Month: December 2022

Wei, Ning published the artcileSynthesis and antifungal activity of 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-(N-butyl-N-substituted benzylamino)-2-propanol, COA of Formula: C12H13F2N3O4S, the publication is Dier Junyi Daxue Xuebao (2009), 30(9), 1052-1057, database is CAplus.

To study the antifungal activity of triazole alcs. by introducing N-Bu and substituted benzyl as side chain, fourteen title compounds were synthesized and characterized by ¹H NMR, IR, and LC-MS. The MICs of the compounds were determined by in vitro test using 8 clin. pathogenic fungi. The title compounds exhibited potent antifungal activities against nearly all fungi tested (except for Aspergillus fumigatus), especially for the deep infection ones. Three compounds showed a 16-fold activity (with a MIC₈₀ value of 0.015 6 μg/mL) as that of fluconazole against Microsporum gypseum. Two compounds showed a 128-fold activity (with a MIC₈₀ value of 0.003 9 μg/mL) as that of fluconazole against Candida albicans, and their activities were higher than those of other pos. controls.

Dier Junyi Daxue Xuebao 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 C4H4N2O2, COA of Formula: C12H13F2N3O4S.

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

Lu, Xiao-juan published the artcileSynthesis of 1-(H-1,2,4-triazole-1-yl)-2-(2,4-difluoro-phenyl)-3-(N-cyclopropyl-N-substituted amino)-2-propanols and its antifungal activity, Synthetic Route of 86386-77-8, the publication is Dier Junyi Daxue Xuebao (2008), 29(11), 1380-1383, database is CAplus.

A method for the synthesis of the title compounds is reported here. The above-mentioned products were characterized by NMR, MS, and element anal. The MICs of the compounds were determined by in vitro tests involving eight fungal strains, such as Trichophyton rubrum, Aspergillus fumigatus, Candida tropicalis, Candida albicans, Cryptococcus neoformans, Candida parapsilosis, Microsporum canis. These compounds exhibited potent antifungal activity against the test systems. Some compounds had MIC₈₀ values less than 0.125 μg/mL^-1 against Candida albicans, showing an activity 4 times higher than that of fluconazole. Thus, the title compounds with cyclopropyl and alky substituents have antifungal activity and the antifungal activity decreases as the alkyl side chains gets longer.

Dier Junyi Daxue Xuebao 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, Synthetic Route of 86386-77-8.

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

Ning, Xiaowen published the artcileGreen and yellow pyridazine-based phosphorescent Iridium(III) complexes for high-efficiency and low-cost organic light-emitting diodes, Application of 2-[5-(Trifluoromethyl)-1H-1,2,4-triazol-3-yl]pyridine, the publication is Dyes and Pigments (2019), 206-212, database is CAplus.

Despite efficient electroluminescence performance, the high fabrication cost due to the utilization of noble metals impedes the commercialization of phosphorescent organic light-emitting diodes (PHOLEDs) based on iridium(III) complexes. In this paper, we designed and synthesized a series of green and yellow phosphorescent iridium(III) complexes with 3-(2,4-difluorophenyl)-6-methylpyridazine as the cyclometalating ligand to fabricate high-performance and low-cost PHOLEDs. By the introduction of a pyridazine moiety to enhance the coordination bond between iridium(III) ion and cyclometalating ligands, these iridium(III) complexes were obtained in high yields and exhibit good thermal stabilities and volatilities, which are beneficial to reduce the device manufacturing cost. Besides, high photoluminescence quantum yields (PLQYs) and short phosphorescent lifetimes of these pyridazine-based iridium(III) complexes endow their PHOLEDs with excellent device performance, which can be promising for practical applications. Particularly, the green emitter (fpdz)₂Irpic exhibited a high PLQY of 0.89 in solid doped thin-film; PHOLED based on (fpdz)₂Irpic achieved an outstanding maximum external quantum efficiency (EQE_max) of 28.7% with ultralow efficiency roll-off of 2% at the high luminance of 1000 cd m^-2, which was superior to the com. green phosphor bis(phenylpyridineyl)iridium(acetylacetonate) [(ppy)₂Ir(acac), EQE_max = 24.2%].

Dyes and Pigments 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 C8H5F3N4, Application of 2-[5-(Trifluoromethyl)-1H-1,2,4-triazol-3-yl]pyridine.

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

Ke, Xuefeng published the artcileSynthesis and antifungal activities of novel triazole derivatives with dithiocarbamates side chain, Safety of 1-((2-(2,4-Difluorophenyl)oxiran-2-yl)methyl)-1H-1,2,4-triazole methanesulfonate, the publication is Yaoxue Fuwu Yu Yanjiu (2016), 16(1), 11-14, 55, database is CAplus.

The title compounds were synthesized and their chem. structures were identified by ¹H-NMR and ¹³C-NMR. The in vitro antifungal activities of the synthesized compounds were evaluated. Ten prepared compounds had certain antifungal activity, and the in vitro antifungal activity of some compounds was superior to that of the control drugs.

Yaoxue Fuwu Yu Yanjiu 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, Safety of 1-((2-(2,4-Difluorophenyl)oxiran-2-yl)methyl)-1H-1,2,4-triazole methanesulfonate.

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

Tao, Peng published the artcileHighly efficient blue phosphorescent iridium(III) complexes with various ancillary ligands for partially solution-processed organic light-emitting diodes, Formula: C8H5F3N4, the publication is Journal of Materials Chemistry C: Materials for Optical and Electronic Devices (2017), 5(36), 9306-9314, database is CAplus.

One homoleptic facial and five novel highly efficient blue heteroleptic iridium(III) complexes were designed and synthesized by selecting 2-(4-fluoro-3-(trifluoromethyl)phenyl)pyridine as cyclometalated ligands and 2,4-pentanedione, 2-(3-(trifluoromethyl)-1H-1,2,4-triazol-5-yl)pyridine, picolinic acid, 2-(1H-imidazol-2-yl)pyridine and 2-(1H-tetrazol-5-yl)pyridine as ancillary ligands, resp. The alternation of ancillary ligands could finely tune the photophys. properties of the phenylpyridine-based complexes, particularly with respect to emission wavelength, photoluminescence quantum yield (Φ_PL), full width at half maximum (FWHM), etc. The phosphors designed not only exhibit excellent solubility in commonly used solvents with robust chem. stability but also show bright emissions in the pure blue region with very high absolute Φ_PL up to 0.98 in solution and relatively narrow FWHMs up to 52 nm. Furthermore, based on these highly efficient blue phosphors, high-performance partially solution-processed blue organic light-emitting diodes have been successfully fabricated. The electroluminescence peak, 1931 Commission Internationale de L’Eclairage coordinate and FWHM of the device based on Ir4 are all superior to the device based on FIrpic. In addition, the maximum efficiencies of the device based on Ir4 (21.15 cd A^-1, 12.07 lm W^-1) are also higher than those of the device based on FIrpic (18.89 cd A^-1, 11.26 lm W^-1) under the same conditions.

Journal of Materials Chemistry C: Materials for Optical and Electronic Devices 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 C13H19Br2ClN2O, Formula: C8H5F3N4.

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

Wu, Shanchao published the artcileFrom Antidiabetic to Antifungal: Discovery of Highly Potent Triazole-Thiazolidinedione Hybrids as Novel Antifungal Agents, Quality Control of 86386-77-8, the publication is ChemMedChem (2014), 9(12), 2639-2646, database is CAplus and MEDLINE.

In an attempt to discover a new generation of triazole antifungal agents, a series of triazole-thiazolidinedione hybrids I [R = Ph, 2-BrC₆H₄, 4-ClC₆H₄, etc.] were designed and synthesized by mol. hybridization of the antifungal agent fluconazole and rosiglitazone (an antidiabetic). Most of the target compounds showed good to excellent inhibitory activity against a variety of clin. important fungal pathogens. In particular, compounds I [R = 2,4-Cl₂C₆H₃], I [R = 2-furyl], I [R = 3-furyl] were highly active against Candida albicans, with MIC₈₀ values in the range of 0.03-0.15 μΜ. Moreover, the last two compounds compounds were found to be effective against four fluconazole-resistant clin. isolates; these two compounds are particularly promising antifungal leads for further optimization. Mol. docking studies revealed that the hydrogen bonding interactions between thiazolidinedione and CYP51 from C. albicans are important for antifungal activity. This study also demonstrates the effectiveness of mol. hybridization in antifungal drug discovery.

ChemMedChem 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 C11H8O3, Quality Control of 86386-77-8.

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

Du, Zhiming published the artcile4,5-Bis(5-tetrazolyl)-1,2,3-triazole: Synthesis and Performance, Application of 1H-1,2,3-Triazole-4,5-dicarbonitrile, the publication is Propellants, Explosives, Pyrotechnics (2015), 40(6), 954-959, database is CAplus.

4,5-Bis(5-tetrazolyl)-1,2,3-triazole (BTT) was synthesized by a new method. Its structure was characterized by IR and ¹³C NMR spectroscopy and elemental anal. (EA). The thermal stability of BTT was investigated by TG-DSC technique. The kinetic parameters including activation energy and pro-exponential factor were calculated by Kissinger equation. The combustion heat, detonation products, hygroscopicity, impact, and friction sensitivity were also measured. The formation heat, detonation pressure, and detonation velocity of BTT were calculated BTT has high detonation pressure and detonation velocity (P=35.36 GPa, D=8.971 km s^-1). BTT has potential application prospect as environmentally friendly gas generant, insensitive explosive and solid propellant.

Propellants, Explosives, Pyrotechnics 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 of 1H-1,2,3-Triazole-4,5-dicarbonitrile.

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

Zheng, Jiyue published the artcileDevelopment of Adenosine A_2A Receptor Antagonists for the Treatment of Parkinson’s Disease: A Recent Update and Challenge, Related Products of triazoles, the publication is ACS Chemical Neuroscience (2019), 10(2), 783-791, database is CAplus and MEDLINE.

A review. Parkinson’s disease (PD) is a neurodegenerative disease with significant unmet medical needs. The current dopamine-centered treatments aim to restore motor functions of patients without slowing the disease progression. Long-term usage of these drugs is associated with diminished efficacy, motor fluctuation, and dyskinesia. Furthermore, the nonmotor features associated with PD such as sleep disorder, pain, and psychiatric symptoms are poorly addressed by the dopaminergic treatments. Adenosine receptor A_2A antagonists have emerged as potential treatment for PD in the past decade. Here we summarize the recent work (2015-2018) on adenosine receptor A_2A antagonists and discuss the challenge and opportunity for the treatment of PD.

ACS Chemical 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 C12H14BNO2, Related Products of triazoles.

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

Slee, Deborah H. published the artcileIdentification of Novel, Water-Soluble, 2-Amino-N-pyrimidin-4-yl Acetamides as A_2A Receptor Antagonists with In Vivo Efficacy, Computed Properties of 377727-87-2, the publication is Journal of Medicinal Chemistry (2008), 51(3), 400-406, database is CAplus and MEDLINE.

Potent adenosine hA_2A receptor antagonists are often accompanied by poor aqueous solubility, which presents issues for drug development. Herein we describe the early exploration of the structure-activity relationships of a lead pyrimidin-4-yl acetamide series to provide potent and selective 2-amino-N-pyrimidin-4-yl acetamides as hA_2A receptor antagonists with excellent aqueous solubility In addition, this series of compounds has demonstrated good bioavailability and in vivo efficacy in a rodent model of Parkinson’s disease, despite having reduced potency for the rat A_2A receptor vs. the human A_2A receptor.

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 C24H26ClNO4, Computed Properties of 377727-87-2.

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

Sun, Qing-Yan published the artcileSynthesis and evaluation of novel 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-[(4-substituted-phenyl)piperazin-1-yl]propan-2-ols as antifungal agents, Formula: C12H13F2N3O4S, the publication is European Journal of Medicinal Chemistry (2007), 42(8), 1151-1157, database is CAplus and MEDLINE.

1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-[(4-substituted-phenyl)piperazin-1-yl]propan-2-ols such as I were designed and synthesized from the structure-activity relations and antimycotic mechanism of azole antifungal agents. Their structures were confirmed by elemental anal., IR, MS, ¹H NMR and ¹³C NMR. Results of preliminary antifungal tests against six human pathogenic fungi (Candida albicans, Candida parapsilosis, Cryptococcus neoformans, Candida tropicalis, inherently fluconazole-resistant Candida krusei, Candida glabrata) in vitro showed that all title compounds exhibited activity against fungi tested to some extent except against C. tropicalis.

European Journal of Medicinal Chemistry 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 C7H10BNO4S, Formula: C12H13F2N3O4S.

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