Month: October 2022

Related Products of 109-01-3In 2021 ,《Discovery and optimization of novel pyrazole-benzimidazole CPL304110 as a potent and selective inhibitor of fibroblast growth factor receptors FGFR (1-3)》 appeared in European Journal of Medicinal Chemistry. The author of the article were Yamani, Abdellah; Zdzalik-Bielecka, Daria; Lipner, Joanna; Stanczak, Aleksandra; Piorkowska, Natalia; Stanczak, Paulina Seweryna; Olejkowska, Patrycja; Hucz-Kalitowska, Joanna; Magdycz, Marta; Dzwonek, Karolina; Dubiel, Krzysztof; Lamparska-Przybysz, Monika; Popiel, Delfina; Pieczykolan, Jerzy; Wieczorek, Maciej. The article conveys some information:

The scaffolds hybridization approach, scaffold-hopping concept, has been employed to synthesize a series of novel pyrazole-benzimidazoles I [R1 = H, Cl; R2 = morpholin-4-yl, 4-methylpiperazin-1-ylcarbonyl, tetrahydropyran-4-ylcarbamoyl, etc.; R3 = H, F]. Compound I [R1 = R3 = H; R2 = 4-methylpiperazin-1-yl] (CPL304110) was identified as a selective and potent pan-FGFR inhibitor for FGFR1, FGFR2, FGFR3 with IC50 of 0.75 nM, 0.50 nM, 3.05 nM resp., and IC50 of 87.90 nM for FGFR4. Due to its favorable pharmacokinetic profile, low toxicity and potent anti-tumor activity in-vivo, this compound I is currently under evaluation in phase I clin. trial for the treatment of bladder, gastric and squamous cell lung cancers (01FGFR2018; NCT04149691). 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

Dow, Robert L.; Paight, Ernest S.; Schneider, Steven R.; Hadcock, John R.; Hargrove, Diane M.; Martin, Kelly A.; Maurer, Tristan S.; Nardone, Nancy A.; Tess, David A.; DaSilva-Jardine, Paul published an article in Bioorganic & Medicinal Chemistry Letters. The title of the article was 《Potent and selective, sulfamide-based human β3-adrenergic receptor agonists》.Name: 4-Methyl-1-piperazinesulfonyl Chloride The author mentioned the following in the article:

A series of sulfamide-based analogs, e.g., I, related to L-796568 were prepared and evaluated for their biol. activity at the human β3-adrenergic receptor (AR). This modification allows for a significant reduction in mol. weight, while maintaining single-digit nanomolar potencies at the β3-AR and high selectivities vs. the β1- or β2-AR.4-Methyl-1-piperazinesulfonyl Chloride(cas: 1688-95-5Name: 4-Methyl-1-piperazinesulfonyl Chloride) 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.Name: 4-Methyl-1-piperazinesulfonyl Chloride

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

Tabushi, Iwao; Shimokawa, Kazuhiro published an article in Journal of the American Chemical Society. The title of the article was 《Model approach to retinal pigments. Remarkable red shift due to proximal ammonium ion》.Synthetic Route of C5H14Cl2N2 The author mentioned the following in the article:

Retinal derivs, I and II, were prepared and the absorption characteristics of a series of retinal derivatives (I, II, III, IV, and V) were investigated as a model study for the remarkable red shift observed for the native retinal pigments such as rhodopsins or bacteriorhodopsins. Remarkable red shifts observed in the following 2 derivatives were interpreted mechanistically; in retinal N’-methylpiperidinium perchlorate, 526 nm in CHCl3, as the electrostatic destabilization of the ground state by the proximal NH4 with a loose counter-anion in a less polar solvent; and in III chloride, 497 nm in water, as the balance between the electrostatic destabilization and the twist of the chromophore. In addition to this study using 1-Methylpiperazine dihydrochloride, there are many other studies that have used 1-Methylpiperazine dihydrochloride(cas: 34352-59-5Synthetic Route of C5H14Cl2N2) 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..Synthetic Route of C5H14Cl2N2

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

Recommanded Product: 1-MethylpiperazineIn 2021 ,《Facile and Cost-Effective Route for the Synthesis of Simmerafil》 was published in Organic Process Research & Development. The article was written by Odilov, Abdullajon; Liu, Yin; Hu, Tianwen; Jiang, Xiangrui; Suo, Jin; Tian, Guanghui; Yang, Feipu; Shen, Jingshan. The article contains the following contents:

An improved synthesis of simmerafil, a potent PDE5 inhibitor as a clin. candidate, is described with a 38.1% overall yield and 99.7% purity. Starting from the safe and inexpensive salicylamide, the key intermediate 2-propoxybenzimidamide, which is also a potential precursor for the preparation of pyrimidinone derivatives, was effectively and conveniently obtained. The subsequent process from 2-propoxybenzimidamide to simmerafil was optimized, which makes it more amenable to scale-up.1-Methylpiperazine(cas: 109-01-3Recommanded Product: 1-Methylpiperazine) was used in this study.

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

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

Recommanded Product: 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: 70006-24-5Recommanded Product: 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).Recommanded Product: 70006-24-5

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

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

《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

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