Month: January 2023

Gas-liquid chromatography of some aliphatic and heterocyclic polyfunctional amines. II. Thermodynamics of the dissolution of amines in fixed phases was written by Andersons, A.;Shimanskaya, M. V.. And the article was included in Latvijas PSR Zinatnu Akademijas Vestis, Kimijas Serija in 1969.Related Products of 21867-64-1 This article mentions the following:

Solution thermodynamics in some nonpolar and polar stationary phases of 19 polyfunctional amines by means of gas-liquid chromatog. has been studied. The heats of solution, the excess heats of solution, the free energies, and entropies of the solution have been estimated The linear dependence of the thermodynamic properties on mol. weight or b.ps. of amines was shown to take place in nonpolar liquid phases. The maximum values of the thermodynamic properties were obtained in cases of polar liquid phases. Specific interactions take place between the amines and polar stationary phases: polyethylene glycols and Reoplex. 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. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 °C and boils at 125â€?30 °C. 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

Synthesis of new and potent analogs of anti-tuberculosis agent 5-nitrofuran-2-carboxylic acid 4-(4-benzylpiperazin-1-yl)benzylamide with improved bioavailability was written by Tangallapally, Rajendra P.;Lee, Robin E. B.;Lenaerts, Anne J. M.;Lee, Richard E.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2006.Synthetic Route of C10H12N4 This article mentions the following:

Previously, the lead compound 5-nitrofuran-2-carboxylic acid 4-(4-benzylpiperazin-1-yl)benzylamide was identified in our anti-tuberculosis drug discovery program. Although this compound demonstrated excellent in vitro activity, it did not meet the expected in vivo profiles due to structural features that resulted in rapid metabolic cleavage and poor absorption, which therefore limited its bioavailability. In efforts to increase the bioavailability, a new series of analogs was successfully synthesized using three modification schemes: replacement of the benzyl group on the piperazine C-ring with carbamate and urea functional groups; introduction of a nitrogen atom into the aromatic ring-B; and expansion of the ring-B to a bicyclic tetrahydroisoquinoline moiety. These modifications retained strong activity and in some case gained superior anti-tuberculosis activity, increased absorption, and serum half life. In the experiment, the researchers used many compounds, for example, 6-(Piperazin-1-yl)nicotinonitrile (cas: 149554-29-0Synthetic Route of C10H12N4).

6-(Piperazin-1-yl)nicotinonitrile (cas: 149554-29-0) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. Although many piperazine derivatives occur naturally, piperazine itself can be synthesized by reacting alcoholic ammonia with 1,2-dichloroethane, by the action of sodium and ethylene glycol on ethylene diamine hydrochloride, or by reduction of pyrazine with sodium in ethanol.Synthetic Route of C10H12N4

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

The use of solid-supported reagents within EOF-based micro reactors was written by Wiles, Charlotte;Watts, Paul;Haswell, Stephen J.. And the article was included in Special Publication – Royal Society of Chemistry in 2004.Formula: C7H16N2 This article mentions the following:

By incorporating a series of silica-supported bases into an EOF (electroosmotic flow)-based flow reactor, we have demonstrated the synthesis of eight condensation products in excellent yields, without the need for addnl. purification steps. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Formula: C7H16N2).

1-Propylpiperazine (cas: 21867-64-1) 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 125â€?30 °C. 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. Formula: C7H16N2

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

Silica-bonded N-propylpiperazine sodium n-propionate as recyclable catalyst for synthesis of 4H-pyran derivatives was written by Niknam, Khodabakhsh;Borazjani, Nassim;Rashidian, Reza;Jamali, Abbas. And the article was included in Cuihua Xuebao in 2013.Computed Properties of C7H16N2 This article mentions the following:

Silica-bonded N-propylpiperazine sodium n-propionate (SBPPSP) was found to act as an efficient solid base for the preparation of a series of 4H-benzo[b]pyran derivatives SBPPSP was used as a recyclable heterogeneous solid base catalyst for the synthesis of 3,4-dihydropyrano[c]chromenes I [R = C₆H₅, 4-BrC₆H₄, 4-ClC₆H₄, etc.], 2-amino-4H-pyrans II, 1,4-dihydropyrano[2,3-c]pyrazoles III and 2-amino-4H-benzo[e]-chromenes IV via condensation reaction of dimedone, Et acetoacetate, 3-methyl-1-phenyl-1H-pyrazol-5(4H)-one, and α-naphthol, resp., with aromatic aldehydes and malononitrile in refluxing aqueous ethanol. The heterogeneous solid base showed similar efficiency when reused in consecutive reactions. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Computed Properties of C7H16N2).

1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Although many piperazine derivatives occur naturally, piperazine itself can be synthesized by reacting alcoholic ammonia with 1,2-dichloroethane, by the action of sodium and ethylene glycol on ethylene diamine hydrochloride, or by reduction of pyrazine with sodium in ethanol.Computed Properties of C7H16N2

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

Discovery of 1,4-Dihydroxy-2-naphthoate Prenyltransferase Inhibitors: New Drug Leads for Multidrug-Resistant Gram-Positive Pathogens was written by Kurosu, Michio;Narayanasamy, Prabagaran;Biswas, Kallolmay;Dhiman, Rakesh;Crick, Dean C.. And the article was included in Journal of Medicinal Chemistry in 2007.Application of 21867-64-1 This article mentions the following:

Since utilization of menaquinone in the electron transport system is a characteristic of Gram-pos. organisms, the 1,4-dihydroxy-2-naphthoate prenyltransferase (MenA) inhibitors (I) and (II) act as selective antibacterial agents against organisms such as methicillin-resistant Staphylococcus aureus (MRSA), Staphylococcus epidermidis (MRSE), and Mycobacterium spp. Growth of drug-resistant Gram-pos. organisms was sensitive to the MenA inhibitors, indicating that menaquinone synthesis is a valid new drug target in Gram-pos. organisms. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Application of 21867-64-1).

1-Propylpiperazine (cas: 21867-64-1) 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 21867-64-1

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

Identification of a 5-HT₄ receptor antagonist clinical candidate through side-chain modification was written by Clark, Robin D.;Jahangir, Alam;Alam, Muzaffar;Rocha, Cynthia;Lin, Lin;Bjorner, Bodil;Nguyen, Khanh;Grady, Carole;Williams, Timothy J.;Stepan, George;Tang, Hai Ming;Ford, Anthony P. D. W.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2005.Quality Control of 1-Propylpiperazine This article mentions the following:

Replacement of the N-Bu side-chain of lead 5-HT₄ receptor antagonist 2 with propanesulfonylpiperidinyl, morpholinyl, and piperazinyl groups led to higher affinity analogs 4-6. In vitro drug metabolism screens and cassette pharmacokinetic studies in the dog led to identification of the N-methylpiperazinyl analog (I), which displayed pharmacokinetic, selectivity, and safety parameters sufficient for advancement to the clinic for the treatment of urinary incontinence. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Quality Control of 1-Propylpiperazine).

1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. 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.Quality Control of 1-Propylpiperazine

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

Antibacterial derivatives of 8-alkyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acids. II. 2-Piperazinyl and 2-(4-alkylpiperazinyl) derivatives was written by Pesson, M.;Antoine, M.;Chabassier, S.;Geiger, S.;Girard, P.;Richer, D.;De Lajudie, P.;Horvath, E.;Leriche, B.;Patte, S.. And the article was included in European Journal of Medicinal Chemistry in 1974.Name: 1-Propylpiperazine This article mentions the following:

Piperazinylpyridopyrimidines I (R = Me, Et, CH2CH2OMe, tetrahydropyranyloxyethyl, CH2CH2OH; R1 = Et; R2 = Me, Et, Pr, allyl, Bu, CH2CH2OH, CH2CH2OMe, CH2CN, CH2CO2Et) were prepared by aminating chloropyridopyrimidines II and were hydrolyzed to acids I (R1 = H). I (R2 = H) were similarly prepared via I (R2 = CHO). I (R1 = H) are bactericidal and their activity is discussed relative to R and R2. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Name: 1-Propylpiperazine).

1-Propylpiperazine (cas: 21867-64-1) 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. 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).Name: 1-Propylpiperazine

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

N,N’-Bisoxalamides Enhance the Catalytic Activity in Cu-Catalyzed Coupling of (Hetero)Aryl Bromides with Anilines and Secondary Amines was written by Bhunia, Subhajit;Kumar, S. Vijay;Ma, Dawei. And the article was included in Journal of Organic Chemistry in 2017.Application of 780705-64-8 This article mentions the following:

N,N’-Bis(furan-2-ylmethyl)oxalamide (BFMO), an inexpensive and conveniently available bidentate ligand, is very effective for promoting Cu-catalyzed N-arylation of anilines and cyclic secondary amines. The method enables coupling of a broad range of (hetero)aryl bromides with various (hetero)aryl amines and cyclic secondary amines at 0.5-5 mol % catalyst loadings at relatively low temperatures For coupling with more sterically hindered acyclic secondary amines, using N,N’-bis(2,4,6-trimethoxyphenyl)oxalamide (BTMPO) as a ligand gives the better results. Addnl., high selectivity is achieved in CuI/BFMO-catalyzed direct monoarylation of piperazine with (hetero)aryl bromides to afford pharmaceutically important building blocks. 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. 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.Application of 780705-64-8

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

Synthesis, biological evaluation and molecular docking studies of 2-piperazin-1-yl-quinazolines as platelet aggregation inhibitors and ligands of integrin α_IIbβ₃ was written by Krysko, Andrei A.;Kornylov, Alexander Yu.;Polishchuk, Pavel G.;Samoylenko, Georgiy V.;Krysko, Olga L.;Kabanova, Tatyana A.;Kravtsov, Victor Ch.;Kabanov, Vladimir M.;Wicher, Barbara;Andronati, Sergei A.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2016.Reference of 162046-66-4 This article mentions the following:

A series of 2-piperazin-1-yl-quinazolines were synthesized and evaluated for their antiaggregative activity. The synthesized small mol. compounds have potently inhibited platelet aggregation in vitro and blocked FITC-Fg binding to α_IIbβ₃ integrin in a suspension of washed human platelets. The key α_IIbβ₃ protein-ligand interactions were determined in docking experiments and some correlations have been observed between values of the affinity and docking scores. In the experiment, the researchers used many compounds, for example, 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid (cas: 162046-66-4Reference of 162046-66-4).

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. 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.Reference of 162046-66-4

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

Fragment-Based Design of Symmetrical Bis-benzimidazoles as Selective Inhibitors of the Trimethoprim-Resistant, Type II R67 Dihydrofolate Reductase was written by Bastien, Dominic;Ebert, Maximilian C. C. J. C.;Forge, Delphine;Toulouse, Jacynthe;Kadnikova, Natalia;Perron, Florent;Mayence, Annie;Huang, Tien L.;Vanden Eynde, Jean Jacques;Pelletier, Joelle N.. And the article was included in Journal of Medicinal Chemistry in 2012.Synthetic Route of C16H22N2O4 This article mentions the following:

The continuously increasing use of trimethoprim as a common antibiotic for medical use and for prophylactic application in terrestrial and aquatic animal farming has increased its prevalence in the environment. This has been accompanied by increased drug resistance, generally in the form of alterations in the drug target, dihydrofolate reductase (DHFR). The most highly resistant variants of DHFR are known as type II DHFR, among which R67 DHFR is the most broadly studied variant. We report the first attempt at designing specific inhibitors to this emerging drug target by fragment-based design. The detection of inhibition in R67 DHFR was accompanied by parallel monitoring of the human DHFR, as an assessment of compound selectivity. By those means, small aromatic mols. of 150-250 g/mol (fragments) inhibiting R67 DHFR selectively in the low millimolar range were identified. More complex, sym. bis-benzimidazoles and a bis-carboxyphenyl were then assayed as fragment-based leads, which procured selective inhibition of the target in the low micromolar range (K_i = 2-4 μM). The putative mode of inhibition is discussed according to mol. modeling supported by in vitro tests. In the experiment, the researchers used many compounds, for example, 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid (cas: 162046-66-4Synthetic Route of C16H22N2O4).

4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid (cas: 162046-66-4) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Although many piperazine derivatives occur naturally, piperazine itself can be synthesized by reacting alcoholic ammonia with 1,2-dichloroethane, by the action of sodium and ethylene glycol on ethylene diamine hydrochloride, or by reduction of pyrazine with sodium in ethanol.Synthetic Route of C16H22N2O4

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