Tag: 100-200

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

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

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

《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

《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

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

Related Products of 109-01-3In 2020 ,《Synthesis, biological evaluation and kinase profiling of novel S-benzo[4,5]thiazolo[2,3-c][1,2,4]triazole derivatives as cytotoxic agents with apoptosis-inducing activity》 was published in Journal of Molecular Structure. The article was written by Abdelazeem, Ahmed H.; Alqahtani, Alaa M.; Omar, Hany A.; Bukhari, Syed Nasir Abbas; Gouda, Ahmed M.. The article contains the following contents:

A novel set of S-benzo[4,5]thiazolo[2,3-c][1,2,4]triazoles I [R = (adamantan-1-yl)aminyl, pyrrolidin-1-ylmethyl, (hexylamino)methyl, [(1,3-benzothiazol-2-yl)amino]methyl, etc.] was synthesized. Cytotoxicity of these compounds was evaluated against three cancer cell lines of different origins, Hep3B, A549, and MCF-7. Three of these compounds I [R = (4-chlorophenyl)aminyl, piperidin-1-ylmethyl, [(adamantan-1-yl)amino]methyl] were screened by NCI for growth inhibitory activities against 60 cancer cell lines. The results revealed significant cytotoxic activities for compounds I [R = pyrrolidin-1-ylmethyl, (hexylamino)methyl, [(1,3-benzothiazol-2-yl)amino]methyl, etc.]. Among these derivatives, compounds I [R = azepan-1-ylmethyl, (4-methylpiperazin-1-yl)methyl (A), (hexylamino)methyl (B), [(adamantan-1-yl)amino]methyl (C), [(1,3-benzothiazol-2-yl)amino]methyl (D)] exhibited the highest cytotoxicity against the selected cancer cell lines with IC50 values between 3.17 and 14.18μM. The structure-activity relationship of compounds I [R = pyrrolidin-1-ylmethyl, (hexylamino)methyl, [(1,3-benzothiazol-2-yl)amino]methyl, etc.] indicated favorable cytotoxic results on the expansion of the cyclic amine and the substitution with aminothiazole moiety. A mechanistic study revealed the activation of caspase-3/7 in A549 cells on treatment with compounds A-D at 5-20μM. Moreover, the results of flow cytometric anal. suggested that compound D efficiently induced apoptosis in a dose-dependent manner. Compounds A, B, D also exhibited a weak to moderate inhibition of multiple kinases where compound D was the most active in inhibiting the activity of CDK2/Cyclin A1 (IC50 = 4.65μM). The current work provided a novel set of compounds I with cytotoxic, kinase inhibition, and apoptosis-inducing activities, which can serve as a lead for further optimization. In the part of experimental materials, we found many familiar compounds, such as 1-Methylpiperazine(cas: 109-01-3Related Products of 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..Related Products of 109-01-3

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

Related Products of 109-01-3In 2019 ,《Solvent-free syntheses of two pcu topological indium phosphite-oxalates with a novel butterfly motif and proton conductivity》 was published in Microporous and Mesoporous Materials. The article was written by Jiang, Yansong; Song, Jianshu; Xiu, Zhijia; Huang, Liangliang; Gao, Fan; Jiao, Shufei; Bi, Yanfeng. The article contains the following contents:

Under solvent-free conditions, two new 3D open-framework indium phosphite-oxalates In5(HPO3)6(H1.5PO3)2(C2O4)2·(H2A)2, where A = C5N2H12 (compound 1) and C6N2H14 (compound 2), are synthesized by using 1-methylpiperazine and 1-ethylpiperazine as the structure-directing agent, resp. Single crystal x-ray diffraction reveals that these two compounds have the analog inorganic framework structures, which may be viewed as the assembly of butterfly motifs and [C2O2-4] groups. Interestingly, the butterfly motif is firstly reported in metal phosphite/phosphite-oxalate. By regarding the butterfly motifs as topol. equivalent 4-connected nodes and thus framework can be simplified into a uninodal pcu network with point symbol of (412, 63). 1 And 2 are also characterized by powder x-ray diffraction, IR spectroscopy, SEM, TGA, ICP-AES and elemental analyses. In addition, proton conduction was investigated by alternating-current impedance anal. and the results demonstrate that both compounds show high proton-conductive properties with the conductivity of 3.4 × 10-3 S cm-1 and 2.1 × 10-3 S cm-1 at 75° and 98% RH, resp. In the part of experimental materials, we found many familiar compounds, such as 1-Methylpiperazine(cas: 109-01-3Related Products of 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..Related Products of 109-01-3

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

Product Details of 109-01-3In 2021 ,《Synthesis and characterization of new potent TLR7 antagonists based on analysis of the binding mode using biomolecular simulations》 appeared in European Journal of Medicinal Chemistry. The author of the article were Pal, Sourav; Paul, Barnali; Bandopadhyay, Purbita; Preethy, Nagothy; Sarkar, Dipika; Rahaman, Oindrila; Goon, Sunny; Roy, Swarnali; Ganguly, Dipyaman; Talukdar, Arindam. The article conveys some information:

Aberrant activation of the endosomal Toll-like receptor 7 (TLR7) has been implicated in myriad autoimmune diseases and is an established therapeutic target in such conditions. Development of diverse TLR7 antagonists is mainly accomplished through random screening. To correlate human TLR7 (hTLR7) antagonistic activity with the structural features in different chemotypes, a hypothetical binding model is derived based on mol. docking anal. along with mol. dynamics (MD) simulations study. The binding hypothesis revealed different pockets, grooves and a central cavity where ligand-receptor interaction with specific residues through hydrophobic and hydrogen bond interactions take place, which correlate with TLR7 antagonistic activity, thus paving the way for rational design using varied chemotypes. Based on the structural insight thus gained, TLR7 antagonists with quinazoline, e.g., I were designed to understand the effect of engagement of these pockets as well as boundaries of the chem. space associated with them. The newly synthesized most potent hTLR7 antagonist, e.g., I, showed IC50 value of 1.03 ± 0.05μM and was validated by performing primary assay in human plasmacytoid dendritic cells (pDC) (ICpDC50: 1.42μM). The biol. validation of the synthesized mols. was performed in TLR7-reporter HEK293 cells as well as in human plasmacytoid dendritic cells (pDCs). This study provides a rational design approach, thus facilitating further development of novel small mol. hTLR7 antagonists based on different chem. scaffolds. After reading the article, we found that the author used 1-Methylpiperazine(cas: 109-01-3Product Details of 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..Product Details of 109-01-3

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

Category: piperazinesIn 2020 ,《Synthesis and Aminoalkylation of N-Propargyl Triterpene Aldimines》 appeared in Russian Journal of Organic Chemistry. The author of the article were Petrova, A. V.; Khusnutdinova, E. F.; Mustafin, A. G.; Kazakova, O. B.. The article conveys some information:

Mannich reaction of N-propargyl triterpene aldimines obtained from betulonic and oleanonic aldehydes gave new aminoalkyl derivatives containing an N-methylpiperazine fragment. 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