Category: 534615-34-4

Recommanded Product: 1-(Isopropylsulfonyl)piperazineOn September 28, 2017 ,《Structure-Activity Relationships of Potent, Targeted Covalent Inhibitors That Abolish Both the Transamidation and GTP Binding Activities of Human Tissue Transglutaminase》 was published in Journal of Medicinal Chemistry. The article was written by Akbar, Abdullah; McNeil, Nicole M. R.; Albert, Marie R.; Ta, Viviane; Adhikary, Gautam; Bourgeois, Karine; Eckert, Richard L.; Keillor, Jeffrey W.. The article contains the following contents:

Human tissue transglutaminase (hTG2) is a multifunctional enzyme. It is primarily known for its calcium-dependent transamidation activity that leads to formation of an isopeptide bond between glutamine and lysine residues found on the surface of proteins, but it is also a GTP binding protein. Overexpression and unregulated hTG2 activity have been associated with numerous human diseases, including cancer stem cell survival and metastatic phenotype. Herein, the authors present a series of targeted covalent inhibitors (TCIs) based on the previously reported Cbz-Lys scaffold. From this structure-activity relationship (SAR) study, novel irreversible inhibitors were identified that block the transamidation activity of hTG2 and allosterically abolish its GTP binding ability with a high degree of selectivity and efficiency (kinact/KI > 105 M-1 min-1). One optimized inhibitor (VA4) was also shown to inhibit epidermal cancer stem cell invasion with an EC50 of 3.9 μM, representing a significant improvement over the previously reported “”hit”” NC9. After reading the article, we found that the author used 1-(Isopropylsulfonyl)piperazine(cas: 534615-34-4Recommanded Product: 1-(Isopropylsulfonyl)piperazine)

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.Recommanded Product: 1-(Isopropylsulfonyl)piperazine

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

Scapecchi, Serena; Martini, Elisabetta; Manetti, Dina; Ghelardini, Carla; Martelli, Cecilia; Dei, Silvia; Galeotti, Nicoletta; Guandalini, Luca; Romanelli, Maria Novella; Teodori, Elisabetta published an article in Bioorganic & Medicinal Chemistry. The title of the article was 《Structure-activity relationship studies on unifiram (DM232) and sunifiram (DM235), two novel and potent cognition enhancing drugs》.Safety of 1-(Isopropylsulfonyl)piperazine The author mentioned the following in the article:

Structure-activity relationships on two novel potent cognition enhancing drugs, unifiram and sunifiram, are reported. Although none of the compounds synthesized reached the potency of the parent drugs, some fairly active compounds have been identified that may represent new leads to develop other cognition enhancing drugs. An interesting result of this research is the identification of two compounds that are endowed with amnesing activity (the opposite of the activity of the original mols.) and are nearly equipotent to scopolamine. Moreover, two other compounds of the series were found endowed with analgesic activity on a rat model of neuropathic pain at the dose of 1 mg/kg. In the experimental materials used by the author, we found 1-(Isopropylsulfonyl)piperazine(cas: 534615-34-4Safety of 1-(Isopropylsulfonyl)piperazine)

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.Safety of 1-(Isopropylsulfonyl)piperazine

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

《2,5-Disubstituted pyridines as potent GPR119 agonists》 was written by Wu, Yulin; Kuntz, Judith D.; Carpenter, Andrew J.; Fang, Jing; Sauls, Howard R.; Gomez, Daniel J.; Ammala, Carina; Xu, Yun; Hart, Shane; Tadepalli, Sarva. Electric Literature of C7H16N2O2S And the article was included in Bioorganic & Medicinal Chemistry Letters on April 15 ,2010. The article conveys some information:

A series of 2-piperazinyl-5-alkoxypyridines were synthesized and screened against human GPR119 receptor. Through SAR anal., compounds containing 2-alkylsulfonylpiperazinyl-5-alkoxypyridines were discovered and found to be potent agonists of the human GPR119 receptor. The experimental process involved the reaction of 1-(Isopropylsulfonyl)piperazine(cas: 534615-34-4Electric Literature of C7H16N2O2S)

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.Electric Literature of C7H16N2O2S

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

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