Month: October 2022

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

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

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

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

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

Ayad, Magda Mohamed; Hosny, Mervat Mohamed; Metias, Youstina Mekhail published an article in 2022. The article was titled 《Green micellar liquid chromatographic analysis of alfuzosin hydrochloride and sildenafil citrate in a binary mixture compared to classical RPLC with stability indicating studies》, and you may find the article in Drug Development and Industrial Pharmacy.Electric Literature of C5H12N2 The information in the text is summarized as follows:

Two simple and validated chromatog. studies were performed for simultaneous estimation of sildenafil citrate (SIL) and alfuzosin hydrochloride (ALF) in bulk, pharmaceuticals, and in the presence of their main degradation products. Two systems of mobile phase were applied isocratically for their first chromatog. separation using conventional and micellar mobile phases. Methanol, acetonitrile, and 0.02 M potassium dihydrogen phosphate (43:14:43 volume/volume; pH 4.66) were pumped at 1.3 mL/min in method I. Meanwhile, method II was based on less hazardous micellar mobile phase of nonionic surfactant (0.005 M Brij-35 in water; pH 2.5 adjusted with 0.1% orthophosphoric acid) with a flow rate of 1 mL/min. Both methods were carried on C18 column and coupled with UV detection at 225 nm at ambient temperature The first method was rectilinear over the concentration range of 5-62.5 μg/mL for both drugs, while the second method showed higher linearity ranges of 0.5-40, 2.5-62.5 μg/mL for ALF and (SIL), resp. The developed methods successfully enabled the quantification of the studied binary mixture in their tablets dosage form and evaluation their stabilities. Validation of the proposed methods according to ICH guidelines and system suitability were ascertained. Moreover, the applied methods were evaluated and compared from the perspective of green anal. chem., employing the National Environmental Methods Index, anal. Eco-Scale score, and Green Anal. Procedure Index, as three assessment tools. The results came from multiple reactions, including the reaction of 1-Methylpiperazine(cas: 109-01-3Electric Literature of 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..Electric Literature of C5H12N2

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

Safety of 4-(3-Aminophenoxy)-5-chloro-N-(2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)pyrimidin-2-amineOn November 1, 2017 ,《Design, synthesis and biological evaluation of WZ4002 analogues as EGFR inhibitors》 appeared in Bioorganic & Medicinal Chemistry Letters. The author of the article were Romu, Aireen A.; Lei, Zining; Zhou, Bin; Chen, Zhe-Sheng; Korlipara, Vijaya. The article conveys some information:

A series of thirty two anilinopyrimidines derived from WZ4002 has been synthesized and evaluated for percentage inhibition of six different EGFR kinases using LanthaScreen binding assay method (EGFR d746 – 750) or Z’LYTE assay method (EGFR-WT, EGFR d746 – 750, EGFR T790M, EGFR T790M L858R, EGFR C797S and EGFR T790M L858R C797S). Ortho-hydroxyacetamide I (R = 2′-NHCOCH2OH) exhibited complete inhibition of all the six kinases at 10 μM. Against the triple mutant, EGFR T790M C797S L858R, compounds I [R = 2′-NHCOCH2OCH2Ph, 2′-NHCOCH2OH, 2′-NHCO(CH2)2OCH2Ph, 2′-NHCO(CH2)2OH] exhibited complete inhibition at 10 μM and nearly complete inhibition at 1 μM. The target compounds were also evaluated using the MTT assay to determine their cytotoxic activity against human non-small cell lung cancer cells (PC9, PC9GR and H460) and mouse leukemic cells (Ba/F3 WT and Ba/F3T 3151). Overall, I [R = 2′-N3, 2′-NHCOCH2OCH2Ph, 2′-NHCOCH2OH, 2′-NHCO(CH2)2OCH2Ph, 2′-NHCO(CH2)2OH, 4′-NHCOCH2OCH2Ph, 4′-NHCOCH2OH] were found to be the most potent compounds across all five cell lines. In the experiment, the researchers used many compounds, for example, 4-(3-Aminophenoxy)-5-chloro-N-(2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)pyrimidin-2-amine(cas: 1213269-26-1Safety of 4-(3-Aminophenoxy)-5-chloro-N-(2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)pyrimidin-2-amine)

4-(3-Aminophenoxy)-5-chloro-N-(2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)pyrimidin-2-amine(cas: 1213269-26-1) is a member of pyrimidine. Pyrimidine derivatives are an important class of N-heterocycles. They are well-known for their wide spectrum of promising biological activities such as antitumors, bactericidals, and fungicidal.Safety of 4-(3-Aminophenoxy)-5-chloro-N-(2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)pyrimidin-2-amine

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

Pullagurla, Manik; Siripurapu, Uma; Kolanos, Renata; Bondarev, Mikhail L.; Dukat, Malgorzata; Setola, V.; Roth, B. L.; Glennon, Richard A. published their research in Bioorganic & Medicinal Chemistry Letters on December 1 ,2005. The article was titled 《Binding of amine-substituted N 1-benzenesulfonylindoles at human 5-HT6 serotonin receptors》.Application In Synthesis of 4-(Piperazin-1-yl)-1H-indole The article contains the following contents:

An examination of several amine-substituted analogs of N1-benzenesulfonylindoles reveals that although they bind at human 5-HT6 serotonin receptors with high affinity, they are likely to bind in a dissimilar manner. The experimental part of the paper was very detailed, including the reaction process of 4-(Piperazin-1-yl)-1H-indole(cas: 84807-09-0Application In Synthesis of 4-(Piperazin-1-yl)-1H-indole)

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.Application In Synthesis of 4-(Piperazin-1-yl)-1H-indole

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

Onder, Ferah Comert; Sahin, Kader; Senturk, Murat; Durdagi, Serdar; Ay, Mehmet published an article in 2022. The article was titled 《Identifying highly effective coumarin-based novel cholinesterase inhibitors by in silico and in vitro studies》, and you may find the article in Journal of Molecular Graphics & Modelling.Computed Properties of C5H12N2 The information in the text is summarized as follows:

Inhibition of high cholinesterase levels including acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), is one of the most important strategies for the treatment of Alzheime′s disease (AD). Clin. limited drugs are used in the treatment of AD, so there is a need to find new effective inhibitors today. Therefore, in this study, synthesized six coumarin carboxamides (A1, A2, B1-B4) were evaluated against AChE and BChE by combined in silico and in vitro studies. The in vitro assessment of studied compounds revealed that A1, A2, B3, and B4 showed highest inhibition potential against AChE and BChE. As demonstrated with our structure activity relationship (SAR) study, the promising inhibition result of AChE at nanomolar concentrations was obtained with heterocyclic amines including pyrrolidine and N-Me piperazine moieties for tertiary amide substituted coumarin compounds B3 and B4, displaying KI values of 9.78 nM and 8.07 nM, resp. Thus, compounds B3 and B4 had around 5.7- and 6.9-fold more potency compared to the reference mol., neostigmine. Moreover, coumarin-3-carboxamide derivative A1 bearing benzylmorpholine moiety on coumarin scaffold at position 3 displayed stronger inhibition potential against BChE. Furthermore, in order to better understand their mol. mechanisms in these targets, we conducted mol. docking and MD simulations. Our promising preclin. results show that the lead compounds A1, A2, B3 and B4 have high potential as effective inhibitors for the treatment of AD. The experimental process involved the reaction of 1-Methylpiperazine(cas: 109-01-3Computed Properties of 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..Computed Properties of C5H12N2

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

《Dopamine D4 receptor involvement in the discriminative stimulus effects in rats of LSD, but not the phenethylamine hallucinogen DOI》 was written by Marona-Lewicka, Danuta; Chemel, Benjamin R.; Nichols, David E.. Application In Synthesis of Abt-724 And the article was included in Psychopharmacology (Berlin, Germany) on April 30 ,2009. The article conveys some information:

Rationale: Lysergic acid diethylamide (LSD) differs from other types of hallucinogens in that it possesses direct dopaminergic effects. The exact nature of this component has not been elucidated. Objective: The present study sought to characterize the effects of several dopamine D4 agonists and antagonists on the discriminative stimulus effect of LSD at two pretreatment times and 2,5-dimethoxy-4-iodoamphetamine (DOI), a selective 5-HT2A/2C agonist. Materials and methods: Male Sprague-Dawley rats were trained in a two-lever, fixed ratio (FR) 50, food-reinforced task with LSD-30 (0.08 mg/kg, i.p., 30-min pretreatment time), LSD-90 (0.16 mg/kg, i.p., 90-min pretreatment time), and DOI (0.4 mg/kg, i.p., 30-min pretreatment time) as discriminative stimuli. Substitution and combination tests with the dopamine D4 agonists, ABT-724 and WAY 100635, were performed in all groups. Combination tests were run using the dopamine D4 antagonists A-381393 and L-745,870 and two antipsychotic drugs, clozapine and olanzapine. Results: WAY 100635 produced full substitution in LSD-90 rats, partial substitution in LSD-30 rats, and saline appropriate responding in DOI-trained rats. ABT-724 partially mimicked the LSD-90 and LSD-30 cues, but produced no substitution in DOI-trained rats. In combination tests, both agonists shifted the dose-response curve of LSD leftward, most potently for the LSD-90 cue. The D4 antagonists significantly attenuated both the LSD-90 and LSD-30 cue, but had no effect on the DOI cue. Conclusion: Dopamine D4 receptor activation plays a significant modulatory role in the discriminative stimulus effects in LSD-90-trained rats, most markedly for the later temporal phase of LSD, but has no effect on the cue produced by DOI.Abt-724(cas: 70006-24-5Application In Synthesis of Abt-724) was used in this study.

Abt-724(cas: 70006-24-5) belongs to piperazines. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines.Application In Synthesis of Abt-724

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