Month: October 2022

Obniska, Jolanta; Kulig, Katarzyna; Zejc, Alfred published an article in Acta Poloniae Pharmaceutica. The title of the article was 《Synthesis and anticonvulsant properties of new N-piperazinylalkyl imides of succinic acid》.Name: 1-Methylpiperazine dihydrochloride The author mentioned the following in the article:

A number of N-[((4-aryl)- or (4-methyl)-1-piperazinyl)alkyl]imides of 3-aryl- or 3,3-pentamethylenesuccinic acid, I [R1 = 3-ClC6H4, 4-ClC6H4, R2 = H, R1R2 = (CH2)5, R3 = Ph, CH2Ph, Me.2HCl, 2-MeOC6H4, 3-ClC6H4, n = 1; R1 = Ph, R2 = Ph, Me, R1R2 = (CH2)5, R3 = H.2HCl, Me.2HBr, Me.2HCl, n = 2, 3; R1 = Ph, R2 = Me, R3 = Ph, n = 3], were synthesized and tested for anticonvulsant activity in the maximum electroshock seizure (MES) and pentylenetetrazole seizure threshold (scMet) tests. Structures of the novel compounds were confirmed by elemental and spectral analyses. In addition to this study using 1-Methylpiperazine dihydrochloride, there are many other studies that have used 1-Methylpiperazine dihydrochloride(cas: 34352-59-5Name: 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..Name: 1-Methylpiperazine dihydrochloride

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

Zhou, Dahui; Zhou, Ping; Evrard, Deborah A.; Meagher, Kristin; Webb, Michael; Harrison, Boyd L.; Huryn, Donna M.; Golembieski, Jeannette; Hornby, Geoffrey A.; Schechter, Lee E.; Smith, Deborah L.; Andree, Terrance H.; Mewshaw, Richard E. published an article in Bioorganic & Medicinal Chemistry. The title of the article was 《Studies toward the discovery of the next generation of antidepressants. Dual 5-HT1A receptor and serotonin transporter affinity within a class of arylpiperazinyl-cyclohexyl indole derivatives》.Application In Synthesis of 4-(Piperazin-1-yl)-1H-indole The author mentioned the following in the article:

Based on the previously reported discovery lead, 3-(cis-4-(4-(1H-indol-4-yl)piperazin-1-yl)cyclohexyl)-5-fluoro-1H-indole (2), a series of related arylpiperazin-4-yl-cyclohexyl indole analogs were synthesized then evaluated as 5-HT transporter inhibitors and 5-HT1A receptor antagonists. The investigation of the structure-activity relationships revealed the optimal pharmacophoric elements required for activities in this series. The best example from this study (I) exhibited equal binding affinities at 5-HT transporter (Ki = 4.9 nM), 5-HT1A receptor (Ki = 6.2 nM) and functioned as a 5-HT1A receptor antagonist. The experimental part of the paper was very detailed, including the reaction process of 4-(Piperazin-1-yl)-1H-indole(cas: 84807-09-0Application In Synthesis of 4-(Piperazin-1-yl)-1H-indole)

4-(Piperazin-1-yl)-1H-indole(cas: 84807-09-0) belongs to piperazines. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines.Application In Synthesis of 4-(Piperazin-1-yl)-1H-indole

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

In 2022,Venkatesh, Rapelly; Shankar, Gauri; Narayanan, Aswathi C.; Modi, Gyan; Sabiah, Shahulhameed; Kandasamy, Jeyakumar published an article in Journal of Organic Chemistry. The title of the article was 《Multicomponent Synthesis of S-Benzyl Dithiocarbamates from para-Quinone Methides and Their Biological Evaluation for the Treatment of Alzheimer’s Disease》.Product Details of 109-01-3 The author mentioned the following in the article:

Multicomponent synthesis of biol. relevant S-benzyl dithiocarbamates I [Ar = Ph, 2-thienyl, 2-naphthyl, etc.; R = methylamino, 1-pyrrolidinyl, benzylamino, etc.] from para-quinone methides, amines and carbon disulfide were described under catalyst and additive-free conditions. The reactions proceeded at room temperature in a short span of time with excellent yields. One of the synthesized compounds, compound I [Ar = Ph, R = isopropylamino] showed considerable acetylcholinesterase (AChE) inhibitory (51.70 + 5.63% at 20μm) and antioxidant (63.52 ± 1.15 at 20μm) activities. In addition to this study using 1-Methylpiperazine, there are many other studies that have used 1-Methylpiperazine(cas: 109-01-3Product Details of 109-01-3) was used in this study.

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Product Details of 109-01-3

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

In 2022,Yamaguchi, Nobuharu; Biniecki, Kristof; Jankowski, Christopher K.; Ciszewski, Lech published an article in Acta Poloniae Pharmaceutica. The title of the article was 《Cardiovascular evaluation of the chemical structure of N-methylpiperazinyl phthalazine analogs》.Product Details of 109-01-3 The author mentioned the following in the article:

The chem. structure of N-methylpiperazinyl phthalazine analogs – KB compounds, having potential cardiovascular effects, were synthesized and its detailed spectral identification is reported. For KB-1, moiety structure, five physiol. cardiovascular tests were performed and the results were discussed. This mol. showed long-lasting antihypertensive properties with similarly long-lasting bradycardia. However, a slight modification of the mol. structure might minimize the cardiac depressant phenomenon, which is a common undesired effect of various antihypertensive drugs on the market. In the experiment, the researchers used many compounds, for example, 1-Methylpiperazine(cas: 109-01-3Product Details of 109-01-3)

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Product Details of 109-01-3

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

Recommanded Product: 109-01-3In 2020 ,《Efficient Synthesis of Sulfenamides through Mitsunobu-type Coupling Reaction of Thiols with Amines using Dibenzyl Azodicarboxylate》 was published in Asian Journal of Organic Chemistry. The article was written by Ryu, Se Hwan; Ra, Jongmin; Ko, Haye Min. The article contains the following contents:

S-H activation reaction of thiols employing dibenzyl azodicarboxylate (DBAD) had been developed for the preparation of sulfenamides I [R = H; R1 = Et, Bn, cyclopropyl, cyclopentyl, cyclohexyl; RR1 = (CH2)4, (CH2)6, (CH2)2O(CH2)2, etc.; X = O, S]. The dehydrogenation of thiols and amines under these reaction conditions involved the formation of dibenzyl hydrazine-1,2-dicarboxylate, which led to the S-N bond formation reaction. The reaction proceeded efficiently with release of dibenzyl hydrazine-1,2-dicarboxylate and afforded various sulfenamides I in good to excellent yields. In addition to this study using 1-Methylpiperazine, there are many other studies that have used 1-Methylpiperazine(cas: 109-01-3Recommanded Product: 109-01-3) was used in this study.

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Recommanded Product: 109-01-3

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

《Thiazolothiazepine Inhibitors of HIV-1 Integrase》 was written by Neamati, Nouri; Turpin, Jim A.; Winslow, Heather E.; Christensen, John L.; Williamson, Karen; Orr, Ann; Rice, William G.; Pommier, Yves; Garofalo, Antonio; Brizzi, Antonella; Campiani, Giuseppe; Fiorini, Isabella; Nacci, Vito. Recommanded Product: 1-Methylpiperazine dihydrochloride And the article was included in Journal of Medicinal Chemistry on August 26 ,1999. The article conveys some information:

A series of thiazolothiazepines were prepared and tested against purified human immunodeficiency virus type-1 integrase (HIV-1 IN) and viral replication. Structure-activity studies reveal that the compounds possessing the pentat. moiety SC(O)CNC(O) with two carbonyl groups are in general more potent against purified IN than those containing only one carbonyl group. Substitution with electron-donating or -withdrawing groups did not enhance nor abolish potency against purified IN. By contrast, compounds with a naphthalene ring system showed enhanced potency, suggesting that a hydrophobic pocket in the IN active site might accommodate an aromatic system rather than a halogen. The position of sulfur in the thiazole ring appears important for potency against IN, as its replacement with an oxygen or carbon abolished activity. Further extension of the thiazole ring diminished potency. I [R, R1 = H, X = S, Y = CH2; RR1 = CH:CHCH:CH; X = S, Y = CH2; X = CH2, Y = S] showed antiviral activity and inhibited IN within similar concentrations These compounds inhibited IN when Mn2+ or Mg2+ was used as cofactor. None of these compounds showed detectable activities against HIV-1 reverse transcriptase, protease, virus attachment, or nucleocapsid protein zinc fingers. Therefore, thiazolothiazepines are potentially important lead compounds for development as inhibitors of IN and HIV replication. In the part of experimental materials, we found many familiar compounds, such as 1-Methylpiperazine dihydrochloride(cas: 34352-59-5Recommanded Product: 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..Recommanded Product: 1-Methylpiperazine dihydrochloride

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

Related Products of 85817-34-1On May 15, 2007 ,《Syntheses and binding affinities of 6-nitroquipazine analogues for serotonin transporter. Part 5: 2′-Substituted 6-nitroquipazines》 appeared in Bioorganic & Medicinal Chemistry. The author of the article were Lee, Jae Hak; Choi, Yong Hyun; Lim, Yoo Jin; Lee, Byoung Se; Chi, Dae Yoon; Jin, Changbae. The article conveys some information:

Five C2′-substituted 6-nitroquipazine (6-NQ) derivatives were prepared and evaluated in terms of their biol. abilities (Ki) to displace [3H]citalopram binding to serotonin transporter. The relationship between their structure and biol. activities revealed that shorter alkyl groups tend to possess higher binding affinity. Both compounds 12a (I, R1 = OH) and 12c (I, R1 = OEt) were found to have the equally highest binding affinity (Ki = 0.43 ± 0.02 nM). The results came from multiple reactions, including the reaction of (4-Benzylpiperazin-2-yl)methanol(cas: 85817-34-1Related Products of 85817-34-1)

(4-Benzylpiperazin-2-yl)methanol(cas: 85817-34-1) belongs to piperazines. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines.Related Products of 85817-34-1

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

Cowart, Marlon; Latshaw, Steven P.; Bhatia, Pramila; Daanen, Jerome F.; Rohde, Jeffrey; Nelson, Sherry L.; Patel, Meena; Kolasa, Teodozyi; Nakane, Masaki; Uchic, Marie E.; Miller, Loan N.; Terranova, Marc A.; Chang, Renjie; Donnelly-Roberts, Diana L.; Namovic, Marian T.; Hollingsworth, Peter R.; Martino, Brenda R.; Lynch, James J. III; Sullivan, James P.; Hsieh, Gin C.; Moreland, Robert B.; Brioni, Jorge D.; Stewart, Andrew O. published an article in Journal of Medicinal Chemistry. The title of the article was 《Discovery of 2-(4-Pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole (ABT-724), a Dopaminergic Agent with a Novel Mode of Action for the Potential Treatment of Erectile Dysfunction》.Category: piperazines The author mentioned the following in the article:

A new class of agents with potential utility for the treatment of erectile dysfunction has been discovered, guided by the hypothesis that selective D4 agonists are erectogenic but devoid of the side effects typically associated with dopaminergic agents. The lead agent 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole (1, ABT-724) was discovered by optimization of a series of benzimidazole arylpiperazines. This highly selective D4 agonist was found to be very potent and efficacious in vivo, eliciting penile erections in rats at a dose of 0.03 μmol/kg, with a pos. response rate of 77% erectile incidence. Even at high doses, it was devoid of side effects in animal models of central nervous system behaviors, emesis, or nausea. The structure-activity relationship of the parent benzimidazole series leading to 1 is described, with the detailed in vitro and in vivo profiles described. Distinctive structural features were discovered that are associated with D4 selective agonism in this series of analogs. The experimental process involved the reaction of Abt-724(cas: 70006-24-5Category: piperazines)

Abt-724(cas: 70006-24-5) belongs to piperazines. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Category: piperazines

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

Muraglia, Ester; Kinzel, Olaf; Gardelli, Cristina; Crescenzi, Benedetta; Donghi, Monica; Ferrara, Marco; Nizi, Emanuela; Orvieto, Federica; Pescatore, Giovanna; Laufer, Ralph; Gonzalez-Paz, Odalys; Di Marco, Annalise; Fiore, Fabrizio; Monteagudo, Edith; Fonsi, Massimiliano; Felock, Peter J.; Rowley, Michael; Summa, Vincenzo published an article on February 28 ,2008. The article was titled 《Design and Synthesis of Bicyclic Pyrimidinones as Potent and Orally Bioavailable HIV-1 Integrase Inhibitors》, and you may find the article in Journal of Medicinal Chemistry.SDS of cas: 1688-95-5 The information in the text is summarized as follows:

HIV integrase is one of the three enzymes encoded by HIV genome and is essential for viral replication, but integrase inhibitors as marketed drugs have just very recently started to emerge. In this study, the evolution from the N-methylpyrimidinone structure to bicyclic pyrimidinones, e.g., I and II, is shown. Introduction of a suitably substituted amino moiety modulated the phys.-chem. properties of the mols. and conferred nanomolar activity in the inhibition of spread of HIV-1 infection in cell culture. An extensive SAR study led to sulfamide I, which inhibited the strand transfer with an IC50 of 7 nM and HIV infection in MT4 cells with a CIC95 of 44 nM, and ketoamide II that inhibited strand transfer with an IC50 of 12 nM and the HIV infection in MT4 cells with a CIC95 of 13 nM and exhibited a good pharmacokinetic profile when dosed orally to preclin. species. The experimental process involved the reaction of 4-Methyl-1-piperazinesulfonyl Chloride(cas: 1688-95-5SDS of cas: 1688-95-5)

4-Methyl-1-piperazinesulfonyl Chloride(cas: 1688-95-5) is a member of sulfamide. Sulfamide was used in the synthesis of: Schiff bases of the type ArCH=NSO2NH2; 1H,3H-2,1,3-benzothiadiazin-4-one-2,2-dioxide (BTDD); sulfamide analogs of oleoylethanolamide analogs in a study of PPARα activation.SDS of cas: 1688-95-5

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

The author of 《Synthesis of dithioacetylenic piperazine derivatives》 were Mukanova, M. S.; Sycheva, Ye. S.; Seilkhanov, T. M.; Yu, V. K.. And the article was published in Khimicheskii Zhurnal Kazakhstana in 2019. COA of Formula: C5H12N2 The author mentioned the following in the article:

The conditions for the three-component one-pot synthesis of dithioacetylenic piperazine derivatives was developed. As a result prop-2-yn-1-yl-4-methylpiperazine-1-carbodithioate (73.4%) and prop-2-yn-1-yl-4-diphenylmethylpiperazine-1-carbodithioate (93.6%) were synthesized. Structure of dithioacetylenic piperazine derivatives were established based on IR and NMR(1H and 13C) spectroscopic data. In addition to this study using 1-Methylpiperazine, there are many other studies that have used 1-Methylpiperazine(cas: 109-01-3COA of Formula: C5H12N2) was used in this study.

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..COA of Formula: C5H12N2

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