Tag: 325.34

Yang, Tao et al. published their research in Journal of Medicinal Chemistry in 2019 | CAS: 154590-34-8

tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate (cas: 154590-34-8) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Piperazine is an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines.Safety of tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate

Discovery of Potent and Orally Effective Dual Janus Kinase 2/FLT3 Inhibitors for the Treatment of Acute Myelogenous Leukemia and Myeloproliferative Neoplasms was written by Yang, Tao;Hu, Mengshi;Qi, Wenyan;Yang, Zhuang;Tang, Minghai;He, Jun;Chen, Yong;Bai, Peng;Yuan, Xue;Zhang, Chufeng;Liu, Kongjun;Lu, Yulin;Xiang, Mingli;Chen, Lijuan. And the article was included in Journal of Medicinal Chemistry in 2019.Safety of tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate This article mentions the following:

Herein, the design, synthesis, and structure-activity relationships of a series of unique 4-(1H-pyrazol-4-yl)-pyrimidin-2-amine derivatives that selectively inhibit Janus kinase 2 (JAK2) and FLT3 kinases is described. These screening cascades revealed that I was a preferred compound with IC50 values of 0.7 and 4 nM for JAK2 and FLT3, resp. Moreover, I was a potent JAK2 inhibitor with 37-fold and 56-fold selectivity over JAK1 and JAK3, resp., and possessed an excellent selectivity profile over the other 100 representative kinases. In a series of cytokine-stimulated cell-based assays, I exhibited a higher JAK2 selectivity over other JAK isoforms. The oral administration of 60 mg/kg of I could significantly inhibit tumor growth, with a tumor growth inhibition rate of 93 and 85% in MV4-11 and SET-2 xenograft models, resp. Addnl., I showed an excellent bioavailability (F = 58%), a suitable half-life time (T1/2 = 4.1 h), a satisfactory metabolic stability, and a weak CYP3A4 inhibitory activity, suggesting that I might be a potential drug candidate for JAK2-driven myeloproliferative neoplasms and FLT3-internal tandem duplication-driven acute myelogenous leukemia. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate (cas: 154590-34-8Safety of tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate).

tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate (cas: 154590-34-8) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Piperazine is an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines.Safety of tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate

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

Patel, Kavitkumar N. et al. published their research in European Journal of Medicinal Chemistry in 2014 | CAS: 154590-34-8

tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate (cas: 154590-34-8) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.Formula: C15H20FN3O4

Design, synthesis and antitubercular evaluation of novel series of N-[4-(piperazin-1-yl)phenyl]cinnamamide derivatives was written by Patel, Kavitkumar N.;Telvekar, Vikas N.. And the article was included in European Journal of Medicinal Chemistry in 2014.Formula: C15H20FN3O4 This article mentions the following:

The analogs of N-[4-(piperazin-1-yl)phenyl]cinnamamide were designed and synthesized by a mol. hybridization approach in which part C of the designed mol. was linked through amide and carbamate functionality that improves the physicochem. properties and govern the pharmacokinetic and pharmacodynamic behavior. The systematic modification was done around the Part C to explore the structure activity relationship of antitubercular cinnamamides. All 52 compounds were evaluated for antitubercular activity against Mycobacterium tuberculosis (M. tb) using Resazurin microtitre plate assay (REMA). Compound I with trifluoromethyl substitution exhibited good antitubercular activity of 3.125 渭g/mL. The synthesized N-[4-(piperazin-1-yl)phenyl]cinnamamide derivatives showed promising activity against M. tb. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate (cas: 154590-34-8Formula: C15H20FN3O4).

tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate (cas: 154590-34-8) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.Formula: C15H20FN3O4

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

Bao, Jiyin et al. published their research in Bioorganic Chemistry in 2020 | CAS: 154590-34-8

tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate (cas: 154590-34-8) belongs to piperazine derivatives. The piperazine scaffold is often found in biologically active compounds in different therapeutic areas. These therapeutic areas include antifungals, antidepressants, antivirals, and serotonin receptor (5-HT) antagonists/agonists. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.Recommanded Product: tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate

Discovery of benzo[d]oxazole derivatives as the potent type-I FLT3-ITD inhibitors was written by Bao, Jiyin;Liu, Haichun;Zhi, Yanle;Yang, Wenqianzi;Zhang, Jiawei;Lu, Tao;Wang, Yue;Lu, Shuai. And the article was included in Bioorganic Chemistry in 2020.Recommanded Product: tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate This article mentions the following:

A series of compounds I [R1 = H, Me, F, MeO; R2 = diethylamino, piperidinyl, piperazin-1-yl, etc.; R3 = Ph, pyridin-3-yl, pyridin-4-yl, etc.] were designed and synthesized based on benzo[d]oxazole-2-amine scaffold to discover new potent Fms-like tyrosine kinase 3 inhibitors. During the medicinal chem. works, flexible mol. docking was used to provide design rationale and study the binding modes of the target compounds Through the mixed SAR exploration based on the enzymic and cellular activities, compound I [R1 = MeO; R2 = piperazin-1-yl; R3 = 3-carbamoylphenyl] was identified with potent FLT3-ITD inhibitory (IC50: 0.41 nM) and anti-proliferative (IC50: 0.037渭M against MV4-11 cells) activities. And the binding mode of I [R1 = MeO; R2 = piperazin-1-yl; R3 = 3-carbamoylphenyl] with ”DFG-in” FLT3 was simulated by a 20-ns mol. dynamics run, providing some insights into further medicinal chem. efforts toward novel FLT3 inhibitors in AML therapy. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate (cas: 154590-34-8Recommanded Product: tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate).

tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate (cas: 154590-34-8) belongs to piperazine derivatives. The piperazine scaffold is often found in biologically active compounds in different therapeutic areas. These therapeutic areas include antifungals, antidepressants, antivirals, and serotonin receptor (5-HT) antagonists/agonists. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.Recommanded Product: tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate

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

Patel, Kavitkumar N. et al. published their research in European Journal of Medicinal Chemistry in 2014 | CAS: 154590-34-8

tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate (cas: 154590-34-8) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.Formula: C15H20FN3O4

Design, synthesis and antitubercular evaluation of novel series of N-[4-(piperazin-1-yl)phenyl]cinnamamide derivatives was written by Patel, Kavitkumar N.;Telvekar, Vikas N.. And the article was included in European Journal of Medicinal Chemistry in 2014.Formula: C15H20FN3O4 This article mentions the following:

The analogs of N-[4-(piperazin-1-yl)phenyl]cinnamamide were designed and synthesized by a mol. hybridization approach in which part C of the designed mol. was linked through amide and carbamate functionality that improves the physicochem. properties and govern the pharmacokinetic and pharmacodynamic behavior. The systematic modification was done around the Part C to explore the structure activity relationship of antitubercular cinnamamides. All 52 compounds were evaluated for antitubercular activity against Mycobacterium tuberculosis (M. tb) using Resazurin microtitre plate assay (REMA). Compound I with trifluoromethyl substitution exhibited good antitubercular activity of 3.125 μg/mL. The synthesized N-[4-(piperazin-1-yl)phenyl]cinnamamide derivatives showed promising activity against M. tb. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate (cas: 154590-34-8Formula: C15H20FN3O4).

tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate (cas: 154590-34-8) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.Formula: C15H20FN3O4

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

Bao, Jiyin et al. published their research in Bioorganic Chemistry in 2020 | CAS: 154590-34-8

tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate (cas: 154590-34-8) belongs to piperazine derivatives. The piperazine scaffold is often found in biologically active compounds in different therapeutic areas. These therapeutic areas include antifungals, antidepressants, antivirals, and serotonin receptor (5-HT) antagonists/agonists. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.Recommanded Product: tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate

Discovery of benzo[d]oxazole derivatives as the potent type-I FLT3-ITD inhibitors was written by Bao, Jiyin;Liu, Haichun;Zhi, Yanle;Yang, Wenqianzi;Zhang, Jiawei;Lu, Tao;Wang, Yue;Lu, Shuai. And the article was included in Bioorganic Chemistry in 2020.Recommanded Product: tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate This article mentions the following:

A series of compounds I [R1 = H, Me, F, MeO; R2 = diethylamino, piperidinyl, piperazin-1-yl, etc.; R3 = Ph, pyridin-3-yl, pyridin-4-yl, etc.] were designed and synthesized based on benzo[d]oxazole-2-amine scaffold to discover new potent Fms-like tyrosine kinase 3 inhibitors. During the medicinal chem. works, flexible mol. docking was used to provide design rationale and study the binding modes of the target compounds Through the mixed SAR exploration based on the enzymic and cellular activities, compound I [R1 = MeO; R2 = piperazin-1-yl; R3 = 3-carbamoylphenyl] was identified with potent FLT3-ITD inhibitory (IC50: 0.41 nM) and anti-proliferative (IC50: 0.037μM against MV4-11 cells) activities. And the binding mode of I [R1 = MeO; R2 = piperazin-1-yl; R3 = 3-carbamoylphenyl] with ”DFG-in” FLT3 was simulated by a 20-ns mol. dynamics run, providing some insights into further medicinal chem. efforts toward novel FLT3 inhibitors in AML therapy. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate (cas: 154590-34-8Recommanded Product: tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate).

tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate (cas: 154590-34-8) belongs to piperazine derivatives. The piperazine scaffold is often found in biologically active compounds in different therapeutic areas. These therapeutic areas include antifungals, antidepressants, antivirals, and serotonin receptor (5-HT) antagonists/agonists. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.Recommanded Product: tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate

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

Patel, Kavitkumar N. et al. published their research in European Journal of Medicinal Chemistry in 2014 | CAS: 154590-34-8

tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate (cas: 154590-34-8) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.Formula: C15H20FN3O4

Design, synthesis and antitubercular evaluation of novel series of N-[4-(piperazin-1-yl)phenyl]cinnamamide derivatives was written by Patel, Kavitkumar N.;Telvekar, Vikas N.. And the article was included in European Journal of Medicinal Chemistry in 2014.Formula: C15H20FN3O4 This article mentions the following:

The analogs of N-[4-(piperazin-1-yl)phenyl]cinnamamide were designed and synthesized by a mol. hybridization approach in which part C of the designed mol. was linked through amide and carbamate functionality that improves the physicochem. properties and govern the pharmacokinetic and pharmacodynamic behavior. The systematic modification was done around the Part C to explore the structure activity relationship of antitubercular cinnamamides. All 52 compounds were evaluated for antitubercular activity against Mycobacterium tuberculosis (M. tb) using Resazurin microtitre plate assay (REMA). Compound I with trifluoromethyl substitution exhibited good antitubercular activity of 3.125 μg/mL. The synthesized N-[4-(piperazin-1-yl)phenyl]cinnamamide derivatives showed promising activity against M. tb. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate (cas: 154590-34-8Formula: C15H20FN3O4).

tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate (cas: 154590-34-8) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.Formula: C15H20FN3O4

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

Bao, Jiyin et al. published their research in Bioorganic Chemistry in 2020 | CAS: 154590-34-8

tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate (cas: 154590-34-8) belongs to piperazine derivatives. The piperazine scaffold is often found in biologically active compounds in different therapeutic areas. These therapeutic areas include antifungals, antidepressants, antivirals, and serotonin receptor (5-HT) antagonists/agonists. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.Recommanded Product: tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate

Discovery of benzo[d]oxazole derivatives as the potent type-I FLT3-ITD inhibitors was written by Bao, Jiyin;Liu, Haichun;Zhi, Yanle;Yang, Wenqianzi;Zhang, Jiawei;Lu, Tao;Wang, Yue;Lu, Shuai. And the article was included in Bioorganic Chemistry in 2020.Recommanded Product: tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate This article mentions the following:

A series of compounds I [R1 = H, Me, F, MeO; R2 = diethylamino, piperidinyl, piperazin-1-yl, etc.; R3 = Ph, pyridin-3-yl, pyridin-4-yl, etc.] were designed and synthesized based on benzo[d]oxazole-2-amine scaffold to discover new potent Fms-like tyrosine kinase 3 inhibitors. During the medicinal chem. works, flexible mol. docking was used to provide design rationale and study the binding modes of the target compounds Through the mixed SAR exploration based on the enzymic and cellular activities, compound I [R1 = MeO; R2 = piperazin-1-yl; R3 = 3-carbamoylphenyl] was identified with potent FLT3-ITD inhibitory (IC50: 0.41 nM) and anti-proliferative (IC50: 0.037μM against MV4-11 cells) activities. And the binding mode of I [R1 = MeO; R2 = piperazin-1-yl; R3 = 3-carbamoylphenyl] with ”DFG-in” FLT3 was simulated by a 20-ns mol. dynamics run, providing some insights into further medicinal chem. efforts toward novel FLT3 inhibitors in AML therapy. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate (cas: 154590-34-8Recommanded Product: tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate).

tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate (cas: 154590-34-8) belongs to piperazine derivatives. The piperazine scaffold is often found in biologically active compounds in different therapeutic areas. These therapeutic areas include antifungals, antidepressants, antivirals, and serotonin receptor (5-HT) antagonists/agonists. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.Recommanded Product: tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate

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