Tag: 100-200

Chemotherapeutically active anthraquinones. II. Aminomethylanthraquinones was written by Winkelmann, E.;Raether, W.. And the article was included in Arzneimittel-Forschung in 1986.SDS of cas: 21867-64-1 This article mentions the following:

Anthraquinones [I, R = OAc, S₂CNEt₂, Sc(:NH)NH₂, NH₂, dialkylamino, heterocyclic, S(CH₂)₂NEt₂, OC₆H₄NH₂, R¹ = H, XR, R² = H, XR, Me, R³ = R⁵ = H, OH, heterocyclic, R⁴ = H, OH] were prepared and tested in vitro and in vivo (in hamster) against Entamoeba闁?em>histolytica and interferon-inducing property in mice. Activity against Trichomonas闁?em>foetus (in mice) was also tested. Most of the compounds showed chemotherapeutic activities in these tests. Structure-activity relations are discussed. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1SDS of cas: 21867-64-1).

1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. 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.SDS of cas: 21867-64-1

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

Synthesis and evaluation of thiopyrano[3,4-c]quinoline-9-carboxamide derivatives as inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1) was written by Park, Chun-Ho;Chun, Kwangwoo;Joe, Bo-Young;Choi, Jong-Hee;Lee, Han-Chang;Ku, Il-Whea;Kim, Hyun Young;Koh, Seong-Ho;Cho, Goang Won;Kim, Seung Hyun;Kim, Myung-Hwa. And the article was included in Medicinal Chemistry Research in 2012.Product Details of 21867-64-1 This article mentions the following:

A series of poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors, 5-oxo-2,4,5,6-tetrahydro-1H-thiopyrano[3,4-c]quinoline-9-carboxamides, were successfully synthesized, and their PARP-1 inhibitory activity was evaluated. These compounds were prepared from the corresponding carboxylate and appropriate amines, and a number of the synthesized compounds were found to have significant PARP-1 activity. Among them, one compound showed potent activity in a PARP-1 enzymic and cell-based assay (IC₅₀ = 0.045 婵炴挾鎷? ED₅₀ = 0.54 婵炴挾鎷?. Mol. modeling confirmed the obtained biol. results. 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. 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. 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.Product Details of 21867-64-1

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

Novel water-soluble sedative-hypnotic agents: isoindolin-1-one derivatives was written by Kanamitsu, Norimasa;Osaki, Takashi;Itsuji, Yutaka;Yoshimura, Masakazu;Tsujimoto, Hisashi;Soga, Manabu. And the article was included in Chemical & Pharmaceutical Bulletin in 2007.Synthetic Route of C7H16N2 This article mentions the following:

The authors developed new i.v. sedative-hypnotic compounds with the isoindolin-1-one skeleton focusing on the water-soluble property and in vivo safety. The authors synthesized approx. 170 derivatives and evaluated their hypnotic effects by i.v. administration of the compounds to mice. A series of the 2-phenyl-3-[2-(4-methyl-1-piperazinyl)-2-oxoethyl]isoindolin-1-one analogs (I–IV) showed potent sedative-hypnotic activity with good water solubility and a wide safety margin. The hypnotic doses (HD₅₀s) of these 4 compounds when administered to mice were 2.35, 1.90, 2.17, and 3.12 mg/kg, resp., and the LDs (LD₅₀s) were 88.67, 64.69, >120, and >120 mg/kg, resp. The therapeutic indexes (LD₅₀/HD₅₀) were 37.73, 34.05, >55.30, and >38.46, resp. Among these IV is being considered as the most potential candidate for clin. trials in humans. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Synthetic Route of 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 鎺矯 and boils at 125閳?30 鎺矯. 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.Synthetic Route of C7H16N2

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

Chemotherapeutically active nitro compounds. 4. 5-Nitroimidazoles. Part II was written by Winkelmann, E.;Raether, W.;Sinharay, A.. And the article was included in Arzneimittel-Forschung in 1978.Application In Synthesis of 1-Propylpiperazine This article mentions the following:

About 190 nitroimidazoles I [R = morpholino, 4-methylpiperazino, N₃, p-ClC₆H₄COCH₂S, PhS, MeOCS₂, H₂NC(:NH)S, MeNH, etc.; R¹ = Me, Et] were prepared Thus, I (R = Cl, R¹ = Me) was treated with 2-mercaptopyridine to give 80% I (R = 2-pyridylthio, R¹ = Me). 1-Methyl-2-(S-isothiouroniummethyl)-5-nitroimidazole-HCl and 2-bromo-5-nitrofuran gave 65% I (R = 5-nitro-2-furylthio, R¹ = Me). The chemotherapeutic effect against several protozoa species was tabulated. Some I were also bactericidal, nematocidal, and fungicidal. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Application In Synthesis of 1-Propylpiperazine).

1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. 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).Application In Synthesis of 1-Propylpiperazine

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

Amino-substituted heterocycles as isosteres of trans-cinnamides: design and synthesis of heterocyclic biaryl sulfides as potent antagonists of LFA-1/ICAM-1 binding was written by Wang, Gary T.;Wang, Sheldon;Gentles, Robert;Sowin, Thomas;Leitza, Sandra;Reilly, Edward B.;von Geldern, Thomas W.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2005.Synthetic Route of C7H16N2 This article mentions the following:

2-Amino-4-Ph pyridine and to a lesser extent, 4-amino-6-Ph pyrimidine were established as isosteres of trans-cinnamide moiety. Applying this isosterism to previously reported p-arylthio cinnamides resulted in the identification of 4-amino-6-(p-arylthio)phenylpyrimidines and 2-amino-4-(p-arylthio)phenylpyridines I (X = N, CH, R¹ = 2-Me₂CH; X = CH, R¹ = 2-MeO, 3,4-OCH₂CH₂O; R²R³N = pyrrolidinyl, 4-hydroxypiperidinyl, 4-formyl-1-piperazinyl, etc.) as potent antagonists of LFA-1/ICAM-1 binding. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Synthetic Route of C7H16N2).

1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. 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.Synthetic Route of C7H16N2

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

Silica-immobilized piperazine: A sustainable organocatalyst for aldol and Knoevenagel reactions was written by Shanmuganathan, Saravanakumar;Greiner, Lasse;Dominguez de Maria, Pablo. And the article was included in Tetrahedron Letters in 2010.Recommanded Product: 1-Propylpiperazine This article mentions the following:

Silica-supported piperazine was found to be an efficient catalyst for aldol reactions of aromatic aldehydes and ketones with straightforward product isolation and catalyst reuse. Furthermore, the catalyst is active in Knoevenagel-type reactions to afford coumarin derivatives, using 2-methyltetrahydrofuran (2-MeTHF) as a novel bio-based solvent. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Recommanded Product: 1-Propylpiperazine).

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. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Recommanded Product: 1-Propylpiperazine

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

New compounds and reactions of sulfonamides with amines. XXXI. Syntheses of some N-[4-[2-(acylamino)ethyl]benzenesulfonyl]-4-alkylpiperazine-1-carboxamides was written by Gajewski, Feliks;Kozakiewicz, Irena. And the article was included in Acta Poloniae Pharmaceutica in 1982.Product Details of 21867-64-1 This article mentions the following:

Nineteen title compounds I (R = Me, R¹ = 2-ClC₆H₄, 3-ClC₆H₄, 2-BrC₆H₄, 2-MeC₆H₄, 4-NO₂C₆H₄, 2,4-Cl₂C₆H₃, 2,5-(MeO)ClC₆H₃, 2-furyl, pyridyl, 2-quinolyl, 2-pyrazinyl, 2-amino-3-pyrazinyl; R = Et, Pr, R¹ = 2,5-(MeO)ClC₆H₃, 2-pyrazinyl; R = Bu, R¹ = 2-pyrazinyl) were prepared as potential hypoglycemic agents. Most I were prepared by heating 4-[R¹CONH(CH₂)₂]C₆H₄SO₂NHCONH₂ with a substituted piperazine in dioxane. I [R = Me, R¹ = 2,5-(MeO)ClC₆H₃] was prepared from 4-[R¹CONH(CH₂)₂]C₆H₄SO₂NHCONHCO₂Me and N-methylpiperazine in PhMe. I (R = Me, R¹ = 2-pyrazinyl) was also obtained via I (R = Me, R¹ = Me) which was deacetylated with aqueous NaOH and the product acylated with pyrazine-2-carboxylic acid chloride in C₆H₁₂. 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. 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. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Product Details of 21867-64-1

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

Influence of external stimuli on the network properties of cationic poly(N-acryloyl-N’-propyl piperazine) hydrogels was written by Deen, G. Roshan;Mah, Chin Hao. And the article was included in Polymer in 2016.Related Products of 21867-64-1 This article mentions the following:

Stimuli-responsive cationic hydrogels based on N-acryloyl-N’-Pr piperazine (AcrNPP) crosslinked with N,N’-methylenebisacrylamide (Mba) and 1,4-butanedioldiacrylate (Bda) were prepared by UV light-initiated free-radical polymerization in bulk. The effect of external stimuli and type of crosslinker on the equilibrium swelling behavior and dynamic swelling was investigated in detail in buffer solution of various pH and temperatures The equilibrium swelling capacity of the gels was large in swelling medium at pH 3.0 than at pH 10.0 due to ionization of polymer network under acidic conditions. With increase in temperature from 25 鎺矯 to 45 鎺矯, the gels exhibited neg. temperature-responsive (thermo-shrinking/thermophobic) behavior with neg. activation energy for diffusion of water. The thermodn. parameters such as Gibbs’ free energy (铻朑), enthalpy (铻朒), and entropy (铻朣) for the swelling of gels as function of temperature were neg. indicating an exothermic swelling process. Water (media) transport mechanism and diffusion process in thin rectangular gels was studied. At pH 3.0, the diffusion process was non-Fickian (anomalous) while at pH 10.0 it was quasi-Fickian. The transport mechanism was partly influenced by the type of crosslinker in the gel. The dynamic swelling data was analyzed using early-time, late-time and Etters diffusion models. From the equilibrium swelling studies the average mol. weight between crosslinks (M_c), the crosslink d. (锜?sub>c), and the mesh size (灏? were determined The M_c was large at pH 3.0 due to ionization of polymer and chain expansion. The exptl. M_c was much larger than the theor. M_c which implied that the gels were loosely crosslinked real networks. The mesh size of gels were between 447 and 786 鑴?in the swollen (ionized) state (pH 3.0), and between 100 and 231 鑴?in the collapsed (non-ionized) state (pH 10.0). The mesh size increased between three to four times during the pH-dependent swelling transition. The state of water in fully swollen hydrogels which influences many important biomaterial properties was determined by differential scanning calorimetry. The bound water content of gels increased linearly with increase in pH of the swelling medium while the unbound water decreased. These hydrogels have potential to be used as controlled drug delivery systems and sorbents for removal of pollutants from water. 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. 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.Related Products of 21867-64-1

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

Design, Synthesis, Biological Screening, and Molecular Docking Studies of Piperazine-Derived Constrained Inhibitors of DPP-IV for the Treatment of Type 2 Diabetes was written by Kushwaha, Ram N.;Srivastava, Rohit;Mishra, Akansha;Rawat, Arun K.;Srivastava, Arvind K.;Haq, Wahajul;Katti, Seturam B.. And the article was included in Chemical Biology & Drug Design in 2015.Application of 149554-29-0 This article mentions the following:

Novel piperazine-derived conformationally constrained compounds were designed, synthesized, and evaluated for in vitro Dipeptidyl peptidase-IV (DPP-IV) inhibitory activities. From a library of compounds synthesized, 1-(2-(4-(7-Chloro-4-quinolyl)piperazin-1-yl)acetyl)pyrrolidine (2g) was identified as a potential DPP-IV inhibitor exhibiting better inhibitory activity than P32/98, reference inhibitor. The in vivo studies carried out in STZ and db/db mice models indicated that the compound 2g showed moderate antihyperglycemic activity as compared to the marketed drug Sitagliptin. A two-week repeated dose study in db/db mice revealed that compound 2g significantly declined blood glucose levels with no evidence of hypoglycemia risk. Furthermore, it showed improvement in insulin resistance reversal and antidyslipidemic properties. Mol. docking studies established good binding affinity of compound 2g at the DPP-IV active site and are in favor of the observed biol. data. These data collectively suggest that compound 2g is a good lead mol. for further optimization studies. In the experiment, the researchers used many compounds, for example, 6-(Piperazin-1-yl)nicotinonitrile (cas: 149554-29-0Application of 149554-29-0).

6-(Piperazin-1-yl)nicotinonitrile (cas: 149554-29-0) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. 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.Application of 149554-29-0

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

Conversion of 4-cyanomethyl-pyrazole-3-carboxamides into CB1 antagonists with lowered propensity to pass the blood-brain-barrier was written by Receveur, Jean-Marie;Murray, Anthony;Linget, Jean-Michel;Norregaard, Pia K.;Cooper, Martin;Bjurling, Emelie;Nielsen, Peter Aadal;Hoegberg, Thomas. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2010.Recommanded Product: 6-(Piperazin-1-yl)nicotinonitrile This article mentions the following:

A series of amides, amidines and amidoximes have been made from the corresponding nitrile compounds, to provide potent antagonists and inverse agonists for the CB1 receptor with considerably lower lipophilicity, higher polar surface area and improved plasma/brain ratios compared to the centrally acting rimonabant. Extensive investigations of ADME and in vivo pharmacol. properties led to selection of the amide series and specifically the 4-(4-fluorophenyl)piperidin-4-ol derivative D4. A clear improvement in the peripheral profile over rimonabant was seen, although some contribution of central effect on the pronounced weight reduction in obese mice cannot be ruled out. In the experiment, the researchers used many compounds, for example, 6-(Piperazin-1-yl)nicotinonitrile (cas: 149554-29-0Recommanded Product: 6-(Piperazin-1-yl)nicotinonitrile).

6-(Piperazin-1-yl)nicotinonitrile (cas: 149554-29-0) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 鎺矯 and boils at 125閳?30 鎺矯. 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.Recommanded Product: 6-(Piperazin-1-yl)nicotinonitrile

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