Day: December 6, 2022

Taylor, E. G. published the artcileDicyanotriazole. I. The conductance of dilute aqueous solutions of dicyanotriazole at 25°, Product Details of C4HN5, the publication is Canadian Journal of Research, Section B: Chemical Sciences (1942), 161-7, database is CAplus.

Previous exptl. studies of dicyanotriazole resulted in statements that the compound is an acid comparable in strength with the strong mineral acids. In the present work, measurements of the equivalent conductivity of dicyanotriazole in dilute aqueous solution give the dissociation constant of the acid as 3.378 × 10^-2 at 25°; this shows it to be an acid possessing about the same strength as dichloroacetic acid. The limiting equivalent conductivity of dicyanotriazole at 25° is 384.9. The earlier work gave 397.44.

Canadian Journal of Research, Section B: Chemical Sciences published new progress about 53817-16-6. 53817-16-6 belongs to triazoles, auxiliary class Triazoles, name is 1H-1,2,3-Triazole-4,5-dicarbonitrile, and the molecular formula is C17H23BO4, Product Details of C4HN5.

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

Salamone, John D. published the artcilePreladenant, a novel adenosine A_2A receptor antagonist for the potential treatment of parkinsonism and other disorders, Formula: C25H29N9O3, the publication is IDrugs (2010), 13(10), 723-731, database is CAplus.

A review. Adenosine A_2A receptor antagonists exert antiparkinsonian effects in animal models and several drugs in this class are currently being assessed in clin. trials. Preladenant (SCH-420814) is an adenosine A_2A receptor antagonist with a high affinity and very high selectivity for adenosine A_2A receptors, which is being developed by Merck & Co Inc (following its acquisition of Schering-Plough Corp) for the potential treatment of Parkinson’s disease. Preclin. studies in rodent and primate models of parkinsonism demonstrated that preladenant can reverse the motor impairments induced by dopamine depletion or antagonism. Phase I and II clin. trials indicated that preladenant was well tolerated. Moreover, preladenant met its major endpoints by reducing OFF time and increasing ON time in L-DOPA-treated patients with Parkinson’s disease, without worsening dyskinesias. Therefore, preladenant may have considerable utility for the treatment of Parkinson’s disease, as well as the parkinsonian side effects of dopamine D₂ receptor antagonists. As research has suggested that adenosine A_2A receptor antagonists are active in animal models of effort-based decision making, it is possible that preladenant could also be useful for treating energy-related symptoms, such as fatigue, psychomotor retardation and anergia in patients with parkinsonism or depression. At the time of publication, phase III clin. trials were recruiting patients with Parkinson’s disease.

IDrugs 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, Formula: C25H29N9O3.

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

Salamone, John D published the artcilePreladenant, a novel adenosine A(2A) receptor antagonist for the potential treatment of parkinsonism and other disorders., Related Products of triazoles, the publication is IDrugs : the investigational drugs journal (2010), 13(10), 723-31, database is MEDLINE.

Adenosine A(2A) receptor antagonists exert antiparkinsonian effects in animal models and several drugs in this class are currently being assessed in clinical trials. Preladenant (SCH-420814) is an adenosine A(2A) receptor antagonist with a high affinity and very high selectivity for adenosine A(2A) receptors, which is being developed by Merck & Co Inc (following its acquisition of Schering-Plough Corp) for the potential treatment of Parkinson’s disease. Preclinical studies in rodent and primate models of parkinsonism demonstrated that preladenant can reverse the motor impairments induced by dopamine depletion or antagonism. Phase I and II clinical trials indicated that preladenant was well tolerated. Moreover, preladenant met its major endpoints by reducing OFF time and increasing ON time in l-DOPA-treated patients with Parkinson’s disease, without worsening dyskinesias. Therefore, preladenant may have considerable utility for the treatment of Parkinson’s disease, as well as the parkinsonian side effects of dopamine D2 receptor antagonists. As research has suggested that adenosine A(2A) receptor antagonists are active in animal models of effort-based decision making, it is possible that preladenant could also be useful for treating energy-related symptoms, such as fatigue, psychomotor retardation and anergia in patients with parkinsonism or depression. At the time of publication, phase III clinical trials were recruiting patients with Parkinson’s disease.

IDrugs : the investigational drugs journal 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, Related Products of triazoles.

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

Ritchie, James P. published the artcileStructures and energies of the tautomers and conjugate bases of some 1,2,4-triazolones, Recommanded Product: 4H-1,2,4-Triazole, the publication is Journal of Organic Chemistry (1989), 54(15), 3553-60, database is CAplus.

MO calculations at the AM1, 3-21G//3-21G, and 6-31G^*//3-21G levels were performed for several possible tautomers of 1,2,4-triazol-5-one and 3-nitro-1,2,4-triazol-5-one. Calculations were also performed at the AM1, 3-21G//3-21G, and 6-31+G//3-21G levels for some conjugate bases of these compounds The results show the 1H,4H tautomer to be most stable. 5-Hydroxy-1H-1,2,4-triazole and 3-nitro-5-hydroxy-1H-1,2,4-triazole are found to lie 9.4 and 7.5 kcal/mol, resp., higher in energy than the corresponding 1H,4H isomer. The calculations may overestimate this relative energy by perhaps 1-3 kcal/mol. The calculations also predict deprotonation is most likely at N-4 of the lowest energy triazolone, but nearly equally likely at N-1 and N-4 for the corresponding nitrotriazolone (although the N-4 position is slightly favored). The substitution effects of the nitro group were examined by comparing calculated geometries, relative energies, and electrostatic potentials of the triazolones and nitrotriazolones. Electronegativity effects predominate for the neutral compounds In the conjugate bases, a significant contribution from resonance participation of the nitro group was found. Problems in using the electrostatic potential to predict the site of electrophilic substitution in the triazolone are discussed.

Journal of Organic Chemistry published new progress about 63598-71-0. 63598-71-0 belongs to triazoles, auxiliary class Triazole, name is 4H-1,2,4-Triazole, and the molecular formula is C2H3N3, Recommanded Product: 4H-1,2,4-Triazole.

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

Pinna, Annalisa published the artcileNovel investigational adenosine A_2A receptor antagonists for Parkinson’s disease, Application of 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 Expert Opinion on Investigational Drugs (2009), 18(11), 1619-1631, database is CAplus and MEDLINE.

A review. The development of non-dopaminergic therapies for Parkinson’s disease (PD) has attracted much interest in recent years. Among new classes of drugs, adenosine A_2A antagonists have emerged as the best candidates. BIIB014, preladenant and ST-1535 are new adenosine A_2A antagonists currently in Phase I and II clin. trials for evaluation of their efficacy in patients with PD. All these compounds have been proven safe and well tolerated. Moreover, results from Phase II trials also demonstrate that BIIB014 and preladenant are effective in reducing the waking time spent in OFF state in patients at the late stage of PD treated with L-DOPA. BIIB014 is also efficacious as monotherapy in patients at the early stage of PD. Finally, ST-1535, at this time, displays a very promising potential in exptl. models of PD and a safe profile in clin. studies. This review summarizes pharmacol. data available on these three A_2A antagonists, their effects in animal models of PD and their profiles in clin. trials.

Expert Opinion on Investigational Drugs 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, Application of 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

Pinna, Annalisa published the artcileAdenosine A_2A Receptor Antagonists in Parkinson’s Disease: Progress in Clinical Trials from the Newly Approved Istradefylline to Drugs in Early Development and Those Already Discontinued, Safety of 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 CNS Drugs (2014), 28(5), 455-474, database is CAplus and MEDLINE.

A review. Neurotransmitters other than dopamine, such as norepinephrine, 5-hydroxytryptamine, glutamate, adenosine and acetylcholine, are involved in Parkinson’s disease (PD) and contribute to its symptomatol. Thus, the progress of non-dopaminergic therapies for PD has attracted much interest in recent years. Among new classes of drugs, adenosine A₂A antagonists have emerged as promising candidates. The development of new highly selective adenosine A₂A receptor antagonists, and their encouraging anti-parkinsonian responses in animal models of PD, has provided a rationale for clin. trials to evaluate the therapeutic potential and the safety of these agents in patients with PD. To date, the clin. research regarding A_2A antagonists and their potential utilization in PD therapy continues to evolve between drugs just or previously discontinued (preladenant and vipadenant), new derivatives in development (tozadenant, PBF-509, ST1535, ST4206 and V81444) and the relatively old drug istradefylline, which has finally been licensed as an anti-parkinsonian drug in Japan. All these compounds have been shown to have a good safety profile and be well tolerated. Moreover, results from phase II and III trials also demonstrate that A₂A antagonists are effective in reducing off-time, without worsening troublesome dyskinesia, and in increasing on-time with a mild increase of non-troublesome dyskinesia, in patients at an advanced stage of PD treated with L-DOPA. In addition, early findings suggest that A_2A antagonists might also be efficacious as monotherapy in patients at an early stage of PD. This review summarizes pharmacol. and clin. data available on istradefylline, tozadenant, PBF-509, ST1535, ST4206, V81444, preladenant and vipadenant.

CNS Drugs 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, Safety of 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

Noorpoor, Zeinab published the artcileThe needle trap extraction capability of a zinc-based metal organic framework with a nitrogen rich ligand, Related Products of triazoles, the publication is Journal of Coordination Chemistry (2021), 74(13), 2213-2226, database is CAplus.

A triple ring nitrogen rich ligand 4,5-Di(1H-tetrazol-5-yl)-2H-1,2,3-triazole (Hdttz) and along that a three-dimensional, zinc-based metal organic framework (MOF) were synthesized. The synthesized MOF was characterized by Fourier transform IR spectroscopy (FT-IR), powder X-ray diffraction (PXRD), energy dispersive X-ray spectroscopy and mapping, SEM (SEM) and Brunauer-Emmett-Teller (BET) analyses. The extraction capability of the synthesized nanostructure was examined toward some analytes as model compounds Properties such as porous structure and considerable surface area make it a suitable and efficient extractive phase. The extraction efficiency of the Zn-based MOF was evaluated for headspace needle trap extraction (HS-NTE) of benzene homologs (BTEX) as model compounds from aquatic media in conjunction with gas chromatog.-mass spectrometry (GC-MS). To increase the sensitivity of the method, parameters including the extraction and desorption conditions were optimized. For some environmental water samples, acceptable relative recovery (RR) values at the concentration level of 20 ng L^-1 ranged from 85 to 96% and showing no significant matrix effect.

Journal of Coordination Chemistry published new progress about 53817-16-6. 53817-16-6 belongs to triazoles, auxiliary class Triazoles, name is 1H-1,2,3-Triazole-4,5-dicarbonitrile, and the molecular formula is C4HN5, Related Products of triazoles.

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

Neuman, Peter N. published the artcileNitro derivatives of phenyl-1,2,3-triazole, Application In Synthesis of 14544-45-7, the publication is Journal of Heterocyclic Chemistry (1971), 8(1), 51-6, database is CAplus.

A number of tri- and tetranitro-N-phenyl-1,2,3-triazolyl compounds were synthesized by a combination of condensation, cycloaddition, and nitration reactions, and their crystal densities, impact sensitivities, and thermal stabilities were determined

Journal of Heterocyclic 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

Liu, Tao published the artcileSynthesis of new antifungal agents-triazole propanol derivatives containing nitrogen, Quality Control of 86386-77-8, the publication is Zhongguo Yaowu Huaxue Zazhi (2002), 12(6), 333-336, database is CAplus.

1-(R-amino)-2-(2,4-difluorophenyl)-3-(1H-1,2,4-triazol-1-yl)- 2-propanol (R = R’-Ph, cyclopropyl, or Me and R’ = H, chloro, Me, ethoxy, or methoxy) hydrochloride or succinate were synthesized by acylating 1,3-difluorobenzene with chloroacetyl chloride, substituting with 1H-1,2,4-triazole, allowing to react with trimethylsulfoxonium iodide, and ring-opening with RNH₂. 11 Compounds were synthesized, their structures were confirmed by IR and ¹H-NMR, and their antifungal activities were tested. Among the 11 compounds, 10 compounds had antifungal activities to different degrees.

Zhongguo Yaowu Huaxue Zazhi published new progress about 86386-77-8. 86386-77-8 belongs to triazoles, auxiliary class Epoxides,Triazole,Fluoride,Salt,Sulfonic acid,Benzene, name is 1-((2-(2,4-Difluorophenyl)oxiran-2-yl)methyl)-1H-1,2,4-triazole methanesulfonate, and the molecular formula is C12H13F2N3O4S, Quality Control of 86386-77-8.

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

Kohler, E. P. published the artcileIsoxazoline oxides. VIII, Application In Synthesis of 53817-16-6, the publication is Journal of the American Chemical Society (1928), 221-8, database is CAplus.

cf. C. A. 21, 583. An investigation of the process by which MeOH-KOAc transforms certain α-bromo-γ-nitro ketones into β-hydroxy-γ-oximido esters indicates that the primary product of the reaction is an isoxazoline oxide. The action of Na₂CO₃ in dry MeOH upon PhCH(CH₂NO₂)CHBrBz gives a mixture of 3 isomeric benzoylphenylnitrocyclopropanes, m. 95° (previously known), 88° and 140-2° and the hydroxamic ether, PhCH[C(OMe):NOH]CH(OH)Bz (I), crystallizing with 1 mol. Me₂CO, m. 190° (decomposition); the solution in cold 20% aqueous NaOH gives with Ac₂O the acetate, m. 185° (decomposition); on standing the solution gives hydroxamic acid, m. about 160° (decomposition); acids appear to rearrange I to the isomeric oximido ester. trans-α-Phenyl-β-benzoylacrylic acid, m. 220°, is the final product of the degradation of these derivatives by acids; its structure was established by oxidation and synthesis.

Journal of the American Chemical Society published new progress about 53817-16-6. 53817-16-6 belongs to triazoles, auxiliary class Triazoles, name is 1H-1,2,3-Triazole-4,5-dicarbonitrile, and the molecular formula is C4HN5, Application In Synthesis of 53817-16-6.

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