Tag: 100-200

Nguyen, William; Dans, Madeline G.; Ngo, Anna; Gancheva, Maria R.; Romeo, Ornella; Duffy, Sandra; de Koning-Ward, Tania F.; Lowes, Kym N.; Sabroux, Helene Jousset; Avery, Vicky M.; Wilson, Danny W.; Gilson, Paul R.; Sleebs, Brad E. published an article in 2021. The article was titled 《Structure activity refinement of phenylsulfonyl piperazines as antimalarials that block erythrocytic invasion》, and you may find the article in European Journal of Medicinal Chemistry.Synthetic Route of C5H12N2 The information in the text is summarized as follows:

The optimization and further characterization of the phenylsulfonyl piperazine class I [R = 4-Me, 3-t-Bu, 4-Br, etc.; R1 = pyrrolidin-1-yl, piperidin-1-yl, 1,2,3,4-tetrahydroisoquinolin-2-yl, etc.; X = -(N(CH2)2N(CH2)2)-CH(CH3), -(NCH(CH3)N(CH2)2)-CH(CH3), -(NC(CH3)2N(CH2)2)-CH(CH3), etc.] was described. During the optimization process the functionality required for P. falciparum asexual stage activity was defined and determined the alpha-carbonyl S-Me isomer was important for antimalarial potency. The optimized compounds I also possessed comparable activity against multidrug resistant strains of P. falciparum and displayed weak activity against sexual stage gametocytes. The optimized compounds I blocked erythrocyte invasion consistent with the asexual activity observed and therefore the phenylsulfonyl piperazine analogs described could serve as useful tools for studying Plasmodium erythrocyte invasion. After reading the article, we found that the author used 1-Methylpiperazine(cas: 109-01-3Synthetic Route of C5H12N2)

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Synthetic Route of C5H12N2

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

Paul, Anirudra; Kim, Jae Hyun; Daniel, Scott D.; Seidel, Daniel published their research in Angewandte Chemie, International Edition in 2021. The article was titled 《Diversification of Unprotected Alicyclic Amines by C-H Bond Functionalization: Decarboxylative Alkylation of Transient Imines》.Recommanded Product: 109-01-3 The article contains the following contents:

Despite extensive efforts by many practitioners in the field, methods for the direct α-C-H bond functionalization of unprotected alicyclic amines remain rare. A new advance in this area utilizes N-lithiated alicyclic amines. These readily accessible intermediates are converted to transient imines through the action of a simple ketone oxidant, followed by alkylation with a β-ketoacid under mild conditions to provide valuable β-amino ketones with unprecedented ease. Regioselective α’-alkylation is achieved for substrates with existing α-substituents. The method is further applicable to the convenient one-pot synthesis of polycyclic dihydroquinolones through the incorporation of a SNAr step. In the experiment, the researchers used many compounds, for example, 1-Methylpiperazine(cas: 109-01-3Recommanded Product: 109-01-3)

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Recommanded Product: 109-01-3

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

In 2019,Journal of the American Chemical Society included an article by Paul, Anirudra; Seidel, Daniel. Electric Literature of C5H12N2. The article was titled 《α-Functionalization of Cyclic Secondary Amines: Lewis Acid Promoted Addition of Organometallics to Transient Imines》. The information in the text is summarized as follows:

Cyclic imines, generated in situ from their corresponding N-lithiated amines and a ketone hydride acceptor, undergo reactions with a range of organometallic nucleophiles to generate α-functionalized amines in a single operation. Activation of the transient imines by Lewis acids that are compatible with the presence of lithium alkoxides is crucial to accommodate a broad range of nucleophiles including lithium acetylides, Grignard reagents, and aryllithiums with attenuated reactivities. In the experimental materials used by the author, we found 1-Methylpiperazine(cas: 109-01-3Electric Literature of C5H12N2)

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Electric Literature of C5H12N2

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

《Synthesis and Biological Activity of Sulfonamide Derivatives of Epipodophyllotoxin》 was written by Guianvarc’h, Dominique; Duca, Maria; Boukarim, Chawki; Kraus-Berthier, Laurence; Leonce, Stephane; Pierre, Alain; Pfeiffer, Bruno; Renard, Pierre; Arimondo, Paola B.; Monneret, Claude; Dauzonne, Daniel. Formula: C5H11ClN2O2S And the article was included in Journal of Medicinal Chemistry on April 22 ,2004. The article conveys some information:

A series of novel 4β-substituted sulfonamide derivatives of 4′-O-demethyl-4-desoxypodophyllotoxin, I [R1 = SO2R, R = Me, n-Pr, (CH2)3NH2, 2-thienyl, piperidino, etc.] (II), has been synthesized. II were synthesized by silylating the alc. I (R1 = H), followed by reaction with RSO2Cl, and desilylation. Their effects on human DNA topoisomerase II and, in some cases, on tubulin polymerization were evaluated. Several of the compounds, e.g. II (R = Me), and the synthetic precursor, the 4β-azido compound, are potent topoisomerase II poisons that induce double-stranded breaks in DNA, with either improved or similar activity compared to etoposide. Only the amino precursor, compound I (R1 = H), was slightly active in tubulin polymerization inhibition assays. We observed that the derivatives bearing an aromatic ring on the 4β-sulfonamide substituent were either less cytotoxic or equivalent to the parent drug, while the sulfonamides containing an aliphatic side chain and the amino-sulfonamide derivatives, except II [R = (CH2)15Me, (CH2)3NH2], exhibited increased cytotoxicity compared to etoposide. In vivo, against the P388 leukemia and the A-549 orthotopic model of lung carcinoma, the most promising compounds were the morpholino- and the piperazino-containing sulfonamides derivatives II (R = morpholino, 4-methylpiperazino). In the part of experimental materials, we found many familiar compounds, such as 4-Methyl-1-piperazinesulfonyl Chloride(cas: 1688-95-5Formula: C5H11ClN2O2S)

4-Methyl-1-piperazinesulfonyl Chloride(cas: 1688-95-5) is a member of sulfamide. Sulfamide was used in the synthesis of: Schiff bases of the type ArCH=NSO2NH2; 1H,3H-2,1,3-benzothiadiazin-4-one-2,2-dioxide (BTDD); sulfamide analogs of oleoylethanolamide analogs in a study of PPARα activation.Formula: C5H11ClN2O2S

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

Zhang, Xiangyu; Huang, Hailan; Zhang, Ziheng; Yan, Jiangkun; Wu, Tianxiao; Yin, Wenbo; Sun, Yixiang; Wang, Xinran; Gu, Yanting; Zhao, Dongmei; Cheng, Maosheng published their research in European Journal of Medicinal Chemistry in 2021. The article was titled 《Design, synthesis and biological evaluation of novel benzofuran derivatives as potent LSD1 inhibitors》.HPLC of Formula: 109-01-3 The article contains the following contents:

A series of benzofurans I [R = 3-aminopropylamino, pyrrolidin-3-ylamino, piperazin-1-yl, etc.; Ar = pyrimidin-5-yl, p-tolyl, 1-methylindazol-5-yl, etc.] were designed, synthesized and biochem. evaluated as LSD1 inhibitors based on scaffold hopping and conformational restriction strategy. Most of the compounds I potently suppressed the enzymic activities of LSD1 and potently inhibited tumor cells proliferation. In particular, the representative compound I [R = (3S)-3-amino-1-piperidyl; Ar = p-tolyl] exhibited excellent LSD1 inhibition at the mol. levels with IC50 = 0.065μM, as well as anti-proliferation against MCF-7, MGC-803, H460, A549 and THP-1 tumor cells with IC50 values of 2.90 ± 0.32, 5.85 ± 0.35, 2.06 ± 0.27, 5.74 ± 1.03 and 6.15 ± 0.49μM, resp. The binding modes of these compounds I were rationalized by mol. docking. Meanwhile, a preliminary druggability evaluation showed that compound I [R = (3S)-3-amino-1-piperidyl; Ar = p-tolyl] displayed favorable liver microsomal stability and weak inhibitory activity against CYPs at 10μM. Remarkably, H460 xenograft tumors studies revealed that compound I [R = (3S)-3-amino-1-piperidyl; Ar = p-tolyl] demonstrated robust in-vivo antitumor efficacy without significant side effects. All the results demonstrated that compound I [R = (3S)-3-amino-1-piperidyl; Ar = p-tolyl] could represent a promising lead for further development. In the experimental materials used by the author, we found 1-Methylpiperazine(cas: 109-01-3HPLC of Formula: 109-01-3)

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..HPLC of Formula: 109-01-3

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

The author of 《Synthesis, crystal structure, vibrational, optical properties, and a theoretical study of a new Pb(II) complex with bis(1-methylpiperazine-1,4-diium): [C5H14N2]2PbCl6·3H2O》 were Mrad, Mohamed Lahbib; Belhajsalah, Souhir; Abdelbaky, Mohammed Said M.; Garcia-Granda, Sergio; Essalah, Khaled; Ben Nasr, C.. And the article was published in Journal of Coordination Chemistry in 2019. Name: 1-Methylpiperazine The author mentioned the following in the article:

A study of the solid-state x-ray structure of the new organic-inorganic compound [C5H14N2]2PbCl6·3H2O shows a layered organization of the (PbCl6)4- anions, with (R2NH2)+ groups and water mols. developed in the [001] plane at x = (2n + 1)/4. The crystal structure is stabilized by N – H···Cl, N – H···O, O – H···Cl, O – H···O, and C – H···Cl hydrogen bonds. The powder x-ray diffraction and X-ray photoelectron spectroscopic (XPS) analyses confirm the phase purity of the crystal sample. The intermol. contacts are quantified using the Hirshfeld surfaces computational method. The major inter-contacts contributing to the Hirshfeld surfaces are H…Cl, H…H, and O…H. The vibrational modes were identified and assigned by IR and Raman spectroscopies. The optical properties were studied by UV-visible and photoluminescence spectroscopic studies. The compound was characterized by thermal anal. to determine its thermal behavior with respect to the temperature Finally, XPS anal. is reported for analyzing the surface chem. of [C5H14N2]2PbCl6·3H2O. In the experiment, the researchers used 1-Methylpiperazine(cas: 109-01-3Name: 1-Methylpiperazine)

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Name: 1-Methylpiperazine

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

Scapecchi, Serena; Martini, Elisabetta; Manetti, Dina; Ghelardini, Carla; Martelli, Cecilia; Dei, Silvia; Galeotti, Nicoletta; Guandalini, Luca; Romanelli, Maria Novella; Teodori, Elisabetta published an article in Bioorganic & Medicinal Chemistry. The title of the article was 《Structure-activity relationship studies on unifiram (DM232) and sunifiram (DM235), two novel and potent cognition enhancing drugs》.Safety of 1-(Isopropylsulfonyl)piperazine The author mentioned the following in the article:

Structure-activity relationships on two novel potent cognition enhancing drugs, unifiram and sunifiram, are reported. Although none of the compounds synthesized reached the potency of the parent drugs, some fairly active compounds have been identified that may represent new leads to develop other cognition enhancing drugs. An interesting result of this research is the identification of two compounds that are endowed with amnesing activity (the opposite of the activity of the original mols.) and are nearly equipotent to scopolamine. Moreover, two other compounds of the series were found endowed with analgesic activity on a rat model of neuropathic pain at the dose of 1 mg/kg. In the experimental materials used by the author, we found 1-(Isopropylsulfonyl)piperazine(cas: 534615-34-4Safety of 1-(Isopropylsulfonyl)piperazine)

1-(Isopropylsulfonyl)piperazine(cas: 534615-34-4) is a member of sulfamide. Sulfamide was used in the synthesis of: Schiff bases of the type ArCH=NSO2NH2; 1H,3H-2,1,3-benzothiadiazin-4-one-2,2-dioxide (BTDD); sulfamide analogs of oleoylethanolamide analogs in a study of PPARα activation.Safety of 1-(Isopropylsulfonyl)piperazine

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

Product Details of 34352-59-5On October 25, 2012 ,《Optimization of Imidazo[4,5-b]pyridine-Based Kinase Inhibitors: Identification of a Dual FLT3/Aurora Kinase Inhibitor as an Orally Bioavailable Preclinical Development Candidate for the Treatment of Acute Myeloid Leukemia》 was published in Journal of Medicinal Chemistry. The article was written by Bavetsias, Vassilios; Crumpler, Simon; Sun, Chongbo; Avery, Sian; Atrash, Butrus; Faisal, Amir; Moore, Andrew S.; Kosmopoulou, Magda; Brown, Nathan; Sheldrake, Peter W.; Bush, Katherine; Henley, Alan; Box, Gary; Valenti, Melanie; Brandon, Alexis de Haven; Raynaud, Florence I.; Workman, Paul; Eccles, Suzanne A.; Bayliss, Richard; Linardopoulos, Spiros; Blagg, Julian. The article contains the following contents:

Optimization of the imidazo[4,5-b]pyridine-based series of Aurora kinase inhibitors led to the identification of 6-chloro-7-(4-(4-chlorobenzyl)piperazin-1-yl)-2-(1,3-dimethyl-1H-pyrazol-4-yl)-3H-imidazo[4,5-b]pyridine (I), a potent inhibitor of Aurora kinases (Aurora-A Kd = 7.5 nM, Aurora-B Kd = 48 nM), FLT3 kinase (Kd = 6.2 nM), and FLT3 mutants including FLT3-ITD (Kd = 38 nM) and FLT3(D835Y) (Kd = 14 nM). FLT3-ITD causes constitutive FLT3 kinase activation and is detected in 20-35% of adults and 15% of children with acute myeloid leukemia (AML), conferring a poor prognosis in both age groups. In an in vivo setting, I strongly inhibited the growth of a FLT3-ITD-pos. AML human tumor xenograft (MV4-11) following oral administration, with in vivo biomarker modulation and plasma free drug exposures consistent with dual FLT3 and Aurora kinase inhibition. Compound I, an orally bioavailable dual FLT3 and Aurora kinase inhibitor, was selected as a preclin. development candidate for the treatment of human malignancies, in particular AML, in adults and children.1-Methylpiperazine dihydrochloride(cas: 34352-59-5Product Details of 34352-59-5) was used in this study.

1-Methylpiperazine dihydrochloride(cas: 34352-59-5) is used in the preparation of 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), 1-methylpiperazine-1,4-diium tetrachloridozincate hemihydrate, 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), an antimicrotubular drug..Product Details of 34352-59-5

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

《2,5-Disubstituted pyridines as potent GPR119 agonists》 was written by Wu, Yulin; Kuntz, Judith D.; Carpenter, Andrew J.; Fang, Jing; Sauls, Howard R.; Gomez, Daniel J.; Ammala, Carina; Xu, Yun; Hart, Shane; Tadepalli, Sarva. Electric Literature of C7H16N2O2S And the article was included in Bioorganic & Medicinal Chemistry Letters on April 15 ,2010. The article conveys some information:

A series of 2-piperazinyl-5-alkoxypyridines were synthesized and screened against human GPR119 receptor. Through SAR anal., compounds containing 2-alkylsulfonylpiperazinyl-5-alkoxypyridines were discovered and found to be potent agonists of the human GPR119 receptor. The experimental process involved the reaction of 1-(Isopropylsulfonyl)piperazine(cas: 534615-34-4Electric Literature of C7H16N2O2S)

1-(Isopropylsulfonyl)piperazine(cas: 534615-34-4) is a member of sulfamide. Sulfamide was used in the synthesis of: Schiff bases of the type ArCH=NSO2NH2; 1H,3H-2,1,3-benzothiadiazin-4-one-2,2-dioxide (BTDD); sulfamide analogs of oleoylethanolamide analogs in a study of PPARα activation.Electric Literature of C7H16N2O2S

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

Category: piperazinesIn 2022 ,《Design and synthesis of novel quinazolinone derivatives as anti-HBV agents with TLR8 agonist effect》 appeared in European Journal of Medicinal Chemistry. The author of the article were Qiu, Jingying; Zhou, Qingqing; Zou, Yueting; Li, Shuqiong; Yang, Lihua; Chen, Wang; Gao, Jian; Gu, Xiaoke. The article conveys some information:

In this work, a series of novel quinazolinone derivatives I [R1 = benzyl, 2-furylmethyl, 2-thienylmethyl, etc.; R2 = H, 2-MeO, 3-F, etc.; R3 = (4-methylpiperazin-1-yl), (4-hydroxy-1-piperidyl), (2-aminopyrimidin-4-yl)oxy, etc.] were synthesized and evaluated as novel anti-HBV agents. Among them, compound I [R1 = 2-furylmethyl; R2 = 2-MeO; R3 = (2-aminopyrimidin-4-yl)oxy] exhibited potent inhibitory effect on HBV DNA replication in both wild type and drug resistant (lamivudine and entecavir) HBV strains with IC50 values of 0.15 and 0.10μM, resp. Notably, the selective index value of I [R1 = 2-furylmethyl; R2 = 2-MeO; R3 = (2-aminopyrimidin-4-yl)oxy] was high above 66.67, indicating the favorable safety profile. Mol. docking study indicated that compound I [R1 = 2-furylmethyl; R2 = 2-MeO; R3 = (2-aminopyrimidin-4-yl)oxy] well fitted into the binding pocket of TLR8 protein-protein interface. Dual-luciferase reporter gene assay further confirmed that compound I [R1 = 2-furylmethyl; R2 = 2-MeO; R3 = (2-aminopyrimidin-4-yl)oxy] could dose-dependently activate TLR8, thus effectively inducing the activity of TLR8-dependent NF-κB. Collectively, compound I [R1 = 2-furylmethyl; R2 = 2-MeO; R3 = (2-aminopyrimidin-4-yl)oxy] displayed potent anti-HBV activities and TLR8 agonist effect in vitro, and might be a potential immunomodulatory anti-HBV agent to warrant further investigation. In the part of experimental materials, we found many familiar compounds, such as 1-Methylpiperazine(cas: 109-01-3Category: piperazines)

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Category: piperazines

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