Tag: 100-200

Optimization of 4-Phenylamino-3-quinolinecarbonitriles as Potent Inhibitors of Src Kinase Activity was written by Boschelli, Diane H.;Ye, Fei;Wang, Yanong D.;Dutia, Minu;Johnson, Steve L.;Wu, Biqi;Miller, Karen;Powell, Dennis W.;Yaczko, Deanna;Young, Mairead;Tischler, Mark;Arndt, Kim;Discafani, Carolyn;Etienne, Carlo;Gibbons, Jay;Grod, Janet;Lucas, Judy;Weber, Jennifer M.;Boschelli, Frank. And the article was included in Journal of Medicinal Chemistry in 2001.Computed Properties of C7H16N2 This article mentions the following:

Subsequent to the discovery of 4-[(2,4-dichlorophenyl)amino]-6,7-dimethoxy-3-quinolinecarbonitrile as an inhibitor of Src kinase activity (IC₅₀ = 30 nM), several addnl. analogs were prepared Optimization of the C-4 anilino group led to I [R = Me]. Replacement of the methoxy group at C-7 with a 3-(morpholin-4-yl)propoxy group provided I [R = morpholinopropyl], resulting in increased inhibition of both Src kinase activity and Src-mediated cell proliferation. Analogs of I [R = morpholinopropyl] with other trisubstituted anilines at C-4 were also potent Src inhibitors, and the propoxy group was preferred over ethoxy, butoxy, or pentoxy. Replacement of the morpholine group with a 4-methylpiperazine group provided I [R = 4-methylpiperazinopropyl], which had an IC₅₀ of 1.2 nM in the Src enzymic assay, an IC₅₀ of 100 nM for the inhibition of Src-dependent cell proliferation and was selective for Src over non-Src family kinases. I [R = 4-methylpiperazinopropyl], which had higher 1 and 4 h plasma levels than I [R = 4-morpholinopropyl], effectively inhibited tumor growth in xenograft models. 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 causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. 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).Computed Properties of C7H16N2

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

Poly(N-acryloyl-N’-propylpiperazine): A New Stimuli-Responsive Polymer was written by Gan, L. H.;Gan, Y. Y.;Deen, G. Roshan. And the article was included in Macromolecules in 2000.Recommanded Product: 1-Propylpiperazine This article mentions the following:

A new water-soluble stimuli-responsive poly(N-acryloyl-N’-propylpiperazine) (PAcrNPP) was synthesized and characterized. The polymer exhibited a lower critical solution temperature (LCST) in water at 37°. The phase transition temperature was highly sensitive to pH changes. The effects of some simple salts and cationic surfactants were studied. The enthalpy of phase separation determined by microcalorimetry was 21.4 kJ mol^-1. This value corresponds to the breaking of one hydrogen bond per monomer unit. Dynamic light scattering studies indicated some aggregations of polymer chains below the LCST. No such aggregations were observed for the lower analogs, poly(N-acryloyl-N’-methylpiperazine) (PAcrNMP) and poly(N-acryloyl-N’-ethylpiperazine) (PAcrNEP) which exhibited no LCST. The crosslinked polymer gels were sensitive to both pH and temperature Their response time to swelling and deswelling was 150 min. The water sorption of the gels was non-Fickian under both acidic and neutral conditions. 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 is a fairly basic compound and is an amine solvent. 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.Recommanded Product: 1-Propylpiperazine

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

Liquid-phase parallel synthesis of 4-sulfanylbenzoic acid derivatives was written by Trifilenkov, A. S.;Il’in, A. P.;Kravchenko, D. V.;Dorogov, M. V.;Tkachenko, S. E.;Ivashchenko, A. V.. And the article was included in Izvestiya Vysshikh Uchebnykh Zavedenii, Khimiya i Khimicheskaya Tekhnologiya in 2005.Category: piperazines This article mentions the following:

Combinatorial libraries of substituted 4-sulfanylbenzamides and their derivatives were synthesized on the basis of 4-fluoro-3-nitrobenzoic acid. The procedure for nucleophilic substitution of fluorine by various thiols has been developed; the resulting 4-sulfenyl-3-nitrobenzoic acids were further converted into the corresponding esters and amides. Oxidation of the sulfide fragment with hydrogen peroxide afforded the corresponding sulfones. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Category: piperazines).

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.Category: piperazines

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

The use of solid-supported reagents for the multi-step synthesis of analytically pure α,β-unsaturated compounds in miniaturized flow reactors was written by Wiles, Charlotte;Watts, Paul;Haswell, Stephen J.. And the article was included in Lab on a Chip in 2007.Electric Literature of C7H16N2 This article mentions the following:

Micro reaction technol. offers a safe, controllable and information rich technique suitable for the long-term production of pharmaceutical agents and fine chems. To date however, few of the syntheses performed using this technol. have addressed the problems associated with product purification The incorporation of multiple supported reagents into EOF-based miniaturized flow reactors for the two-step synthesis of anal. pure compounds is reported. Using this approach, the successful synthesis of 20 α,β-unsaturated compounds in excellent yields (>99.1%) and purities (>99.9%) has been achieved, illustrating significant improvements compared to traditional batch techniques. 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. 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. 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. Electric Literature of C7H16N2

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

1-Amino-4-benzylphthalazines as Orally Bioavailable Smoothened Antagonists with Antitumor Activity was written by Miller-Moslin, Karen;Peukert, Stefan;Jain, Rishi K.;McEwan, Michael A.;Karki, Rajesh;Llamas, Luis;Yusuff, Naeem;He, Feng;Li, Yanhong;Sun, Yingchuan;Dai, Miao;Perez, Lawrence;Michael, Walter;Sheng, Tao;Lei, Huangshu;Zhang, Rui;Williams, Juliet;Bourret, Aaron;Ramamurthy, Arun;Yuan, Jing;Guo, Ribo;Matsumoto, Melissa;Vattay, Anthony;Maniara, Wieslawa;Amaral, Adam;Dorsch, Marion;Kelleher, Joseph F. III. And the article was included in Journal of Medicinal Chemistry in 2009.COA of Formula: C10H12N4 This article mentions the following:

Abnormal activation of the Hedgehog (Hh) signaling pathway has been linked to several types of human cancers, and the development of small-mol. inhibitors of this pathway represents a promising route toward novel anticancer therapeutics. A cell-based screen performed in our laboratories identified a new class of Hh pathway inhibitors, 1-amino-4-benzylphthalazines, e.g. I, that act via antagonism of the Smoothened receptor. A variety of analogs were synthesized and their structure-activity relationships determined This optimization resulted in the discovery of high affinity Smoothened antagonists, one of which was further profiled in vivo. This compound displayed a good pharmacokinetic profile and also afforded tumor regression in a genetic mouse model of medulloblastoma. In the experiment, the researchers used many compounds, for example, 6-(Piperazin-1-yl)nicotinonitrile (cas: 149554-29-0COA of Formula: C10H12N4).

6-(Piperazin-1-yl)nicotinonitrile (cas: 149554-29-0) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. 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: C10H12N4

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

Silica-functionalized N-propylpiperazine for immobilization of palladium nanoparticles as efficient heterogeneous catalyst for cyanation reactions was written by Niknam, Khodabakhsh;Deris, Abdollah;Panahi, Farhad. And the article was included in Cuihua Xuebao in 2013.Recommanded Product: 21867-64-1 This article mentions the following:

An efficient heterogeneous Pd catalytic system has been developed, based on immobilization of Pd nanoparticles (PNPs) on a silica-bonded N-propylpiperazine (SBNPP) substrate. The SBNPP substrate effectively stabilizes the PNPs and improves their stability against aggregation. The catalytic activity of this catalyst was investigated in the cyanation of aryl halides with K₄[Fe(CN)₆] as the cyanide source. The catalyst could be recycled several times without appreciable loss of catalytic activity. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Recommanded Product: 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.Recommanded Product: 21867-64-1

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

Organocatalytic synthesis of novel purine and pyrimidine acyclic nucleosides was written by Palazzolo, Martin A.;Perez-Sanchez, Maria;Iribarren, Adolfo M.;Lewkowicz, Elizabeth S.;Dominguez de Maria, Pablo. And the article was included in Tetrahedron Letters in 2012.Electric Literature of C7H16N2 This article mentions the following:

Organocatalysis is assessed for the first time in the synthesis of purine and pyrimidine acyclic nucleosides providing high yields and straightforward work-up procedures. Nucleobases containing aldehydes are catalytically ligated (C-C bond formation) to acetone or to phosphonate-containing ketones by means of pyrrolidine or silica-immobilized piperazine as amine-based organocatalysts. 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. 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.Electric Literature of C7H16N2

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

Novel and High Affinity 2-[(Diphenylmethyl)sulfinyl]acetamide (Modafinil) Analogues as Atypical Dopamine Transporter Inhibitors was written by Cao, Jianjing;Slack, Rachel D.;Bakare, Oluyomi M.;Burzynski, Caitlin;Rais, Rana;Slusher, Barbara S.;Kopajtic, Theresa;Bonifazi, Alessandro;Ellenberger, Michael P.;Yano, Hideaki;He, Yi;Bi, Guo-Hua;Xi, Zheng-Xiong;Loland, Claus J.;Newman, Amy Hauck. And the article was included in Journal of Medicinal Chemistry in 2016.Safety of 1-Propylpiperazine This article mentions the following:

The development of pharmacotherapeutic treatments of psychostimulant abuse has remained a challenge, despite significant efforts made toward relevant mechanistic targets, such as the dopamine transporter (DAT). The atypical DAT inhibitors have received attention due to their promising pharmacol. profiles in animal models of cocaine and methamphetamine abuse. Herein the authors report a series of modafinil analogs that have an atypical DAT inhibitor profile. The authors extended SAR by chem. manipulating the oxidation states of the sulfoxide and the amide functional groups, halogenating the Ph rings, and/or functionalizing the terminal nitrogen with substituted piperazines, resulting in several novel leads such as 1-(4-(2-((bis(4-fluorophenyl)methyl)sulfinyl)ethyl)piperazin-1-yl)-3-phenylpropan-2-ol (compound 11b), which demonstrated high DAT affinity (K_i = 2.5 nM) and selectivity without producing concomitant locomotor stimulation in mice, as compared to cocaine. These results are consistent with an atypical DAT inhibitor profile and suggest that 11b may be a potential lead for development as a psychostimulant abuse medication. 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. 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.Safety of 1-Propylpiperazine

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

Evaluation of functionalized silica’s for the adsorptive recovery of homogeneous catalysts through interaction with the metal centre was written by Djekic, T.;van der Ham, A. G. J.;de Haan, A. B.. And the article was included in Journal of Chromatography A in 2007.Application of 21867-64-1 This article mentions the following:

The goal of this paper is the evaluation of functionalized silicas for the recovery of homogeneous catalysts by adsorption via its metal center. As model catalysts, we selected bis(triphenylphosphine)cobalt(II)dichloride (CoCl₂(PPh₃)₂), bis(triphenylphosphine)palladium(II)dichloride (PdCl₂(PPh₃)₂) and tris(triphenylphosphine)rhodium(I)dichloride (RhCl(PPh₃)₃). Twelve functionalized groups selected from four classes containing one or more N-, O-, P- or S-atoms were evaluated. A preliminary selection of the adsorbents was done by investigating the adsorption of the metal salts for the cobalt and the palladium complex. The results could be explained by the Hard and Soft Acid Base (HSAB) theory. For the most suitable functionalized adsorbents, these experiments were extended by introducing the ligand in the system which promoted the competition of the functionalized groups on adsorbent and the ligands present in solution These experiments demonstrated that different complex species are adsorbed. 2-(2Pyridyl)ethyl-functionalized silica is selected as a promising adsorbent for adsorption of the CoCl₂(PPh₃)₂ from acetonitrile, while 3-(mercapto)propyl-functionalized silica is selected as a promising adsorbent for adsorption of the PdCl₂(PPh₃)₂ and RhCl(PPh₃)₃ from DMF. The presence of a ligand, an increase of the temperature and the presence of a solvent with the donor properties can decrease the adsorption equilibrium and need to be taken into account. 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 belongs to the family of medicines called anthelmintics. 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 of 21867-64-1

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

Synthesis and investigation of novel benzimidazole derivatives as antifungal agents was written by Chandrika, Nishad Thamban;Shrestha, Sanjib K.;Ngo, Huy X.;Garneau-Tsodikova, Sylvie. And the article was included in Bioorganic & Medicinal Chemistry in 2016.SDS of cas: 21867-64-1 This article mentions the following:

The rise and emergence of resistance to antifungal drugs by diverse pathogenic fungal strains have resulted in an increase in demand for new antifungal agents. Various heterocyclic scaffolds with different mechanisms of action against fungi have been investigated in the past. Herein, we report the synthesis and antifungal activities of 18 alkylated mono-, bis-, and trisbenzimidazole derivatives, their toxicities against mammalian cells, as well as their ability to induce reactive oxygen species (ROS) in yeast cells. Many of our bisbenzimidazole compounds exhibited moderate to excellent antifungal activities against all tested fungal strains, with MIC values ranging from 15.6 to 0.975 μg/mL. The fungal activity profiles of our bisbenzimidazoles were found to be dependent on alkyl chain length. Our most potent compounds were found to display equal or superior antifungal activity when compared to the currently used agents amphotericin B, fluconazole, itraconazole, posaconazole, and voriconazole against many of the strains tested. 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. 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.SDS of cas: 21867-64-1

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