Category: piperazines

Johnson, Mark published the artcileStructure-Activity Relationship Study of N⁶-(2-(4-(1H-Indol-5-yl)piperazin-1-yl)ethyl)-N⁶-propyl-4,5,6,7-tetrahydrobenzo[d]thiazole-2,6-diamine Analogues: Development of Highly Selective D3 Dopamine Receptor Agonists along with a Highly Potent D2/D3 Agonist and Their Pharmacological Characterization [Erratum to document cited in CA157:094154], Recommanded Product: tert-Butyl 4-(2-oxoethyl)piperazine-1-carboxylate, the publication is Journal of Medicinal Chemistry (2013), 56(2), 589-590, database is CAplus and MEDLINE.

On page 5826, the abstract contained an incorrect structure; the corrected structure is given. On page 5828, Scheme 2 contained several incorrect structures; the corrected scheme is given. Corrected elemental anal. and mass spectrometry data are given for the Supporting Information and Table 1.

Journal of Medicinal Chemistry published new progress about 945953-41-3. 945953-41-3 belongs to piperazines, auxiliary class Piperazine,Amide,Aldehyde, name is tert-Butyl 4-(2-oxoethyl)piperazine-1-carboxylate, and the molecular formula is C11H20N2O3, Recommanded Product: tert-Butyl 4-(2-oxoethyl)piperazine-1-carboxylate.

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

Modi, Gyan published the artcileStructural Modifications of Neuroprotective Anti-Parkinsonian (-)-N6-(2-(4-(Biphenyl-4-yl)piperazin-1-yl)-ethyl)-N6-propyl-4,5,6,7-tetrahydrobenzo[d]thiazole-2,6-diamine (D-264): An Effort toward the Improvement of in Vivo Efficacy of the Parent Molecule, Related Products of piperazines, the publication is Journal of Medicinal Chemistry (2014), 57(4), 1557-1572, database is CAplus and MEDLINE.

In our overall goal to develop multifunctional dopamine D₂/D₃ agonist drugs for the treatment of Parkinson’s disease (PD), we previously synthesized potent D₃ preferring agonist D-264 (1a), which exhibited neuroprotective properties in two animal models of PD. To enhance the in vivo efficacy of 1a, a structure-activity relationship study was carried out. Competitive binding and [³⁵S]GTPγS functional assays identified compound (-)-9b as one of the lead mols. with preferential D₃ agonist activity (EC₅₀(GTPγS); D₃ = 0.10 nM; D₂/D₃ (EC₅₀): 159). Compounds (-)-9b and (-)-8b exhibited high in vivo activity in two PD animal models, reserpinized and 6-hydroxydopamine (OHDA)-induced unilateral lesioned rats. On the other hand, 1a failed to show any in vivo activity in these models unless the compound was dissolved in 5-10% beta-hydroxy Pr cyclodextrin solution Lead compounds exhibited appreciable radical scavenging activity. In vitro experiments with dopaminergic MN9D cells indicated neuroprotection by both 1a and (-)-9b from toxicity of MPP+.

Journal of Medicinal Chemistry published new progress about 180698-19-5. 180698-19-5 belongs to piperazines, auxiliary class Piperazine,Benzene, name is 1-Biphenyl-4-yl-piperazine, and the molecular formula is C16H18N2, Related Products of piperazines.

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

Meddad-Belhabich, Nadia published the artcileDesign of new potent and selective secretory phospholipase A₂ inhibitors. 6-Synthesis, structure-activity relationships and molecular modelling of 1-substituted-4-[4,5-dihydro-1,2,4-(4H)-oxadiazol-5-one-3-yl(methyl)]-functionalized aryl piperazin/one/dione derivatives, Computed Properties of 67914-60-7, the publication is Bioorganic & Medicinal Chemistry (2010), 18(10), 3588-3600, database is CAplus and MEDLINE.

The group IIA human non-pancreatic secretory phospholipase A₂ (hnp-sPLA₂) is one of the enzymes implied in the inflammatory process. In the course of our work on inhibitors of this enzyme we investigated the influence of rigidity of the piperazine region on the biol. activity. Several modifications were explored. Various linkers, such as amide, urea, carbamate, or alkoxyphenyl were inserted between the piperazine and the lipophilic chain. Also, modification of the piperazine core to incorporate carbonyl groups was studied. In an in vitro fluorimetric assay using the human GIIA (HPLA₂) and porcine pancreatic GIB enzymes, compound 60a (I) had the optimal activity with an IC₅₀ = 30 nM on HPLA₂. By means of mol. modeling we attempted to get informations towards comprehension of differences in activity.

Bioorganic & Medicinal Chemistry published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C12H16N2O2, Computed Properties of 67914-60-7.

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

Stefancich, Giorgio published the artcileAntibacterial and antifungal agents. XV. Synthesis and antifungal activity of structural analogs of bifonazole and ketoconazole, SDS of cas: 67914-60-7, the publication is Archiv der Pharmazie (Weinheim, Germany) (1992), 325(11), 687-94, database is CAplus and MEDLINE.

The synthesis and antifungal activities of the cis– and trans-1-acetyl-4-{4-[[2-(1,1′-biphenyl-4-yl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl}piperazines I are reported. Stereochem. assignments to diastereomeric pairs of cis/trans isomers were made on the basis of ¹H and ¹³C NMR data. Among test derivatives the best activity was shown by the benzoyl esters of the cis– and trans-[2-(1,1′-biphenyl-4-yl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methanols II (R = H, SO₂CH₃).

Archiv der Pharmazie (Weinheim, Germany) published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C7H7IN2O, SDS of cas: 67914-60-7.

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

Goodarzi, Hassan published the artcileElectrochemical Synthesis of a New Derivative of 1,4-Dihydroxybenzene: Embedded Nucleophile in the Structure of Electrophile, SDS of cas: 67914-60-7, the publication is Journal of the Electrochemical Society (2018), 165(10), H667-H672, database is CAplus.

The electrochem. oxidation of 4-(Piperazin-1-yl)phenols (1a,b) was studied in the H₂O, MeCN and nitromethan by cyclic voltammetry and controlled-potential coulometry. P-quinone-imines generated of oxidation 4-(Piperazin-1-yl)phenols after the hydrolysis reaction participate in Michael-addition reactions with released piperazine of hydrolysis reaction of p-quinone imines. The present work led to the development of a facile and environmentally friendly electrochem. method for the synthesis of a new derivative of 1,4-dihydroxybenzene under green conditions. The effect of H₂O as a solute on the electrochem. response of 4-(Piperazin-1-yl)phenols (1a,b) was examined in the MeCN (AN) and nitromethane (NM) solvent.

Journal of the Electrochemical Society published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C12H16N2O2, SDS of cas: 67914-60-7.

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

Ariawan, Daryl published the artcileThe nature of diamino linker and halogen bonding define selectivity of pyrrolopyrimidine-based LIMK1 Inhibitors, Name: (S)-N-(3-Bromophenyl)-N’-cyano-2-methyl-4-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperazine-1-carboximidamide, the publication is Frontiers in Chemistry (Lausanne, Switzerland) (2021), 781213, database is CAplus and MEDLINE.

The LIM-domain kinase (LIMK) family consists of two isoforms, LIMK1 and LIMK2, which are highly homologous, making selective inhibitor development challenging. LIMK regulates dynamics of the actin cytoskeleton, thereby impacting many cellular functions including cell morphol. and motility. Here, we designed and synthesized analogs of a known pyrrolopyrimidine LIMK inhibitor with moderate selectivity for LIMK1 over LIMK2 to gain insights into which features contribute to both activity and selectivity. We incorporated a different stereochem. around a cyclohexyl central moiety to achieve better selectivity for different LIMK isoforms. Inhibitory activity was assessed by kinase assays, and biol. effects in cells were determined using an in vitro wound closure assay. Interestingly, a slight change in stereochem. alters LIMK isoform selectivity. Finally, a docking study was performed to predict how the new compounds interact with the target.

Frontiers in Chemistry (Lausanne, Switzerland) published new progress about 1116571-01-7. 1116571-01-7 belongs to piperazines, auxiliary class Other Aromatic Heterocyclic,Piperazine,Chiral,Nitrile,Bromide,Carbamidine,Amine,Benzene, name is (S)-N-(3-Bromophenyl)-N’-cyano-2-methyl-4-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperazine-1-carboximidamide, and the molecular formula is C20H21BrN8, Name: (S)-N-(3-Bromophenyl)-N’-cyano-2-methyl-4-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperazine-1-carboximidamide.

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

Heeres, J. published the artcileAntimycotic azoles. 7. Synthesis and antifungal properties of a series of novel triazol-3-ones, Category: piperazines, the publication is Journal of Medicinal Chemistry (1984), 27(7), 894-900, database is CAplus and MEDLINE.

The antifungal triazolone derivatives I [R = H, Me, Q (X = N, CH); R¹ = H, alkyl; R² = H, Me) were prepared by a multistep sequence from 1-(p-methoxyphenyl)piperazine or MeSO₃Q via piperazines III (R³ = H, Bz) and cyclization of III [R³ = C(:NH)NH₂] with R²C(:NH)NH₂. In vitro and in vivo antifungal properties of I are reported. Compound I [R = Q (X = N), R¹ = MeEtCH, R² = H], which displays a pronounced oral activity against vaginal candidosis in rats and against microsporosis in guinea pigs, was selected for clin. evaluation.

Journal of Medicinal Chemistry published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C12H16N2O2, Category: piperazines.

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