Tag: 288.34

Multifaceted activity of polycyclic MDR revertant agents in drug-resistant leukemic cells: Role of the spacer was written by Caciolla, Jessica;Picone, Giovanna;Farruggia, Giovanna;Valenti, Dario;Rampa, Angela;Malucelli, Emil;Belluti, Federica;Trezza, Alfonso;Spiga, Ottavia;Iotti, Stefano;Gobbi, Silvia;Cappadone, Concettina;Bisi, Alessandra. And the article was included in Bioorganic Chemistry in 2021.HPLC of Formula: 27469-60-9 This article mentions the following:

A small library of derivatives carrying a polycyclic scaffold recently identified by us as a new privileged structure in medicinal chem. was designed and synthesized, aiming at obtaining potent MDR reverting agents also endowed with antitumor properties. In particular, as a follow-up of our previous studies, attention was focused on the role of the spacer connecting the polycyclic core with a properly selected nitrogen-containing group. A relevant increase in reverting potency was observed, going from the previously employed but-2-ynyl- to a pent-3-ynylamino moiety, as in compounds 3d and 3e, while the introduction of a triazole ring proved to differently impact on the activity of the compounds The docking results supported the data obtained by biol. tests, showing, for the most active compounds, the ability to establish specific bonds with P-glycoprotein. Moreover, a multifaceted anticancer profile and dual in vitro activity was observed for all compounds, showing both revertant and antitumor effects on leukemic cells. In this respect, 3c emerged as a “triple-target” agent, endowed with a relevant reverting potency, a considerable antiproliferative activity and a collateral sensitivity profile. In the experiment, the researchers used many compounds, for example, 4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9HPLC of Formula: 27469-60-9).

4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9) 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. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.HPLC of Formula: 27469-60-9

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

1-{4-[Bis(4-fluorophenyl)methyl]piperazin-1-yl}ethanone was written by Dayananda, A. S.;Yathirajan, H. S.;Keeley, Amanda C.;Jasinski, Jerry P.. And the article was included in Acta Crystallographica, Section E: Structure Reports Online in 2012.Electric Literature of C17H18F2N2 This article mentions the following:

In the title compound, C₁₉H₂₀F₂N₂O, the six-membered piperazine group adopts a slightly distorted chair conformation. The dihedral angle between the mean planes of the two benzene rings is 73.4(6)°. The mean plane of the ethanone group is twisted from the mean planes of the two benzene rings by 66.7(8) and 86.2(6)°. In the crystal, C-H···O and C-H···F interactions link the mols., forming a three-dimensional structure. Crystallog. data and at. coordinates are given. In the experiment, the researchers used many compounds, for example, 4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9Electric Literature of C17H18F2N2).

4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9) 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. Electric Literature of C17H18F2N2

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

Synthesis, molecular docking and biological evaluation of metronidazole derivatives containing piperazine skeleton as potential antibacterial agents was written by Wang, She-Feng;Yin, Yong;Qiao, Fang;Wu, Xun;Sha, Shao;Zhang, Li;Zhu, Hai-Liang. And the article was included in Bioorganic & Medicinal Chemistry in 2014.Related Products of 27469-60-9 This article mentions the following:

Metronidazole has a broad-spectrum antibacterial activity. Hereby a series of novel metronidazole derivatives were designed and synthesized based on nitroimidazole scaffold in order to find some more potent antibacterial drugs. For these compounds which were reported for the first time, their antibacterial activities against Escherichia coli, Pseudomonas aeruginosa, Bacillus subtilis and Staphylococcus aureus were tested. These compounds showed good antibacterial activities against Gram-pos. strains. One compound represented the most potent antibacterial activity against S. aureus ATCC 25923 with MIC of 0.003 μg/mL and it showed the most potent activity against S. aureus TyrRS with IC₅₀ of 0.0024 μM. Mol. docking of one compound into S. aureus tyrosyl-tRNA synthetase active site were also performed to determine the probable binding mode. In the experiment, the researchers used many compounds, for example, 4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9Related Products of 27469-60-9).

4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9) 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. Related Products of 27469-60-9

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

α-Adrenoceptor antagonistic and hypotensive properties of novel arylpiperazine derivatives of pyrrolidin-2-one was written by Zareba, Paula;Dudek, Magdalena;Lustyk, Klaudia;Siwek, Agata;Starowicz, Gabriela;Bednarski, Marek;Nowinski, Leszek;Razny, Katarzyna;Sapa, Jacek;Malawska, Barbara;Kulig, Katarzyna. And the article was included in Bioorganic & Medicinal Chemistry in 2015.SDS of cas: 27469-60-9 This article mentions the following:

This study focused on a series of pyrrolidin-2-one derivatives connected via two or four methylene units to arylpiperazine fragment. The compounds obtained for α₁– and α₂-adrenoceptors were assessed. The compound with highest affinity for the α₁-adrenoceptors was 1-{4-[4-(2-chloro-phenyl)-piperazin-1-yl]-butyl}-pyrrolidin-2-one I with pK_i = 7.30. Compound with pK_i (α₁) ≥6.44 were evaluated in functional bioassays for intrinsic activity at α_1A– and α_1B-adrenoceptors. All compounds tested were antagonists of the α_1B-adrenoceptors. Addnl., compounds II and I were α_1A-adrenoceptors antagonist. The dual α_1A-/α_1B-adrenoceptors antagonists, compounds II and I were also tested in vivo for their hypotensive activity in rats. These compounds, when dosed of 1.0 mg/kg iv in normotensive, anesthetized rats, significantly decreased systolic and diastolic pressure and their hypotensive effects lasted for longer than one hour. In the experiment, the researchers used many compounds, for example, 4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9SDS of cas: 27469-60-9).

4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9) 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. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.SDS of cas: 27469-60-9

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

(E)-1-{4-[Bis(4-fluorophenyl)methyl]piperazin-1-yl}-3-(4-ethoxyphenyl)prop-2-en-1-one was written by Zhong, Yan;Zhang, XiaoPing;Wu, Bin. And the article was included in Acta Crystallographica, Section E: Structure Reports Online in 2011.Category: piperazines This article mentions the following:

In (E)-1-{4-[bis(4-fluorophenyl)methyl]piperazin-1-yl}-3-(4-ethoxyphenyl)prop-2-en-1-one, C₂₈H₂₈F₂N₂O₂, the ethene bond exhibits an E conformation and the piperazine ring adopts a chair conformation. The amide-N atom of the piperazine ring is almost planar (bond-angle sum = 358.8°) whereas the other N atom is clearly pyramidal (bond-angle-sum = 330.5°). The dihedral angle between the fluorobenzene rings is 76.36(17)°. In the crystal, inversion dimers linked by pairs of C-H···O H bonds generate R²₂(22) loops. Crystallog. data are given. In the experiment, the researchers used many compounds, for example, 4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9Category: piperazines).

4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. 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 simple and efficient synthesis of the antimigraine drug lomerizine was written by Narsaiah, A. Venkat;Kumar, J. Kranthi. And the article was included in Synthesis in 2010.SDS of cas: 27469-60-9 This article mentions the following:

The synthesis of the antimigraine drug 1-[bis(4-fluorophenyl)methyl]-4-(2,3,4-trimethoxybenzyl)piperazine was carried out in very good yields. The 5-step synthesis started from bis(4-fluorophenyl)methanone. This route can be applied for large-scale preparation of lomerizine. In the experiment, the researchers used many compounds, for example, 4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9SDS of cas: 27469-60-9).

4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.SDS of cas: 27469-60-9

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

Discovery of Benzenesulfonamide Derivatives as Carbonic Anhydrase Inhibitors with Effective Anticonvulsant Action: Design, Synthesis, and Pharmacological Evaluation was written by Mishra, Chandra Bhushan;Kumari, Shikha;Angeli, Andrea;Bua, Silvia;Tiwari, Manisha;Supuran, Claudiu T.. And the article was included in Journal of Medicinal Chemistry in 2018.HPLC of Formula: 27469-60-9 This article mentions the following:

Two series of novel benzenesulfonamide derivatives were synthesized and evaluated for their human carbonic anhydrase (CA, EC 4.2.1.1) inhibitory activity against four isoforms, hCA I, hCA II, hCA VII, and hCA IX. It was found that compounds of both series showed low to medium nanomolar inhibitory potential against all isoforms. Some of these derivatives displayed selective inhibition against the epileptogenesis related isoforms hCA II and VII, within the nanomolar range. These potent hCA II and VII inhibitors were evaluated as anticonvulsant agents against MES and s.c.-PTZ induced convulsions. These sulfonamides effectively abolished induced seizures in both models. Furthermore, time dependent seizure protection capability of the most potent compound I was also evaluated. A long duration of action was displayed, with efficacy up to 6 h after drug administration. The compound appeared as an orally active anticonvulsant agent without showing neurotoxicity in a rotarod test, a nontoxic chem. profile being observed in subacute toxicity study. In the experiment, the researchers used many compounds, for example, 4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9HPLC of Formula: 27469-60-9).

4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9) 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 formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.HPLC of Formula: 27469-60-9

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

Multifaceted activity of polycyclic MDR revertant agents in drug-resistant leukemic cells: Role of the spacer was written by Caciolla, Jessica;Picone, Giovanna;Farruggia, Giovanna;Valenti, Dario;Rampa, Angela;Malucelli, Emil;Belluti, Federica;Trezza, Alfonso;Spiga, Ottavia;Iotti, Stefano;Gobbi, Silvia;Cappadone, Concettina;Bisi, Alessandra. And the article was included in Bioorganic Chemistry in 2021.HPLC of Formula: 27469-60-9 This article mentions the following:

A small library of derivatives carrying a polycyclic scaffold recently identified by us as a new privileged structure in medicinal chem. was designed and synthesized, aiming at obtaining potent MDR reverting agents also endowed with antitumor properties. In particular, as a follow-up of our previous studies, attention was focused on the role of the spacer connecting the polycyclic core with a properly selected nitrogen-containing group. A relevant increase in reverting potency was observed, going from the previously employed but-2-ynyl- to a pent-3-ynylamino moiety, as in compounds 3d and 3e, while the introduction of a triazole ring proved to differently impact on the activity of the compounds The docking results supported the data obtained by biol. tests, showing, for the most active compounds, the ability to establish specific bonds with P-glycoprotein. Moreover, a multifaceted anticancer profile and dual in vitro activity was observed for all compounds, showing both revertant and antitumor effects on leukemic cells. In this respect, 3c emerged as a “triple-target” agent, endowed with a relevant reverting potency, a considerable antiproliferative activity and a collateral sensitivity profile. In the experiment, the researchers used many compounds, for example, 4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9HPLC of Formula: 27469-60-9).

4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9) 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. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.HPLC of Formula: 27469-60-9

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

1-{4-[Bis(4-fluorophenyl)methyl]piperazin-1-yl}ethanone was written by Dayananda, A. S.;Yathirajan, H. S.;Keeley, Amanda C.;Jasinski, Jerry P.. And the article was included in Acta Crystallographica, Section E: Structure Reports Online in 2012.Electric Literature of C17H18F2N2 This article mentions the following:

In the title compound, C₁₉H₂₀F₂N₂O, the six-membered piperazine group adopts a slightly distorted chair conformation. The dihedral angle between the mean planes of the two benzene rings is 73.4(6)°. The mean plane of the ethanone group is twisted from the mean planes of the two benzene rings by 66.7(8) and 86.2(6)°. In the crystal, C-H···O and C-H···F interactions link the mols., forming a three-dimensional structure. Crystallog. data and at. coordinates are given. In the experiment, the researchers used many compounds, for example, 4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9Electric Literature of C17H18F2N2).

4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9) 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. Electric Literature of C17H18F2N2

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

1-{4-[Bis(4-fluorophenyl)methyl]piperazin-1-yl}ethanone was written by Dayananda, A. S.;Yathirajan, H. S.;Keeley, Amanda C.;Jasinski, Jerry P.. And the article was included in Acta Crystallographica, Section E: Structure Reports Online in 2012.Electric Literature of C17H18F2N2 This article mentions the following:

In the title compound, C₁₉H₂₀F₂N₂O, the six-membered piperazine group adopts a slightly distorted chair conformation. The dihedral angle between the mean planes of the two benzene rings is 73.4(6)°. The mean plane of the ethanone group is twisted from the mean planes of the two benzene rings by 66.7(8) and 86.2(6)°. In the crystal, C-H···O and C-H···F interactions link the mols., forming a three-dimensional structure. Crystallog. data and at. coordinates are given. In the experiment, the researchers used many compounds, for example, 4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9Electric Literature of C17H18F2N2).

4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9) 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. Electric Literature of C17H18F2N2

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