the following:

Piperazinylquinazolines, e.g. I [R = Me, Ph, CH₂Ph, CH₂CH:CH₂, (CH₂)_nMe, R¹ = Me, CH₂Ph, (CH₂)_nMe, n = 2-4] were prepared and examined for anticonvulsive and antihypoxic activities. The anal. of quant. structure-activity relationships indicated that the anticonvulsive activity was related to the lipophilicity of the compounds Most of the alkoxyquinazolines I showed potent anticonvulsive and antihypoxic activities. There is a good correlation between the potencies of these activities. 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 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. 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

III. Identification of novel CXCR3 chemokine receptor antagonists with a pyrazinyl-piperazinyl-piperidine scaffold was written by Kim, Seong Heon;Anilkumar, Gopinadhan N.;Zawacki, Lisa Guise;Zeng, Qingbei;Yang, De-Yi;Shao, Yuefei;Dong, Guizhen;Xu, Xiaolian;Yu, Wensheng;Jiang, Yueheng;Jenh, Chung-Her;Hall, James W. III;Carroll, Carolyn DiIanni;Hobbs, Doug W.;Baldwin, John J.;McGuinness, Brian F.;Rosenblum, Stuart B.;Kozlowski, Joseph A.;Shankar, Bandarpalle B.;Shih, Neng-Yang. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2011.Recommanded Product: (S)-2-Ethylpiperazine This article mentions the following:

The SAR of a novel pyrazinyl-piperazinyl-piperidine scaffold with CXCR3 receptor antagonist activity was explored. Optimization of the DMPK profile and reduction of hERG inhibition is described. One compound with single-digit CXCR3 affinity and good rat PK and hERG profiles has been identified as a lead for further study. In the experiment, the researchers used many compounds, for example, (S)-2-Ethylpiperazine (cas: 207284-20-6Recommanded Product: (S)-2-Ethylpiperazine).

(S)-2-Ethylpiperazine (cas: 207284-20-6) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. 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.Recommanded Product: (S)-2-Ethylpiperazine

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

Iridium-Catalyzed C-H Borylation of Heteroarenes: Scope, Regioselectivity, Application to Late-Stage Functionalization, and Mechanism was written by Larsen, Matthew A.;Hartwig, John F.. And the article was included in Journal of the American Chemical Society in 2014.SDS of cas: 780705-64-8 This article mentions the following:

A study on the iridium-catalyzed C-H borylation of heteroarenes is reported. Several heteroarenes containing multiple heteroatoms were amenable to C-H borylation catalyzed by the combination of an iridium(I) precursor and tetramethylphenanthroline. The investigations of the scope of the reaction led to the development of powerful rules for predicting the regioselectivity of borylation, foremost of which is that borylation occurs distal to nitrogen atoms. One-pot functionalizations are reported of the heteroaryl boronate esters formed in situ, demonstrating the usefulness of the reported methodol. for the synthesis of complex heteroaryl structures. Application of this methodol. to the synthesis and late-stage functionalization of biol. active compounds is also demonstrated. Mechanistic studies show that basic heteroarenes can bind to the catalyst and alter the resting state from the olefin-bound complex observed during arene borylation to a species containing a bound heteroarene, leading to catalyst deactivation. Studies on the origins of the observed regioselectivity show that borylation occurs distal to N-H bonds due to rapid N-H borylation, creating an unfavorable steric environment for borylation adjacent to these bonds. Computational studies and mechanistic studies show that the lack of observable borylation of C-H bonds adjacent to basic nitrogen is not the result of coordination to a bulky Lewis acid prior to C-H activation, but the combination of a higher-energy pathway for the borylation of these bonds relative to other C-H bonds and the instability of the products formed from borylation adjacent to basic nitrogen. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(pyrimidin-2-yl)piperazine-1-carboxylate (cas: 780705-64-8SDS of cas: 780705-64-8).

tert-Butyl 4-(pyrimidin-2-yl)piperazine-1-carboxylate (cas: 780705-64-8) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 掳C and boils at 125鈥?30 掳C. 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: 780705-64-8

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

Molecular Simplification of 1,4-Diazabicyclo[4.3.0]nonan-9-ones Gives Piperazine Derivatives That Maintain High Nootropic Activity was written by Manetti, Dina;Ghelardini, Carla;Bartolini, Alessandro;Dei, Silvia;Galeotti, Nicoletta;Gualtieri, Fulvio;Romanelli, Maria Novella;Teodori, Elisabetta. And the article was included in Journal of Medicinal Chemistry in 2000.SDS of cas: 21867-64-1 This article mentions the following:

Several 4-substituted 1-acylpiperazines, obtained by mol. simplification of 4-substituted 1,4-diazabicyclo[4.3.0]nonan-9-ones, have been synthesized and tested in vivo on the mouse passive avoidance test, to evaluate their nootropic activity. The results show that, apparently, an N-acylpiperazine group can mimic the 2-pyrrolidinone ring of 1,4-diazabicyclo[4.3.0]nonan-9-one, as the compounds of the new series maintain high nootropic activity. Moreover mol. simplification produces more clear-cut structure-activity relationships with respect to the parent series. The mechanism of action also appears to be similar in the two series. In fact, although the mol. mechanism remains to be elucidated, the most potent compound of each class is able to increase acetylcholine release in rat brain. Piperazine derivatives represent a new class of nootropic drugs with an in vivo pharmacol. profile very similar to that of piracetam, showing much higher potency with respect to the reference compound Among the compounds studied, 1-benzoyl-4-propionylpiperazine (DM235) shows outstanding potency, being active at a dose of 0.001 mg kg^-1 s.c. 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. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. 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.SDS of cas: 21867-64-1

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

Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors was written by Zhao, Bin;Li, Yixuan;Xu, Pan;Dai, Yang;Luo, Cheng;Sun, Yiming;Ai, Jing;Geng, Meiyu;Duan, Wenhu. And the article was included in ACS Medicinal Chemistry Letters in 2016.Computed Properties of C16H22N2O4 This article mentions the following:

Fibroblast growth factor receptors (FGFRs) are important targets for cancer therapy. Herein, we describe the design, synthesis, and biol. evaluation of a novel series of 1H-pyrazolo[3,4-b]pyridine derivatives as potent and selective FGFR kinase inhibitors. On the basis of its excellent in vitro potency and favorable pharmacokinetic properties, compound I was selected for in vivo evaluation and showed significant antitumor activity in a FGFR1-driven H1581 xenograft model. These results indicated that I would be a promising candidate for further drug development. In the experiment, the researchers used many compounds, for example, 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid (cas: 162046-66-4Computed Properties of C16H22N2O4).

4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid (cas: 162046-66-4) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. 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. Computed Properties of C16H22N2O4

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

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 渭M, CC₅₀ 10.2-110 渭M) and 2-(1,2,3a,4,5,6-hexahydropyrazino[3,2,1-jk]carbazol-3-yl)acetamide (EC₅₀ 1.69卤0.5 渭M, CC₅₀ 114卤42 渭M). 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 掳C and boils at 125鈥?30 掳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 渭M, 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 掳C and boils at 125鈥?30 掳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