Month: February 2023

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

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 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

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

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

Design, synthesis and antitubercular evaluation of novel series of N-[4-(piperazin-1-yl)phenyl]cinnamamide derivatives was written by Patel, Kavitkumar N.;Telvekar, Vikas N.. And the article was included in European Journal of Medicinal Chemistry in 2014.Application of 182618-86-6 This article mentions the following:

The analogs of N-[4-(piperazin-1-yl)phenyl]cinnamamide were designed and synthesized by a mol. hybridization approach in which part C of the designed mol. was linked through amide and carbamate functionality that improves the physicochem. properties and govern the pharmacokinetic and pharmacodynamic behavior. The systematic modification was done around the Part C to explore the structure activity relationship of antitubercular cinnamamides. All 52 compounds were evaluated for antitubercular activity against Mycobacterium tuberculosis (M. tb) using Resazurin microtitre plate assay (REMA). Compound I with trifluoromethyl substitution exhibited good antitubercular activity of 3.125 μg/mL. The synthesized N-[4-(piperazin-1-yl)phenyl]cinnamamide derivatives showed promising activity against M. tb. In the experiment, the researchers used many compounds, for example, 1-Boc-4-(4-Nitrophenyl)piperazine (cas: 182618-86-6Application of 182618-86-6).

1-Boc-4-(4-Nitrophenyl)piperazine (cas: 182618-86-6) 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. Application of 182618-86-6

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

Synthesis and Biological Evaluation of a Novel Series of “Ortho-Nitrated” Inhibitors of Catechol-O-methyltransferase was written by Learmonth, David A.;Bonifacio, Maria Joao;Soares-da-Silva, Patricio. And the article was included in Journal of Medicinal Chemistry in 2005.HPLC of Formula: 21867-64-1 This article mentions the following:

Novel regioisomeric ortho-nitrated catechols related to the catechol-O-methyltransferase (COMT) inhibitors BIA 3-202 and BIA 3-335 were synthesized and biol. evaluated. Changing the position of the nitro group from the classical meta- to the ortho-position relative to the side-chain substituent of the nitrocatechol pharmacophore exerted profound effects on selectivity and duration of COMT inhibition. 2,3,4-O₂N(HO)₂C₆H₂CO(CH₂)_nPh (I, n = 1-4) possessed shorter duration of action than their regioisomers, but I (n = 2) displayed reversed selectivity over BIA 3-202 at 3 and 6 h, exhibiting preferential central inhibition. In the amino-substituted series, 2,3,4-O₂N(HO)₂C₆H₂COCH₂CH₂R (II, R = 4-benzylpiperidino) was less peripherally selective than BIA 3-335 and short-acting, whereas II (R = decahydroquinolino, III) displayed an unprecedented combination of long-acting and selective peripheral inhibition. I (n = 2) could provide a useful tool to probe the pharmacol. utility of short-acting, centrally selective COMT inhibitors in the treatment of depression in Parkinsonian patients, and III represents a promising candidate for clin. evaluation as an adjunct to L-Dopa therapy. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1HPLC of Formula: 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. 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).HPLC of Formula: 21867-64-1

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

Azetidinones as vasopressin V1a antagonists was written by Guillon, Christophe D.;Koppel, Gary A.;Brownstein, Michael J.;Chaney, Michael O.;Ferris, Craig F.;Lu, Shi-Fang;Fabio, Karine M.;Miller, Marvin J.;Heindel, Ned D.;Hunden, David C.;Cooper, Robin D. G.;Kaldor, Stephen W.;Skelton, Jeffrey J.;Dressman, Bruce A.;Clay, Michael P.;Steinberg, Mitchell I.;Bruns, Robert F.;Simon, Neal G.. And the article was included in Bioorganic & Medicinal Chemistry in 2007.Safety of 1-Propylpiperazine This article mentions the following:

The azetidinone LY307174 (I) was identified as a screening lead for the vasopressin V1a receptor (IC₅₀ 45 nM at the human V1a receptor) based on mol. similarity to ketoconazole, a known antagonist of the LH releasing hormone receptor. Structure-activity relationships for the series, e.g., II, were explored to optimize receptor affinity and pharmacokinetic properties, resulting in compounds with K _i values <1 nM and brain levels after oral dosing ∼100-fold higher than receptor affinities. Display Omitted. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Safety of 1-Propylpiperazine).

1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. 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. Safety of 1-Propylpiperazine

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

Discovery of N-(4-(6-acetamidopyrimidin-4-yloxy)phenyl)-2-(2-(trifluoromethyl)phenyl)acetamide (CHMFL-FLT3-335) as a potent FMS-like tyrosine kinase 3 internal tandem duplication (FLT3-ITD) mutant selective inhibitor for acute myeloid leukemia was written by Liang, Xiaofei;Wang, Beilei;Chen, Cheng;Wang, Aoli;Hu, Chen;Zou, Fengming;Yu, Kailin;Liu, Qingwang;Li, Feng;Hu, Zhenquan;Lu, Tingting;Wang, Junjie;Wang, Li;Weisberg, Ellen L.;Li, Lili;Xia, Ruixiang;Wang, Wenchao;Ren, Tao;Ge, Jian;Liu, Jing;Liu, Qingsong. And the article was included in Journal of Medicinal Chemistry in 2019.Recommanded Product: 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline This article mentions the following:

Most of the current FMS-like tyrosine kinase 3 (FLT3) inhibitors lack selectivity between FLT3 kinase and cKIT kinase as well as the FLT3 wt and internal tandem duplication (ITD) mutants. We report a new compound I, which displays GI₅₀ values of 30-80 nM against different ITD mutants and achieves selectivity over both FLT3 wt (8-fold) and cKIT kinase in the transformed BaF3 cells (>300-fold). I potently inhibits the proliferation of the FLT3-ITD-pos. acute myeloid leukemia cancer lines through suppression of the phosphorylation of FLT3 kinase and downstream signaling pathways, induction of apoptosis, and arresting the cell cycle into the G0/G1 phase. I also displays potent antiproliferative effect against FLT3-ITD-pos. patient primary cells, whereas it does not apparently affect FLT3 wt primary cells. In addition, it also exhibits a good therapeutic window to PBMC compared to PKC412. In the in vivo studies, I demonstrates favorable PK profiles and suppresses the tumor growth in the MV4-11 cell inoculated mouse xenograft model. 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 belongs to the family of medicines called anthelmintics. 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).Recommanded Product: 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline

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

Selective Inhibition of the Myeloid Src-Family Kinase Fgr Potently Suppresses AML Cell Growth in Vitro and in Vivo was written by Weir, Mark C.;Shu, Sherry T.;Patel, Ravi K.;Hellwig, Sabine;Chen, Li;Tan, Li;Gray, Nathanael S.;Smithgall, Thomas E.. And the article was included in ACS Chemical Biology in 2018.Category: piperazines This article mentions the following:

Acute myelogenous leukemia (AML) is the most common hematol. malignancy in adults and is often associated with constitutive tyrosine kinase signaling. These pathways involve the nonreceptor tyrosine kinases Fes, Syk, and the three Src-family kinases expressed in myeloid cells (Fgr, Hck, and Lyn). In this study, we report remarkable anti-AML efficacy of an N-phenylbenzamide kinase inhibitor, TL02-59. This compound potently suppressed the proliferation of bone marrow samples from 20 of 26 AML patients, with a striking correlation between inhibitor sensitivity and expression levels of the myeloid Src family kinases Fgr, Hck, and Lyn. No correlation was observed with Flt3 expression or mutational status, with the four most sensitive patient samples being wild-type for Flt3. Kinome-wide target specificity profiling coupled with in vitro kinase assays demonstrated a narrow overall target specificity profile for TL02-59, with picomolar potency against the myeloid Src-family member Fgr. In a mouse xenograft model of AML, oral administration of TL02-59 for 3 wk at 10 mg/kg completely eliminated leukemic cells from the spleen and peripheral blood while significantly reducing bone marrow engraftment. These results identify Fgr as a previously unrecognized kinase inhibitor target in AML and TL02-59 as a possible lead compound for clin. development in AML cases that overexpress this kinase independent of Flt3 mutations. In the experiment, the researchers used many compounds, for example, 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6Category: piperazines).

4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. 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.Category: piperazines

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