Month: December 2022

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

Keshavarz, Mohammad Hossein published the artcileA New General Correlation for Predicting Impact Sensitivity of Energetic Compounds, Name: 4-Nitro-2H-1,2,3-triazole, the publication is Propellants, Explosives, Pyrotechnics (2013), 38(6), 754-760, database is CAplus.

This paper describes an improved simple model for prediction of impact sensitivity of different classes of energetic compounds containing nitropyridines, nitroimidazoles, nitropyrazoles, nitrofurazanes, nitrotriazoles, nitropyrimidines, polynitroarenes, benzofuroxans, polynitroarenes with α-CH, nitramines, nitroaliphatics, nitroaliph. containing other functional groups, and nitrate energetic compounds The model is based on some mol. structural parameters. It is applied for 90 explosives, which have different mol. structures. The predicted results are compared with outputs of complex neural network approach as one of the best available methods. Root mean squares (rms) of deviations of different energetic compounds are 24 and 49 cm, corresponding to 5.88 and 12.01 J with 2.5 kg dropping mass, for new and neural network methods, resp. The novel model also predicts good results for eight new synthesized and miscellaneous explosives with respect to exptl. data.

Propellants, Explosives, Pyrotechnics published new progress about 84406-63-3. 84406-63-3 belongs to triazoles, auxiliary class Triazole,Nitro Compound, name is 4-Nitro-2H-1,2,3-triazole, and the molecular formula is C2H2N4O2, Name: 4-Nitro-2H-1,2,3-triazole.

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

Jano, Issam published the artcileComparison between approximate methods for calculating ionization potentials and the use of σ-ionization potentials as a measure of relative basicity of azoles, Safety of 4H-1,2,4-Triazole, the publication is Journal of Physical Chemistry (1991), 95(20), 7694-9, database is CAplus.

Approx. methods for calculating valence-shell ionization energies are compared at the INDO level of approximation These methods are based on Koopmans, many-body Green function, and perturbation theories. The method based on perturbation theory is presented for the first time in this work. Some characteristics and limitations of these methods are pointed out. In addition, a linear relationship between the σ-ionization potentials of azole mols. and their protonation energies is found and analyzed on the basis of Mulliken’s resonance structure theory of the charge-transfer complexes. It is concluded that the polarization, charge-transfer, and exchange energies are responsible for the stabilization of the protonated systems, whereas the electrostatic energy plays a rather small and destabilizing role.

Journal of Physical 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, Safety of 4H-1,2,4-Triazole.

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

Hauser, Robert A. published the artcileFuture Treatments for Parkinson’s Disease: Surfing the PD Pipeline, HPLC of Formula: 377727-87-2, the publication is International Journal of Neuroscience (2011), 121(S2), 53-62, database is CAplus and MEDLINE.

A review. Our current wish list for the treatment of Parkinson’s disease (PD) includes therapies that will provide robust and sustained antiparkinsonian benefit through the day, ameliorate or prevent dyskinesia, and slow or prevent the progression of the disease. In this article, I review selected new therapies in clin. development for motor features or treatment complications of PD, and some that may slow disease progression. These include adenosine 2a (A2a) antagonists (istradefylline, preladenant, and SYN115), levodopa/carbidopa intestinal gel (LCIG), IPX066-an extended-release formulation of carbidopa/levodopa, XP21279-a sustained-release levodopa prodrug, ND0611-a carbidopa s.c. patch, safinamide-a mixed mechanism of action medication that may provide both MAO-B and glutamate inhibition, PMY50028-an oral neurotrophic factor inducer, antidyskinesia medications (AFQ056 and fipamezole), and gene therapies (AAV2-neurturin and glutamic acid decarboxylase gene transfer). Some of these therapies will never be proven efficacious and will not come to market while others may play a key role in the future treatment of PD.

International Journal of Neuroscience 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

Gryszkiewicz-Trochimowski, E. published the artcileComposition and structure of the polymer of hydrocyanic acid, Related Products of triazoles, the publication is Roczniki Chemii (1928), 165-74, database is CAplus.

cf. C. A. 17, 1424; 18, 1985; Bull. soc. chim. 35, 366(1924). The formula of a 4,5-dicyano-1,2,3-triazole proposed for the polymer (I) by G. is made probable by Bedel’s finding that I is C₄H₄N₄. It was confirmed by condensation with glyoxylic acid. When prepared by polymerazation of an aqueous (90%) HCN with 10% aqueous NH₃ at the b. p. the product is black and the yield very small. A brown product with a yield of 20-5% is obtained by using anhydrous HCN containing 0.5% KCN at room temperature The crystals are easily separated form amorphous matter by extraction with boiling ether or cold acetone. The acetone extract is evaporated at room temperature since it reacts on heating. I recrystallized from water or aqueous MeOH with bone coal, is almost colorless, m. 180° (decomposition). Ten g. powd. I was added to 5.5 g. polyglyoxal in 50 cc. hot water. The dark crystalline reaction product seps. instantaneously. Yield 80%. Recrystallized from alc. or water, then from benzene, it m. 132.5°. The mol. weight (ebullioscopic) is 131.0, which points to C₆N₄H₂. It yields on saponification of 2 g. with 3 g. NaOH in 10 cc. 50% alc., neutralization with HNO₃, precipitation with AgNO₃ and liberation with HCl 1.2 g. pyrazine-2,3-dicarboxylic acid, m. 182-5° (decomposition). It is therefore 2,3-dicyanopyrazine, and I is accordingly cis-dicyanodiaminoethylene or diaminomaleic dinitrile. The saponification of I probably first leads to HO(NH₂)C:C(NH₂)CN and in the second stage to NH₂CO₂H and NCCH₂NH₂ which finally are decomposed to CO₂, NH₃ and glycine. The polymerization probably takes place over the dimer, diiminoethylene.

Roczniki Chemii 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

Griszkiewicz-Trochimowski, E. published the artcileProducts of polymerization of hydrocyanic acid, Recommanded Product: 1H-1,2,3-Triazole-4,5-dicarbonitrile, the publication is Roczniki Chemii (1921), 468-78, database is CAplus.

The constitution NH₂CH(CN)₂ has been suggested for the trimeride of HCN. In order to verify the presence of the NH₂ group, 2 reactions were investigated, viz., condensation with aldehydes and the action of HNO₂. The 1st reaction followed the course expected, and the following compounds were obtained. With salicylaldehyde, the salicylidene derivative, CH(CN)₂N:CHC₆H₄OH, yellowish green needles, m. about 235° (decomposition). With anisaldehyde, the anisylidene derivative With BzH, the benzylidene derivative, brown plates, m. 190° (decomposition). A benzoyl derivative of the trimeride was also prepared, brown plates, m. 220° (decomposition), together with its unstable hydrochloride. The results with HNO₂ were not those expected; it was thought that a diazo compound would be formed, from which tartaric acid could be obtained by the following reaction: CH(CN)₂NH₂ → CH(CN)₂N:NOH → (CN)₂CHOH → [CH(OH)CO₂H]₂. The product of the reaction does not, however, decompose on boiling; it is obtained from the solution in orange prisms, m. about 145°, and is shown to be 4,5-di-cyano-1,2,.3-triazole. On sublimation at 140°, this is obtained in a colorless modification, for which the constitution NH.N:C(CN).C(CN):N is suggested. The Ag, Cu, Ba, K, and NH₄ salts of the dicyanotriazole were prepared, also its l-methyl derivative, m. 57.5-8.5°. Hydrolysis with HCl gives the 4-amide of 1,2,3-triazole-4,5-dicarboxylic acid, m. 275°. By passing HCl through the substance in Et₂O is obtained ethyl 4-cyano-1,2,3-triazole-5-carboxylate, m. 114-5° from which the acid, m. 225-6°, is obtained, and from this by hydrolysis with H₂SO₄ the 4,5-di-CO₂H acid, m. 195-6°, is produced. It is suggested that the dicyanotriazole may be produced from the HNO₂ by condensation of a diazotized mol. of it with an undiazotized one. The results both with aldehydes and with HNO₂, therefore, support the view that the trimeride of HCN is CH(CN)₂NH₂.

Roczniki Chemii 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, Recommanded Product: 1H-1,2,3-Triazole-4,5-dicarbonitrile.

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