Tag: 200-300

On April 12, 2018, Crew, Andrew P.; Hornberger, Keith R.; Snyder, Lawrence B.; Zimmermann, Kurt; Wang, Jing; Berlin, Michael; Crews, Craig M.; Dong, Hanqing published a patent.Category: piperazines The title of the patent was Preparation of bifunctional compounds for the targeted degradation of androgen receptor. And the patent contained the following:

The invention relates to bifunctional compounds, which find utility to degrade and (inhibit) androgen receptor. In particular, the invention is directed to compounds, which contain on one end a cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds androgen receptor, such that androgen receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of androgen receptor. The invention exhibits a broad range of pharmacol. activities associated with compounds according to the present invention, consistent with the degradation/inhibition of androgen receptor (data given). The invention compounds are claimed to be useful for the treatment of cancer or Kennedy’s disease, or both. The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).Category: piperazines

The Article related to protac modulator preparation targeted ubiquitination androgen receptor degradation inhibition, preparation bifunctional compound degradation androgen receptor, treatment cancer kennedy disease preparation bifunctional compound and other aspects.Category: piperazines

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

On September 23, 2010, Hansen, C. Henrik published a patent.Computed Properties of 890092-19-0 The title of the patent was Preparation of substituted 2-phenyl-3H-quinazolin-4-ones and analogs as antiinflammatory and cardiovascular agents. And the patent contained the following:

The invention is related to the preparation of 2-phenyl-3H-quinazolin-4-ones and analogs, e.g, 2-[4-(4-hydroxypiperidin-1-yl)phenyl]-5,7-dimethoxypyrido[2,3-d]pyrimidin-4(3H)-one (I), that are useful in regulating the expression of interleukin-6 (IL-6) and/or vascular cell adhesion mol.-1 (VCAM-1), and their use in the treatment and/or prevention of cardiovascular and inflammatory diseases and related disease states, such as atherosclerosis, asthma, arthritis, cancer, multiple sclerosis, psoriasis, and inflammatory bowel diseases, and autoimmune disease(s). Thus, cyclization of 2-amino-4,6-dimethoxynicotinamide with 4-(4-hydroxypiperidin-1-yl)benzaldehyde gave pyridopyrimidinone I which caused a ≥ 20% inhibition in IL-6 mRNA and in VCAM-1 mRNA at a concentration ≤ 10 μM. Pharmaceutical compositions containing title compounds are also disclosed. The experimental process involved the reaction of 4-(4-Acetylpiperazin-1-yl)benzaldehyde(cas: 890092-19-0).Computed Properties of 890092-19-0

The Article related to phenylquinazolinone preparation interleukin 6 proliferation inhibitor antiinflammatory cardiovascular, vascular cell adhesion mol 1 inhibitor phenylquinazolinone pyridopyrimidinone preparation and other aspects.Computed Properties of 890092-19-0

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

On February 5, 2022, Degirmencioglu, Ismail; Iren, Kubra; Yalcin, Izzet; Gol, Cem; Durmus, Mahmut published an article.Name: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was Synthesis of axially disubstituted silicon(IV) phthalocyanines and investigation of their photophysical and photochemical properties. And the article contained the following:

In this study, the axially 1-(4-(3-(6-hydroxyhexyl)-3,4-dihydro-2H-benzo[e][1,3]oxazin-6-yl)piperazin-1-yl)ethanone and 1-(4-(3-(2-(2-hydroxyethoxy)ethyl)-3,4-dihydro-2H-benzo[e][1,3]oxazin-6-yl)piperazin-1-yl)ethanone disubstituted silicon(IV) phthalocyanines and their corresponding quaternized derivatives were synthesized for the first time as candidate photosensitizers for photodynamic therapy (PDT) in cancer treatment. The structures of these novel compounds were confirmed by some spectroscopic techniques such as FT-IR, 1H NMR, 13C NMR, UV-Vis, and mass. The axially substitution increased the solubility of the silicon(IV) phthalocyanines. The prepared silicon(IV) phthalocyanines showed great results achieved from photochem. and photophys. investigations in DMSO solution Especially, high singlet oxygen and the fluorescence quantum yield values of the quaternized silicon (IV) phthalocyanines indicates that these compounds have major potential as photosensitizers in PDT. Furthermore, studied silicon(IV) phthalocyanine complexes could be classified as the stable photosensitizer in accordance with photodegradation study results. The fluorescence quenching behavior of these phthalocyanine complexes was also examined using fluorescence quenching method by 1,4-benzoquinone (BQ). The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Name: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

The Article related to silicon phthalocyanine disubstituted axial preparation photophys photochem property, fluorescence quenching solubility absorbance photolysis silicon phthalocyanine disubstituted axial and other aspects.Name: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

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

On May 10, 2018, Yu, Le-Mao; Hu, Zhu; Chen, Yu; Ravji, Azhar; Lopez, Sophia; Plescia, Caroline B.; Yu, Qian; Yang, Hui; Abdelmalak, Monica; Saha, Sourav; Agama, Keli; Kiselev, Evgeny; Marchand, Christophe; Pommier, Yves; An, Lin-Kun published an article.COA of Formula: C12H16N2O2 The title of the article was Synthesis and structure-activity relationship of furoquinolinediones as inhibitors of Tyrosyl-DNA phosphodiesterase 2 (TDP2). And the article contained the following:

Tyrosyl-DNA phosphodiesterase 2 (TDP2) is a recently discovered enzyme specifically repairing topoisomerase II (TOP2)-mediated DNA damage. It has been shown that inhibition of TDP2 synergize with TOP2 inhibitors. Herein, we report the discovery of the furoquinolinedione chemotype as a suitable skeleton for the development of selective TDP2 inhibitors. Compound 1 was identified as a TDP2 inhibitor as a result of screening our inhouse compound library for compounds selective for TDP2 vs. TDP1. Further SAR studies provide several selective TDP2 inhibitors at low-micromolar range. The most potent compound 74 shows inhibitory activity with IC50 of 1.9 and 2.1 μM against recombinant TDP2 and TDP2 in whole cell extracts (WCE), resp. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).COA of Formula: C12H16N2O2

The Article related to furoquinoline dione derivative preparation structure tyrosyl dna phosphodiesterase inhibitor, dna repair, furoquinolinedione, inhibitor, topoisomerase, tyrosyl-dna phosphodiesterase and other aspects.COA of Formula: C12H16N2O2

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

On September 27, 2017, Beyzavi, Hudson; Mandal, Debashis; Strebl, Martin G.; Neumann, Constanze N.; D’Amato, Erica M.; Chen, Junting; Hooker, Jacob M.; Ritter, Tobias published an article.Formula: C12H16N2O2 The title of the article was 18F-Deoxyfluorination of Phenols via Ru π-Complexes. And the article contained the following:

The deficiency of robust and practical methods for 18F-radiofluorination is a bottleneck for positron emission tomog. (PET) tracer development. Here, we report the first transition-metal-assisted 18F-deoxyfluorination of phenols. The transformation benefits from readily available phenols as starting materials, tolerance of moisture and ambient atm., large substrate scope, and translatability to generate doses appropriate for PET imaging. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Formula: C12H16N2O2

The Article related to transition metal assisted deoxyfluorination phenol ruthenium complex, crystal mol structure fluorophenyl ruthenium cyclopentenyl complex, radiofluorination phenol ruthenium complex and other aspects.Formula: C12H16N2O2

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

On October 31, 1980, Carissimi, M.; Picciola, G.; Ravenna, F.; Carenini, G.; Gentili, P. published an article.Computed Properties of 59695-29-3 The title of the article was 2-(2-Thienyl)morpholines active on the central nervous system. And the article contained the following:

Morpholinones I [R = H, PhCH2, CHMe2, substituted 3-(1-piperazinyl)propionyl, substituted 3-(1-piperazinyl)propyl; Z = O] underwent LiAlH4 reduction to yield I (Z = H2), which showed antidepressant activity. Cyclocondensation of 2-benzylamin-1-(2-thienyl)ethanol with ClCH2COCl gave I (R = PhCH2, Z = 0). The experimental process involved the reaction of 3-(4-Methylpiperazin-1-yl)propanoic acid dihydrochloride(cas: 59695-29-3).Computed Properties of 59695-29-3

The Article related to morpholine thienyl preparation antidepressant, thienylmorpholine preparation antidepressant, analgesic thienylmorpholine preparation, antiinflammatory thienylmorpholine preparation and other aspects.Computed Properties of 59695-29-3

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

On November 1, 2015, Dong, Yan; Li, Kehuang; Xu, Zhixiang; Ma, Haikuo; Zheng, Jiyue; Hu, Zhilin; He, Sudan; Wu, Yiyuan; Sun, Zhijian; Luo, Lusong; Li, Jiajun; Zhang, Hongjian; Zhang, Xiaohu published an article.Category: piperazines The title of the article was Exploration of the linkage elements of porcupine antagonists led to potent Wnt signaling pathway inhibitors. And the article contained the following:

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. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Category: piperazines

The Article related to protein palmitoyltransferase porcupine antagonist synthesis inhibitor wnt signaling secretion, antagonist, cancer therapy, porcupine, scaffold hybridization, wnt signaling pathway and other aspects.Category: piperazines

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

On June 30, 2004, Liu, Chaomei; Xu, Fan; Liang, Shuang; Sun, Qingyan; Jiang, Yuanying published an article.HPLC of Formula: 67914-60-7 The title of the article was Synthesis and antifungal activities of 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-substituted group-2-propanols. And the article contained the following:

The title compounds 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-(4-alkyloxyphenylpiperazin-1-yl)-2-propanols, e.g. I, and 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-substituted sulfur ether-2-propanols, e.g. II, were synthesized through the reaction of an intermediate epoxide and 4-alkyloxyphenylpiperazines or substituted sulfur alcs. The structures were confirmed by the elementary anal., 1H-MR and IR spectra. MIC80 of all the title compounds were determined by the method recommended by the National Committee for Clin. Laboratory Standards (NCCLS) using the RPMI1640 test medium. The results of the preliminary antifungal test show that all the title compounds exhibited potent antifungal activities to a certain extent. The antifungal activity of 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-(4-alkyloxyphenylpiperazin-1-yl)-2-propanols was more potent than that of 1-(1H,1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-substituted sulfur ether-2-propanols in vitro. The antifungal activities of the four compounds in 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-(4-alkyloxyphenylpiperazin-1-yl)-2-propanols are more potent than that of fluconazole or equal to that of ketoconazole in vitro. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).HPLC of Formula: 67914-60-7

The Article related to alkyloxyphenylpiperazinyl sulfur ether substituted triazolyl difluorophenyl propanol preparation, triazolyl difluorophenyl propanol antifungal activity fungal infection msbar and other aspects.HPLC of Formula: 67914-60-7

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

On July 7, 2022, Huo, Changxin; Wang, Hexiang; Lv, Gang; Wang, Zhiwei; Liu, Huaqing published a patent.COA of Formula: C15H29N3O2 The title of the patent was Degradation of bruton’s tyrosine kinase (BTK) by conjugation of BTK inhibitors with E3 ligase ligand and methods of use. And the patent contained the following:

Disclosed herein are novel bifunctional compounds formed by conjugating BTK inhibitor moieties with E3 ligase ligand moieties, which function to recruit targeted proteins to E3 ubiquitin ligase for degradation, and methods of preparation and uses thereof. The title compounds I [ring A and B = (independently) an aromatic ring comprising 0-3 heteroatoms selected from N, S and O as ring member(s); Z1-Z4 = (independently) N or CRz; L = (independently) a bond, alkylene, O, etc.; m, n and q = (independently) 0-4; t = 0-2; R1 and R2 = (independently) H, alkyl, cycloalkyl, etc.; R3, R5 and R6 = (independently) H, halo, alkyl, etc.; Rz = the bond between moiety and Linker-Degron moiety, H, halo, etc.; the Linker = a bond or a divalent linking group; and the Degron = E3 Ubiquitin ligase moiety] or pharmaceutically acceptable salts thereof, were prepared E.g., a multi-step synthesis of II, starting from 4-phenoxybenzaldehyde and 4-methylbenzenesulfonohydrazide, was described. Exemplified compounds I were evaluated for their activity as BTK degradation (data given). Pharmaceutical composition comprising compound I was disclosed. The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).COA of Formula: C15H29N3O2

The Article related to bifunctional compound preparation bruton’s tyrosine kinase btk degradation, targeted protein degrader btk e3 ubiquitin ligase bifunctional compound, btk inhibitor e3 ligase conjugation bifunctional compound preparation and other aspects.COA of Formula: C15H29N3O2

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

On July 15, 2020, Ramesh, Deepthi; Joji, Annu; Vijayakumar, Balaji Gowrivel; Sethumadhavan, Aiswarya; Mani, Maheswaran; Kannan, Tharanikkarasu published an article.SDS of cas: 67914-60-7 The title of the article was Indole chalcones: Design, synthesis, in vitro and in silico evaluation against Mycobacterium tuberculosis. And the article contained the following:

Indole chalcones were designed and synthesized as a promising set of compounds against H37Rv strain of Mycobacterium tuberculosis. Within this library of compounds, (E)-1-(furan-3-yl)-3-(1H-indol-3-yl)prop-2-en-1-one (18), (E)-3-(1H-indol-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one (20) and (E)-2-((1H-indol-2-yl)methylene)cyclopentan-1-one (24) displayed high anti-tubercular activity at 50 μg/mL with MIC values of 210, 197 and 236 μM resp. The in-silico studies revealed that compound 18 exhibit binding modes similar to FAS-II inhibitors like INH or Thiolactomycin against KasA protein. Cytotoxicity assay results suggest that the compounds 18, 20 and 24 are non-cytotoxic to human megakaryocytes and murine B cells. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).SDS of cas: 67914-60-7

The Article related to indole chalcones tuberculostatics mycobacterium, anti-tubercular, cytotoxicity, h(37)rv strain, indole chalcones, kasa protein, luciferase reporter mycobacteriophages (lrp), mycobacterium tuberculosis, sars and other aspects.SDS of cas: 67914-60-7

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