Month: February 2023

Kinetic study of the decomposition of hydrogen peroxide catalyzed by Co(II) acetylacetonate supported on a silica-propylpiperazine matrix was written by Oliveira, Severino F.;Espinola, Jose G. P.;Lemus, Wolfango Eloy S.;de Souza, Antonio G.;Airoldi, Claudio. And the article was included in Colloids and Surfaces, A: Physicochemical and Engineering Aspects in 1998.Related Products of 21867-64-1 This article mentions the following:

The catalytic decomposition of hydrogen peroxide by Co(II)acetylacetonate supported on a propylpiperazine-silica matrix (Co(II)(acac)-PPS) was studied in aqueous media. The results showed that the reaction was first order in H₂O₂. It was found that the reaction rate was pH dependent with a maximum at around pH=8. Activation parameters were determined in the temperature range 30-45°C. The low value obtained for the activation energy is in accordance with the proposed free-radical mechanism. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Related Products of 21867-64-1).

1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Piperazine is an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines.Related Products of 21867-64-1

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

Discovery and Development of First-in-Class ACKR3/CXCR7 Superagonists for Platelet Degranulation Modulation was written by Bayrak, Alp;Mohr, Florian;Kolb, Kyra;Szpakowska, Martyna;Shevchenko, Ekaterina;Dicenta, Valerie;Rohlfing, Anne-Katrin;Kudolo, Mark;Pantsar, Tatu;Guenther, Marcel;Kaczor, Agnieszka A.;Poso, Antti;Chevigne, Andy;Pillaiyar, Thanigaimalai;Gawaz, Meinrad;Laufer, Stefan A.. And the article was included in Journal of Medicinal Chemistry in 2022.Application In Synthesis of tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate This article mentions the following:

The atypical chemokine receptor 3 (ACKR3), formerly known as CXC-chemokine receptor 7 (CXCR7), has been postulated to regulate platelet function and thrombus formation. Herein, we report the discovery and development of first-in-class ACKR3 agonists, which demonstrated superagonistic properties with E_max values of up to 160% compared to the endogenous reference ligand CXCL12 in a β-arrestin recruitment assay. Initial in silico screening using an ACKR3 homol. model identified two hits, C10 (EC₅₀ 19.1 μM) and C11 (EC₅₀ 11.4 μM). Based on these hits, extensive structure-activity relationship studies were conducted by synthesis and testing of derivatives It resulted in the identification of the novel thiadiazolopyrimidinone-based compounds 26 (LN5972, EC₅₀ = 3.4 μM) and 27 (LN6023, EC₅₀ = 3.5 μM). These compounds are selective for ACKR3 vs. CXCR4 and show metabolic stability. In a platelet degranulation assay, these agonists effectively reduced P-selectin expression by up to 97%, suggesting potential candidates for the treatment of platelet-mediated thrombosis. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate (cas: 373608-48-1Application In Synthesis of tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate).

tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate (cas: 373608-48-1) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.Application In Synthesis of tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate

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

Synthesis of substituted 4-oxo-7-sulfamoyl-2,3,4,5-tetrahydrobenzo[b][1,4]thiazepines was written by Kravchenko, D. V.;Ivanovskii, S. A.;Korsakov, M. K.;Dorogov, M. V.;Tkachenko, S. E.;AsHchenko, A. V.. And the article was included in Izvestiya Vysshikh Uchebnykh Zavedenii, Khimiya i Khimicheskaya Tekhnologiya in 2005.Product Details of 21867-64-1 This article mentions the following:

A combinatorial library of substituted 4-oxo-7-sulfamoyl-2,3,4,5-tetrahydrobenzo[b][1,4]thiazepines was synthesized via chlorosulfonylation of tetrahydrobenzothiazepinones followed by reaction with a range of primary and secondary amines. Physicochem. parameters of some of the products, such as lipophilicity, number of rotating bonds and number of hydrogen bond donors and acceptors have been calculated In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Product Details of 21867-64-1).

1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. Product Details of 21867-64-1

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

Synthesis, Antibacterial and Anthelmintic Activity of Novel 3-(3-Pyridyl)-oxazolidinone-5-methyl Ester Derivatives was written by Jin, Bo;Chen, Jia-yi;Sheng, Zun-lai;Sun, Meng-qing;Yang, Hong-liang. And the article was included in Molecules in 2022.Related Products of 119285-07-3 This article mentions the following:

In this study, a series of 3-(3-pyridyl)-oxazolidone-5-Me ester derivatives I [X = O, C(O)CH₂Bn, C(O)NCy, etc.; R¹ = C(O)Me, C(O)Cy, S(O)₂Me, etc.] was synthesized and characterized by ¹H NMR, ¹³C NMR and LC-MS. The conducted screening antibacterial studies of the new 3-(3-pyridyl)-oxazolidone-5-Me ester derivatives I established that the Me sulfonic acid esters have broad activity spectrum toward Staphylococcus aureus, Streptococcus pneumoniae, Bacillus subtilis and Staphylococcus epidermidis. Among them, compound I [X = O; R¹ = C(O)NCy] was the most potent activity, with an MIC of 16μg/mL against B.subtilis and could reduce the instantaneous growth rate of bacteria. Furthermore, mol. docking studies were also simulated for compound I [X = O; R¹ = C(O)NCy] to predict the specific binding mode of this compound In addition, anthelmintic activity of these compounds was also evaluated against adult Indian earthworms (Pheretima posthuman). The results showed that compound I [X = O, R¹ = C(O)Cy] had the best effect. These results above could provided exptl. reference for the development of novel antibacterial and anthelmintic drugs. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(5-aminopyridin-2-yl)piperazine-1-carboxylate (cas: 119285-07-3Related Products of 119285-07-3).

tert-Butyl 4-(5-aminopyridin-2-yl)piperazine-1-carboxylate (cas: 119285-07-3) belongs to piperazine derivatives. The piperazine scaffold is often found in biologically active compounds in different therapeutic areas. These therapeutic areas include antifungals, antidepressants, antivirals, and serotonin receptor (5-HT) antagonists/agonists. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.Related Products of 119285-07-3

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

Producing of a novel condensed heterocycles and combinatorial libraries on the basis of 2-amino-5-bromopyridine-3-sulfochloride was written by Dorogov, M. V.;Solov’ev, M. Yu.;Kravchenko, D. V.;Blyumina, M. V.;Tkachenko, S. E.;Ivashchenko, A. V.. And the article was included in Izvestiya Vysshikh Uchebnykh Zavedenii, Khimiya i Khimicheskaya Tekhnologiya in 2005.COA of Formula: C7H16N2 This article mentions the following:

2-Amino-5-bromopyridine-3-sulfonyl chloride (I) was readily prepared by chlorosulfonylation of 2-amino-5-bromopyridine. Subsequent amination of I with primary or secondary amines or with amino acids, such as sarcosine or β-alanine, gave the libraries of the corresponding 2-amino-5-bromo-3-pyridinesulfonamides and 2-amino-5-bromo-3-pyridinesulfonylamino-substituted carboxylic acids, resp. The latter were further amidated with various primary and secondary amines to afford the libraries of pyridylsulfonylamino-functionalized carboxamides. On the other hand, N-(2-amino-5-bromopyridine-3-sulfonyl)-N-Me aminoacetic acid, available from I and sarcosine, undergoes intramol. cyclization on treatment with 1,1′-carbonyldiimidazole (CDI) at 40-100° to form novel pyrido[2,3-f][1,2,5]thiadiazepinone S,S-dioxide II. The reaction of N,N’-unsubstituted 2-amino-5-bromopyridine-3-sulfonamide with succinic anhydride afforded novel trioxocyclopenta[3,4]pyrido[2,3-e][1,2,4]thiadiazine III, which readily reacts with amines in the presence of CDI to provide the combinatorial library of pyrido[2,3-e][1,2,4]thiadiazines IV (R¹R²NH is primary or secondary aliphatic cycloaliphatic, aromatic or heterocyclic amine). The mol. parameters, such as mol. weight, lipophilicity or a total number of hydrogen bond donors and acceptors, have been calculated for some of the products. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1COA of Formula: C7H16N2).

1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. 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).COA of Formula: C7H16N2

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

Non-imidazole histamine H₃ ligands. Part III. New 4-n-propylpiperazines as non-imidazole histamine H₃-antagonists was written by Walczynski, Krzysztof;Zuiderveld, Obbe P.;Timmerman, Henk. And the article was included in European Journal of Medicinal Chemistry in 2005.Safety of 1-Propylpiperazine This article mentions the following:

Propylpiperazinyl benzoxazoles, benzothiazoles, oxazolopyridines, and thiazolopyridines I [X = O, S; Y, Z, A, B = CH, N (either none or one of the variable groups is N)] and their hydrobromide salts are prepared as selective histamine H₃ receptor antagonists; their histamine H₃ antagonist activities and the relationship between their structures and activities are discussed. Propylpiperazinyl-substituted thiazolopyridines and a propylpiperazinyl-substituted benzothiazole are better histamine H₃ antagonists than propylpiperazinyl-substituted oxazolopyridines and a propylpiperazinyl-substituted benzooxazole. I (X = S; Y = A = B = CH; Z = N) is the most potent histamine H₃ antagonist of the series, with a pA₂ value of 7.25, while the corresponding oxazolopyridine I (X = O; Y = A = B = CH; Z = N) has a pA₂ value of 6.9. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Safety of 1-Propylpiperazine).

1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Safety of 1-Propylpiperazine

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

Benzamide capped peptidomimetics as non-ATP competitive inhibitors of CDK2 using the REPLACE strategy was written by Premnath, Padmavathy Nandha;Craig, Sandra N.;Liu, Shu;McInnes, Campbell. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2016.Category: piperazines This article mentions the following:

Inhibition of cyclin dependent kinase 2 (CDK2) in complex with cyclin A in G1/S phase of the cell cycle has been shown to promote selective apoptosis of cancer cells through the E2F1 pathway. An alternative approach to catalytic inhibition is to target the substrate recruitment site also known as the cyclin binding groove (CBG) to generate selective non-ATP competitive inhibitors. The REPLACE strategy has been applied to identify fragment alternatives and substituted benzoic acid derivatives were evaluated as a promising scaffold to present appropriate functionality to mimic key peptide determinants. Fragment Ligated Inhibitory Peptides (FLIPs) are described which potently inhibit both CDK2/cyclin A and CDK4/cyclin D1 and have preliminary antitumor activity. A structural rationale for binding was obtained through mol. modeling further demonstrating their potential for further development as next generation non ATP competitive CDK inhibitors. In the experiment, the researchers used many compounds, for example, 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid (cas: 162046-66-4Category: piperazines).

4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid (cas: 162046-66-4) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.Category: piperazines

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

Photocatalyzed Dehydrogenation of Aliphatic N-Heterocycles Releasing Dihydrogen was written by Ritu;Das, Saikat;Tian, Ya-Ming;Karl, Tobias;Jain, Nidhi;Konig, Burkhard. And the article was included in ACS Catalysis in 2022.Application of 780705-64-8 This article mentions the following:

Author’s report the iridium-nickel dual photocatalytic acceptorless and redox neutral dehydrogenation of aliphatic heterocycles yielding cyclic alkenes without overoxidn. at room temperature Excitation of the iridium photocatalyst initiates the formation of a nickel hydride intermediate that yields alkenes and H₂ via β-hydride elimination. The reaction proceeds regioselectively and the scope was demonstrated by the synthesis of 12 biol. relevant mols. and drugs. In addition, com. and easily available N-heterocyclic alkane starting materials were converted into functionalized alkenes of high synthetic and com. value using the method. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(pyrimidin-2-yl)piperazine-1-carboxylate (cas: 780705-64-8Application of 780705-64-8).

tert-Butyl 4-(pyrimidin-2-yl)piperazine-1-carboxylate (cas: 780705-64-8) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.Application of 780705-64-8

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

Bis(β-haloethyl)amines. VII. A new synthesis of N-monoalkylpiperazines was written by Prelog, V.;Stepan, V.. And the article was included in Collection of Czechoslovak Chemical Communications in 1935.Electric Literature of C7H16N2 This article mentions the following:

The N- and N,N’ -substituted piperazines are readily obtained by interaction of primary amines with (XCH₂CH₂)₂NR (X = Cl or, better, Br). (HOCH₂CH₂)₂NMe (I) (60 g.) in 100 g. 48% HBr, evaporated to a sirup and heated 6 hrs. at 160-80°, yields 66% (BrCH₂CH₂)₂NMe (II), m. 151-2° (picrate, m. 121-2°). In 170 g. CHCl₃, 20 g. I and 87 g. SOCl₂, refluxed 1 hr. give 56% (ClCH₂CH₂)₂NMe (III), m. 116-17°. Refluxed 15 hrs. in 100 cc. MeOH, 48 g. II and 28 g. PhNH₂ give, after fractional distillation, 58% N-methyl-N’-phenylpiperazine (IV), b₃ 140-2°; similarly, III gives the HCl salt, m. 233.5°, in 26% yield. With MeI. IV gives an impure methiodide, m. 238-9°, which with AgCl yields a methochloride, decomposing at 215°. Treated with NaNO₂ followed by SO₂ (cf. Friedländer, III, 957), IV is decomposed to N-methyl-piperazine (V), b. 134-6° (dihydrochloride monohydrate, m. 242-3°; dichloroplatinate; dipicrate, decomposing at 272°; addition compound with CS₂, subliming without decomposition about 180°). With BzCl, V gives C₁₂H₁₇ON₂Cl, m. 240°. Prepared like II, in 58% yield, (BrCH₂CH₂)₂NEt m. 170° (picrate, m. 120.5°) and yields 63.5% N-ethyl-N’-phenylpiperazine,m. 50-1°. This, with NaNO₂, gives the unstable di-HCl salt of N-ethyl-N’-p-nitrosophenylpiperazine, decomposing near 210°, which with SO₂ yields N-ethylpiperazine (di-HCl salt, m. 210-11°; dipicrate,decomposes at 257°). Similarly obtained are (BrCH₂CH₂)₂N-Pr, m. 157° (picrate, m. 101-2°); N-propyl-N’-phenylpiperazine, b<0.1 102-3° (HBr salt, m. 231-2°) and N-propylpiperazine (di-HCl salt, decomposes at 256°; dipicrate, m. 241-2° (decomposition)). In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Electric Literature of C7H16N2).

1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.Electric Literature of C7H16N2

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

Discovery of A031 as effective proteolysis targeting chimera (PROTAC) androgen receptor (AR) degrader for the treatment of prostate cancer was written by Chen, Linrong;Han, Liuquan;Mao, Shujun;Xu, Ping;Xu, Xinxin;Zhao, Ruibo;Wu, Zhihua;Zhong, Kai;Yu, Guangliang;Wang, Xiaolei. And the article was included in European Journal of Medicinal Chemistry in 2021.Formula: C16H22N2O4 This article mentions the following:

Herein the design, synthesis, and biol. evaluation of highly effective proteolysis targeting chimeras (PROTAC) androgen receptor (AR) degraders, such as compound I was reported. It could induce the degradation of AR protein in VCaP cell lines in a time-dependent manner, achieving the IC₅₀ value of less than 0.25μM. The I was 5 times less toxic than EZLA and works with an appropriate half-life (t 1/2) or clearance rate (Cl). Also, it had a significant inhibitory effect on tumor growth in zebrafish transplanted with human prostate cancer (VCaP). Therefore, I provided a further idea of developing novel drugs for prostate cancer. In the experiment, the researchers used many compounds, for example, 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid (cas: 162046-66-4Formula: C16H22N2O4).

4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid (cas: 162046-66-4) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 °C and boils at 125–130 °C. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.Formula: C16H22N2O4

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