Category: piperazines

Electric Literature of C5H14Cl2N2On October 31, 1983 ,《Imidazole systems. I. Imidazo[2,1-b][1,3,5]benzothiadiazepine derivatives as potential antipsychotic agents》 appeared in Journal of Heterocyclic Chemistry. The author of the article were Della Vecchia, Laurence; Dellureficio, James; Kisis, Biruta; Vlattas, Isidoros. The article conveys some information:

Imidazo[2,1-b][1,3,5]benzothiadiazepine (I, R-R2 = H) constitutes a novel ring system, and I [R = H, Me; R1 = H, Cl, F, CF3, OMe; R2 = (un)substituted piperazino, imidazole, perhydro-1,4-diazepino] were synthesized to investigate their antipsychotic activity. The synthesis of I was achieved by reaction of 2-aminophenylthioimidazoles with COCl2 or CSCl2 or by ring closure of the 1-[2-(2-imidazolyl)thiophenyliminocarbonyl]-1-piperazines. An efficient method for the conversion of I (R2 = SH) to I (R2 = amino) via I (R2 = thiocyanato) was also developed. The results came from multiple reactions, including the reaction of 1-Methylpiperazine dihydrochloride(cas: 34352-59-5Electric Literature of C5H14Cl2N2)

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..Electric Literature of C5H14Cl2N2

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

Recommanded Product: 1-MethylpiperazineIn 2019 ,《Sulfonamide Synthesis through Electrochemical Oxidative Coupling of Amines and Thiols》 was published in Journal of the American Chemical Society. The article was written by Laudadio, Gabriele; Barmpoutsis, Efstathios; Schotten, Christiane; Struik, Lisa; Govaerts, Sebastian; Browne, Duncan L.; Noel, Timothy. The article contains the following contents:

Sulfonamides are key motifs in pharmaceuticals and agrochems., spurring the continuous development of novel and efficient synthetic methods to access these functional groups. Herein, the authors report an environmentally benign electrochem. method which enables the oxidative coupling between thiols and amines, two readily available and inexpensive commodity chems. The transformation is completely driven by electricity, does not require any sacrificial reagent or addnl. catalysts and can be carried out in only 5 min. Hydrogen is formed as a benign byproduct at the counter electrode. Owing to the mild reaction conditions, the reaction displays a broad substrate scope and functional group compatibility. The experimental process involved the reaction of 1-Methylpiperazine(cas: 109-01-3Recommanded Product: 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..Recommanded Product: 1-Methylpiperazine

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

Zhang, Bo-Sheng; Li, Yuke; Zhang, Zhe; An, Yang; Wen, Yu-Hua; Gou, Xue-Ya; Quan, Si-Qi; Wang, Xin-Gang; Liang, Yong-Min published an article in Journal of the American Chemical Society. The title of the article was 《Synthesis of C4-Aminated Indoles via a Catellani and Retro-Diels-Alder Strategy》.Category: piperazines The author mentioned the following in the article:

Highly functionalized 4-aminoindoles were synthesized via the three-component cross-coupling of o-iodoaniline, N-benzoyloxyamines, and norbornadiene. The Catellani and retro-Diels-Alder strategy was used in this domino process. o-Iodoaniline, with electron-donating and sterically hindered protecting groups, made the reaction selective toward o-C-H amination. On the basis of d. functional theory calculations, the intramol. Buchwald coupling of this reaction underwent a dearomatization and a 1,3-palladium migration process. The reasons for the control of the chem. selectivity by the protecting groups are given. Moreover, synthetic applications toward 4-piperazinylindole and a GOT1 inhibitor were realized. After reading the article, we found that the author used 4-(Piperazin-1-yl)-1H-indole(cas: 84807-09-0Category: piperazines)

4-(Piperazin-1-yl)-1H-indole(cas: 84807-09-0) belongs to piperazines. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines.Category: piperazines

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

In 2011,Bioorganic & Medicinal Chemistry Letters included an article by Kim, Heung Jae; Kwak, Woo Young; Min, Jong Pil; Lee, Jae Young; Yoon, Tae Hyun; Kim, Ha Dong; Shin, Chang Yell; Kim, Mi Kyung; Choi, Song Hyen; Kim, Hae Sun; Yang, Eun Kyoung; Cheong, Ye Hwang; Chae, Yu Na; Park, Kyung Jin; Jang, Ji Myun; Choi, Soo Jung; Son, Moon Ho; Kim, Soon Hoe; Yoo, Moohi; Lee, Bong Jin. COA of Formula: C9H11N3O. The article was titled 《Discovery of DA-1229: A potent, long acting dipeptidyl peptidase-4 inhibitor for the treatment of type 2 diabetes》. The information in the text is summarized as follows:

A series of β-amino amide containing substituted piperazine-2-one derivatives was synthesized and evaluated as inhibitors of dipeptidyl peptidase-4 (DPP-4) for the treatment of type 2 diabetes. As results of intensive SAR study of the series, (R)-4-[(R)-3-amino-4-(2,4,5-trifluorophenyl)-butanoyl]-3-(t-butoxymethyl)-piperazin-2-one (DA-1229, I) displayed potent DPP-4 inhibition pattern in several animal models, was selected for clin. development. In addition to this study using 1-(Pyridin-2-yl)piperazin-2-one, there are many other studies that have used 1-(Pyridin-2-yl)piperazin-2-one(cas: 345310-98-7COA of Formula: C9H11N3O) was used in this study.

1-(Pyridin-2-yl)piperazin-2-one(cas: 345310-98-7) belongs to piperazines. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines.COA of Formula: C9H11N3O

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

Chen, Jianyang; Peng, Haixia; He, Jinxue; Huan, Xiajuan; Miao, Zehong; Yang, Chunhao published an article in Bioorganic & Medicinal Chemistry Letters. The title of the article was 《Synthesis of isoquinolinone-based tricycles as novel poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors》.Related Products of 534615-34-4 The author mentioned the following in the article:

The isoquinolinone-based tricyclic compounds were designed and synthesized. Preliminary biol. study of these compounds provided potent compounds I, II, III, and IV with low nanomolar IC50s against PARP-1 enzyme. In the experiment, the researchers used many compounds, for example, 1-(Isopropylsulfonyl)piperazine(cas: 534615-34-4Related Products of 534615-34-4)

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.Related Products of 534615-34-4

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

Akama, Tsutomu; Zhang, Yong-Kang; Freund, Yvonne R.; Berry, Pamela; Lee, Joanne; Easom, Eric E.; Jacobs, Robert T.; Plattner, Jacob J.; Witty, Michael J.; Peter, Rosemary; Rowan, Tim G.; Gillingwater, Kirsten; Brun, Reto; Nare, Bakela; Mercer, Luke; Xu, Musheng; Wang, Jiangong; Liang, Hao published an article in Bioorganic & Medicinal Chemistry Letters. The title of the article was 《Identification of a 4-fluorobenzyl L-valinate amide benzoxaborole (AN11736) as a potential development candidate for the treatment of Animal African Trypanosomiasis (AAT)》.SDS of cas: 123987-13-3 The author mentioned the following in the article:

Novel L-valinate amide benzoxaboroles and analogs were designed and synthesized for a structure-activity-relationship (SAR) investigation to optimize the growth inhibitory activity against Trypanosoma congolense (T. congolense) and Trypanosoma vivax (T. vivax) parasites. The study identified 4-fluorobenzyl (1-hydroxy-7-methyl-1,3-dihydrobenzo[c][1,2]oxaborole-6-carbonyl)-L-valinate (5, AN11736), which showed IC50 values of 0.15 nM against T. congolense and 1.3 nM against T. vivax, and demonstrated 100% efficacy with a single dose of 10 mg/kg against both T. congolense and T. vivax in mouse models of infection (IP dosing) and in the target animal, cattle, dosed i.m. AN11736 has been advanced to early development studies.(3-(4-Methylpiperazin-1-yl)phenyl)methanol(cas: 123987-13-3SDS of cas: 123987-13-3) was used in this study.

(3-(4-Methylpiperazin-1-yl)phenyl)methanol(cas: 123987-13-3) belongs to piperazines. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines.SDS of cas: 123987-13-3

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

《Yawning and hypothermia in rats: effects of dopamine D3 and D2 agonists and antagonists》 was written by Collins, Gregory T.; Newman, Amy Hauck; Grundt, Peter; Rice, Kenner C.; Husbands, Stephen M.; Chauvignac, Cedric; Chen, Jianyong; Wang, Shaomeng; Woods, James H.. Related Products of 70006-24-5 And the article was included in Psychopharmacology (Berlin, Germany) on August 31 ,2007. The article conveys some information:

Identification of behaviors specifically mediated by the dopamine D2 and D3 receptors would allow for the determination of in vivo receptor selectivity and aide the development of novel therapeutics for dopamine-related diseases. These studies were aimed at evaluating the specific receptors involved in the mediation of D2/D3 agonist-induced yawning and hypothermia. The relative potencies of a series of D2-like agonists to produce yawning and hypothermia were determined The ability of D3-selective and D2-selective antagonists to inhibit the induction of yawning and hypothermia were assessed and a series of D2/D3 antagonists were characterized with respect to their ability to alter yawning induced by a low and high dose of PD-128,907 and sumanirole-induced hypothermia. D3-preferring agonists induced yawning at lower doses than those required to induce hypothermia and the D2-preferring agonist, sumanirole, induced hypothermia at lower doses than were necessary to induce yawning. The rank order of D3 selectivity was pramipexole > PD-128,907=7-OH-DPAT = quinpirole = quinelorane > apomorphine = U91356A. Sumanirole had only D2 agonist effects. PG01037, SB-277011A, and U99194 were all D3-selective antagonists, whereas haloperidol and L-741,626 were D2-selective antagonists and nafadotride’s profile of action was more similar to the D2 antagonists than to the D3 antagonists. D3 and D2 receptors have specific roles in the mediation of yawning and hypothermia, resp., and the anal. of these effects allow inferences to be made regarding the selectivity of D2/D3 agonists and antagonists with respect to their actions at D2 and D3 receptors. The results came from multiple reactions, including the reaction of Abt-724(cas: 70006-24-5Related Products of 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).Related Products of 70006-24-5

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

The author of 《Synthesis and antifungal activity of 1-aminomethyl-3-[4′-(4”-fluorobenzyloxy)-benzohydrazono] isatins》 were Rastogi, Nisheeth. And the article was published in Indian Journal of Heterocyclic Chemistry in 2019. Reference of 1-Methylpiperazine The author mentioned the following in the article:

A new series of 1-aminomethyl-3-[4′-(4”-fluorobenzyloxy)benzohydrazono]isatins (Mannich bases) I [R = H, Me, morpholinomethyl, etc.] were synthesized and screened for their antifungal potential against human pathogenic fungi. The structures of the compounds were established by means of elemental anal. and spectral data (IR and 1H NMR). The experimental part of the paper was very detailed, including the reaction process of 1-Methylpiperazine(cas: 109-01-3Reference 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..Reference of 1-Methylpiperazine

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

Product Details of 84807-09-0On September 1, 2018 ,《Discovery and optimization of aspartate aminotransferase 1 inhibitors to target redox balance in pancreatic ductal adenocarcinoma》 was published in Bioorganic & Medicinal Chemistry Letters. The article was written by Anglin, Justin; Zavareh, Reza Beheshti; Sander, Philipp N.; Haldar, Daniel; Mullarky, Edouard; Cantley, Lewis C.; Kimmelman, Alec C.; Lyssiotis, Costas A.; Lairson, Luke L.. The article contains the following contents:

Pancreatic ductal adenocarcinoma (PDAC) is a lethal malignancy that is extremely refractory to the therapeutic approaches that have been evaluated to date. Recently, it has been demonstrated that PDAC tumors are dependent upon a metabolic pathway involving aspartate aminotransferase 1, also known as glutamate-oxaloacetate transaminase 1 (GOT1), for the maintenance of redox homeostasis and sustained proliferation. As such, small mol. inhibitors targeting this metabolic pathway may provide a novel therapeutic approach for the treatment of this devastating disease. To this end, from a high throughput screen of ∼800,000 mols., 4-(1H-indol-4-yl)-N-phenylpiperazine-1-carboxamide was identified as an inhibitor of GOT1. Mouse pharmacokinetic studies revealed that potency, rather than inherent metabolic instability, would limit immediate cell- and rodent xenograft-based experiments aimed at validating this potential cancer metabolism-related target. Medicinal chem.-based optimization resulted in the identification of multiple derivatives with >10-fold improvements in potency, as well as the identification of a tryptamine-based series of GOT1 inhibitors.4-(Piperazin-1-yl)-1H-indole(cas: 84807-09-0Product Details of 84807-09-0) was used in this study.

4-(Piperazin-1-yl)-1H-indole(cas: 84807-09-0) belongs to piperazines. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines.Product Details of 84807-09-0

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