Month: November 2022

He, Qiuqin published the artcileSynthesis and antifungal activity of 1-(1H-1,2,4-triazol-1-yl)-2-(3,3-dimethyl)-3-[(4-substituted)-1-piperazinyl]-2-propanol derivatives, Name: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, the publication is Zhongguo Yaowu Huaxue Zazhi (2005), 15(5), 262-265, database is CAplus.

Antifungal activity of triazole derivatives bearing a side chain containing tert-Bu and 4-[4-(alkoxy)phenyl]-1-piperazine was studied and their antifungal activities were compared with that of fluconazole and itraconazole. According to the structure of fluconazole, ten target compounds were designed and synthesized. The target compounds thus prepared included α-(1,1-dimethylethyl)-4-[4-(pyridinylmethoxy)phenyl]-α-[(1H-1,2,4-triazolyl)methyl]-1-piperazineethanol isomers, α-(1,1-dimethylethyl)-4-[4-[(2-methylphenyl)methoxy]phenyl]-α-[(1H-1,2,4-triazolyl)methyl]-1-piperazineethanol, α-(1,1-dimethylethyl)-4-(4-ethoxyphenyl)-α-[(1H-1,2,4-triazolyl)methyl]-1-piperazineethanol, etc. The MIC₈₀ of all the target compounds were determined by the method recommended by the national committee for clin. laboratory standards (NCCLS) using the RPMI-1640 test medium. All the target compounds were firstly reported. The results of the preliminary antifungal test showed that all the target compounds had potent antifungal activities to a certain extent. The activities of four target compounds were 4 times as high as that of fluconazole and equal to that of itraconazole against Candida albicans in vitro. More hydrophobic groups can be introduced to design triazole compounds and stereochem. have important influence on the antifungal activities of the target compounds

Zhongguo Yaowu Huaxue Zazhi 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, Name: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone.

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

He, Qiu Qin published the artcileDesign, synthesis of novel antifungal triazole derivatives with high activities against Aspergillus fumigatus, Category: piperazines, the publication is Chinese Chemical Letters (2007), 18(4), 421-423, database is CAplus.

Based on the active site of Aspergillus fumigatus lanosterol 14α-demethylase (AF-CYP51), novel triazole compounds I (R = aryl) were designed. Their chem. synthesis and the antifungal activities were reported. The results showed that all the target compounds exhibited excellent activities with broad spectrum, in which I (R = 4-FC₆H₄, 4-H₂NCOC₆H₄, pyridin-4-yl) showed comparable activities against A. fumigatus to the control drug Itraconazole.

Chinese Chemical Letters 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

Siu, Tony published the artcileDiscovery of potent and cell-active allosteric dual Akt 1 and 2 inhibitors, Quality Control of 55403-35-5, the publication is Bioorganic & Medicinal Chemistry Letters (2008), 18(14), 4186-4190, database is CAplus and MEDLINE.

This paper describes the improvement of cell potency in a class of allosteric Akt 1 and 2 inhibitors. Key discoveries include identifying the solvent exposed region of the mol. and appending basic amines to enhance the physiochem. properties of the mols. Findings from the structure-activity relationships are discussed.

Bioorganic & Medicinal Chemistry Letters published new progress about 55403-35-5. 55403-35-5 belongs to piperazines, auxiliary class Pyridine,Piperazine,Amine, name is 6-(4-Methylpiperazin-1-yl)pyridin-3-amine, and the molecular formula is C9H8BNO2, Quality Control of 55403-35-5.

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

Nirantar, Saurabh R. published the artcileRapid screening of protein-protein interaction inhibitors using the protease exclusion assay, Formula: C12H16N2O2, the publication is Biosensors & Bioelectronics (2014), 250-257, database is CAplus and MEDLINE.

We have previously developed a sensitive and modular homogenous biosensor system using peptides to detect target ligands. By transposing the basic mechanistic principle of the nuclease protection assay into this biosensor framework, we have developed the protease exclusion (PE) assay which can discern antagonists of protein-protein interactions in a rapid, single-step format. We demonstrate the concept with multiple protein-peptide pairs and validate the method by successfully screening a small mol. library for compounds capable of inhibiting the therapeutically relevant p53-Mdm2 interaction. The Protease Exclusion method adds to the compendium of assays available for rapid analyte detection and is particularly suited for drug screening applications.

Biosensors & Bioelectronics 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, Formula: C12H16N2O2.

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

Diab, Sarah published the artcileUnveiling new chemical scaffolds as Mnk inhibitors, SDS of cas: 55403-35-5, the publication is Future Medicinal Chemistry (2016), 8(3), 271-285, database is CAplus and MEDLINE.

The discovery of small mols. that selectively inhibit Mnks is considered of paramount importance towards deciphering the exact role of these proteins in carcinogenesis and to further validate them as anti-cancer drug targets. However, the dearth of structural information of Mnks is a major hurdle. This study unveils the 7H-pyrrolo[2,3-d]pyrimidine derivatives as potent inhibitors of Mnks. ATP and substrate competition assays showed that this scaffold interacts with the ATP binding site, but not with the substrate site. Screened against a panel of cancer cells, Mnk inhibitors were most potent against MV4-11 acute myeloid leukemia cells. The induction of apoptosis was shown to be mediated by downregulation of Mcl-1.

Future Medicinal Chemistry published new progress about 55403-35-5. 55403-35-5 belongs to piperazines, auxiliary class Pyridine,Piperazine,Amine, name is 6-(4-Methylpiperazin-1-yl)pyridin-3-amine, and the molecular formula is C10H16N4, SDS of cas: 55403-35-5.

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

Dong, Yan published the artcileExploration of the linkage elements of porcupine antagonists led to potent Wnt signaling pathway inhibitors, Category: piperazines, the publication is Bioorganic & Medicinal Chemistry (2015), 23(21), 6855-6868, database is CAplus and MEDLINE.

The Wnt signaling pathway is a pivotal developmental pathway. It operates through control of cellular functions such as proliferation, differentiation, migration and polarity. Aberrant Wnt signaling has been implicated in the formation and metastasis of tumors. Porcupine is a component of the Wnt signaling pathway. It is a member of the membrane-bound O-acyltransferase family of proteins. Porcupine catalyzes the palmitoylation of Wnt proteins, a process which is essential to their secretion and activity. Here we report a novel series of compounds obtained by a scaffold hybridization strategy from two known porcupine inhibitor classes. The leading compound 62 demonstrated subnanomolar (IC₅₀ 0.11 nM) inhibition of Wnt signaling in a paracrine cellular reporter gene assay. Compound 62 also potently inhibited Wnt secretion into culture medium, an indication of direct inhibition of the porcupine protein. Furthermore, compound 62 showed excellent chem., plasma and liver microsomal stabilities. Collectively, these results strongly support further optimization of this novel scaffold to develop better Wnt pathway inhibitors.

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, Category: piperazines.

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

He, Qiu Qin published the artcileDesign, synthesis and molecular docking studies of novel triazole antifungal compounds, Related Products of piperazines, the publication is Chinese Chemical Letters (2007), 18(6), 663-666, database is CAplus.

Based on the active site of Candida albicans lanosterol 14α-demethylase (CACYP51), novel triazole compounds structurally different from the current triazole drugs were designed and synthesized. In vitro antifungal activities showed that compounds I (R = R¹ = Me; R = CMe₃, CN, NO₂, R¹ = H) exhibited strong activities. In addition, the first three also displayed certain activities against fluconazole-resistant fungi.

Chinese Chemical Letters 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, Related Products of piperazines.

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

Li, Xianjie published the artcileSynthetic technology of 1-acetyl-4-(4-hydroxyphenyl)piperazine, Synthetic Route of 67914-60-7, the publication is Huaxi Yaoxue Zazhi (2005), 20(3), 243-244, database is CAplus.

An important intermediate of antifungal drug ketoconazole, 1-acetyl-4-(4-hydroxyphenyl)piperazine [i.e., 1-[4-(4-hydroxyphenyl)-1-piperazinyl]ethanone], was synthesized from piperazine-6H₂O and p-chloronitrobenzene by substitution, N- acetylation with acetic anhydride, reduction with Ni/hydrazine, diazotization, and hydrolysis in the presence of Cu/Cu(NO₃)₂, and its possibility of com. use was studied. The compound was obtained with yield excelled present route. The route may be used in com. production (no data).

Huaxi Yaoxue Zazhi 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, Synthetic Route of 67914-60-7.

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

Lacivita, Enza published the artcileDetermination of 1-aryl-4-propylpiperazine pK_a values: The substituent on aryl modulates basicity, Quality Control of 178928-58-0, the publication is Bioorganic & Medicinal Chemistry (2009), 17(3), 1339-1344, database is CAplus and MEDLINE.

In order to design a potential drug, it is important to know its pK_a because the protonation state of the mol. will be critical for ligand-receptor interaction and for the pharmacokinetic of the mol. pK_a values of a series of 1-(substitutedphenyl)-4-propylpiperazines were measured to study how the presence of a substituent on the Ph ring modulates the basicity of N-4 nitrogen. pK_a values indicated that the position of the substituent was crucial. In general, the introduction of the substituent in ortho-position of the Ph ring increased the basicity of the mol. This effect appeared to be related to steric and conformational effects and not to the electronic properties of the substituent. On the other hand, meta- and para-substituted derivatives showed a slight decrease of pK_a that was qual. consistent with the electronic properties of the substituent.

Bioorganic & Medicinal Chemistry published new progress about 178928-58-0. 178928-58-0 belongs to piperazines, auxiliary class Piperazine,Nitrile,Benzene, name is 1-(3-Cyanophenyl)piperazine, and the molecular formula is C11H13N3, Quality Control of 178928-58-0.

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

Kong, Jeong-Ok published the artcileNematicidal activity of cassia and cinnamon oil compounds and related compounds toward Bursaphelenchus xylophilus (Nematoda: Parasitaphelenchidae), Recommanded Product: (E)-1-Cinnamylpiperazine, the publication is Journal of Nematology (2007), 39(1), 31-36, database is CAplus and MEDLINE.

The nematicidal activity of two cassia, Cinnamomum cassia, oils (Especial and true), four cinnamon, Cinnamomum zeylanicum, oils (tech., #500, bark and green leaf), and their compounds (e.g., trans-cinnamaldehyde and trans-cinnamic acid) toward adult Bursaphelenchus xylophilus was examined by a direct contact bioassay. Results were compared with those of 34 related compounds As judged by 24-h LC₅₀ values, two cassia oils (0.084-0.085 mg/mL) and four cinnamon oils (0.064-0.113 mg/mL) were toxic toward adult B. xylophilus. Of 45 test compounds, trans-cinnamaldehyde (0.061 mg/mL) was the most active nematicide, followed by Et cinnamate, α-methyl-trans-cinnamaldehyde, Me cinnamate and allyl cinnamate (0.114-0.195 mg/mL). Potent nematicidal activity was also observed with 4-methoxycinnamonitrile, trans-4-methoxycinnamaldehyde, trans-2-methoxycinnamaldehyde, Et α-cyanocinnamate, cinnamonitrile and cinnamyl bromide (0.224-0.502 mg/mL). Structure-activity relationships indicate that structural characteristics, such as types of functional groups, saturation and carbon skeleton, appear to play a role in determining the toxicities to adult B. xylophilus. Cassia and cinnamon oils and test compounds described merit further study as potential nematicides or leads for the control of pine wilt disease caused by B. xylophilus.

Journal of Nematology published new progress about 87179-40-6. 87179-40-6 belongs to piperazines, auxiliary class Benzenes, name is (E)-1-Cinnamylpiperazine, and the molecular formula is C13H18N2, Recommanded Product: (E)-1-Cinnamylpiperazine.

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