Tag: 200-300

On July 15, 2018, Moustakim, Moses; Riedel, Kerstin; Schuller, Marion; Gehring, Andre P.; Monteiro, Octovia P.; Martin, Sarah P.; Fedorov, Oleg; Heer, Jag; Dixon, Darren J.; Elkins, Jonathan M.; Knapp, Stefan; Bracher, Franz; Brennan, Paul E. published an article.Computed Properties of 59695-29-3 The title of the article was Discovery of a novel allosteric inhibitor scaffold for polyadenosine-diphosphate-ribose polymerase 14 (PARP14) macrodomain 2. And the article contained the following:

The polyadenosine-diphosphate-ribose polymerase 14 (PARP14) has been implicated in DNA damage response pathways for homologous recombination. PARP14 contains three (ADP ribose binding) macrodomains (MD) whose exact contribution to overall PARP14 function in pathol. remains unclear. A medium throughput screen led to the identification of N-(2(-9H-carbazol-1-yl)phenyl)acetamide (GeA-69, 1) as a novel allosteric PARP14 MD2 (second MD of PARP14) inhibitor. We herein report medicinal chem. around this novel chemotype to afford a sub-micromolar PARP14 MD2 inhibitor. This chem. series provides a novel starting point for further development of PARP14 chem. probes. 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 carbazole scaffold preparation allosteric inhibitor parp14 macrodomain md2, inhibitor design, macrodomain, parp, poly-adp ribsose, Enzymes: Substrates-Cofactors-Inhibitors-Activators-Coenzymes-Products and other aspects.Computed Properties of 59695-29-3

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

On December 7, 2010, Bachovchin, Daniel A.; Ji, Tianyang; Li, Weiwei; Simon, Gabriel M.; Blankman, Jacqueline L.; Adibekian, Alexander; Hoover, Heather; Niessen, Sherry; Cravatt, Benjamin F. published an article.Recommanded Product: 67914-60-7 The title of the article was Superfamily-wide portrait of serine hydrolase inhibition achieved by library-versus-library screening. And the article contained the following:

Serine hydrolases (SHs) are-one of the largest and most diverse enzyme classes in mammals. They play fundamental roles in virtually all physiol. processes and are targeted by drugs to treat diseases such as diabetes, obesity, and neurodegenerative disorders. Despite this, we lack biol. understanding for most of the 110+ predicted mammalian metabolic SHs, in large part because of a dearth of assays to assess their biochem. activities and a lack of selective inhibitors to probe their function in living systems. We show here that the vast majority (>80%) of mammalian metabolic SHs can be labeled in proteomes by a single, active site-directed fluorophosphonate probe. We exploit this universal activity-based assay in a library-vs.-library format to screen 70+ SHs against 140+ structurally diverse carbamates. Lead inhibitors were discovered for ∼40% of the screened enzymes, including many poorly characterized SHs: Global profiles identified carbamate inhibitors that discriminate among highly sequence-related SHs and, conversely, enzymes that share inhibitor sensitivity profiles despite lacking sequence homol. These findings indicate that sequence relatedness is not a strong predictor of shared pharmaol. within the SH superfamily. Finally, we show that lead carbamate inhibitors can be optimized into pharmacol. probes that inactivate individual SHs with high specificity in vivo. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Recommanded Product: 67914-60-7

The Article related to serine hydrolase carbamate library screening, Enzymes: Substrates-Cofactors-Inhibitors-Activators-Coenzymes-Products and other aspects.Recommanded Product: 67914-60-7

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

On October 24, 2013, McLure, Kevin G.; Young, Peter R. published a patent.HPLC of Formula: 890092-19-0 The title of the patent was Preparation of quinazolin-4(3H)-one derivatives and for the treatment of diseases by epigenetic regulation. And the patent contained the following:

The present disclosure provides non-naturally occurring polyphenol compounds that inhibit the bromodomain and extra terminal domain (BET) proteins. Title compounds I [Q and V independently = CH or N; Ra1 and Ra3 independently = H, alkyl,alkoxy, halogen, amino, amide, hydroxy, heterocycle, or cycloalkyl; Rb2 and Rb6independently = H; Rb3 and Rb5 independently = H, halogen, alkyl, alkoxy, cycloalkyl,hydroxy, or amino; W = C or N; Z = O, S, S(O), SO2; R3, R4, and R5 independently = H, alkyl,alkenyl, alkynyl, alkoxy, cycloalkyl, aryl, aryloxy, etc.], and their stereoisomers, tautomers, pharmaceutically acceptable salts, or hydrates, are prepared and disclosed. Thus, e.g., II was prepared by reaction of 5,7-dimethoxy-2-[4-(piperazin-1-yl)phenyl]quinazolin-4(3H)-one with 2-bromoethanol. Compounds of the invention showed tetra-acetylated histone H4 binding individual BET bromodomains and had an IC50 value less than 50 μM. The disclosed compositions and methods can be used for treatment and prevention of diseases or disorders that are susceptible to administration of a BET inhibitor. The experimental process involved the reaction of 4-(4-Acetylpiperazin-1-yl)benzaldehyde(cas: 890092-19-0).HPLC of Formula: 890092-19-0

The Article related to preparation epigenetic regulation bet protein, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.HPLC of Formula: 890092-19-0

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

On November 28, 2013, Mclure, Kevin G.; Young, Peter Ronald published a patent.Quality Control of 4-(4-Acetylpiperazin-1-yl)benzaldehyde The title of the patent was Preparation of quinazolin-4(3H)-one derivatives and for the treatment of diseases by epigenetic regulation. And the patent contained the following:

The present disclosure provides non-naturally occurring polyphenol compounds that inhibit the bromodomain and extra terminal domain (BET) proteins. Title compounds I [Q and V independently = CH or N; Ra1 and Ra3 independently = H, alkyl,alkoxy, halogen, amino, amide, hydroxy, heterocycle, or cycloalkyl; Rb2 and Rb6independently = H; Rb3 and Rb5 independently = H, halogen, alkyl, alkoxy, cycloalkyl,hydroxy, or amino; W = C or N; Z = O, S, S(O), SO2; R3, R4, and R5 independently = H, alkyl,alkenyl, alkynyl, alkoxy, cycloalkyl, aryl, aryloxy, etc.], and their stereoisomers, tautomers, pharmaceutically acceptable salts, or hydrates, are prepared and disclosed. Thus, e.g., II was prepared by reaction of 5,7-dimethoxy-2-[4-(piperazin-1-yl)phenyl]quinazolin-4(3H)-one with 2-bromoethanol. Compounds of the invention showed tetra-acetylated histone H4 binding individual BET bromodomains and had an IC50 value less than 50 μM. The disclosed compositions and methods can be used for treatment and prevention of diseases or disorders that are susceptible to administration of a BET inhibitor. The experimental process involved the reaction of 4-(4-Acetylpiperazin-1-yl)benzaldehyde(cas: 890092-19-0).Quality Control of 4-(4-Acetylpiperazin-1-yl)benzaldehyde

The Article related to preparation epigenetic regulation bet protein, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Quality Control of 4-(4-Acetylpiperazin-1-yl)benzaldehyde

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

Mrachkovskaya, L. B.; Turchin, K. F.; Yakhontov, L. N. published an article in 1975, the title of the article was Reduction fragmentation of 4-methyl-1-piperazinylmethylidenemalonate.Quality Control of 3-(4-Methylpiperazin-1-yl)propanoic acid dihydrochloride And the article contains the following content:

Di-Et 4-methyl-1-piperazinylmethylidenemalonate (I), prepared in 83.5% yield from 1-methylpiperazine (II) and EtOCH:C(CO2Et)2, was reductively cleaved by NaBH4 in absolute EtOH at 20-5° to give 65% of a mixture of II and methylmalonic acid (III). Analogous reduction in dioxane gave 11% II-III and in cyclohexane 5% II-III were obtained. Similar results were obtained by catalytic reduction with Pt. The experimental process involved the reaction of 3-(4-Methylpiperazin-1-yl)propanoic acid dihydrochloride(cas: 59695-29-3).Quality Control of 3-(4-Methylpiperazin-1-yl)propanoic acid dihydrochloride

The Article related to reduction cleavage piperazinylmethylenemalonic acid, pyruvoyl hydrazone reaction hydrazide, triazole acetyl anilino, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines and other aspects.Quality Control of 3-(4-Methylpiperazin-1-yl)propanoic acid dihydrochloride

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

Mrachkovskaya, L. B.; Anisimova, O. S.; Turchin, K. F.; Yakhontov, L. N. published an article in 1976, the title of the article was Formation of the bis(N-methylpiperazide) of monothiooxalic acid from 3-(N-methylpiperazinyl)propionic acid under conditions of the Zelinsky reaction.Formula: C8H18Cl2N2O2 And the article contains the following content:

The title compound I was obtained from piperazinepropionic acid (II) by boiling 2 hr with SOCl2, 2 hr with Br-CHCl3, and 5 hr with EtOH. The experimental process involved the reaction of 3-(4-Methylpiperazin-1-yl)propanoic acid dihydrochloride(cas: 59695-29-3).Formula: C8H18Cl2N2O2

The Article related to piperazine thiooxalylbismethyl, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines and other aspects.Formula: C8H18Cl2N2O2

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

On February 6, 2015, Fujimoto, Teppei; Ritter, Tobias published an article.Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was PhenoFluorMix: Practical Chemoselective Deoxyfluorination of Phenols. And the article contained the following:

A practical deoxyfluorination with novel deoxyfluorinating reagent PhenoFluorMix, a mixture of N,N’-1,3-bis(2,6-diisopropylphenyl)chloroimidazolium chloride and CsF, is presented. PhenoFluorMix overcomes the challenges associated with hydrolysis of PhenoFluor. PhenoFluorMix does not hydrolyze, is readily available on decagram scale, and is storable in air. In this paper, we demonstrate the practicality of the reagent and exhibit the deoxyfluorination of a variety of phenols and heterocycles. 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 aryl halide chemoselective synthesis, phenol heterocycle deoxyfluorination phenofluormix, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Halides and Halonium Compounds and other aspects.Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

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

On May 27, 2010, Aissaoui, Hamed; Boss, Christoph; Corminboeuf, Olivier; Frantz, Marie-Celine; Grisostomi, Corinna published a patent.HPLC of Formula: 890092-19-0 The title of the patent was Novel bis-amides as antimalarial agents and their preparation and use in the treatment of protozoal infections. And the patent contained the following:

The invention relates to bis-amide derivatives of formula I and their use as active ingredients in the preparation of pharmaceutical compositions The invention also concerns related aspects including pharmaceutical compositions containing one or more of those compounds and their use as medicaments for the treatment or prevention of protozoal infections, such as especially malaria. Compounds of formula I wherein R1 is (un)substituted aryl and (un)substituted heteroaryl; R2 is (un)substituted aryl and (un)substituted heteroaryl: R3 is (un)substituted aryl and (un)substituted heteroaryl; R4R5 together with the N they are attached form morpholinyl, 2,3-dihydroindolinyl, 1,3-dihydroisoindolinyl, etc.; when R4 is H and C1-4 alkyl, then R5 is 1-benzylpyrrolidin-3-yl and 1-azabicyclo[2.2.2]oct-3-yl; when R4 is C1-4 alkyl then R5 is hydroxyethyl, alkoxyethyl, aminoethyl, etc.; and salts thereof, are claimed. Example compound II was prepared by a general procedure (procedure given). All the invention compounds were evaluated for their antimalarial activity. From the assay, it was determined that compound II exhibited an IC value of 5 nM. The experimental process involved the reaction of 4-(4-Acetylpiperazin-1-yl)benzaldehyde(cas: 890092-19-0).HPLC of Formula: 890092-19-0

The Article related to bis amide preparation antimalarial treatment protozoal infection, Aliphatic Compounds: Amides, Amidines, Imidic Esters, Hydrazides, and Hydrazonic Esters and other aspects.HPLC of Formula: 890092-19-0

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

On June 30, 1985, Takeuchi, Isao; Sugiura, Michiharu; Yamamoto, Kazuko; Ito, Tomiyoshi; Hamada, Yoshiki published an article.Safety of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was Syntheses and antimicrobial activities of cis-1-[2-phenyl-4-(phenoxy or phenylthio)methyl-1,3-dioxolan-2-ylmethyl]-1H-imidazole derivatives. And the article contained the following:

Substitution reactions of glycerol ketals I (R, R1 = H, MeO; Br, Br; Cl, Cl) with heterocycles gave II (R2 = 1-imidazolyl, 1-pyrazolyl, 1,2,4-triazol-1-yl) which underwent successive saponification, mesylation, and substitution reaction with R3R4C6H3XH (R3, R4 = H, MeO, Cl, Me, Br; X = O, S) to give ketoconazole analogs III. Antimicrobial test of the synthesized compounds III (R2 = 1-imidazolyl; R, R1, R3, R4, X = Cl, Cl, H, 4-Cl, S; Cl, Cl, 2-Cl, 6-Cl, S; Br, Br, 2-Cl, 6-Cl, S) showed strong antimicrobial activities against Penicillium chrysogenum and Trichophyton rubrum. Most compounds synthesized had strong preventive effects against downy mildew and sheath blight. Triazole derivatives III (R2 = 1-triazolyl; R = R1 = Cl; R3 = H, 2-Cl; R4 = Cl; X = S, O) showed similar effects against not only such diseases but gray mold rot. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Safety of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

The Article related to ketoconazole analog preparation bactericide fungicide, dioxolanylmethylimidazole phenoxy phenylthio, Heterocyclic Compounds (More Than One Hetero Atom): Dioxoles, Oxathioles, Dithioles and other aspects.Safety of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

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

On February 1, 2022, Zhang, Chen; Liao, Yuting; He, Ping; Chen, Xiaogang; Xuan, Zhaoli; Ye, Fei; Tang, Pingming; Wan, Songlin; Li, Yao; Ni, Jia; Yan, Pangke published a patent.COA of Formula: C15H29N3O2 The title of the patent was Preparation of BTK inhibitor cyclic derivative and its pharmaceutical application in treatment of BTK-related diseases. And the patent contained the following:

The present invention relates to preparation of BTK inhibitor cyclic derivative and its pharmaceutical application in treatment of BTK-related diseases. In particular, the BTK inhibitor ring derivative B-L-K (wherein, L = -Ak1-Cy1-Ak2-Cy2-Ak3-Cy3-Ak4-Cy4-Ak5-; Ak1 – Ak5 = CH2, O, -NRb0-, C=O, C=C or bond; Cy1 – Cy4 = optionally substituted 3-12 membered heterocycle, optionally substituted 3-12 membered cycloalkyl, optionally substituted 6-10 membered aryl, or bond; B = B1-W1-B2-B3-B4- or I, when B = B1-W1-B2-B3-B4-, Cy1, Cy2, Cy3, and Cy4 cannot be bonds at the same time; when B = B1-W1-B2-B3-B4-, and Ak1, Ak2, Ak3, Ak4 or Ak5 are not bonds, they cannot be directly connected to each other). Further, (B1 and B2 = optionally substituted 6-membered heteroaromatic ring or phenyl; W1 = -O-, -S-, -NH-, -NHCO- or -CONH-; B3 = optionally substituted heterocyclic ring; B4 = optionally substituted 4-7-membered monocycloalkyl, optionally substituted 6-12-membered spirocycloalkyl, optionally substituted 5-10-membered cycloalkyl derivative etc.; B5 or B6 = optionally substituted Ph or 5-6-membered heteroaryl; Rb6 = H, C1-4 alkyl, halogen-substituted C1-4 alkyl or hydroxy-substituted C1-4 alkyl; Rb7 and Rb8 = H, F, Cl, Br, I, OH, NH2, CN, CF3, -C(=O)NH2 etc.; m = 0, 1 or 2; K = heterocyclic group, cycloalkyl carbonyl-group, aralkyl carbonyl-group etc.) or stereoisomer, solvate, prodrug, metabolite, pharmaceutically acceptable salt or co-crystal thereof were prepared The inventive BTK inhibitor cyclic derivatives are useful for treating BTK-related diseases such as tumors or autoimmune system diseases. 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 azaheterocyclic compound preparation btk inhibitor antitumor autoimmune disease treatment, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.COA of Formula: C15H29N3O2

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