Tag: 200-300

Deka, Nabajyoti; Bajare, Swapnil; Anthony, Jessy; Nair, Amrutha; Damre, Anagha; Patel, Dharmeshkumar; B.-Rao, Chandrika; Sivaramakrishnan, H.; Mutt, Shivaprakash Jagalur; Wilankar, Chandan; Marita, Rosalind published an article in 2013, the title of the article was Synthesis of N-(6-(4-(piperazin-1-yl)phenoxy)pyridin-3-yl)benzenesulfonamide derivatives for the treatment of metabolic syndrome.Recommanded Product: 67914-60-7 And the article contains the following content:

Metabolic syndrome is a widely prevalent multifactorial disorder associated with an increased risk of cardiovascular disease and type 2 diabetes mellitus. High plasma levels of insulin and glucose due to insulin resistance are a major component of the metabolic disorder. Thiazolidinediones (TZDs) are potent PPARγ ligands and used as insulin sensitizers in the treatment of type 2 diabetes mellitus. They are potent insulin-sensitizing agents but due to adverse effects like hepatotoxicity, a safer alternative of TZDs is highly demanded. The synthesis of N-(6-(4-(piperazin-1-yl)phenoxy)pyridin-3-yl)benzenesulfonamide derivatives I (R = 2,4-Cl2C6H3, 2,5-(OCH3)2C6H3, 2-thienyl, etc.) an alternate remedy for insulin resistance is reported. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Recommanded Product: 67914-60-7

The Article related to piperazinyl pyridinyl benzenesulfonamide preparation metabolic syndrome, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Recommanded Product: 67914-60-7

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

On January 27, 2022, Lee, Song Hee; Ryu, Je Ho; Ahn, Jung Min; Choi, Yu Ri; Lee, Ho Hyun; Jang, Mi Young; Woo, Yae Jin; Kim, Hanwool; Kim, Ji Young; Park, Ji Youn published a patent.Related Products of 1211568-27-2 The title of the patent was Amide compound for androgen receptor degradation, and pharmaceutical use thereof. And the patent contained the following:

The present invention provides a compound I [R1 = H, alkyl, halogen, etc.; R2 = H, alkyl, halogen, etc.; X1, X3, X4 and X5 = independently CH or N; X2 = CR3 or N; R3 = H, alkyl, halogen, etc.; n = 0, 1, or 2; m = 0 or 1; L = -(CH2)q1-A1-(CH2)q2-B1-(CH2)q3-A2-(CH2)q4-B2-(CH2)q5-A3-(CH2)q6-B3-; A1, A2 and A3 = independently direct bond, -O-, -N(R4)-, etc.; R4 = H, alkyl or haloalkyl; B1, B2 and B3 = independently direct bond, cycloalkyl, heterocycle, etc.; q1-q6 = independently 0-6; E = Q1 or Q2; X6, X7, X8 and X9 = independently CH or N; Y = -C(R6)2-, -C(O)-, -C(R6)2-C(R6′)2-, etc.; Z = direct bond, -C(R6)2-, -O-, etc.; R5 and R5′ = independently H, alkyl, halogen, etc.; R6 and R6′ = independently H, alkyl, halogen, etc.] of a specific chem. structure, having androgen receptor (AR) degradation activity, or a pharmaceutically acceptable salt thereof. The present invention also provides a composition containing the compound or a pharmaceutically acceptable salt thereof. According to present invention, provided is a pharmaceutical use of the compound, the salt thereof, and the composition containing same for treating or preventing AR-related diseases. According to the present invention, further provided is a method for treating or preventing AR-related diseases, the method comprising administering, to a subject in need of treatment, an effective amount of the compound, the salt thereof, or the composition containing same. For example, compound II (preparation given) was coupled with compound III (preparation given) to provide compound IV. The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).Related Products of 1211568-27-2

The Article related to amide compound preparation androgen receptor degradation activity, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Related Products of 1211568-27-2

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

On August 11, 1998, De Laszlo, Stephen E.; Liverton, Nigel J.; Ponticello, Gerald S.; Selnick, Harold G.; Mantlo, Nathan B. published a patent.Electric Literature of 890092-19-0 The title of the patent was Preparation of arylpyrroles as cytokine inhibitors. And the patent contained the following:

Title compounds [I; R1 = H, alkyl, heterocyclyl, aryl, etc.; R2 = alk(en)yl, alkynyl, heterocyclyl, etc.; R3 = H, halo, alkyl, heterocyclyl, etc.; R4 = (un)substituted heteroaryl; R5 = ZR; R = 1-3 of halo, alkyl, acyl, (hetero)aryl, etc.; Z = (hetero)arylene] were prepared Thus, R5COCH2R4 (R4 = 4-pyridyl, R5 = 4-FC6H4) was α-alkylated by ClCH2COR2 (R2 = 1-benzyloxycarbonyl-4-piperidinyl)(preparation each given) and the product cyclocondensed with NH4Ac to give, after reduction, I (R1 = R3 = H, R2 = 1-methyl-4-piperidinyl, R4 = 4-pyridyl, R5 = 4-FC6H4). Data for biol. activity of I were given. The experimental process involved the reaction of 4-(4-Acetylpiperazin-1-yl)benzaldehyde(cas: 890092-19-0).Electric Literature of 890092-19-0

The Article related to arylpyrrole preparation cytokine inhibitor, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Electric Literature of 890092-19-0

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

On March 16, 1986, Orjales Venero, Aurelio; Toledo Avello, Antonio published a patent.Synthetic Route of 59695-29-3 The title of the patent was Process for the preparation of amide derivatives of 4-amino-1,2,3,4,4a,9b-hexahydro-8,9b-dimethyldibenzofuran-3-one. And the patent contained the following:

The title amides I (R = alkyl; n = 1-4), known to be useful as analgesics and antitussives, are prepared by amidation of the title amine (II) with the corresponding (alkylpiperazinyl)alkanoic acids III in an anhydrous organic solvent and in the presence of a dehydrating agent. Thus, a solution of II.HCl in DMF was neutralized with K2CO3, filtered, and added to a solution of III.2HCl (R = Me, n = 2) and DCC in DMF, followed by workup and acidification, to give 50% I.2HCl (R = Me, n = 2). The experimental process involved the reaction of 3-(4-Methylpiperazin-1-yl)propanoic acid dihydrochloride(cas: 59695-29-3).Synthetic Route of 59695-29-3

The Article related to dibenzofuranone piperazinylalkanoylamino preparation analgesic antitussive, piperazinylalkanoylaminodibenzofuranone preparation analgesic antitussive, Heterocyclic Compounds (One Hetero Atom): Furans and other aspects.Synthetic Route of 59695-29-3

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

On October 15, 2022, Biyiklioglu, Zekeriya; Keles, Turgut; Sahin, Huseyin published an article.Electric Literature of 67914-60-7 The title of the article was Synthesis and acetylcholinesterase enzyme inhibition properties of axially disubstituted silicon phthalocyanines and their quaternized derivatives. And the article contained the following:

In this paper, axial 1,3-bis[4-(4-acetylpiperazin-1-yl)phenoxy]propanoxy and {2-[4-(4-acetylpiperazin-1-yl)phenoxy]ethoxy}ethoxy groups substituted silicon(IV) phthalocyanines PCSi(OR)2 [PP-D-Si, PP-OH2-Si; R = CH[CH2O-1,4-C6H4N(CH2CH2)2NCOMe]2, CH2CH2OCH2CH2O-1,4-C6H4N(CH2CH2)2NCOMe] and their quaternized derivatives (PP-D-SiQ, PP-OH2-SiQ) were synthesized and characterized. The acetylcholinesterase inhibition values of 1,3-bis[4-(4-acetylpiperazin-1-yl)phenoxy]propanoxy and {2-[4-(4-acetylpiperazin-1-yl)phenoxy]ethoxy}ethoxy groups substituted silicon(IV) phthalocyanines (PP-D-Si, PP-OH2-Si) and their quaternized derivatives (PP-D-SiQ, PP-OH2-SiQ) were measured by IC50 that reduces enzyme activity to 50% refers to the concentration of inhibitor. The synthesis compounds were classified as silicon and their quaternized derivatives and tagged as PP-D-Si, PP-OH2-Si, PP-D-SiQ and PP-OH2-SiQ. Except for the result of PP-D-SiQ was 1.586 ± 0.129μM, the results were expressed as mM ranged between 0.553 and 3.626 mM. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Electric Literature of 67914-60-7

The Article related to silicon phthalocyanine piperazine alkoxy derivative preparation cholinesterase inhibition, Organometallic and Organometalloidal Compounds: Silicon Compounds and other aspects.Electric Literature of 67914-60-7

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

On March 10, 2006, Huang, Jian-Dong; Liu, Feng-Ran; Chen, Yan-Mei; Sun, Jian-Cheng; Jiang, Zhou published an article.Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was Tetra-(acetyl piperazine phenoxy) phthalocyaninato zinc complexes and their proteins conjugates: synthesis, characterisation and photodynamic activities. And the article contained the following:

Two zinc phthalocyanines, tetra-α-[4-(4-acetyl piperazine) phenoxy] phthalocyaninato zinc (C80H72N16O8Zn) and tetra-β-[4-(4-acetyl piperazine) phenoxy] phthalocyaninato zinc (C80H72N16O8Zn), have been synthesized and characterized with 1H NMR, MS, IR and elemental anal. The electronic absorption spectra of two complexes in common organic solvents (N,N-DMF, THF, n-octanol) were typical for nonaggregated phthalocyanines, showing a Q band at 693∼698 nm for 1 and 681 ∼ 682 nm for 2. This indicates that the Q band of zinc phthalocyanine with the substituted groups located in the α position is largely red shifted than that in the β position. The spectral features of complexes 1 and 2 in aqueous media suggest the α-substituted groups are more effective than β-substituted groups to hinder the aggregation of phthalocyanine mol. The interactions between two complexes with serum albumin and transferrin (BSA, HSA and apoTf) were investigated by absorption and fluorescence spectroscopy. The binding constants were found to be (1 ∼ 20) × 105 mol-1·L. By comparison, β-substituted 2 had stronger combining ability with albumin than that of α-substituted 1. The non-covalent conjugates (1-BSA, 2-BSA, 1-HSA, 1-apoTf and 1-FeTf) with the molar ratio of about 1 : 1 have also been prepared The photodynamic activities of two complexes and their bioconjugates against MCF-7 mammary tumor cells were examined The result shows that the photocytotoxicities of conjugates are higher than that of complexes 1 ∼ 2 and follows the order 1-BSA > 1-FeTf > 1-HSA, 1-apoTf > 2-BSA > 1>2. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

The Article related to tetra acetyl piperazine phenoxy phthalocyaninato zinc protein conjugate photodynamic, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

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

Sunagar, Manjunath G.; Gaonkar, Supreet; Sunagar, Santosh G.; Deshapande, Narahari; Belavagi, Ningaraddi S.; Khazi, Imtiyaz Ahmed M. published an article in 2016, the title of the article was Synthesis of novel N-9 substituted 6-(4-(4-propoxyphenyl)piperazin-1-yl)-9H-purine derivatives as inducers of apoptosis in MCF-7 breast cancer cells.Application of 67914-60-7 And the article contains the following content:

A series of N-9 substituted 6-(4-(4-propoxyphenyl)piperazin-1-yl)-9H-purine derivatives (PP05-PP21) were prepared and evaluated for their anticancer activity against a panel of human cancer cell lines. Evaluation of results revealed that some of the synthesized compounds exhibited promising anticancer activity against the examined cancer cell lines. The structure-activity relationship (SAR) studies in the present work revealed that simple N-9 alkyl substituted 6-(4-(4-propoxyphenyl)piperazin-1-yl)-9H-purines are potent anticancer agents. Among all the compounds, PP17 (9-sec-butyl-6-(4-(4-propoxyphenyl)piperazin-1-yl)-9H-purine) showed good inhibitory activity against MCF-7 cells. Cell cycle anal. of the compound suggested that induces G2/M phase arrest. Biochem. experiments showed that PP17 significantly induced MCF-7 cell apoptosis. Therefore, compound PP17 with a potent in vitro anticancer activity can serve as a promising lead compound for further study. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Application of 67914-60-7

The Article related to anticancer agent apoptosis breast cancer cell structure activity relationship, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Application of 67914-60-7

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

On October 15, 2022, Biyiklioglu, Zekeriya; Keles, Turgut; Sahin, Huseyin published an article.Electric Literature of 67914-60-7 The title of the article was Synthesis and acetylcholinesterase enzyme inhibition properties of axially disubstituted silicon phthalocyanines and their quaternized derivatives. And the article contained the following:

In this paper, axial 1,3-bis[4-(4-acetylpiperazin-1-yl)phenoxy]propanoxy and {2-[4-(4-acetylpiperazin-1-yl)phenoxy]ethoxy}ethoxy groups substituted silicon(IV) phthalocyanines PCSi(OR)2 [PP-D-Si, PP-OH2-Si; R = CH[CH2O-1,4-C6H4N(CH2CH2)2NCOMe]2, CH2CH2OCH2CH2O-1,4-C6H4N(CH2CH2)2NCOMe] and their quaternized derivatives (PP-D-SiQ, PP-OH2-SiQ) were synthesized and characterized. The acetylcholinesterase inhibition values of 1,3-bis[4-(4-acetylpiperazin-1-yl)phenoxy]propanoxy and {2-[4-(4-acetylpiperazin-1-yl)phenoxy]ethoxy}ethoxy groups substituted silicon(IV) phthalocyanines (PP-D-Si, PP-OH2-Si) and their quaternized derivatives (PP-D-SiQ, PP-OH2-SiQ) were measured by IC50 that reduces enzyme activity to 50% refers to the concentration of inhibitor. The synthesis compounds were classified as silicon and their quaternized derivatives and tagged as PP-D-Si, PP-OH2-Si, PP-D-SiQ and PP-OH2-SiQ. Except for the result of PP-D-SiQ was 1.586 ± 0.129μM, the results were expressed as mM ranged between 0.553 and 3.626 mM. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Electric Literature of 67914-60-7

The Article related to silicon phthalocyanine piperazine alkoxy derivative preparation cholinesterase inhibition, Organometallic and Organometalloidal Compounds: Silicon Compounds and other aspects.Electric Literature of 67914-60-7

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

On March 10, 2006, Huang, Jian-Dong; Liu, Feng-Ran; Chen, Yan-Mei; Sun, Jian-Cheng; Jiang, Zhou published an article.Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was Tetra-(acetyl piperazine phenoxy) phthalocyaninato zinc complexes and their proteins conjugates: synthesis, characterisation and photodynamic activities. And the article contained the following:

Two zinc phthalocyanines, tetra-α-[4-(4-acetyl piperazine) phenoxy] phthalocyaninato zinc (C80H72N16O8Zn) and tetra-β-[4-(4-acetyl piperazine) phenoxy] phthalocyaninato zinc (C80H72N16O8Zn), have been synthesized and characterized with 1H NMR, MS, IR and elemental anal. The electronic absorption spectra of two complexes in common organic solvents (N,N-DMF, THF, n-octanol) were typical for nonaggregated phthalocyanines, showing a Q band at 693∼698 nm for 1 and 681 ∼ 682 nm for 2. This indicates that the Q band of zinc phthalocyanine with the substituted groups located in the α position is largely red shifted than that in the β position. The spectral features of complexes 1 and 2 in aqueous media suggest the α-substituted groups are more effective than β-substituted groups to hinder the aggregation of phthalocyanine mol. The interactions between two complexes with serum albumin and transferrin (BSA, HSA and apoTf) were investigated by absorption and fluorescence spectroscopy. The binding constants were found to be (1 ∼ 20) × 105 mol-1·L. By comparison, β-substituted 2 had stronger combining ability with albumin than that of α-substituted 1. The non-covalent conjugates (1-BSA, 2-BSA, 1-HSA, 1-apoTf and 1-FeTf) with the molar ratio of about 1 : 1 have also been prepared The photodynamic activities of two complexes and their bioconjugates against MCF-7 mammary tumor cells were examined The result shows that the photocytotoxicities of conjugates are higher than that of complexes 1 ∼ 2 and follows the order 1-BSA > 1-FeTf > 1-HSA, 1-apoTf > 2-BSA > 1>2. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

The Article related to tetra acetyl piperazine phenoxy phthalocyaninato zinc protein conjugate photodynamic, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

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

Sunagar, Manjunath G.; Gaonkar, Supreet; Sunagar, Santosh G.; Deshapande, Narahari; Belavagi, Ningaraddi S.; Khazi, Imtiyaz Ahmed M. published an article in 2016, the title of the article was Synthesis of novel N-9 substituted 6-(4-(4-propoxyphenyl)piperazin-1-yl)-9H-purine derivatives as inducers of apoptosis in MCF-7 breast cancer cells.Application of 67914-60-7 And the article contains the following content:

A series of N-9 substituted 6-(4-(4-propoxyphenyl)piperazin-1-yl)-9H-purine derivatives (PP05-PP21) were prepared and evaluated for their anticancer activity against a panel of human cancer cell lines. Evaluation of results revealed that some of the synthesized compounds exhibited promising anticancer activity against the examined cancer cell lines. The structure-activity relationship (SAR) studies in the present work revealed that simple N-9 alkyl substituted 6-(4-(4-propoxyphenyl)piperazin-1-yl)-9H-purines are potent anticancer agents. Among all the compounds, PP17 (9-sec-butyl-6-(4-(4-propoxyphenyl)piperazin-1-yl)-9H-purine) showed good inhibitory activity against MCF-7 cells. Cell cycle anal. of the compound suggested that induces G2/M phase arrest. Biochem. experiments showed that PP17 significantly induced MCF-7 cell apoptosis. Therefore, compound PP17 with a potent in vitro anticancer activity can serve as a promising lead compound for further study. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Application of 67914-60-7

The Article related to anticancer agent apoptosis breast cancer cell structure activity relationship, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Application of 67914-60-7

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