Tag: 200-300

A Kinome-Wide Selective Radiolabeled TrkB/C Inhibitor for in Vitro and in Vivo Neuroimaging: Synthesis, Preclinical Evaluation, and First-in-Human was written by Bernard-Gauthier, Vadim;Bailey, Justin J.;Mossine, Andrew V.;Lindner, Simon;Vomacka, Lena;Aliaga, Arturo;Shao, Xia;Quesada, Carole A.;Sherman, Phillip;Mahringer, Anne;Kostikov, Alexey;Grand’Maison, Marilyn;Rosa-Neto, Pedro;Soucy, Jean-Paul;Thiel, Alexander;Kaplan, David R.;Fricker, Gert;Wangler, Bjorn;Bartenstein, Peter;Schirrmacher, Ralf;Scott, Peter J. H.. And the article was included in Journal of Medicinal Chemistry in 2017.Formula: C9H8ClN3O2 This article mentions the following:

The proto-oncogenes NTRK1/2/3 encode the tropomyosin receptor kinases TrkA/B/C which play pivotal roles in neurobiol. and cancer. We describe herein the discovery of [¹¹C]-(R)-3 ([¹¹C]-(R)-IPMICF16), a first-in-class positron emission tomog. (PET) TrkB/C-targeting radiolabeled kinase inhibitor lead. Relying on extensive human kinome vetting, we show that (R)-3 is the most potent and most selective TrkB/C inhibitor characterized to date. It is demonstrated that [¹¹C]-(R)-3 readily crosses the blood-brain barrier (BBB) in rodents and selectively binds to TrkB/C receptors in vivo, as evidenced by entrectinib blocking studies. Substantial TrkB/C-specific binding in human brain tissue is observed in vitro, with specific reduction in the hippocampus of Alzheimer’s disease (AD) vs. healthy brains. We addnl. provide preliminary translational data regarding the brain disposition of [¹¹C]-(R)-3 in primates including first-in-human assessment. These results illustrate for the first time the use of a kinome-wide selective radioactive chem. probe for endogenous kinase PET neuroimaging in human. In the experiment, the researchers used many compounds, for example, Ethyl 6-chloroimidazo[1,2-b]pyridazine-3-carboxylate (cas: 1150566-27-0Formula: C9H8ClN3O2).

Ethyl 6-chloroimidazo[1,2-b]pyridazine-3-carboxylate (cas: 1150566-27-0) belongs to pyrazine derivatives. Pyrazine has the elements of symmetry for the point group D2h. It has three mutually perpendicular two-fold axes. It also has three mutually perpendicular planes of symmetry. As a result, pyrazine also has a centre of symmetry. Pyrazine and a variety of alkylpyrazines are flavor and aroma compounds found in baked and roasted goods. Tetramethylpyrazine (also known as ligustrazine) is reported to scavenge superoxide anion and decrease nitric oxide production in human Granulocytes.Formula: C9H8ClN3O2

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Two-component gel of a D-π-A-π-D carbazole donor and a fullerene acceptor was written by Xue, Pengchong;Xu, Qiuxia;Gong, Peng;Qian, Chong;Zhang, Zhenqi;Jia, Junhui;Zhao, Xin;Lu, Ran;Ren, Aimin;Zhang, Tierui. And the article was included in RSC Advances in 2013.Electric Literature of C8H4Br2N2 This article mentions the following:

A D-π-A-π-D carbazole derivative (PCQ) with a quinoxaline moiety was designed and synthesized. Its photophys. properties in solution were studied. Moreover, PCQ was found to be a highly efficient gelator toward various apolar and polar organic solvents with the critical gelation concentrations (CGCs) as low as 0.06 wt/vol%. Spectral studies and mol. dynamic stimulation revealed that the intermol. H-bonds and π-π stacking interactions might be responsible for guiding the self-assembly processes and the gel formation. Interestingly, PCQ could construct two-component gel with fullerene derivative driven by intermol. hydrogen bonds. Moreover, the two-component gel film could generate photocurrent under light irradiation, indicating photo-induced electron transfer from the PCQ aggregate to the fullerene derivative In the experiment, the researchers used many compounds, for example, 5,8-Dibromoquinoxaline (cas: 148231-12-3Electric Literature of C8H4Br2N2).

5,8-Dibromoquinoxaline (cas: 148231-12-3) belongs to pyrazine derivatives. Pyrazine has the elements of symmetry for the point group D2h. It has three mutually perpendicular two-fold axes. It also has three mutually perpendicular planes of symmetry. As a result, pyrazine also has a centre of symmetry. Pyrazine-based skeletons were incorporated into agents targeting a range of ailments. Many derivatives were synthesized and evaluated as potential cancer treatments.Electric Literature of C8H4Br2N2

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Donor-Acceptor Polymers for Electrochemical Supercapacitors: Synthesis, Testing, and Theory was written by DiCarmine, Paul M.;Schon, Tyler B.;McCormick, Theresa M.;Klein, Philipp P.;Seferos, Dwight S.. And the article was included in Journal of Physical Chemistry C in 2014.Application of 148231-12-3 This article mentions the following:

Donor-acceptor polymers can store both a pos. and neg. charge allowing them to function as both the pos. and neg. charge storage material in a supercapacitor device, however few were explored for this application. Here, the synthesis is described of several donor-acceptor polymers and their electrodeposited polymer electrodes. Differing mol. structures are used to examine the effect of electron acceptor concentration and show that device stability can be improved significantly by increasing the acceptor concentration Further, the computational insight is provided into the important chem. requirements for achieving even higher performance supercapacitors based on donor-acceptor conjugated polymers. Supercapacitor devices with specific energy and specific power as high as 11 Wh kg^-1 (at 0.5 A g^-1) and 20 kW kg^-1 (at 50 A g^-1 with an energy of 3.6 Wh kg^-1) are reported, which are some of the highest values achieved to date. In the experiment, the researchers used many compounds, for example, 5,8-Dibromoquinoxaline (cas: 148231-12-3Application of 148231-12-3).

5,8-Dibromoquinoxaline (cas: 148231-12-3) belongs to pyrazine derivatives. Pyrazine is a symmetrical molecule with point group D2h. Pyrazine is less basic than pyridine, pyridazine and pyrimidine. Pyrazine heterocycles and their benzo derivatives possess many interesting properties, including chemical reactivity profiles, and have diverse applications in total synthesis, medicine, chemical biology, materials, dyes, and imaging.Application of 148231-12-3

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Are molecular 5,8-π-extended quinoxaline derivatives good chromophores for photoluminescence applications? was written by Mancilha, Fabiana S.;Da Silveira Neto, Brenno A.;Lopes, Aline S.;Moreira, Paulo F. Jr.;Quina, Frank H.;Goncalves, Reinaldo S.;Dupont, Jairton. And the article was included in European Journal of Organic Chemistry in 2006.Recommanded Product: 5,8-Dibromoquinoxaline This article mentions the following:

The synthesis of a new series of photoluminescent compounds, namely 5,8-diarylquinoxalines (aryl = Ph, 4-FC₆H₄,4-MeOC₆H₄, $-NCC₆H₄), was achieved by a direct Suzuki cross-coupling reaction using a NCP-pincer palladacycle. The electrochem. and photophys. properties of these compounds were also investigated. Four new 4,8-diaryl-2,1,3-benzothiadiazoles were also synthesized in order to enable a comparison between the two types of nitrogen-containing π-extended heterocycles. The substitution of a hydrogen atom at the 4-position of the aryl group attached to the quinoxaline or benzothiadiazole base by either electron-donating or -withdrawing groups results in an increase in the bandgap energy (from 2.21 to 2.52 eV) of π-extended 5,8-quinoxaline derivatives and a decrease in the bandgap energy (from 2.65 to 2.40 eV) of π-extended 2,1,3-benzothiadiazoles. Moreover, π-extension at the 5- and 8-positions of the quinoxaline core is not essential for the photoluminescence of these compounds and 4,7-π-extended 2,1,3-benzothiadiazoles are far better candidates for luminescence applications than are the quinoxaline derivatives In the experiment, the researchers used many compounds, for example, 5,8-Dibromoquinoxaline (cas: 148231-12-3Recommanded Product: 5,8-Dibromoquinoxaline).

5,8-Dibromoquinoxaline (cas: 148231-12-3) belongs to pyrazine derivatives. Pyrazines are volatile compounds that are used in the cosmetic, food, flavor, and fragrance industries. Pyrazine-based skeletons were incorporated into agents targeting a range of ailments. Many derivatives were synthesized and evaluated as potential cancer treatments.Recommanded Product: 5,8-Dibromoquinoxaline

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

New, Highly Stable Electrochromic Polymers from 3,4-Ethylenedioxythiophene-Bis-Substituted Quinoxalines toward Green Polymeric Materials was written by Durmus, Asuman;Gunbas, Gorkem E.;Toppare, Levent. And the article was included in Chemistry of Materials in 2007.Recommanded Product: 5,8-Dibromoquinoxaline This article mentions the following:

Two new highly stable electrochromic polymers, poly(5,8-bis(2,3-dihydrothieno[3,4-b][1,4]dioxin-5-yl)-2,3-di(thiophen-2-yl)quinoxaline) (PDETQ) and poly(5,8-bis(2,3-dihydrothieno[3,4-b][1,4]dioxin-5-yl)quinoxaline) (PDEQ) were synthesized, and their potential use as neutral state green polymeric materials was investigated. Spectroelectrochem. showed that both polymers reveal two distinct absorption bands as expected for this type of donor-acceptor polymer, at 410 and 660 nm for PDEQ and 405 and 780 nm for PDETQ. The colorimetry anal. revealed that while PDEQ has a green-blue color, PDETQ showed a saturated green color in the neutral state which is a unique property of conjugated polymers for the completion of the RGB color system. Both polymers have excellent switching properties with satisfactory optical contrasts and very fast switching times. In addition, via both electrochem. and spectral analyses PDETQ was proven to be an n-type dopable polymer. Outstanding optical contrasts in the NIR region, perfect stability, and fast switching times make these polymers excellent candidates for many applications like smart windows and data storage technologies. It should be noted that PDETQ is one of the few examples of neutral state green polymeric materials in literature with a relatively transmissive oxidized state, high stability, and superior switching properties. Hence, PDETQ can be a paramount choice as a green polymeric material for display applications. In the experiment, the researchers used many compounds, for example, 5,8-Dibromoquinoxaline (cas: 148231-12-3Recommanded Product: 5,8-Dibromoquinoxaline).

5,8-Dibromoquinoxaline (cas: 148231-12-3) belongs to pyrazine derivatives. Pyrazine is an N-heterocyclic moiety, and it can be easily prepared from ethylenediamine and 1,2-diketone, α-hydroxyketone, α-methyl ketone. Pyrazine heterocycles and their benzo derivatives possess many interesting properties, including chemical reactivity profiles, and have diverse applications in total synthesis, medicine, chemical biology, materials, dyes, and imaging.Recommanded Product: 5,8-Dibromoquinoxaline

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Three new conjugated polymers based on benzo[2,1-b:3,4-b’]dithiophene: synthesis, characterization, photoinduced charge transfer and theoretical calculation studies was written by Chen, Shaojie;Zhang, Qiuyu;Zhang, Hepeng;Gu, Junwei;Ma, Mingliang;Xin, Tiejun;Zhou, Yanyang;Zhou, Jian;Liu, Qing. And the article was included in Polymer Chemistry in 2012.COA of Formula: C8H4Br2N2 This article mentions the following:

Three new conjugated polymers have been designed and synthesized via the alternate copolymerization of the electron-donating monomer benzodithiophene (BDT) and three different electron-accepting monomers: 5,8-dibromoquinoxaline, 5,8-dibromo-2,3-diphenylquinoxaline, 10,13-dibromodibenzo[a,c]phenazine. The synthesized polymers show good solubility in common organic solvents as well as broader absorptions in the visible region and narrower optical band gaps compared to homopolymers made from BDT units. It is found that the absorptions of the copolymers are red-shifted by increasing the electron-withdrawing ability of the co-monomer. In particular, the absorption edge of the P3 film extends to 778 nm, whereas that of the P1 film is only at 636 nm. Theor. calculation studies of structure-property relations indicated that polymer chains with better coplanarity or π-π* delocalization will lead to lower band gaps. Photoinduced charge transfer (PCT) studies disclosed that exciton dissociation of photoexcited PX (X = 1, 2, 3) via electron-transfer may occur at the interface with CHL-C₆₀, enabling the photogeneration of electrons and holes. The P3/CHL-C₆₀ blended film was chosen as a representative sample to test the applicability of the polymer P3 for energy conversion, a 1.76% PCE was finally obtained. In the experiment, the researchers used many compounds, for example, 5,8-Dibromoquinoxaline (cas: 148231-12-3COA of Formula: C8H4Br2N2).

5,8-Dibromoquinoxaline (cas: 148231-12-3) belongs to pyrazine derivatives. Pyrazines are part of several biologically active polycyclic compounds; examples are quinoxalines, phenazines; and the bio-luminescent natural products pteridines, flavins, and their derivatives. A number of pyrazine-based derivatives were used as dyes or fluorescent probes.COA of Formula: C8H4Br2N2

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Homo- and Copolymers Based on Carbon-Bridged Oligo(p-phenylenevinylene)s for Efficient Fluorescence over the Entire Visible Region was written by Nishioka, Hiroki;Tsuji, Hayato;Nakamura, Eiichi. And the article was included in Macromolecules (Washington, DC, United States) in 2018.COA of Formula: C8H4Br2N2 This article mentions the following:

Highly efficient emissive conjugated polymers are desired for optoelectronic applications. While efficient blue to green emissive polymers have been successfully developed, efficient red emission is still challenging, mainly because of the increased nonradiative process rates upon decreasing the energy gap by extension of the π-system. Suppression of this nonradiative decay would be the key for efficient red-emitting polymers. We have previously developed carbon-bridged oligo(p-phenylenevinylene)s (COPVs), which could be promising backbones for efficient light-emitting polymers because of the suppression of rotational disorder by the rigidified coplanar structures. In this work, we report that a series of COPV-based homopolymers and copolymers show fluorescence over a wide range of the visible region (437-667 nm) with high to excellent fluorescence quantum yield: 0.60-0.94 for the blue to green emission and 0.50 for red. The polymers also exhibited high thermal and electrochem. stabilities, which could be promising for future application in optoelectronic devices. In the experiment, the researchers used many compounds, for example, 5,8-Dibromoquinoxaline (cas: 148231-12-3COA of Formula: C8H4Br2N2).

5,8-Dibromoquinoxaline (cas: 148231-12-3) belongs to pyrazine derivatives. Pyrazine is a symmetrical molecule with point group D2h. Pyrazine is less basic than pyridine, pyridazine and pyrimidine. Substituted pyrazines have been found as subunits of multiple synthetically constructed therapeutic agents, as well as several natural products.COA of Formula: C8H4Br2N2

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

A Kinome-Wide Selective Radiolabeled TrkB/C Inhibitor for in Vitro and in Vivo Neuroimaging: Synthesis, Preclinical Evaluation, and First-in-Human was written by Bernard-Gauthier, Vadim;Bailey, Justin J.;Mossine, Andrew V.;Lindner, Simon;Vomacka, Lena;Aliaga, Arturo;Shao, Xia;Quesada, Carole A.;Sherman, Phillip;Mahringer, Anne;Kostikov, Alexey;Grand’Maison, Marilyn;Rosa-Neto, Pedro;Soucy, Jean-Paul;Thiel, Alexander;Kaplan, David R.;Fricker, Gert;Wangler, Bjorn;Bartenstein, Peter;Schirrmacher, Ralf;Scott, Peter J. H.. And the article was included in Journal of Medicinal Chemistry in 2017.Formula: C9H8ClN3O2 This article mentions the following:

The proto-oncogenes NTRK1/2/3 encode the tropomyosin receptor kinases TrkA/B/C which play pivotal roles in neurobiol. and cancer. We describe herein the discovery of [¹¹C]-(R)-3 ([¹¹C]-(R)-IPMICF16), a first-in-class positron emission tomog. (PET) TrkB/C-targeting radiolabeled kinase inhibitor lead. Relying on extensive human kinome vetting, we show that (R)-3 is the most potent and most selective TrkB/C inhibitor characterized to date. It is demonstrated that [¹¹C]-(R)-3 readily crosses the blood-brain barrier (BBB) in rodents and selectively binds to TrkB/C receptors in vivo, as evidenced by entrectinib blocking studies. Substantial TrkB/C-specific binding in human brain tissue is observed in vitro, with specific reduction in the hippocampus of Alzheimer’s disease (AD) vs. healthy brains. We addnl. provide preliminary translational data regarding the brain disposition of [¹¹C]-(R)-3 in primates including first-in-human assessment. These results illustrate for the first time the use of a kinome-wide selective radioactive chem. probe for endogenous kinase PET neuroimaging in human. In the experiment, the researchers used many compounds, for example, Ethyl 6-chloroimidazo[1,2-b]pyridazine-3-carboxylate (cas: 1150566-27-0Formula: C9H8ClN3O2).

Ethyl 6-chloroimidazo[1,2-b]pyridazine-3-carboxylate (cas: 1150566-27-0) belongs to pyrazine derivatives. Pyrazine has the elements of symmetry for the point group D2h. It has three mutually perpendicular two-fold axes. It also has three mutually perpendicular planes of symmetry. As a result, pyrazine also has a centre of symmetry. Pyrazine and a variety of alkylpyrazines are flavor and aroma compounds found in baked and roasted goods. Tetramethylpyrazine (also known as ligustrazine) is reported to scavenge superoxide anion and decrease nitric oxide production in human Granulocytes.Formula: C9H8ClN3O2

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Two-component gel of a D-π-A-π-D carbazole donor and a fullerene acceptor was written by Xue, Pengchong;Xu, Qiuxia;Gong, Peng;Qian, Chong;Zhang, Zhenqi;Jia, Junhui;Zhao, Xin;Lu, Ran;Ren, Aimin;Zhang, Tierui. And the article was included in RSC Advances in 2013.Electric Literature of C8H4Br2N2 This article mentions the following:

A D-π-A-π-D carbazole derivative (PCQ) with a quinoxaline moiety was designed and synthesized. Its photophys. properties in solution were studied. Moreover, PCQ was found to be a highly efficient gelator toward various apolar and polar organic solvents with the critical gelation concentrations (CGCs) as low as 0.06 wt/vol%. Spectral studies and mol. dynamic stimulation revealed that the intermol. H-bonds and π-π stacking interactions might be responsible for guiding the self-assembly processes and the gel formation. Interestingly, PCQ could construct two-component gel with fullerene derivative driven by intermol. hydrogen bonds. Moreover, the two-component gel film could generate photocurrent under light irradiation, indicating photo-induced electron transfer from the PCQ aggregate to the fullerene derivative In the experiment, the researchers used many compounds, for example, 5,8-Dibromoquinoxaline (cas: 148231-12-3Electric Literature of C8H4Br2N2).

5,8-Dibromoquinoxaline (cas: 148231-12-3) belongs to pyrazine derivatives. Pyrazine has the elements of symmetry for the point group D2h. It has three mutually perpendicular two-fold axes. It also has three mutually perpendicular planes of symmetry. As a result, pyrazine also has a centre of symmetry. Pyrazine-based skeletons were incorporated into agents targeting a range of ailments. Many derivatives were synthesized and evaluated as potential cancer treatments.Electric Literature of C8H4Br2N2

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Donor-Acceptor Polymers for Electrochemical Supercapacitors: Synthesis, Testing, and Theory was written by DiCarmine, Paul M.;Schon, Tyler B.;McCormick, Theresa M.;Klein, Philipp P.;Seferos, Dwight S.. And the article was included in Journal of Physical Chemistry C in 2014.Application of 148231-12-3 This article mentions the following:

Donor-acceptor polymers can store both a pos. and neg. charge allowing them to function as both the pos. and neg. charge storage material in a supercapacitor device, however few were explored for this application. Here, the synthesis is described of several donor-acceptor polymers and their electrodeposited polymer electrodes. Differing mol. structures are used to examine the effect of electron acceptor concentration and show that device stability can be improved significantly by increasing the acceptor concentration Further, the computational insight is provided into the important chem. requirements for achieving even higher performance supercapacitors based on donor-acceptor conjugated polymers. Supercapacitor devices with specific energy and specific power as high as 11 Wh kg^-1 (at 0.5 A g^-1) and 20 kW kg^-1 (at 50 A g^-1 with an energy of 3.6 Wh kg^-1) are reported, which are some of the highest values achieved to date. In the experiment, the researchers used many compounds, for example, 5,8-Dibromoquinoxaline (cas: 148231-12-3Application of 148231-12-3).

5,8-Dibromoquinoxaline (cas: 148231-12-3) belongs to pyrazine derivatives. Pyrazine is a symmetrical molecule with point group D2h. Pyrazine is less basic than pyridine, pyridazine and pyrimidine. Pyrazine heterocycles and their benzo derivatives possess many interesting properties, including chemical reactivity profiles, and have diverse applications in total synthesis, medicine, chemical biology, materials, dyes, and imaging.Application of 148231-12-3

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem