Tanaka, Akito’s team published research in Chemical & Pharmaceutical Bulletin in 1994 | CAS: 34352-59-5

1-Methylpiperazine dihydrochloride(cas: 34352-59-5) is used in the preparation of 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), 1-methylpiperazine-1,4-diium tetrachloridozincate hemihydrate, 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), an antimicrotubular drug..Application In Synthesis of 1-Methylpiperazine dihydrochloride

Application In Synthesis of 1-Methylpiperazine dihydrochlorideOn September 30, 1994 ,《Studies on anti-platelet agents. IV. A series of 2-substituted 4,5-bis(4-methoxyphenyl)pyrimidines as novel anti-platelet agents》 was published in Chemical & Pharmaceutical Bulletin. The article was written by Tanaka, Akito; Motoyama, Yukio; Takasugi, Hisashi. The article contains the following contents:

The syntheses and structure-activity relationships of a series of 2-substituted 4,5-bis(4-methoxyphenyl)pyrimidines, designed on the basis of structural analyses of several cyclooxygenase (CO) inhibitors, and their derivatives as anti-platelet agents based on CO inhibition are described. Among them, 4,5-bis(4-methoxyphenyl)-2-morpholinopyrimidine and 4,5-bis(4-methoxyphenyl)-2-(3,5-dimethylmorpholin-4-yl)pyrimidine showed potent inhibitory activity on malondialdehyde, formed by the CO-catalyzed oxygenation of arachidonic acid (A.A.) in prostanoids, production in vitro (73.4% inhibition at 10-8 M and IC50 = 1.4 × 10-8 M, resp.). Certain compounds were also examined in ex vivo studies. Of these compounds, 4,5-bis(4-methoxyphenyl)-2-(1-methyl-1,2,3,6,-tetrahydropyrid-4-yl)pyrimidine (11a) exhibited potent and long-lasting anti-platelet activity ex vivo, i.e., 11a showed 97% inhibition of platelet aggregation induced by A.A. even 24 h after oral administration of 3.2 mg/kg in guinea pigs, and 60-70% inhibition at 6 h after lower doses (1.0 mg/kg). The ex vivo activity of 11a is more than three times that of aspirin (aspirin showed 81% inhibitory activity on platelet aggregation induced by A.A. at 6 h after oral administration at 10 mg/kg is this study). Compound 11a also showed vasodilatory activity (ED50 = 5.3 × 10-6 M, while aspirin has no vasodilatory activity at 6.0 × 10-4 M). In addition to this study using 1-Methylpiperazine dihydrochloride, there are many other studies that have used 1-Methylpiperazine dihydrochloride(cas: 34352-59-5Application In Synthesis of 1-Methylpiperazine dihydrochloride) was used in this study.

1-Methylpiperazine dihydrochloride(cas: 34352-59-5) is used in the preparation of 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), 1-methylpiperazine-1,4-diium tetrachloridozincate hemihydrate, 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), an antimicrotubular drug..Application In Synthesis of 1-Methylpiperazine dihydrochloride

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

Hubert, Terrance D.’s team published research in Journal of Organic Chemistry in 1984 | CAS: 34352-59-5

1-Methylpiperazine dihydrochloride(cas: 34352-59-5) is used in the preparation of 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), 1-methylpiperazine-1,4-diium tetrachloridozincate hemihydrate, 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), an antimicrotubular drug..Electric Literature of C5H14Cl2N2

Hubert, Terrance D.; Eyman, Darrell P.; Wiemer, David F. published an article in Journal of Organic Chemistry. The title of the article was 《A convenient synthesis of bis(N-methylpiperazinyl)aluminum hydride: a reagent for the reduction of carboxylic acids to aldehydes》.Electric Literature of C5H14Cl2N2 The author mentioned the following in the article:

The reaction of LiAlH4 with N-methylpiperazine (HL) and N-methylpiperazine dihydrochloride (2:3:1) is a convenient method for the preparation of AlL2H. AlL2H reduces aliphatic, aromatic, and unsaturated carboxylic acids directly to the analogous aldehydes. The facile preparation of the reagent, together with the high yields and the ease of work-up in the reductions, make AlL2H an attractive reagent for this transformation. The results came from multiple reactions, including the reaction of 1-Methylpiperazine dihydrochloride(cas: 34352-59-5Electric Literature of C5H14Cl2N2)

1-Methylpiperazine dihydrochloride(cas: 34352-59-5) is used in the preparation of 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), 1-methylpiperazine-1,4-diium tetrachloridozincate hemihydrate, 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), an antimicrotubular drug..Electric Literature of C5H14Cl2N2

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

Latacz, Gniewomir’s team published research in Chemical Biology & Drug Design in 2016 | CAS: 34352-59-5

1-Methylpiperazine dihydrochloride(cas: 34352-59-5) is used in the preparation of 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), 1-methylpiperazine-1,4-diium tetrachloridozincate hemihydrate, 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), an antimicrotubular drug..Quality Control of 1-Methylpiperazine dihydrochloride

The author of 《The Synthesis of 1,3,5-triazine Derivatives and JNJ7777120 Analogues with Histamine H4 Receptor Affinity and Their Interaction with PTEN Promoter》 were Latacz, Gniewomir; Kechagioglou, Petros; Papi, Rigini; Lazewska, Dorota; Wiecek, Malgorzata; Kaminska, Katarzyna; Wencel, Przemyslaw; Karcz, Tadeusz; Schwed, Johannes S.; Stark, Holger; Kyriakidis, Dimitrios A.; Kiec-Kononowicz, Katarzyna. And the article was published in Chemical Biology & Drug Design in 2016. Quality Control of 1-Methylpiperazine dihydrochloride The author mentioned the following in the article:

The involvement of histamine and H4 receptor (H4R) in cancer has been investigated recently using the H4R agonists and antagonists. The scope of the research project was synthesis and exploration of the consequences of a group of compounds with histamine H4 receptor (H4R) affinity on the promoter of PTEN gene encoding the antitumor PTEN protein. The series of novel compounds based either on H4R antagonists JNJ7777120 structure or 1,3,5-triazine scaffold were synthesized, evaluated for histamine H4R affinity and used in this study. Compounds 5 and 7 belonging to the group of JNJ7777120 analogs showed the highest interaction with the promoter of PTEN gene and weak affinity against H4R with Ki value >100 μm. These compounds showed no significant effect on neuroblastoma IMR-32 cells viability indicating no correlation between PTEN gene promoter affinity and antitumor activity. Compound 6, another JNJ7777120 analog, showed the highest effect on IMR-32 viability with calculated IC50 = 23.27 μm. The 1,3,5-triazine derivatives exhibited generally low or medium interaction with PTEN gene promoter. However, the 1,3,5-triazine derivative 11 with the para-bromo substituent showed the highest affinity against H4R with Ki value of 520 nm and may be considered as a new lead structure. The experimental process involved the reaction of 1-Methylpiperazine dihydrochloride(cas: 34352-59-5Quality Control of 1-Methylpiperazine dihydrochloride)

1-Methylpiperazine dihydrochloride(cas: 34352-59-5) is used in the preparation of 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), 1-methylpiperazine-1,4-diium tetrachloridozincate hemihydrate, 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), an antimicrotubular drug..Quality Control of 1-Methylpiperazine dihydrochloride

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

Ben Salah, Assila Maatar’s team published research in Monatshefte fuer Chemie in 2014 | CAS: 34352-59-5

1-Methylpiperazine dihydrochloride(cas: 34352-59-5) is used in the preparation of 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), 1-methylpiperazine-1,4-diium tetrachloridozincate hemihydrate, 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), an antimicrotubular drug..Category: piperazines

Category: piperazinesOn October 31, 2014 ,《Crystal growth, thermal and magnetic characterizations of a new ferromagnetic Ni(II) dimer》 appeared in Monatshefte fuer Chemie. The author of the article were Ben Salah, Assila Maatar; Walha, Sondra; Yahyaoui, Samia; Abdalrahman, Mahmoud; Turnbull, Mark M.; Mhiri, Tahar; Naili, Houcine. The article conveys some information:

Abstract: Single crystals of 1-methylpiperazine-1,4-diium hexaaquatetrachlorodinickel(II) dichloride, (C5H14N2)[Ni2Cl4(H2O)6]Cl2, were grown by hydrothermal techniques in aqueous solution The compound was characterized by DTA (TG-TDXD), single crystal x-ray diffraction, and variable temperature magnetic susceptibility. The compound crystallizes in the triclinic system (space group P1̅, Z = 2) with the following unit cell dimensions: a 6.611(3), b 8.776(4), c 17.457(8) Å, α 101.34(2), β 96.31(2), and γ 105.38(2)°. The structure was solved using 4,243 independent reflections and refined to R = 0.024. The structure of (C5H14N2)[Ni2Cl4(H2O)6]Cl2 can be described as mixed organic-inorganic layers along the [-101] direction. The Ni dimers show ferromagnetic exchange (J ∼ 15 K), while the interactions between the dimers are antiferromagnetic (J approx. -3 K). The 3-dimensional network is further linked by three types of H bonds (N-H···Cl, OW-H···Cl, and N-H···O), to build cation-anion cohesion. Dehydration of the precursor proceeds through three stages, leading to crystalline intermediary hydrate phases and an anhydrous compound Crystallog. data are given. In the part of experimental materials, we found many familiar compounds, such as 1-Methylpiperazine dihydrochloride(cas: 34352-59-5Category: piperazines)

1-Methylpiperazine dihydrochloride(cas: 34352-59-5) is used in the preparation of 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), 1-methylpiperazine-1,4-diium tetrachloridozincate hemihydrate, 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), an antimicrotubular drug..Category: piperazines

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

Tanaka, Akito’s team published research in Chemical & Pharmaceutical Bulletin in 1994 | CAS: 34352-59-5

1-Methylpiperazine dihydrochloride(cas: 34352-59-5) is used in the preparation of 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), 1-methylpiperazine-1,4-diium tetrachloridozincate hemihydrate, 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), an antimicrotubular drug..Application In Synthesis of 1-Methylpiperazine dihydrochloride

Application In Synthesis of 1-Methylpiperazine dihydrochlorideOn September 30, 1994 ,《Studies on anti-platelet agents. IV. A series of 2-substituted 4,5-bis(4-methoxyphenyl)pyrimidines as novel anti-platelet agents》 was published in Chemical & Pharmaceutical Bulletin. The article was written by Tanaka, Akito; Motoyama, Yukio; Takasugi, Hisashi. The article contains the following contents:

The syntheses and structure-activity relationships of a series of 2-substituted 4,5-bis(4-methoxyphenyl)pyrimidines, designed on the basis of structural analyses of several cyclooxygenase (CO) inhibitors, and their derivatives as anti-platelet agents based on CO inhibition are described. Among them, 4,5-bis(4-methoxyphenyl)-2-morpholinopyrimidine and 4,5-bis(4-methoxyphenyl)-2-(3,5-dimethylmorpholin-4-yl)pyrimidine showed potent inhibitory activity on malondialdehyde, formed by the CO-catalyzed oxygenation of arachidonic acid (A.A.) in prostanoids, production in vitro (73.4% inhibition at 10-8 M and IC50 = 1.4 × 10-8 M, resp.). Certain compounds were also examined in ex vivo studies. Of these compounds, 4,5-bis(4-methoxyphenyl)-2-(1-methyl-1,2,3,6,-tetrahydropyrid-4-yl)pyrimidine (11a) exhibited potent and long-lasting anti-platelet activity ex vivo, i.e., 11a showed 97% inhibition of platelet aggregation induced by A.A. even 24 h after oral administration of 3.2 mg/kg in guinea pigs, and 60-70% inhibition at 6 h after lower doses (1.0 mg/kg). The ex vivo activity of 11a is more than three times that of aspirin (aspirin showed 81% inhibitory activity on platelet aggregation induced by A.A. at 6 h after oral administration at 10 mg/kg is this study). Compound 11a also showed vasodilatory activity (ED50 = 5.3 × 10-6 M, while aspirin has no vasodilatory activity at 6.0 × 10-4 M). In addition to this study using 1-Methylpiperazine dihydrochloride, there are many other studies that have used 1-Methylpiperazine dihydrochloride(cas: 34352-59-5Application In Synthesis of 1-Methylpiperazine dihydrochloride) was used in this study.

1-Methylpiperazine dihydrochloride(cas: 34352-59-5) is used in the preparation of 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), 1-methylpiperazine-1,4-diium tetrachloridozincate hemihydrate, 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), an antimicrotubular drug..Application In Synthesis of 1-Methylpiperazine dihydrochloride

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

Hubert, Terrance D.’s team published research in Journal of Organic Chemistry in 1984 | CAS: 34352-59-5

1-Methylpiperazine dihydrochloride(cas: 34352-59-5) is used in the preparation of 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), 1-methylpiperazine-1,4-diium tetrachloridozincate hemihydrate, 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), an antimicrotubular drug..Electric Literature of C5H14Cl2N2

Hubert, Terrance D.; Eyman, Darrell P.; Wiemer, David F. published an article in Journal of Organic Chemistry. The title of the article was 《A convenient synthesis of bis(N-methylpiperazinyl)aluminum hydride: a reagent for the reduction of carboxylic acids to aldehydes》.Electric Literature of C5H14Cl2N2 The author mentioned the following in the article:

The reaction of LiAlH4 with N-methylpiperazine (HL) and N-methylpiperazine dihydrochloride (2:3:1) is a convenient method for the preparation of AlL2H. AlL2H reduces aliphatic, aromatic, and unsaturated carboxylic acids directly to the analogous aldehydes. The facile preparation of the reagent, together with the high yields and the ease of work-up in the reductions, make AlL2H an attractive reagent for this transformation. The results came from multiple reactions, including the reaction of 1-Methylpiperazine dihydrochloride(cas: 34352-59-5Electric Literature of C5H14Cl2N2)

1-Methylpiperazine dihydrochloride(cas: 34352-59-5) is used in the preparation of 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), 1-methylpiperazine-1,4-diium tetrachloridozincate hemihydrate, 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), an antimicrotubular drug..Electric Literature of C5H14Cl2N2

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

Latacz, Gniewomir’s team published research in Chemical Biology & Drug Design in 2016 | CAS: 34352-59-5

1-Methylpiperazine dihydrochloride(cas: 34352-59-5) is used in the preparation of 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), 1-methylpiperazine-1,4-diium tetrachloridozincate hemihydrate, 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), an antimicrotubular drug..Quality Control of 1-Methylpiperazine dihydrochloride

The author of 《The Synthesis of 1,3,5-triazine Derivatives and JNJ7777120 Analogues with Histamine H4 Receptor Affinity and Their Interaction with PTEN Promoter》 were Latacz, Gniewomir; Kechagioglou, Petros; Papi, Rigini; Lazewska, Dorota; Wiecek, Malgorzata; Kaminska, Katarzyna; Wencel, Przemyslaw; Karcz, Tadeusz; Schwed, Johannes S.; Stark, Holger; Kyriakidis, Dimitrios A.; Kiec-Kononowicz, Katarzyna. And the article was published in Chemical Biology & Drug Design in 2016. Quality Control of 1-Methylpiperazine dihydrochloride The author mentioned the following in the article:

The involvement of histamine and H4 receptor (H4R) in cancer has been investigated recently using the H4R agonists and antagonists. The scope of the research project was synthesis and exploration of the consequences of a group of compounds with histamine H4 receptor (H4R) affinity on the promoter of PTEN gene encoding the antitumor PTEN protein. The series of novel compounds based either on H4R antagonists JNJ7777120 structure or 1,3,5-triazine scaffold were synthesized, evaluated for histamine H4R affinity and used in this study. Compounds 5 and 7 belonging to the group of JNJ7777120 analogs showed the highest interaction with the promoter of PTEN gene and weak affinity against H4R with Ki value >100 μm. These compounds showed no significant effect on neuroblastoma IMR-32 cells viability indicating no correlation between PTEN gene promoter affinity and antitumor activity. Compound 6, another JNJ7777120 analog, showed the highest effect on IMR-32 viability with calculated IC50 = 23.27 μm. The 1,3,5-triazine derivatives exhibited generally low or medium interaction with PTEN gene promoter. However, the 1,3,5-triazine derivative 11 with the para-bromo substituent showed the highest affinity against H4R with Ki value of 520 nm and may be considered as a new lead structure. The experimental process involved the reaction of 1-Methylpiperazine dihydrochloride(cas: 34352-59-5Quality Control of 1-Methylpiperazine dihydrochloride)

1-Methylpiperazine dihydrochloride(cas: 34352-59-5) is used in the preparation of 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), 1-methylpiperazine-1,4-diium tetrachloridozincate hemihydrate, 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), an antimicrotubular drug..Quality Control of 1-Methylpiperazine dihydrochloride

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

Bavetsias, Vassilios’s team published research in Journal of Medicinal Chemistry in 2012 | CAS: 34352-59-5

1-Methylpiperazine dihydrochloride(cas: 34352-59-5) is used in the preparation of 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), 1-methylpiperazine-1,4-diium tetrachloridozincate hemihydrate, 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), an antimicrotubular drug..Product Details of 34352-59-5

Product Details of 34352-59-5On October 25, 2012 ,《Optimization of Imidazo[4,5-b]pyridine-Based Kinase Inhibitors: Identification of a Dual FLT3/Aurora Kinase Inhibitor as an Orally Bioavailable Preclinical Development Candidate for the Treatment of Acute Myeloid Leukemia》 was published in Journal of Medicinal Chemistry. The article was written by Bavetsias, Vassilios; Crumpler, Simon; Sun, Chongbo; Avery, Sian; Atrash, Butrus; Faisal, Amir; Moore, Andrew S.; Kosmopoulou, Magda; Brown, Nathan; Sheldrake, Peter W.; Bush, Katherine; Henley, Alan; Box, Gary; Valenti, Melanie; Brandon, Alexis de Haven; Raynaud, Florence I.; Workman, Paul; Eccles, Suzanne A.; Bayliss, Richard; Linardopoulos, Spiros; Blagg, Julian. The article contains the following contents:

Optimization of the imidazo[4,5-b]pyridine-based series of Aurora kinase inhibitors led to the identification of 6-chloro-7-(4-(4-chlorobenzyl)piperazin-1-yl)-2-(1,3-dimethyl-1H-pyrazol-4-yl)-3H-imidazo[4,5-b]pyridine (I), a potent inhibitor of Aurora kinases (Aurora-A Kd = 7.5 nM, Aurora-B Kd = 48 nM), FLT3 kinase (Kd = 6.2 nM), and FLT3 mutants including FLT3-ITD (Kd = 38 nM) and FLT3(D835Y) (Kd = 14 nM). FLT3-ITD causes constitutive FLT3 kinase activation and is detected in 20-35% of adults and 15% of children with acute myeloid leukemia (AML), conferring a poor prognosis in both age groups. In an in vivo setting, I strongly inhibited the growth of a FLT3-ITD-pos. AML human tumor xenograft (MV4-11) following oral administration, with in vivo biomarker modulation and plasma free drug exposures consistent with dual FLT3 and Aurora kinase inhibition. Compound I, an orally bioavailable dual FLT3 and Aurora kinase inhibitor, was selected as a preclin. development candidate for the treatment of human malignancies, in particular AML, in adults and children.1-Methylpiperazine dihydrochloride(cas: 34352-59-5Product Details of 34352-59-5) was used in this study.

1-Methylpiperazine dihydrochloride(cas: 34352-59-5) is used in the preparation of 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), 1-methylpiperazine-1,4-diium tetrachloridozincate hemihydrate, 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), an antimicrotubular drug..Product Details of 34352-59-5

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

Yabuuchi, Takahiro’s team published research in Chemical & Pharmaceutical Bulletin in 1975 | CAS: 34352-59-5

1-Methylpiperazine dihydrochloride(cas: 34352-59-5) is used in the preparation of 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), 1-methylpiperazine-1,4-diium tetrachloridozincate hemihydrate, 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), an antimicrotubular drug..Formula: C5H14Cl2N2

《Synthesis of new antimicrobials. IV. Synthesis of alkylenebis(thiourea) derivatives and their related compounds》 was published in Chemical & Pharmaceutical Bulletin in 1975. These research results belong to Yabuuchi, Takahiro; Hisaki, Masakatu; Matuda, Masahiro; Kimura, Ryuichi. Formula: C5H14Cl2N2 The article mentions the following:

3,3′-Substituted 1,1′-alkylenebis(thiourea) derivatives, e.g. Et2NCH2CH2NHCSNHCH2CH2NHCSNHCH2CH2NEt2 were prepared from alkylenebis(isothiocyanates) and amines. Also, 3,3′-alkylenebis[2-thio-2,4(1H,3H)quinazolinediones] I (m = 3, 4, 6) were prepared by the reaction of alkylenebis(isothiocyanates) and anthranilic acid, or alkylene diamines and Et o-isothiocyanatobenzoate, resp. In the experiment, the researchers used 1-Methylpiperazine dihydrochloride(cas: 34352-59-5Formula: C5H14Cl2N2)

1-Methylpiperazine dihydrochloride(cas: 34352-59-5) is used in the preparation of 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), 1-methylpiperazine-1,4-diium tetrachloridozincate hemihydrate, 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), an antimicrotubular drug..Formula: C5H14Cl2N2

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

Sudol, Sylwia’s team published research in European Journal of Medicinal Chemistry in 2020 | CAS: 34352-59-5

1-Methylpiperazine dihydrochloride(cas: 34352-59-5) is used in the preparation of 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), 1-methylpiperazine-1,4-diium tetrachloridozincate hemihydrate, 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), an antimicrotubular drug..Product Details of 34352-59-5

Product Details of 34352-59-5On October 1, 2020 ,《Chlorine substituents and linker topology as factors of 5-HT6R activity for novel highly active 1,3,5-triazine derivatives with procognitive properties in vivo》 was published in European Journal of Medicinal Chemistry. The article was written by Sudol, Sylwia; Kucwaj-Brysz, Katarzyna; Kurczab, Rafal; Wilczynska, Natalia; Jastrzebska-Wiesek, Magdalena; Satala, Grzegorz; Latacz, Gniewomir; Gluch-Lutwin, Monika; Mordyl, Barbara; Zeslawska, Ewa; Nitek, Wojciech; Partyka, Anna; Buzun, Kamila; Doroz-Plonka, Agata; Wesolowska, Anna; Bielawska, Anna; Handzlik, Jadwiga. The article contains the following contents:

This study had supplied highly potent 5-HT6R agents with procognitive effects, which represent an original chem. class of 1,3,5-triazines, different than widely studied sulfone and indole-like 5-HT6R ligands. The new compounds I (R1 = Ph, 2,3-Cl2C6H3, 2,5-Cl2C6H3, 3,4-Cl2C6H3, 3,5-Cl2C6H3, 2,4-Cl2C6H3; R2 = H, Me, Et, n-Pr, n-Bu, X = nothing; R2 = H, X = CH2CH2) were rationally designed as modifications of lead, 4-(1-(2-chlorophenoxy)ethyl)-6-(4-methylpiperazin-1-yl)-1,3,5-triazin-2-amine, involving an introduction of: (i) two chlorines at the benzene ring and (ii) varied linkers joining the triazine ring to aromatic ethers. Synthesis, in vitro and in vivo biol. tests and computer-aided SAR anal. for new compounds were carried out. Most of the new triazines displayed high affinity and selectivity toward 5-HT6R with respect to 5-HT2AR, 5-HT7R and D2R. The crystallog.-supported docking studies, including quantum-polarized ligand docking (QPLD), indicated that chlorine atoms might be involved in different type of halogen bonding, however, the linker properties seem to predominately affect the 5-HT6R affinity. Compound I (R1 = 2,5-Cl2C6H3; R2 = Et; X = nothing), which displayed: the highest affinity (Ki = 6 nM), very strong 5-HT6R antagonistic action (KB = 27 pM), procognitive effects in vivo in novel object recognition (NOR) test in rats, a very good permeability in PAMPA model and satisfying safety in vitro, was identified as the most potent 1,3,5-triazine agent so far, useful as a new lead for further research. In the experiment, the researchers used 1-Methylpiperazine dihydrochloride(cas: 34352-59-5Product Details of 34352-59-5)

1-Methylpiperazine dihydrochloride(cas: 34352-59-5) is used in the preparation of 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), 1-methylpiperazine-1,4-diium tetrachloridozincate hemihydrate, 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), an antimicrotubular drug..Product Details of 34352-59-5

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