Tag: 200-300

On October 31, 2005, He, Qiuqin; Liu, Chaomei; Men, Xiufeng; Zhao, Jingxia published an article.Electric Literature of 67914-60-7 The title of the article was Synthesis and antifungal activity of 1-(1H-1,2,4-triazol-1-yl)-2-(3,3-dimethyl)-3-[(4-substituted)-1-piperazinyl]-2-propanol derivatives. And the article contained the following:

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

The Article related to butyl triazole antifungal activity, piperazineethanol pyridinylmethoxy phenyl triazolylmethyl preparation antifungal agent, triazolylmethyl alkoxyphenylmethyl piperazineethanol preparation antifungal agent and other aspects.Electric Literature of 67914-60-7

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

On May 31, 2020, Nadaf, Afra Quasar A.; Najare, Mahesh S.; Garbhagudi, Manjunatha; Mantur, Shivaraj; Sunagar, Manjunath G.; Gaonkar, Supreet; Joshi, Shrinivas; Khazi, Imtiyaz Ahmed M. published an article.Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was Synthesis of 6-[4-(4-Propoxyphenyl)piperazin-1-yl]-9H-purine Derivatives as Antimycobacterial and Antifungal Agents: In Vitro Evaluation and In Silico Study. And the article contained the following:

A series of novel alkyl substituted purines were synthesized. 6-[4-(4-Propoxyphenyl)piperazin-1-yl]-9H-purine was used as the key starting material, which was synthesized via a multistep protocol and finally subjected for N-alkylation with various alkyl halides with an aim to get prospective antimicrobial agents. The structures of the novel compounds were established by substantiating them through spectral techniques like 1H-NMR, 13C-NMR, FT-IR and EI-MS. They were explored for antitubercular activity against Mycobacterium tuberculosis H37RV. Furthermore, they were checked for their antimicrobial activity concerning bacterial and fungal strains. The title compounds exhibited considerable antimicrobial activity without any significant toxicity. In silico studies depicted their good binding profile against Mycobacterium tuberculosis enoyl reductase (InhA; PDB ID: 4TZK) and Candida albicans dihydrofolate reductase (PDB ID: 1AI9). The title compounds obeyed Lipinski’s parameters and have exhibited good drug-like properties. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

The Article related to propoxyphenyl piperazinyl purine preparation antimicrobial antibacterial antifungal, mycobacterium tuberculosis, docking study, antimicrobial activity, antitubercular activity, propoxyphenylpiperazin-1-yl and other aspects.Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

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

On April 30, 2004, Liang, Shuang; Liu, Chaomei; Jin, Yongsheng; He, Qiuqin published an article.Formula: C12H16N2O2 The title of the article was Synthesis and antifungal activity of 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-[(4-substituted)-1-piperazinyl]-2-propanols. And the article contained the following:

The effect of the side chain in (4-substituted)-1-piperazinyl on the antifungal activity of fluconazole compounds was studied. Thirteen title compounds were synthesized and confirmed by the elementary anal., 1H-NMR and IR spectra. The MICs 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 showed that all the title compounds exhibited potent antifungal activities. The activities of the eight compounds thus prepared were more than 4 times as high as that of fluconazole and equal to that of ketoconazole against Candida albicans in vitro. The lipid/water distribution coefficient and stereochem. have important influence on the antifungal activities of the title compounds 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 triazole piperazine difluorophenyl preparation antifungal agent, lipid water distribution coefficient stereochem antifungal, structure activity fungicidal triazole piperazine difluorophenyl preparation and other aspects.Formula: C12H16N2O2

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

On December 21, 2012, Amani, Amene; Nematollahi, Davood published an article.Name: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was Electrochemical Synthesis Based on the Oxidation of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone in the Presence of Nucleophiles. And the article contained the following:

Electrochem. oxidation of piperazinylphenol I (R = R1 = H) with 2-benzoxazolethiol or 2-benzothiazolethiol yielded the bis(benzoxazolethiyl)phenol I (R = R1 = 2-benzoxazolylthio) and bis(benzothiazolethiyl)phenol I (R = R1 = 2-benzothiazolylthio) in 87% and 93% yields, resp. Further electrochem. oxidation of I (R = R1 = 2-benzothiazolylthio) in the presence of p-toluenesulfinic acid (TsH) gave (tosyl)(benzothiazolylthio)quinone II (Ts = 4-MeC6H4SO2); attempted direct electrochem. synthesis of II from I (R = R1 = H), 2-benzothiazolethiol, and TsH, from I (R = R1 = 2-benzothiazolylthio) and TsH in the absence of elec. potential, and from I (R = Ts; R1 = H) and 2-benzothiazolethiol were not successful. Cyclic voltammetric measurements during the reactions of I (R = H, 2-benzothiazolylthio, Ts; R1 = H, 2-benzothiazolylthio) were used to delineate the mechanisms of formation of I (R = R1 = 2-benzothiazolylthio) and II. 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 benzothiazolylthio benzoxazolylthio piperazinylphenol electrochem preparation, toluenesulfonyl benzothiazolylthio benzoquinone chemoselective electrochem preparation, electrochem oxidation piperazinylphenol benzothiazolethiol benzoxazolethiol, toluenesulfinic acid electrochem oxidation substitution benzothiazolylthio piperazinylphenol and other aspects.Name: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

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

On October 10, 2019, Crew, Andrew P.; Hornberger, Keith R.; Wang, Jing; Dong, Hanqing; Berlin, Michael; Crews, Craig M. published a patent.SDS of cas: 1211568-27-2 The title of the patent was Preparation of bifunctional compounds as modulators of proteolysis useful for treating cancer. And the patent contained the following:

The present disclosure relates to bifunctional compounds ULM-L-PTM [the ULM = a small mol. E3 ubiquitin ligase binding moiety that binds an E3 ubiquitin ligase;the PTM = a small mol. comprising a Kirsten rat sarcoma protein (KRas) targeting moiety; the L = a bond or a chem. linking moiety connecting the ULM and the PTM] or pharmaceutically acceptable salts, enantiomers, stereoisomers, solvates, polymorphs or prodrugs thereof, which find utility as modulators of Kirsten rat sarcoma protein (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, inhibitors of apoptosis proteins (IAP) or mouse double-minute homolog 2 ligand which binds to the resp. E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. Over 500 title compounds were prepared E.g., a multi-step synthesis of I, starting from 2,2,5-trimethyl-4-oxo-3,8,11-trioxa-5-azatridecan-13-yl 4-methylbenzenesulfonate and 2-(2,6-dioxopiperidin-3-yl)-5-hydroxyisoindoline-1,3-dione, was described. The present disclosure exhibits a broad range of pharmacol. activities associated with degradation/inhibition of target protein (data given for representative title compounds). Diseases or disorders that result from aggregation, accumulation, and/or overactivation of the target protein are treated or prevented with compounds and compositions of the present disclosure. The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).SDS of cas: 1211568-27-2

The Article related to bifunctional compound preparation kras modulator antitumor e3 ubiquitin ligase, von hippel lindau cereblon protein bifunctional compound preparation antitumor, apoptosis protein inhibitor antitumor bifunctional compound quinazolinamine preparation, mouse double minute 2 homolog mdm2 bifunctional compound preparation and other aspects.SDS of cas: 1211568-27-2

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

On February 15, 2020, Sirim, Mustafa Mert; Krishna, Vagolu Siva; Sriram, Dharmarajan; Unsal Tan, Oya published an article.Product Details of 890092-19-0 The title of the article was Novel benzimidazole-acrylonitrile hybrids and their derivatives: Design, synthesis and antimycobacterial activity. And the article contained the following:

The synthesis and evaluation of some benzimidazole-acrylonitrile hybrid derivatives I [R = Me, cyclohexyl, benzyl, etc.] was described for their in-vitro antimycobacterial activities against Mycobacterium tuberculosis H37Rv. Among the derivatives studied, I [R = p-tolyl] was found to be the most active compound with MIC of 0.78μg/mL against M. tuberculosis. This was a quite good activity compared with ethambutol (MIC = 1.56μg/mL). Moreover, I [R = p-tolyl] showed 2.8 log fold reduction in bacterial count of dormant forms of mycobacterium which was more potent than first line drugs isoniazid, ciprofloxacin, rifampicin and moxifloxacin. Having activities against both active and dormant forms of M. tuberculosis, I [R = p-tolyl] may be a useful candidate for the development of new drugs to treat tuberculosis. The experimental process involved the reaction of 4-(4-Acetylpiperazin-1-yl)benzaldehyde(cas: 890092-19-0).Product Details of 890092-19-0

The Article related to benzoimidazolyl phenylpiperazinyl acrylonitrile preparation antimycobacterial activity sar lipophilicity, propanenitrile benzoimidazolyl phenylpiperazinyl preparation antimycobacterial activity sar lipophilicity, acrylonitrile, antimycobacterial activity, benzimidazole, nutrient starvation test, propanenitrile and other aspects.Product Details of 890092-19-0

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

On November 14, 2003, Tanoury, Gerald J.; Hett, Robert; Wilkinson, H. Scott; Wald, Stephen A.; Senanayake, Chris H. published an article.Reference of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was Total synthesis of (2R,4S,2’S,3’R)-hydroxyitraconazole: implementations of a recycle protocol and a mild and safe phase-transfer reagent for preparation of the key chiral units. And the article contained the following:

A convergent total synthesis of enantiomerically-pure (2R,4S,2’S,3’R)-hydroxyitraconazole is described. The left dioxolane portion of the mol. was prepared in good yield by the conversion of (4S)-2,2-dimethyl-1,3-dioxolane-4-methanol to the corresponding enantiomerically and diastereomerically-pure acetonide (2R,4R)-2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolane-4-methanol by a recycle protocol involving diastereoselective crystallization of the tosylate salt, followed by re-equilibration of the mother liquor and crystallization The right-hand triazolone moiety was generated by alkylation of a triazolone derivative with an enantiomerically pure cyclic sulfate [(4R,5R)-4,5-dimethyl-1,2,3-dioxathiolane 2,2-dioxide] under mild and essentially non-hazardous reaction conditions (TDA-1, K2CO3, acetonitrile). The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Reference of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

The Article related to hydroxyitraconazole total synthesis preparation, tda cost effective hydroxyitraconazole total synthesis preparation, alkylation tda cost effective hydroxyitraconazole total synthesis preparation, cost effective hydroxyitraconazole total synthesis preparation, asym synthesis hydroxyitraconazole preparation and other aspects.Reference of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

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

On June 30, 1980, Carissimi, M.; Picciola, G.; Ravenna, F.; Gentili, P.; Carenini, G. published an article.Reference of 3-(4-Methylpiperazin-1-yl)propanoic acid dihydrochloride The title of the article was Antidepressant activity of cyclohexylphenoxymorpholines. And the article contained the following:

2-[(Cyclohexylphenoxy)methyl]morpholines I (R = H, alkyl, aminoalkyl, piperazinopropionyl or -propyl, benzoylalkyl; R1 = 2-, 3-, or 4-cyclohexyl) were prepared by different methods and they showed antidepressant, tranquilizer, analgesic, and spasmolytic activity; I also inhibited blood platelet aggregation. The phenoxyisopropanolamine II reacted with ClCH2COCl to yield a 2-(phenoxymethyl)morpholin-5-one, the product was reduced (LiAlH4) to give a N-benzylmorpholine derivative, and hydrogenolysis of the latter gave I (R = H, R1 = 2-cyclohexyl). The experimental process involved the reaction of 3-(4-Methylpiperazin-1-yl)propanoic acid dihydrochloride(cas: 59695-29-3).Reference of 3-(4-Methylpiperazin-1-yl)propanoic acid dihydrochloride

The Article related to morpholine phenoxymethyl preparation antidepressant, phenoxymethylmorpholine preparation antidepressant analgesic, tranquilizer phenoxymethylmorpholine preparation, spasmolytic phenoxymethylmorpholine preparation, blood platelet phenoxymethylmorpholine preparation and other aspects.Reference of 3-(4-Methylpiperazin-1-yl)propanoic acid dihydrochloride

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

On February 15, 2006, Power, Eoin C.; Ganellin, C. Robin; Benton, David C. H. published an article.Application of 67914-60-7 The title of the article was Partial structures of ketoconazole as modulators of the large conductance calcium-activated potassium channel (BKCa). And the article contained the following:

A series of partial structures of ketoconazole has been synthesized and tested for activity on the large conductance calcium-activated potassium channel (BK) in bovine smooth muscle cells. This has provided openers and blockers of the channel. The results suggest that the Ph and phenoxy moieties are important for interaction with BK, whereas the imidazole group is unimportant. The properties of the phenoxy moiety seem to determine whether the compounds act to open or block the channel. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Application of 67914-60-7

The Article related to potassium channel calcium activated large conductance ketoconazole fragment preparation, kcnm family potassium channel ketoconazole fragment preparation, channel blocker opener potassium calcium ketoconazole analog preparation and other aspects.Application of 67914-60-7

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

On August 1, 2017, Lin, Xiao-Xiao; Zhang, Xiao-Fang; Wang, Ai-Jun; Fang, Ke-Ming; Yuan, Junhua; Feng, Jiu-Ju published an article.Computed Properties of 67914-60-7 The title of the article was Simple one-pot aqueous synthesis of AuPd alloy nanocrystals/reduced graphene oxide as highly efficient and stable electrocatalyst for oxygen reduction and hydrogen evolution reactions. And the article contained the following:

Herein, the authors develop a simple 1-pot aqueous method to prepare AuPd alloy nanocrystals on reduced graphene oxide (AuPd NCs/rGO), by using 1-acetyl-4-(p-hydroxyphenyl) piperazine (AHPP) as the reductant, stabilizing agent and structure-director, without any other additives (e.g., seed, surfactant or polymer). The product is mainly characterized by TEM, XPS, x-ray diffraction and TGA. The obtained AuPd NCs/rGO displays enlarged electrochem. active surface area and superior catalytic performances toward O reduction reaction (ORR) and H evolution reaction (HER) relative to Pt/C, Pd/C, Pd/rGO and Au/rGO catalysts, showing promising applications in energy storage and conversion. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Computed Properties of 67914-60-7

The Article related to synthesis gold palladium alloy nanocrystal reduced graphene oxide catalyst, electrocatalyst oxygen reduction hydrogen evolution, aupd nanocrystals, hydrogen evolution reaction, oxygen reduction reaction, reduced graphene oxide and other aspects.Computed Properties of 67914-60-7

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