Month: October 2022

SDS of cas: 182868-72-0On October 31, 1996 ,《Structure-activity relationships of quinolone agents against mycobacteria: effect of structural modifications at the 8 position》 appeared in Antimicrobial Agents and Chemotherapy. The author of the article were Renau, Thomas E.; Gage, Jeffrey W.; Dever, Julie A.; Roland, Gregory E.; Joannides, E. Themis; Shapiro, Martin A.; Sanchez, Joseph P.; Gracheck, Stephen J.; Domagala, John M.. The article conveys some information:

A series of quinolones with substitutions at the 8 position has been prepared as part of a study to examine the relation between structural modifications at this position and activity against mycobacteria. The compounds were prepared by procedures described in the literature and were evaluated for their activities against Mycobacterium fortuitum and Mycobacterium smegmatis. The activities of the compounds against these two organisms were used as a measure of Mycobacterium tuberculosis activity. The results demonstrate that the contribution of the 8 position to antimycobacterial activity was dependent on the substituent at N-1 and was in the order (i) COMe ≈ CBr > CCl > CH ≈ CF ≈ COEt > N > CCF3 when N-1 was cyclopropyl; (ii) N ≈ CH > CF > COMe when N-1 was 2,4-difluorophenyl; (iii) N ≥ CH when N-1 was tert-butyl; and (i.v.) N > CH when N-1 was Et. In general, derivatives with piperazine substitutions at C-7 were slightly less active against mycobacteria than the analogs with pyrrolidine substitutions, regardless of the pattern of substitution at the 8 position. Several of the best compounds were evaluated for their potential side effects as well as their activities against Mycobacterium aurum, Mycobacterium avium-M. Intracellularle, and M. tuberculosis. These agents exhibited biol. profiles similar to or better than those of the pos. controls ciprofloxacin and sparfloxacin. In addition to this study using 1-Cyclopropyl-8-ethoxy-6-fluoro-7-(3-methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid, there are many other studies that have used 1-Cyclopropyl-8-ethoxy-6-fluoro-7-(3-methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid(cas: 182868-72-0SDS of cas: 182868-72-0) was used in this study.

1-Cyclopropyl-8-ethoxy-6-fluoro-7-(3-methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid(cas: 182868-72-0) is a member of aromaticfluorinated building blocks. Depending on which substituents are present, fluoroaromatic intermediates can be converted into fluorinated or fluorine-free commercial end products.Fluorine-containing aromatics have been incorporated into drugs (hypnotics, tranquilizers, antiinflammatory agents, analgesics, antibacterials).SDS of cas: 182868-72-0

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

Product Details of 70006-24-5On October 31, 2015 ,《Role of dopamine D4 receptors in copulatory behavior: Studies with selective D4 agonists and antagonists in male rats》 appeared in Pharmacology, Biochemistry and Behavior. The author of the article were Sanna, Fabrizio; Contini, Andrea; Melis, Maria Rosaria; Argiolas, Antonio. The article conveys some information:

Dopamine influences the anticipatory and consummatory phases of sexual behavior, by acting on receptors of the D2 family (D2, D3 and D4) and in particular of the D2 subtype, although evidence for a role of D4 receptors in erectile function and copulatory behavior is also available. In order to clarify such a role of D4 receptors, the effect of selective D4 receptor agonists and antagonists on copulatory behavior of sexually potent male rats in classic copulation tests with a receptive female, was compared with that of apomorphine and haloperidol, a classic dopamine receptor agonist and antagonist, resp. PD-168,077 (0.05-0.2 mg/kg) and ABT-724 (0.01-0.04 mg/kg), two selective D4 receptor agonists, given s.c., improved dose-dependently copulatory behavior as shown by the decrease of mount frequency and post ejaculatory interval induced by PD-168,077, and of mount frequency, ejaculation latency, post ejaculatory and inter intromission intervals induced by ABT-724, and by the increase of ejaculation frequency and copulatory efficacy induced by both drugs. Conversely, L-745,870 (1-5 mg/kg), a selective D4 receptor antagonist, given i.p., impaired dose-dependently copulatory behavior, as shown by the increase in intromission and ejaculation latencies, mount frequency, post ejaculatory interval and the decrease in ejaculation frequency and copulatory efficacy induced by this drug. L-745,870 (5 mg/kg) administered before PD-168,077 (0.2 mg/kg) or ABT-724 (0.04 mg/kg), also abolished completely the facilitatory effects of both PD-168,077 and ABT-724 on sexual behavior. These results confirm the involvement of D4 receptors in specific aspects of male rat copulatory behavior that overlap only partially with those influenced by apomorphine and haloperidol. In the experiment, the researchers used Abt-724(cas: 70006-24-5Product Details 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).Product Details of 70006-24-5

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

Safety of 4-(Piperazin-1-yl)-1H-indoleOn 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: 84807-09-0Safety of 4-(Piperazin-1-yl)-1H-indole) 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.Safety of 4-(Piperazin-1-yl)-1H-indole

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. Category: piperazines 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: 109-01-3Category: 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

《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.. HPLC of Formula: 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: 70006-24-5HPLC 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

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)》.Product Details of 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: 123987-13-3Product Details of 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.Product Details of 123987-13-3

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》.Product Details 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: 534615-34-4Product Details 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.Product Details of 534615-34-4

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. Application In Synthesis of 1-(Pyridin-2-yl)piperazin-2-one. 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: 345310-98-7Application In Synthesis of 1-(Pyridin-2-yl)piperazin-2-one) 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.Application In Synthesis of 1-(Pyridin-2-yl)piperazin-2-one

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》.COA of Formula: C12H15N3 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: 84807-09-0COA of Formula: C12H15N3)

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.COA of Formula: C12H15N3

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

SDS of cas: 109-01-3In 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: 109-01-3SDS of cas: 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..SDS of cas: 109-01-3

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