Month: October 2022

Application In Synthesis of 1-MethylpiperazineIn 2020 ,《Design, synthesis, molecular docking and antiproliferative activity of some novel benzothiazole derivatives targeting EGFR/HER2 and TS》 was published in Bioorganic Chemistry. The article was written by Abdellatif, Khaled R. A.; Belal, Amany; El-Saadi, Mohamed T.; Amin, Noha H.; Said, Eman G.; Hemeda, Loah R.. The article contains the following contents:

A new series of benzothiazoles hybridized with a pyrimidine moiety, e.g., I (R = Cl), was designed and synthesized using the lead compound II (R1 = Ph). Various chem. modifications on the pyrimidine ring of II (R1 = Ph) at four different positions were done in a trial to get new multi-targeted anticancer agents. The structures of the newly synthesized compounds were established by their elemental analyses and spectral data. All final synthesized derivatives were submitted to the National Cancer Institute (NCI), USA, to be screened for their in vitro anticancer activity. Further evaluation for the cytotoxic activity of the most active compounds was performed using the MTT assay method. Compounds I [R = (4-acetylphenyl)amino, morpholin-4-yl, 4-methylpiperazin-1-yl], II (R1 = 4-oxo-4H-chromen-3-yl), and III were then selected for examination of their in vitro inhibitory activities against EGFR, HER2 and TS enzymes using lapatinib and 5FU as standards Furthermore, cell cycle anal. and apoptosis induction detection were also evaluated. Finally, mol. docking studies were carried out for compounds I [R = (4-acetylphenyl)amino, morpholin-4-yl, 4-methylpiperazin-1-yl], II (R1 = 4-oxo-4H-chromen-3-yl), and III to interpret their observed enzymic activities based on the ligand-protein interactions. The results came from multiple reactions, including the reaction of 1-Methylpiperazine(cas: 109-01-3Application In Synthesis of 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..Application In Synthesis of 1-Methylpiperazine

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

Naylor, Alan; Judd, Duncan B.; Lloyd, Jane E.; Scopes, David I. C.; Hayes, Ann G.; Birch, Philip J. published an article in Journal of Medicinal Chemistry. The title of the article was 《A potent new class of κ-receptor agonist: 4-substituted 1-(arylacetyl)-2-[(dialkylamino)methyl]piperazines》.Application In Synthesis of (4-Benzylpiperazin-2-yl)methanol The author mentioned the following in the article:

The synthesis of 4-substituted 1-(arylacetyl)-2-[(alkylamino)methyl]piperazines I [R = CO2Me, R1 = R2 = Me; R = CO2Me, R1R2 = CH2CH:CHCH2CH2; R = COR3, R1R2 = (CH2)4, R3 = H, Me, Et, Pr, CH2OMe, CH:CH2, Ph, PhCH2; R = CO2R4, R1R2 = (CH2)4, R4 = Me, Et, Pr, Ph, PhCH2] and II [X = CHOH, CO, C:CHCO2Me-(E), -(Z)] and their activities as κ-opioid receptor agonists are described. This includes a range of 4-acyl and 4-carboalkoxy derivatives with the latter series showing the greatest κ-agonist activity. In particular, Me 4-[3,4-dichlorophenyl)acetyl]-3-[(1-pyrrolidinyl)methyl]-1-piperazinecarboxylate [I; R = CO2Me; R1R2 = (CH2)4] displays exceptional potency and selectivity. It showed the following activities in functional in vitro assays: rabbit vas deferens (κ-specific tissue) IC50 = 0.041 nM, rat vas deferens (μ-specific tissue) IC50 > 10 000 nM, and hamster vas deferens (δ-specific tissue) IC50 > 10 000 nM. Compound I [R = CO2Me; R1R2 = (CH2)4] is also a highly potent antinociceptive agent, as determined in the mouse acetylcholine-induced abdominal constriction test: ED50 = 0.000 52 mg/kg, s.c. The activity of I resides solely in its 3(R)-enantiomer. The κ-agonist activity in both the 4-acyl and the 4-carbamate series is sensitive to the size of the 4-substituent. In addition, it would appear that an appreciable neg. electrostatic potential in this region of the mol. is an important requirement for optimal potency.(4-Benzylpiperazin-2-yl)methanol(cas: 85817-34-1Application In Synthesis of (4-Benzylpiperazin-2-yl)methanol) was used in this study.

(4-Benzylpiperazin-2-yl)methanol(cas: 85817-34-1) belongs to piperazines. 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).Application In Synthesis of (4-Benzylpiperazin-2-yl)methanol

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

Raja Sekhara Reddy, B.; Pratap Reddy Gajulapalli, V.; Madhu Rekha, Estharla; Siva Krishna, Vagolu; Sriram, Dharmarajan; Sudakar Babu, K.; Kim, Eunha published an article on January 31 ,2022. The article was titled 《Design, synthesis, and in vitro biological evaluation of dehydroaripiprazole derivatives as antituberculosis agents and molecular docking study》, and you may find the article in Results in Chemistry.Recommanded Product: 34352-59-5 The information in the text is summarized as follows:

In this study, we describe the synthesis of novel piperazine-substituted 7-(4-chlorobutoxy) quinolin-2(1H) derivatives 5a-z, which were designed through specific structural modifications of aripiprazole. Furthermore, the synthesized derivatives were described as potent in vitro inhibitors of Mycobacterium tuberculosis (MTB) H37Rv strain growth. Among these compounds, 5c, 5 h, and 5r were found to be the most active ones with a MIC of 0.78 μg/mL. This activity is better compared to that of ethambutol (MIC = 1.56 μg/mL). These compounds failed to inhibit normal RAW 264.7 macrophages. Moreover, in vitro findings were supported by mol. docking studies with the known anti-TB target (InhA). The mol. docking studies on 5c, 5 h, and 5r hit compounds clearly validated hydrogen bonds interactions with the Enoyl-acp reductase (INHA). Therefore, these results indicate that this class of compounds may provide candidates for future development, and hopefully provide drug alternatives for tuberculosis treatment. In the experimental materials used by the author, we found 1-Methylpiperazine dihydrochloride(cas: 34352-59-5Recommanded Product: 34352-59-5)

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..Recommanded Product: 34352-59-5

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

Zhao, Yujun; Aguilar, Angelo; Bernard, Denzil; Wang, Shaomeng published an article on February 12 ,2015. The article was titled 《Small-Molecule Inhibitors of the MDM2-p53 Protein-Protein Interaction (MDM2 Inhibitors) in Clinical Trials for Cancer Treatment》, and you may find the article in Journal of Medicinal Chemistry.Name: 1-(3-(Methylsulfonyl)propyl)piperazine dihydrochloride The information in the text is summarized as follows:

A review. Design of small-mol. inhibitors (MDM2 inhibitors) to block the MDM2-p53 protein-protein interaction has been pursued as a new cancer therapeutic strategy. In recent years, potent, selective, and efficacious MDM2 inhibitors have been successfully obtained and seven such compounds have been advanced into early phase clin. trials for the treatment of human cancers. Here, we review the design, synthesis, properties, preclin., and clin. studies of these clin.-stage MDM2 inhibitors. In the part of experimental materials, we found many familiar compounds, such as 1-(3-(Methylsulfonyl)propyl)piperazine dihydrochloride(cas: 939983-66-1Name: 1-(3-(Methylsulfonyl)propyl)piperazine dihydrochloride)

1-(3-(Methylsulfonyl)propyl)piperazine dihydrochloride(cas: 939983-66-1) is a member of sulfones.The sulfones, like the sulfonamides, are structural analogs of para-aminobenzoic acid that interfere with folic acid metabolism by acting as competitive inhibitors of dihydropteroate synthetase. All sulfones of clinical value are derivatives of dapsone, the most widely used member of this class.Name: 1-(3-(Methylsulfonyl)propyl)piperazine dihydrochloride

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

《Synthesis and structure-activity relationships for tetrahydroisoquinoline-based inhibitors of Mycobacterium tuberculosis》 was written by Lu, Guo-Liang; Tong, Amy S. T.; Conole, Daniel; Sutherland, Hamish S.; Choi, Peter J.; Franzblau, Scott G.; Upton, Anna M.; Lotlikar, Manisha U.; Cooper, Christopher B.; Denny, William A.; Palmer, Brian D.. COA of Formula: C5H12N2 And the article was included in Bioorganic & Medicinal Chemistry in 2020. The article conveys some information:

A series of 5,8-disubstituted tetrahydroisoquinolines e.g., 2-((5-(4-chlorophenyl)pyridin-2-yl)methyl)-8-(4-methylpiperazin-1-yl)-1,2,3,4-tetrahydroisoquinoline were shown to be effective inhibitors of M. tb in culture and modest inhibitors of M. tb ATP synthase. There was a broad general trend of improved potency with higher lipophilicity. Large substituents (e.g., Bn) at the tetrahydroquinoline 5-position were well-tolerated, while N-methylpiperazine was the preferred 8-substituent. Structure-activity relationships for 7-linked side chains showed that the nature of the 7-linking group was important; -CO- and -COCH2- linkers were less effective than -CH2- or -CONH- ones. This suggests that the positioning of a terminal aromatic ring is important for target binding. Selected compounds showed much faster rates of microsomal clearance than the clin. ATP synthase inhibitor bedaquiline, and modest inhibition of mycobacterial ATP synthase. The experimental part of the paper was very detailed, including the reaction process of 1-Methylpiperazine(cas: 109-01-3COA of Formula: 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..COA of Formula: C5H12N2

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

《An exit beyond the pharmacophore model for 5-HT6R agents – a new strategy to gain dual 5-HT6/5-HT2A action for triazine derivatives with procognitive potential》 was written by Kucwaj-Brysz, Katarzyna; Ali, Wesam; Kurczab, Rafal; Sudol-Talaj, Sylwia; Wilczynska-Zawal, Natalia; Jastrzebska-Wiesek, Magdalena; Satala, Grzegorz; Mordyl, Barbara; Zeslawska, Ewa; Agnieszka-Olejarz-Maciej; Czarnota, Kinga; Latacz, Gniewomir; Partyka, Anna; Wesolowska, Anna; Nitek, Wojciech; Handzlik, Jadwiga. Quality Control of 1-Methylpiperazine dihydrochloride And the article was included in Bioorganic Chemistry on April 30 ,2022. The article conveys some information:

Herein, the first highly potent 5-HT6/5-HT2A receptor (5-HT6/5-HT2AR) dual antagonists in a group of 1,3,5-triazine compounds have been discovered as a result of an exit beyond the hydrophobic feature of the pharmacophore model for 5-HT6R antagonists. Design and synthesis of the series I (X = O, S; R1 = 4-PhOC6H4, 4-PhC6H4, 2-naphthyl, 1-naphthyl; R2 = H, Me, Et, n-Bu, R3 = H; R2 = R3 = Me) of ether and thioether derivatives of 1,3,5-triazines with the double-ring aromatic region have been performed. The new compounds I were examined within the comprehensive pharmacol. screening, including: radioligand binding assays, functional and ADMET studies in vitro as well as behavioral tests in rats. Crystallog. aspects and computer-aided structure-activity relationship were analyzed as well. This comprehensive approach led to selection of the compound I [X = S; R1 = 2-naphthyl; R2 = R3 = Me; (II)] with the most significant dual 5-HT6/5-HT2AR antagonistic action (5-HT6R Ki = 11 nM, 5-HT2AR Ki = 39 nM). Moreover, the compound II has satisfactory ADMETox properties in vitro, i.e.: the high permeability through biol. membranes, high metabolic stability, neither mutagenic nor hepatotoxic effects and moderate ability to inhibit CYP3A4. Above all, the compound II showed ability to reverse the pharmacol.-induced (MK-801) memory impairment at low doses (1-3 mg/kg) in Novel Object Recognition (NOR) test in rats. These results indicate a promising potency of dual 5-HT6/5-HT2AR antagonism in the search for novel strategy to fight Alzheimer’s disease, which remains an unmet clin. need. In the experiment, the researchers used 1-Methylpiperazine dihydrochloride(cas: 34352-59-5Quality Control of 1-Methylpiperazine dihydrochloride)

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..Quality Control of 1-Methylpiperazine dihydrochloride

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

Synthetic Route of C5H11ClN2O2SOn March 11, 2013, Moukha-chafiq, Omar; Reynolds, Robert C. published an article in ACS Combinatorial Science. The article was 《Parallel Solution-Phase Synthesis of an Adenosine Antibiotic Analog Library》. The article mentions the following:

A library of eighty one adenosine antibiotic analogs was prepared under the Pilot Scale Library Program of the NIH Roadmap initiative from 5′-amino-5′-deoxy-2′,3′-O-isopropylidene-adenosine (I). Diverse aldehyde, sulfonyl chloride and carboxylic acid reactant sets were condensed to I, in solution-phase fashion, leading after acid-mediated hydrolysis to the targeted compounds in good yields and high purity. No marked antituberculosis or anticancer activity was noted on preliminary cellular testing, but these nucleoside analogs should be useful candidates for other types of biol. activity.4-Methyl-1-piperazinesulfonyl Chloride(cas: 1688-95-5Synthetic Route of C5H11ClN2O2S) was used in this study.

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.Synthetic Route of C5H11ClN2O2S

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

Cheng, Chuanjie; Sun, Jianwei; Xing, Lixin; Xu, Jimin; Wang, Xinyan; Hu, Yuefei published their research in Journal of Organic Chemistry on August 7 ,2009. The article was titled 《Highly Chemoselective Pd-C Catalytic Hydrodechlorination Leading to the Highly Efficient N-Debenzylation of Benzylamines》.Application of 34352-59-5 The article contains the following contents:

In the presence of 1,1,2-trichloroethane, a novel procedure for the Pd-C catalytic N-debenzylation of benzylamines was established. The method proceeded in a synergistic catalytic system and directly gave the products as crystalline amine hydrochlorides in practically quant. yields. In the experiment, the researchers used many compounds, for example, 1-Methylpiperazine dihydrochloride(cas: 34352-59-5Application of 34352-59-5)

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..Application of 34352-59-5

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

Chubanov, V.; Schnitzler, M. Mederos; Meissner, M.; Schaefer, S.; Abstiens, K.; Hofmann, T.; Gudermann, T. published an article in British Journal of Pharmacology. The title of the article was 《Natural and synthetic modulators of SK (KCa2) potassium channels inhibit magnesium-dependent activity of the kinase-coupled cation channel TRPM7》.HPLC of Formula: 70006-24-5 The author mentioned the following in the article:

Background and Purpose Transient receptor potential cation channel subfamily M member 7 (TRPM7) is a bifunctional protein comprising a TRP ion channel segment linked to an α-type protein kinase domain. TRPM7 is essential for proliferation and cell growth. Up-regulation of TRPM7 function is involved in anoxic neuronal death, cardiac fibrosis and tumor cell proliferation. The goal of this work was to identify non-toxic inhibitors of the TRPM7 channel and to assess the effect of blocking endogenous TRPM7 currents on the phenotype of living cells. Exptl. Approach We developed an aequorin bioluminescence-based assay of TRPM7 channel activity and performed a hypothesis-driven screen for inhibitors of the channel. The candidates identified were further assessed electrophysiol. and in cell biol. experiments Key Results TRPM7 currents were inhibited by modulators of small conductance Ca2+-activated K+ channels (KCa2.1-2.3; SK) channels, including the antimalarial plant alkaloid quinine, CyPPA, dequalinium, NS8593, SKA31 and UCL 1684. The most potent compound NS8593 (IC50 1.6 μM) specifically targeted TRPM7 as compared with other TRP channels, interfered with Mg2+-dependent regulation of TRPM7 channel and inhibited the motility of cultured cells. NS8593 exhibited full and reversible block of native TRPM7-like currents in HEK 293 cells, freshly isolated smooth muscle cells, primary podocytes and ventricular myocytes. Conclusions and Implications This study reveals a tight overlap in the pharmacol. profiles of TRPM7 and KCa2.1-2.3 channels. NS8593 acts as a neg. gating modulator of TRPM7 and is well-suited to study functional features and cellular roles of endogenous TRPM7. In the part of experimental materials, we found many familiar compounds, such as Abt-724(cas: 70006-24-5HPLC of Formula: 70006-24-5)

Abt-724(cas: 70006-24-5) belongs to piperazines. 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: 70006-24-5

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

Liu, Xiaohua; Zhang, Yu; Huang, Wenjing; Tan, Wenfu; Zhang, Ao published an article on January 15 ,2018. The article was titled 《Design, synthesis and pharmacological evaluation of new acyl sulfonamides as potent and selective Bcl-2 inhibitors》, and you may find the article in Bioorganic & Medicinal Chemistry.HPLC of Formula: 1688-95-5 The information in the text is summarized as follows:

The antiapoptotic protein Bcl-2, overexpressed in many tumor cells, is an attractive target for potential small mol. anticancer drug discovery. Herein, we report a different structural modification approach on ABT-263 by merging the piperazinyl-Ph fragment into a bicyclic framework leading to a series of novel analogs, among which tetrahydroisoquinoline 13 was nearly equally potent against Bcl-2 as ABT-263. Further SAR in the P4-interaction pocket afforded the difluoroazetidine substituted analog 55, which retained good Bcl-2 activity with improved Bcl-2/Bcl-xL selectivity. In the experiment, the researchers used many compounds, for example, 4-Methyl-1-piperazinesulfonyl Chloride(cas: 1688-95-5HPLC of Formula: 1688-95-5)

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.HPLC of Formula: 1688-95-5

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