Robinson, Sarel J.’s team published research in Bioorganic & Medicinal Chemistry Letters in 26 | CAS: 377727-87-2

Bioorganic & Medicinal Chemistry Letters published new progress about 377727-87-2. 377727-87-2 belongs to triazoles, auxiliary class GPCR/G Protein,Adenosine Receptor, name is 2-(Furan-2-yl)-7-(2-(4-(4-(2-methoxyethoxy)phenyl)piperazin-1-yl)ethyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine, and the molecular formula is C25H29N9O3, Recommanded Product: 2-(Furan-2-yl)-7-(2-(4-(4-(2-methoxyethoxy)phenyl)piperazin-1-yl)ethyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine.

Robinson, Sarel J. published the artcileCarbamate substituted 2-amino-4,6-diphenylpyrimidines as adenosine receptor antagonists, Recommanded Product: 2-(Furan-2-yl)-7-(2-(4-(4-(2-methoxyethoxy)phenyl)piperazin-1-yl)ethyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine, the publication is Bioorganic & Medicinal Chemistry Letters (2016), 26(3), 734-738, database is CAplus and MEDLINE.

A novel series of carbamate substituted 2-amino-4,6-diphenylpyrimidines was evaluated as potential dual adenosine A1 and A2A receptor antagonists. The majority of the synthesized compounds exhibited promising dual affinities, with A1Ki values ranging from 0.175 to 10.7 nM and A2AKi values ranging from 1.58 to 451 nM. The in vivo activity illustrated for 3-(2-amino-6-phenylpyrimidin-4-yl)phenyl morpholine-4-carboxylate (4c) is indicative of the potential of these compounds as therapeutic agents in the treatment of Parkinson’s disease, although physicochem. properties may require optimization.

Bioorganic & Medicinal Chemistry Letters published new progress about 377727-87-2. 377727-87-2 belongs to triazoles, auxiliary class GPCR/G Protein,Adenosine Receptor, name is 2-(Furan-2-yl)-7-(2-(4-(4-(2-methoxyethoxy)phenyl)piperazin-1-yl)ethyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine, and the molecular formula is C25H29N9O3, Recommanded Product: 2-(Furan-2-yl)-7-(2-(4-(4-(2-methoxyethoxy)phenyl)piperazin-1-yl)ethyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine.

Referemce:
https://en.wikipedia.org/wiki/1,2,3-Triazole,
Triazoles – an overview | ScienceDirect Topics

Meldal, Morten et al. published their research in Angewandte Chemie, International Edition in 2010 | CAS: 156311-83-0

((3H-[1,2,3]Triazolo[4,5-b]pyridin-3-yl)oxy)tri(pyrrolidin-1-yl)phosphonium hexafluorophosphate(V) (cas: 156311-83-0) belongs to triazole derivatives. Triazoles are important five-member nitrogen heterocycles involved in a wide range of industrial applications such as agrochemicals, corrosion inhibitors, dyes, optical brighteners, as well as biologically active agents. 1,2,3-Triazoles are usually prepared following (3+2) cycloaddition protocols. A common technique for unsubstituted triazoles is the Huisgen azide-alkyne 1,3-dipolar cycloaddition: a azide and an alkyne react at high temperature to form a ring. However, the Huisgen strategy produces a mixture of isomers (typically 1,4- and 1,5-disubstituted) when used to produce substituted triazoles.Application In Synthesis of ((3H-[1,2,3]Triazolo[4,5-b]pyridin-3-yl)oxy)tri(pyrrolidin-1-yl)phosphonium hexafluorophosphate(V)

Microparticle Matrix Encoding of Beads was written by Meldal, Morten;Christensen, Soeren Flygering. And the article was included in Angewandte Chemie, International Edition in 2010.Application In Synthesis of ((3H-[1,2,3]Triazolo[4,5-b]pyridin-3-yl)oxy)tri(pyrrolidin-1-yl)phosphonium hexafluorophosphate(V) The following contents are mentioned in the article:

The authors present a versatile, simple encoding principle that may solve many problems in solid-phase screening and decoding: optical microparticle matrix encoding (MPM encoding) with fluorescent microparticles. The utility of this technique has been demonstrated in the identification of avidin ligands from a focused library, in which compounds could not be distinguished with mass spectrometric methods. The library design was based upon previously reported L– and D-amino acid libraries for avidin and streptavidin, thus indicating selectivity for aromatic residues. Uniform 10 μm Tentagel microparticles labeled with a chem. stable fluorophore ATOTA [tris(dialkylamino)trioxatriangulenium ion] were randomly distributed in a bis(acrylamido)polyethylene glycol (PEG) macromonomer (64,000 cm-3) by ultrasound and homogenization. Inverse suspension polymerization of the microparticle-containing macromonomer in the presence of bis(tert-butyldiphenylmethylsilyl)PEG1500 stabilizer provided 500,000 uniform, amino-functionalized, uniquely encoded beads (72 mL; ca 6.5 g dry weight), which contained an average of 8 microparticles per bead, with a bead size of (550±100) μm. This study involved multiple reactions and reactants, such as ((3H-[1,2,3]Triazolo[4,5-b]pyridin-3-yl)oxy)tri(pyrrolidin-1-yl)phosphonium hexafluorophosphate(V) (cas: 156311-83-0Application In Synthesis of ((3H-[1,2,3]Triazolo[4,5-b]pyridin-3-yl)oxy)tri(pyrrolidin-1-yl)phosphonium hexafluorophosphate(V)).

((3H-[1,2,3]Triazolo[4,5-b]pyridin-3-yl)oxy)tri(pyrrolidin-1-yl)phosphonium hexafluorophosphate(V) (cas: 156311-83-0) belongs to triazole derivatives. Triazoles are important five-member nitrogen heterocycles involved in a wide range of industrial applications such as agrochemicals, corrosion inhibitors, dyes, optical brighteners, as well as biologically active agents. 1,2,3-Triazoles are usually prepared following (3+2) cycloaddition protocols. A common technique for unsubstituted triazoles is the Huisgen azide-alkyne 1,3-dipolar cycloaddition: a azide and an alkyne react at high temperature to form a ring. However, the Huisgen strategy produces a mixture of isomers (typically 1,4- and 1,5-disubstituted) when used to produce substituted triazoles.Application In Synthesis of ((3H-[1,2,3]Triazolo[4,5-b]pyridin-3-yl)oxy)tri(pyrrolidin-1-yl)phosphonium hexafluorophosphate(V)

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Muttenthaler, Markus et al. published their research in Journal of Medicinal Chemistry in 2010 | CAS: 156311-83-0

((3H-[1,2,3]Triazolo[4,5-b]pyridin-3-yl)oxy)tri(pyrrolidin-1-yl)phosphonium hexafluorophosphate(V) (cas: 156311-83-0) belongs to triazole derivatives. Triazoles exhibit substantial isomerism, depending on the positioning of the nitrogen atoms within the ring. The presence of the three nitrogen atoms in triazole structures afforded opportunities for a plethora of structural modification with the generation of novel therapeutically potential agents, which is different from other heterocyclic compounds.Recommanded Product: 156311-83-0

Modulating Oxytocin Activity and Plasma Stability by Disulfide Bond Engineering was written by Muttenthaler, Markus;Andersson, Asa;de Araujo, Aline D.;Dekan, Zoltan;Lewis, Richard J.;Alewood, Paul F.. And the article was included in Journal of Medicinal Chemistry in 2010.Recommanded Product: 156311-83-0 The following contents are mentioned in the article:

Disulfide bond engineering is an important approach to improve the metabolic half-life of cysteine-containing peptides. Eleven analogs of oxytocin were synthesized including disulfide bond replacements by thioether, selenylsulfide, diselenide, and ditelluride bridges, and their stabilities in human plasma and activity at the human oxytocin receptor were assessed. The cystathionine (Ki = 1.5 nM, and EC50 = 32 nM), selenylsulfide (Ki = 0.29/0.72 nM, and EC50 = 2.6/154 nM), diselenide (Ki = 11.8 nM, and EC50 = 18 nM), and ditelluride analogs (Ki = 7.6 nM, and EC50 = 27.3 nM) retained considerable affinity and functional potency as compared to oxytocin (Ki = 0.79 nM, and EC50 = 15 nM), while shortening the disulfide bridge abolished binding and functional activity. The mimetics showed a 1.5-3-fold enhancement of plasma stability as compared to oxytocin (t1/2 = 12 h). By contrast, the all-D-oxytocin and head to tail cyclic oxytocin analogs, while significantly more stable with half-lives greater than 48 h, had little or no detectable binding or functional activity. This study involved multiple reactions and reactants, such as ((3H-[1,2,3]Triazolo[4,5-b]pyridin-3-yl)oxy)tri(pyrrolidin-1-yl)phosphonium hexafluorophosphate(V) (cas: 156311-83-0Recommanded Product: 156311-83-0).

((3H-[1,2,3]Triazolo[4,5-b]pyridin-3-yl)oxy)tri(pyrrolidin-1-yl)phosphonium hexafluorophosphate(V) (cas: 156311-83-0) belongs to triazole derivatives. Triazoles exhibit substantial isomerism, depending on the positioning of the nitrogen atoms within the ring. The presence of the three nitrogen atoms in triazole structures afforded opportunities for a plethora of structural modification with the generation of novel therapeutically potential agents, which is different from other heterocyclic compounds.Recommanded Product: 156311-83-0

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Pryde, David C.’s team published research in Journal of Medicinal Chemistry in 49 | CAS: 14544-45-7

Journal of Medicinal Chemistry published new progress about 14544-45-7. 14544-45-7 belongs to triazoles, auxiliary class Triazoles, name is 5-Nitro-1H-1,2,3-triazole, and the molecular formula is C2H2N4O2, Application In Synthesis of 14544-45-7.

Pryde, David C. published the artcileNovel Selective Inhibitors of Neutral Endopeptidase for the Treatment of Female Sexual Arousal Disorder. Synthesis and Activity of Functionalized Glutaramides, Application In Synthesis of 14544-45-7, the publication is Journal of Medicinal Chemistry (2006), 49(14), 4409-4424, database is CAplus and MEDLINE.

Female sexual arousal disorder (FSAD) is a highly prevalent sexual disorder affecting up to 40% of women. Efforts to identify a selective neutral endopeptidase (NEP) inhibitor as a potential treatment for FSAD are reported. The rationale for this approach, together with a description of the medicinal chem. strategy, lead compounds, and SAR investigations are detailed. In particular, the strategy of starting with the clin. precedented selective NEP inhibitor, Candoxatrilat, and targeting low mol. weight and relatively polar mono-carboxylic acids is described. This led ultimately to the prototype development candidate I, for which detailed pharmacol. and pharmacokinetic parameters are presented.

Journal of Medicinal Chemistry published new progress about 14544-45-7. 14544-45-7 belongs to triazoles, auxiliary class Triazoles, name is 5-Nitro-1H-1,2,3-triazole, and the molecular formula is C2H2N4O2, Application In Synthesis of 14544-45-7.

Referemce:
https://en.wikipedia.org/wiki/1,2,3-Triazole,
Triazoles – an overview | ScienceDirect Topics

Tong, Bi-hai’s team published research in RSC Advances in 6 | CAS: 219508-27-7

RSC Advances published new progress about 219508-27-7. 219508-27-7 belongs to triazoles, auxiliary class Trifluoromethylated Building Blocks, name is 2-[5-(Trifluoromethyl)-1H-1,2,4-triazol-3-yl]pyridine, and the molecular formula is C10H16O2, Category: triazoles.

Tong, Bi-hai published the artcileHigh-brightness solution-processed phosphorescent OLEDs with pyrimidine-based iridium(III) complexes, Category: triazoles, the publication is RSC Advances (2016), 6(41), 34970-34976, database is CAplus.

Two heteroleptic cyclometalated iridium(III) complexes, Ir(ppm)2(pic) and Ir(ppm)2(taz), using 4,6-di-Ph pyrimidine (Hppm) as a cyclometalating ligand, were successfully synthesized and characterized. Strong emission at 555 and 532 nm with high photoluminescence quantum yields of 83% and 86% in PMMA at 298 k were obtained for Ir(ppm)2(pic) and Ir(ppm)2(taz), resp. Solution-processed organic light-emitting diodes (OLEDs) based on Ir(ppm)2(pic) and Ir(ppm)2(taz) showed high-brightness of 112 233 and 125 072 cd m-2, peak current efficiencies of 30.6 and 40.4 cd A-1 and maximum external quantum efficiencies of 10.4 and 17.3%, resp., accompanied by very low efficiency roll-off values. The ancillary ligand taz tuned the emission to saturated green, and more importantly, it can significantly increase the spectral stability and device efficiency.

RSC Advances published new progress about 219508-27-7. 219508-27-7 belongs to triazoles, auxiliary class Trifluoromethylated Building Blocks, name is 2-[5-(Trifluoromethyl)-1H-1,2,4-triazol-3-yl]pyridine, and the molecular formula is C10H16O2, Category: triazoles.

Referemce:
https://en.wikipedia.org/wiki/1,2,3-Triazole,
Triazoles – an overview | ScienceDirect Topics

Guney, Emre’s team published research in Nature Communications in 7 | CAS: 377727-87-2

Nature Communications published new progress about 377727-87-2. 377727-87-2 belongs to triazoles, auxiliary class GPCR/G Protein,Adenosine Receptor, name is 2-(Furan-2-yl)-7-(2-(4-(4-(2-methoxyethoxy)phenyl)piperazin-1-yl)ethyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine, and the molecular formula is C25H29N9O3, HPLC of Formula: 377727-87-2.

Guney, Emre published the artcileNetwork-based in silico drug efficacy screening, HPLC of Formula: 377727-87-2, the publication is Nature Communications (2016), 10331, database is CAplus and MEDLINE.

The increasing cost of drug development together with a significant drop in the number of new drug approvals raises the need for innovative approaches for target identification and efficacy prediction. Here, we take advantage of our increasing understanding of the network-based origins of diseases to introduce a drug-disease proximity measure that quantifies the interplay between drugs targets and diseases. By correcting for the known biases of the interactome, proximity helps us uncover the therapeutic effect of drugs, as well as to distinguish palliative from effective treatments. Our anal. of 238 drugs used in 78 diseases indicates that the therapeutic effect of drugs is localized in a small network neighborhood of the disease genes and highlights efficacy issues for drugs used in Parkinson and several inflammatory disorders. Finally, network-based proximity allows us to predict novel drug-disease associations that offer unprecedented opportunities for drug repurposing and the detection of adverse effects.

Nature Communications published new progress about 377727-87-2. 377727-87-2 belongs to triazoles, auxiliary class GPCR/G Protein,Adenosine Receptor, name is 2-(Furan-2-yl)-7-(2-(4-(4-(2-methoxyethoxy)phenyl)piperazin-1-yl)ethyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine, and the molecular formula is C25H29N9O3, HPLC of Formula: 377727-87-2.

Referemce:
https://en.wikipedia.org/wiki/1,2,3-Triazole,
Triazoles – an overview | ScienceDirect Topics

Shainyan, B. A.’s team published research in Russian Journal of General Chemistry in 85 | CAS: 14544-45-7

Russian Journal of General Chemistry published new progress about 14544-45-7. 14544-45-7 belongs to triazoles, auxiliary class Triazoles, name is 5-Nitro-1H-1,2,3-triazole, and the molecular formula is C14H28O5S, Name: 5-Nitro-1H-1,2,3-triazole.

Shainyan, B. A. published the artcileTriflamidomethyl and oxymethyl derivatives of 1,2,3-triazoles, Name: 5-Nitro-1H-1,2,3-triazole, the publication is Russian Journal of General Chemistry (2015), 85(10), 2309-2312, database is CAplus.

The reactions of some 1,2,3-triazoles with formaldehyde and triflamide have been studied. N-(Hydroxy-methyl)-2-phenyl-2H-1,2,3-triazole-4-carboxamide reacted with triflamide in sulfuric acid to afford 2-phenyl-2H-1,2,3-triazole-4-carboxamide, bis(triflamido)methane, and N,N-bis[(trifluoromethylsulfonyl)aminomethyl]-triflamide. In the presence of K2CO3, 4-amino-5-nitro-2-ethyl-1,2,3-triazole was reduced with hydrazine hydrate to 2-ethyl-2H-1,2,3-triazole-4,5-diamine, and with formaldehyde in the presence of K2CO3, it resulted in N,N-bis(2-ethyl-5-nitro-2H-1,2,3-triaxol-4-yl)methanediamine, which reacted with paraformaldehyde under acidic conditions with the formation of 4-aminomethyl-5-nitro-2-ethyl-1,2,3-triazole.

Russian Journal of General Chemistry published new progress about 14544-45-7. 14544-45-7 belongs to triazoles, auxiliary class Triazoles, name is 5-Nitro-1H-1,2,3-triazole, and the molecular formula is C14H28O5S, Name: 5-Nitro-1H-1,2,3-triazole.

Referemce:
https://en.wikipedia.org/wiki/1,2,3-Triazole,
Triazoles – an overview | ScienceDirect Topics

Tao, Peng’s team published research in Organic Electronics in 45 | CAS: 219508-27-7

Organic Electronics published new progress about 219508-27-7. 219508-27-7 belongs to triazoles, auxiliary class Trifluoromethylated Building Blocks, name is 2-[5-(Trifluoromethyl)-1H-1,2,4-triazol-3-yl]pyridine, and the molecular formula is C15H21BO3, Formula: C8H5F3N4.

Tao, Peng published the artcileHighly efficient thienylquinoline-based phosphorescent iridium(III) complexes for red and white organic light-emitting diodes, Formula: C8H5F3N4, the publication is Organic Electronics (2017), 293-301, database is CAplus.

Highly efficient 2-(thiophen-2-yl)quinoline-based phosphorescent iridium(III) complexes bearing 2-(3-(trifluoromethyl)-1H-1,2,4-triazol-5-yl)pyridine or picolinic acid as ancillary ligands are designed and synthetised. The variation of ancillary ligands is attempted to finely tune the photophys. properties of these complexes, especially the solution phosphorescent quantum yields (ΦPL), full width at half maximum (FWHM), etc. The picolinic acid-based complex displays the slightly red-shifted dual-peak emission compared to triazolpyridine-based one. The complexes show bright emission with broad FWHM up to 83 nm, and the emissions are in red region with the very high absolute ΦPL up to 0.76 in solution Moreover, high-performance red and three-color-based white organic light-emitting diodes (OLEDs) with excellent color stability have been fabricated. The maximum external quantum efficiencies of red and white OLEDs can reach 16.2% and 15.1%, resp. The maximum current efficiency and power efficiency of white OLED are as high as 35.5 cd A-1 and 34.0 lm W-1, resp. Especially, the designed white OLED exhibits excellent spectral stability under wide operating voltage range, and the 1931 Commission Internationale de L’Eclairage of white OLED only changes from (0.43, 0.42) to (0.44, 0.44), the color rendering index is in a narrow range of 75-77.

Organic Electronics published new progress about 219508-27-7. 219508-27-7 belongs to triazoles, auxiliary class Trifluoromethylated Building Blocks, name is 2-[5-(Trifluoromethyl)-1H-1,2,4-triazol-3-yl]pyridine, and the molecular formula is C15H21BO3, Formula: C8H5F3N4.

Referemce:
https://en.wikipedia.org/wiki/1,2,3-Triazole,
Triazoles – an overview | ScienceDirect Topics

Zuniga-Ramirez, Carlos’s team published research in Future Neurology in 8 | CAS: 377727-87-2

Future Neurology published new progress about 377727-87-2. 377727-87-2 belongs to triazoles, auxiliary class GPCR/G Protein,Adenosine Receptor, name is 2-(Furan-2-yl)-7-(2-(4-(4-(2-methoxyethoxy)phenyl)piperazin-1-yl)ethyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine, and the molecular formula is C20H19NO4, Category: triazoles.

Zuniga-Ramirez, Carlos published the artcilePreladenant: an adenosine A2A receptor antagonist for Parkinson’s disease, Category: triazoles, the publication is Future Neurology (2013), 8(6), 639-648, database is CAplus.

A review. Preladenant (SCH 420814) is a potent selective antagonist at the adenosine A2A receptor that is being studied for treatment in early Parkinson’s disease (PD) as a monotherapy, and in moderate-to-severe PD as an add on to levodopa therapy. Unlike other drugs used for this disease, preladenant modulates adenosine action at the striatal level in order to block the inhibitory action of the basal ganglia output nuclei. Animal models of PD suggested that preladenant could be an effective treatment, which was further supported in a Phase II study of subjects with idiopathic PD who demonstrated a benefit in reducing off-time with an increase in on-time. In this article, we review current perspectives concerning pharmacol. approaches to PD, the pharmacol. properties of preladenant, its efficiency and safety, as well as the results reported for parkinsonian subjects treated with this drug.

Future Neurology published new progress about 377727-87-2. 377727-87-2 belongs to triazoles, auxiliary class GPCR/G Protein,Adenosine Receptor, name is 2-(Furan-2-yl)-7-(2-(4-(4-(2-methoxyethoxy)phenyl)piperazin-1-yl)ethyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine, and the molecular formula is C20H19NO4, Category: triazoles.

Referemce:
https://en.wikipedia.org/wiki/1,2,3-Triazole,
Triazoles – an overview | ScienceDirect Topics

Sams, Anette G.’s team published research in Journal of Medicinal Chemistry in 54 | CAS: 377727-87-2

Journal of Medicinal Chemistry published new progress about 377727-87-2. 377727-87-2 belongs to triazoles, auxiliary class GPCR/G Protein,Adenosine Receptor, name is 2-(Furan-2-yl)-7-(2-(4-(4-(2-methoxyethoxy)phenyl)piperazin-1-yl)ethyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine, and the molecular formula is C25H29N9O3, HPLC of Formula: 377727-87-2.

Sams, Anette G. published the artcileDiscovery of Phosphoric Acid Mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} Ester (Lu AA47070): A Phosphonooxymethylene Prodrug of a Potent and Selective hA2A Receptor Antagonist, HPLC of Formula: 377727-87-2, the publication is Journal of Medicinal Chemistry (2011), 54(3), 751-764, database is CAplus and MEDLINE.

The discovery and structure-activity relationship of a series of hA2A receptor antagonists is described. Compound 28 was selected from the series as a potent and selective compound and was shown to be efficacious in an in vivo model of Parkinson’s disease. It had acceptable ADME properties; however, the low intrinsic solubility of this compound was limiting for its developability, because the oral bioavailability from dosing in suspension was significantly lower than the oral bioavailability from solution dosage. As a consequence, prodrugs of 28 were prepared with dramatically increased aqueous solubility The prodrugs efficiently delivered 28 into systemic circulation, with no detectable levels of prodrug in plasma samples. From this investigation, we selected 32 (Lu AA47070), a phosphonooxymethylene prodrug of 28, as a drug candidate.

Journal of Medicinal Chemistry published new progress about 377727-87-2. 377727-87-2 belongs to triazoles, auxiliary class GPCR/G Protein,Adenosine Receptor, name is 2-(Furan-2-yl)-7-(2-(4-(4-(2-methoxyethoxy)phenyl)piperazin-1-yl)ethyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine, and the molecular formula is C25H29N9O3, HPLC of Formula: 377727-87-2.

Referemce:
https://en.wikipedia.org/wiki/1,2,3-Triazole,
Triazoles – an overview | ScienceDirect Topics