Tag: 100-200

HPLC of Formula: 109-01-3In 2022 ,《Structural and PK-guided identification of indole-based non-acidic autotaxin (ATX) inhibitors exhibiting high in vivo anti-fibrosis efficacy in rodent model》 was published in European Journal of Medicinal Chemistry. The article was written by Lei, Hongrui; Cao, Zhi; Wu, Huinan; Li, Tong; Wang, Xinyu; Chen, Yuxiang; Ma, Enlong; Sun, Lixin; Zhai, Xin. The article contains the following contents:

In recent decades, pharmacol. targeting of the autotaxin (ATX)/lysophosphatidic acid (LPA) axis accounted for excellent disease management benefits. Herein, to extend the scope of structure-activity relationships (SARs), fifteen indole-based carbamate derivatives I [R = 4-Me, 3,4-difluoro, 2,3-dichloro; R1 = pyrrolidin-1-yl, (4-methyl-1-piperidyl), (4-methylpiperazin-1-yl); R2 = H, CH3, etc] were prepared to evaluate the ATX inhibitory potency. Among them, compound I [R = 3,5-dichloro; R1 = morpholino; R2 = H] bearing morpholine moiety was identified as the optimal ATX inhibitor (0.41 nM), superior to the pos. control GLPG1690 (2.90 nM). To resolve the intractable issue of poor pharmacokinetic (PK) property, urea moiety was introduced as a surrogate of carbamate which furnished compounds II [R3 = morpholino, (4-hydroxy-1-piperidyl), [2-(hydroxymethyl)pyrrolidin-1-yl]; R4 = H, 4-Cl, 4-F, etc]. The dedicated modification identified the diethanolamine entity II [R3 = [bis(2-hydroxyethyl)amino]; R4 = (3-chloro-4-methoxy-phenyl)] with satisfactory water solubility and PK profiles with a min. sacrifice of ATX inhibition (2.17 nM). The most promising candidate II [R3 = [bis(2-hydroxyethyl)amino]; R4 = (3-chloro-4-methoxy-phenyl)] was evaluated for anti-fibrosis effect in a bleomycin challenged mice lung fibrosis model. Upon treatment with II [R3 = [bis(2-hydroxyethyl)amino]; R4 = (3-chloro-4-methoxy-phenyl)], the in vivo ATX activity in both lung homogenate and broncheoalveolar fluid (BALF) sample was significantly down-regulated. Furthermore, the gene expression of pro-fibrotic cytokines transforming growth factor-β (TGF-β), interleukin- 6 (IL-6) and tumor necrosis factor-α (TNF-α) in lung tissue was reduced to normal level. Collectively, the promising biol. effects may advocate potential application of II [R3 = [bis(2-hydroxyethyl)amino]; R4 = (3-chloro-4-methoxy-phenyl)] in fibrosis relevant diseases. In the part of experimental materials, we found many familiar compounds, such as 1-Methylpiperazine(cas: 109-01-3HPLC of Formula: 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..HPLC of Formula: 109-01-3

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

《Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors》 was published in European Journal of Medicinal Chemistry in 2020. These research results belong to Rani, Sudesh; Paul, Kamaldeep. SDS of cas: 109-01-3 The article mentions the following:

To structurally relate anticancer drug tamoxifen used in the treatment of breast cancer, a sequence of compounds I [R = piperidinyl, morpholino, 4-methylpiperazinyl, 4-ethylpiperazinyl, etc.] were designed and synthesized as potential drug candidates. McMurry coupling reaction was used as the key synthetic step in the preparation of these compounds I and the ratios of E/Z-isomers were determined on the basis of NMR and HPLC experiments The new compounds I were found to be cytotoxic in the micromolar range with 60 human tumor cell lines at one dose and five dose concentration levels. Detailed studies on the most active compounds I [R = 2-morpholinoethyl amine, cyclohexylamine and diethylamine] show these compounds were capable to inhibit the growth of cancer cells. Finally, with the aim to correlate the antiproliferative activity with an intracellular target(s), the effect on relaxation activity of DNA topoisomerase-II was assayed. The relevance of interaction of most active compounds with topoisomerase-II was demonstrated which was also supported by docking studies. 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

The author of 《Discovery of novel mutant-combating ALK and ROS1 dual inhibitors bearing imidazolidin-2-one moiety with reasonable PK properties》 were Lei, Hongrui; Jiang, Nan; Miao, Xiuqi; Xing, Lingyun; Guo, Ming; Liu, Yang; Xu, Haowen; Gong, Ping; Zuo, Daiying; Zhai, Xin. And the article was published in European Journal of Medicinal Chemistry in 2019. Reference of 1-Methylpiperazine The author mentioned the following in the article:

Aiming to identify novel potent ALK and ROS1 dual inhibitors, the relatively bulky piperidine fragment in ceritinib was replaced with substituted imidazolidin-2-one moiety which gave rise to a series of 2,4-diaryl-aminopyrimidine (DAAP) analogs. SAR studies were conducted based on cellular assays on five cell lines and most compounds exerted moderated to excellent activities. Among them, 15(I) showed excellent inhibitory activities against ROS1 and ALK pos. cell lines, especially Ba/F3G1202R, with IC50 values ranging from 14 to 37 nM. As a continuation, several compounds were tested in enzymic assays and I displayed encouraging activities against wild-type ALK (1.2 nM), ROS1(0.43 nM) as well as extremely resistant ALKL1196M and ALKG1202R mutants with IC50 values of 0.73 nM and 6.7 nM, resp. To our delight, both cellular and enzymic results of I were in good accordance with western blot assays on H2228 and HCC78 cell lines. Importantly, pharmacokinetic (PK) profiles of I were obtained with quite satisfying AUC and Cmax values. Besides, the binding models of I with ALKWT, ALKG1202R and ROS1 clearly present the essential interactions within the active site. 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

Zhang, Xin; Lv, Xiao-Qin; Tang, Sheng; Mei, Lin; Li, Ying-Hong; Zhang, Jing-Pu; Jiang, Jian-Dong; Peng, Zong-Gen; Song, Dan-Qing published an article in European Journal of Medicinal Chemistry. The title of the article was 《Discovery and evolution of aloperine derivatives as a new family of HCV inhibitors with novel mechanism》.HPLC of Formula: 1688-95-5 The author mentioned the following in the article:

Aloperine (I), a Chinese natural product with a unique endocyclic scaffold, was first identified to be a potent hepatitis C virus (HCV) inhibitor in our laboratory Thirty-four new aloperine derivatives were designed, synthesized and evaluated for their anti-HCV activities taking I as the lead. Among them, compound II exhibited the potential potency with EC50 values in a micromolar range against both wild-type and direct-acting antiviral agents (DAAs)-resistant variants, and synergistically inhibited HCV replication with approved DAAs. Furthermore, it also owned a good oral pharmacokinetic and safety profile, suggesting a highly druglike nature. The primary mechanism showed that II might target host components, distinctly different from the DAAs currently used in clinic. Therefore, we consider aloperine derivatives to be a novel class of anti-HCV agents, and compound II has been selected as a promising antiviral candidate for further investigation. In the experimental materials used by the author, we found 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

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

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

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

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