Category: 113534-02-4

Chen, Zimin published the artcileN-Cyanation of Primary and Secondary Amines with Cyanobenziodoxolone (CBX) Reagent, Related Products of piperazines, the publication is Chemistry – A European Journal (2021), 27(60), 14836-14840, database is CAplus and MEDLINE.

An efficient electrophilic N-cyanation of amines e.g., pyrrolidine with a stable and less-toxic 1-cyano-1,2-benziodoxol-3-(1H)-one reagent towards the synthesis of cyanamides e.g., Pyrrolidine-1-carbonitrile was disclosed. This synthetically practicable strategy allows the construction of a wide variety of cyanamides under very mild and simple conditions with a broad functional group compatibility, and showcases a huge potential in late-stage modification of complex mols.

Chemistry – A European Journal published new progress about 113534-02-4. 113534-02-4 belongs to piperazines, auxiliary class Piperazine,Nitrile,Amide, name is tert-Butyl 4-cyanopiperazine-1-carboxylate, and the molecular formula is C10H17N3O2, Related Products of piperazines.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Manojkumar, K. E. published the artcileSynthesis, characterization and biological evaluation of novel substituted acid amides containing piperazine-1,2,4-oxadiazole nucleus, Product Details of C10H17N3O2, the publication is Journal of Applicable Chemistry (Lumami, India) (2013), 2(4), 730-737, database is CAplus.

Some new (substituted)(4-{5-[3-(trifluoromethoxy)phenyl]-1,2,4-oxadiazol-3-yl}piperazin-1-yl)methanone was synthesized using piperazine containing 1,2,4-oxadiazole as core moiety with substituted acids. The newly synthesized compounds were characterized by spectroscopic evidences such as IR, ¹H NMR, ¹³C NMR and CHN elemental anal. All the synthesized compounds were screened for their in vitro antibacterial activity, some of them showed good activity.

Journal of Applicable Chemistry (Lumami, India) published new progress about 113534-02-4. 113534-02-4 belongs to piperazines, auxiliary class Piperazine,Nitrile,Amide, name is tert-Butyl 4-cyanopiperazine-1-carboxylate, and the molecular formula is C10H17N3O2, Product Details of C10H17N3O2.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Nadigar, Mohan R. published the artcileSynthesis and in vitro antibacterial activity of some novel sulfonamide derivatives bearing 1,4-disubstituted-1,2,4-oxadiazole moiety, SDS of cas: 113534-02-4, the publication is Journal of Applicable Chemistry (Lumami, India) (2013), 2(4), 722-729, database is CAplus.

A strategic synthesis of 1-[(2,5-dimethoxyphenyl)sulfonyl]-4-{5-[substituted]-1,2,4-oxadiazol-3-yl}piperazine, involves construction of 1,2,4-oxadiazole ring by intermol. condensation of tert-butyl-4-(N-hydroxycarbamimidoyl)piperazine-1-carboxylate with 3-(trifluromethoxy)benzoic acid. Structures of the newly synthesized compounds were established by IR, ¹H NMR, ¹³C NMR, LC-MS and CHNS spectroscopic evidences. All the newly synthesized compounds were tested for their in vitro antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Bacillus cereus. Tested compounds showed good antibacterial activities when compared to the reference ciprofloxacin. Five compounds showed good activity against tested organisms.

Journal of Applicable Chemistry (Lumami, India) published new progress about 113534-02-4. 113534-02-4 belongs to piperazines, auxiliary class Piperazine,Nitrile,Amide, name is tert-Butyl 4-cyanopiperazine-1-carboxylate, and the molecular formula is C10H17N3O2, SDS of cas: 113534-02-4.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Ruan, Banfeng published the artcileSynthesis and Biological Evaluation of Novel Phthalide Analogs-1,2,4-Oxadiazole Hybrids as Potential Anti-Inflammatory Agents, Formula: C10H17N3O2, the publication is Chemistry & Biodiversity (2022), 19(8), e202200039, database is CAplus and MEDLINE.

A series of novel pathalide-1,2,4-oxadiazole analogs were synthesized for discovering novel anti-inflammatory agents. After the assessment of their cytotoxicity in vitro, all compounds had been screened for their anti-inflammatory activity by evaluating their inhibitory effect on LPS-induced NO production in RAW 264.7 macrophages. SARs had been concluded, and finally compound E13 was found to be the most potent compound This compound could also significantly decrease the production of iNOS and COX-2. Preliminary mechanism studies indicated that compound E13 could inhibit the TLR4/NF-κB and ERK/p38 signaling pathways. These findings indicate that E13 holds great potential to be a lead compound for discovering novel anti-inflammatory drugs.

Chemistry & Biodiversity published new progress about 113534-02-4. 113534-02-4 belongs to piperazines, auxiliary class Piperazine,Nitrile,Amide, name is tert-Butyl 4-cyanopiperazine-1-carboxylate, and the molecular formula is C10H17N3O2, Formula: C10H17N3O2.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Kondo, Takashi published the artcileDesign and synthesis of DPP-IV inhibitors lacking the electrophilic nitrile group, Related Products of piperazines, the publication is Bioorganic & Medicinal Chemistry (2008), 16(4), 1613-1631, database is CAplus and MEDLINE.

A series of (4β-substituted)-L-prolylpyrrolidine analogs lacking the electrophilic nitrile function were synthesized and their dipeptidyl peptidase IV (DPP-IV) inhibitory activity and duration of ex vivo activity were evaluated. Structural optimization of the analog (I), which was found by high-speed analog synthesis, was carried out to improve the potency and duration of action. A representative compound (II) was evaluated to assess its effect on the plasma glucose level after the oGTT (oral glucose tolerance test) in normal rats. Structure-activity relationships (SAR) are also presented.

Bioorganic & Medicinal Chemistry published new progress about 113534-02-4. 113534-02-4 belongs to piperazines, auxiliary class Piperazine,Nitrile,Amide, name is tert-Butyl 4-cyanopiperazine-1-carboxylate, and the molecular formula is C10H17N3O2, Related Products of piperazines.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Li, Gang published the artcileThe optimization of xanthine derivatives leading to HBK001 hydrochloride as a potent dual ligand targeting DPP-IV and GPR119, SDS of cas: 113534-02-4, the publication is European Journal of Medicinal Chemistry (2020), 112017, database is CAplus and MEDLINE.

A series of xanthine compounds derived from the previous hit I with modification on the terminal side chain was discovered through ring formation strategy. Systematic optimization of the compounds with rigid heterocycles in the hydrophobic side chain led to the new lead compound HBK001 (II) with the improved DPP-IV inhibition and moderate GPR119 agonism activity in vitro. As a continuing work to further study the PK and PD profiles, II and its hydrochloride (22) were synthesized on grams scale and evaluated on the ADME/T and oral glucose tolerance test (OGTT) in ICR mice. Compound 22 showed the improved bioavailability and blood glucose-lowering effect in vivo compared to its free base 21h probably attributed to its improved solubility and permeability. The preliminary toxicity studies on compound 22 exhibited that the result of mini-Ames was neg. and the preliminary acute toxicity LD₅₀ in mice was above 1.5 g/kg, while it showed moderate inhibition on hERG channel with IC₅₀ 4.9¦ÌM maybe due to its high lipophilicity. These findings will be useful for the future drug design for more potent and safer dual ligand targeting DPP-IV and GPR119 for the treatment of diabetes.

European Journal of Medicinal Chemistry published new progress about 113534-02-4. 113534-02-4 belongs to piperazines, auxiliary class Piperazine,Nitrile,Amide, name is tert-Butyl 4-cyanopiperazine-1-carboxylate, and the molecular formula is C10H17N3O2, SDS of cas: 113534-02-4.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Kulkarni, B. published the artcileDesign, synthesis and molecular docking studies of some 1-(5-(2-fluoro-5-(trifluoromethoxy)phenyl)-1,2,4-oxadiazol-3-yl)piperazine derivatives as potential anti-inflammatory agents, Category: piperazines, the publication is Molecular Diversity, database is CAplus and MEDLINE.

The facile synthesis of a series of piperazinyl-substituted 1,2,4-oxadiazoles I (R = 4-ClC₆H₄CH₂, PhSO₂, 2-pyrazinylcarbonyl, etc.) in good to excellent yields is reported. The anti-inflammatory potential of the newly synthesized compounds was evaluated by anti-denaturation assay using diclofenac sodium as the reference standard Some of the compounds exhibited profound activity profile when compared to the standard drug. The mol. docking and SAR studies were carried out at the later stage to gain more insights about the promising activity profile of the synthesized mols.

Molecular Diversity published new progress about 113534-02-4. 113534-02-4 belongs to piperazines, auxiliary class Piperazine,Nitrile,Amide, name is tert-Butyl 4-cyanopiperazine-1-carboxylate, and the molecular formula is C10H17N3O2, Category: piperazines.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Sreenivasa, S. published the artcile(E)-tert-Butyl 4-(N’-hydroxycarbamimidoyl)piperazine-1-carboxylate, Name: tert-Butyl 4-cyanopiperazine-1-carboxylate, the publication is Acta Crystallographica, Section E: Structure Reports Online (2012), 68(12), o3347, database is CAplus and MEDLINE.

In the title compound, C₁₀H₂₀N₄O₃, the piperazine ring adopts a chair conformation. The mol. adopts an E conformation across the C=N double bond, with the -OH group and the piperazine ring trans to one another. Further, the H atom of the hydroxy group is directed away from the NH₂ group. An intramol. N-H¡¤¡¤¡¤O contact occurs involving the NH₂ group and the oxime O atom. In the crystal, mols. are linked via strong N-H¡¤¡¤¡¤O and O-H¡¤¡¤¡¤N H bonds with alternating R₂²(6) and C(9) motifs into tetrameric units forming R₄⁴(28) motifs. Crystallog. data and at. coordinates are given.

Acta Crystallographica, Section E: Structure Reports Online published new progress about 113534-02-4. 113534-02-4 belongs to piperazines, auxiliary class Piperazine,Nitrile,Amide, name is tert-Butyl 4-cyanopiperazine-1-carboxylate, and the molecular formula is C12H14O2, Name: tert-Butyl 4-cyanopiperazine-1-carboxylate.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Li, Gang published the artcileThe optimization of xanthine derivatives leading to HBK001 hydrochloride as a potent dual ligand targeting DPP-IV and GPR119, SDS of cas: 113534-02-4, the publication is European Journal of Medicinal Chemistry (2020), 112017, database is CAplus and MEDLINE.

A series of xanthine compounds derived from the previous hit I with modification on the terminal side chain was discovered through ring formation strategy. Systematic optimization of the compounds with rigid heterocycles in the hydrophobic side chain led to the new lead compound HBK001 (II) with the improved DPP-IV inhibition and moderate GPR119 agonism activity in vitro. As a continuing work to further study the PK and PD profiles, II and its hydrochloride (22) were synthesized on grams scale and evaluated on the ADME/T and oral glucose tolerance test (OGTT) in ICR mice. Compound 22 showed the improved bioavailability and blood glucose-lowering effect in vivo compared to its free base 21h probably attributed to its improved solubility and permeability. The preliminary toxicity studies on compound 22 exhibited that the result of mini-Ames was neg. and the preliminary acute toxicity LD₅₀ in mice was above 1.5 g/kg, while it showed moderate inhibition on hERG channel with IC₅₀ 4.9¦ÌM maybe due to its high lipophilicity. These findings will be useful for the future drug design for more potent and safer dual ligand targeting DPP-IV and GPR119 for the treatment of diabetes.

European Journal of Medicinal Chemistry published new progress about 113534-02-4. 113534-02-4 belongs to piperazines, auxiliary class Piperazine,Nitrile,Amide, name is tert-Butyl 4-cyanopiperazine-1-carboxylate, and the molecular formula is C10H17N3O2, SDS of cas: 113534-02-4.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Kulkarni, B. published the artcileDesign, synthesis and molecular docking studies of some 1-(5-(2-fluoro-5-(trifluoromethoxy)phenyl)-1,2,4-oxadiazol-3-yl)piperazine derivatives as potential anti-inflammatory agents, Category: piperazines, the publication is Molecular Diversity, database is CAplus and MEDLINE.

The facile synthesis of a series of piperazinyl-substituted 1,2,4-oxadiazoles I (R = 4-ClC₆H₄CH₂, PhSO₂, 2-pyrazinylcarbonyl, etc.) in good to excellent yields is reported. The anti-inflammatory potential of the newly synthesized compounds was evaluated by anti-denaturation assay using diclofenac sodium as the reference standard Some of the compounds exhibited profound activity profile when compared to the standard drug. The mol. docking and SAR studies were carried out at the later stage to gain more insights about the promising activity profile of the synthesized mols.

Molecular Diversity published new progress about 113534-02-4. 113534-02-4 belongs to piperazines, auxiliary class Piperazine,Nitrile,Amide, name is tert-Butyl 4-cyanopiperazine-1-carboxylate, and the molecular formula is C10H17N3O2, Category: piperazines.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics