Category: 86386-77-8

Blokhina, Svetlana V. published the artcileSynthesis and antifungal activity of new hybrids thiazolo[4,5-d]pyrimidines with (1H-1,2,4)triazole, SDS of cas: 86386-77-8, the publication is Bioorganic & Medicinal Chemistry Letters (2021), 127944, database is CAplus and MEDLINE.

Fluconazole analogs substituted with thioxothiazolopyrimidinone moieties such as I were prepared as antifungal agents. The solubility and lipophilicity of the fluconazole analogs was determined Compounds with a methylpiperazinylalkyl linker exhibited significant antifungal activities against filamentous and yeast fungi.

Bioorganic & Medicinal Chemistry Letters 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, SDS of cas: 86386-77-8.

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

Han, Guiyan published the artcileDiscovery of Novel Fungal Lanosterol 14α-Demethylase (CYP51)/Histone Deacetylase Dual Inhibitors to Treat Azole-Resistant Candidiasis, Application In Synthesis of 86386-77-8, the publication is Journal of Medicinal Chemistry (2020), 63(10), 5341-5359, database is CAplus and MEDLINE.

Invasive fungal infections (particularly candidiasis) are emerging as severe infectious diseases worldwide. Because of serious antifungal drug resistance, therapeutic efficacy of the current treatment for candidiasis is limited and associated with high mortality. However, it is highly challenging to develop novel strategies and effective therapeutic agents to combat drug resistance. Herein, the first generation of lanosterol 14α-demethylase (CYP51)-histone deacetylase (HDAC) dual inhibitors was designed, which exhibited potent antifungal activity against azole-resistant clin. isolates. In particular, compounds 12h(II) and 15j(I) were highly active both in vitro and in vivo to treat azole-resistant candidiasis. Antifungal mechanism studies revealed that they acted by blocking ergosterol biosynthesis and HDAC catalytic activity in fungus, suppressing the function of efflux pump, yeast-to-hypha morphol. transition, and biofilm formation. Therefore, CYP51-HDAC dual inhibitors represent a promising strategy to develop novel antifungal agents against azole-resistant candidiasis.

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 C12H13F2N3O4S, Application In Synthesis of 86386-77-8.

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

Liang, Shuang published the artcileSynthesis and antifungal activity of 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-(4-substituted acyl piperazin-1-yl)-2-propanols, Quality Control of 86386-77-8, the publication is Journal of Medical Colleges of PLA (2004), 19(3), 142-145, database is CAplus.

The objective was to study the effect of fluconazole derivatives from a side chain containing 4-substituted acyl piperazine-1-yl on antifungal activity. Fourteen title compounds, e.g., I, were synthesized and confirmed by the elementary anal., ¹HNMR and IR spectra. Five deep fungal strains and 3 shallow fungal strains were chosen as the exptl. strains. Min. inhibitory concentrations(MICs) of all title compounds were determined by the method recommended by the National Committee for Clin. Laboratory Standards (NCCLS) using RPMI 1640 test medium. Among the 14 title compounds, 12 were first reported. The results of preliminary antifungal test showed that all the title compounds exhibited potent antifungal activities to a certain extent. The activity of 4 compounds were more than 4 times as high as that of fluconazole and equal to that of ketoconazole against Candida albicans in vitro (MIC₈₀ value ≤ 0.125 μg/mL). Introduction of a side chain containing 4-substituted acyl piperazine-1-yl into the main part of fluconazole has important influence on antifungal activities of title compounds

Journal of Medical Colleges of PLA 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

Sun, Qingyan published the artcileSynthesis and antifungal activity of 1-(1H-1,2,4-triazolyl)-2-(2′,4′-difluorophenyl)-3-substituted with side chain containing sulfur atom-2-propanols, Category: triazoles, the publication is Dier Junyi Daxue Xuebao (2001), 22(9), 871-874, database is CAplus.

Fifteen title compounds 3-R-1-(1H-1,2,4-triazolyl)-2-(2,4- difluorophenyl)-2-propanol (I; R = side chain containing sulfur) were synthesized and characterized by elemental anal., ¹HNMR, and IR spectra. MICs of all title compounds were determined by the method recommended by the National committee of clin. laboratory standards (NCCLS) using RPMI1640 test medium. The results of preliminary antifungal test showed that all title compounds exhibited potent antifungal activities to a certain extent.

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 C8H11NO, Category: triazoles.

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

Sun, Qingyan published the artcileSynthesis and antifungal activity of triazole derivatives, SDS of cas: 86386-77-8, the publication is Zhongguo Yaowu Huaxue Zazhi (2004), 14(1), 14-18, database is CAplus.

The effect of the triazole derivatives from introducing a side chain containing nitrogen on the antifungal activity was studied. Twenty-two title compounds were synthesized and confirmed by elementary anal., ¹H-NMR and IR spectra. MIC₈₀ of all the title compounds were determined using the RPM1640 test medium. The results of the preliminary antifungal test showed that all the title compounds exhibited potent antifungal activities. One compound showed equal or more potent activities when compared with ketoconazole and was markedly superior to fluconazole. Proper lipid/water distribution coefficient might be important to the antifungal activities of the title compounds in vitro.

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 C4H4N2O2, SDS of cas: 86386-77-8.

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

Liang, Shuang published the artcileSynthesis and antifungal activity of 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-[(4-substituted)-1-piperazinyl]-2-propanols, Application of 1-((2-(2,4-Difluorophenyl)oxiran-2-yl)methyl)-1H-1,2,4-triazole methanesulfonate, the publication is Zhongguo Yaowu Huaxue Zazhi (2004), 14(2), 71-75, database is CAplus.

The effect of the side chain in (4-substituted)-1-piperazinyl on the antifungal activity of fluconazole compounds was studied. Thirteen title compounds were synthesized and confirmed by the elementary anal., ¹H-NMR and IR spectra. The MICs of all the title compounds were determined by the method recommended by the National Committee for Clin. Laboratory Standards (NCCLS) using the RPMI1640 test medium. The results of the preliminary antifungal test showed that all the title compounds exhibited potent antifungal activities. The activities of the eight compounds thus prepared were more than 4 times as high as that of fluconazole and equal to that of ketoconazole against Candida albicans in vitro. The lipid/water distribution coefficient and stereochem. have important influence on the antifungal activities of the title compounds

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, Application 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

He, Qiuqin published the artcileSynthesis and antifungal activities of 1-(1H-1,2,4-triazol-1-y1)-2-(2,4-difluorophenyl)-3-[(4-substituted)-piperazin-1-y1]-2-propanol, Recommanded Product: 1-((2-(2,4-Difluorophenyl)oxiran-2-yl)methyl)-1H-1,2,4-triazole methanesulfonate, the publication is Zhongguo Yaowu Huaxue Zazhi (2007), 17(1), 8-12, database is CAplus.

According to the structure of fluconazole, eleven target compounds were designed and synthesized. All of them were confirmed by H-NMR or IR spectra, resp. The MIC₈₀ of all the target compounds were determined by the method recommended by the national committee for clin. laboratory standards (NCCLS) using the RPMI 1640 test medium. Eleven target compounds were firstly reported. The results of the preliminary antifungal test showed that all the target compounds exhibited potent antifungal activities to a certain extent. Most of the target compounds showed higher antifungal activities than that of fluconazole. Especially, compound I showed strong antifungal activity with broad antifungal spectrum and was chosen for further study.

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, Recommanded Product: 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

He, Qiu Qin published the artcileDesign, synthesis of novel antifungal triazole derivatives with high activities against Aspergillus fumigatus, SDS of cas: 86386-77-8, the publication is Chinese Chemical Letters (2007), 18(4), 421-423, database is CAplus.

Based on the active site of Aspergillus fumigatus lanosterol 14α-demethylase (AF-CYP51), novel triazole compounds I (R = aryl) were designed. Their chem. synthesis and the antifungal activities were reported. The results showed that all the target compounds exhibited excellent activities with broad spectrum, in which I (R = 4-FC₆H₄, 4-H₂NCOC₆H₄, pyridin-4-yl) showed comparable activities against A. fumigatus to the control drug Itraconazole.

Chinese Chemical Letters 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, SDS of cas: 86386-77-8.

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

Xia, Yajun published the artcileSynthesis of new antifungal agents sulfur-containing triazole compounds, Category: triazoles, the publication is Zhejiang Yike Daxue Xuebao (1995), 24(2), 70-4, database is CAplus.

Title compounds I (R = PhS, 2-pyridylthio, benzimidazolylthio, benzothiazolylthio, triazolylthio, etc.) were prepared by reaction of epoxides II methanesulfonates with RH. The in vitro antifungal activities of these compounds were determined

Zhejiang Yike 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 C22H32O2, Category: triazoles.

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

Wang, Nan published the artcileDesign, synthesis and in vitro antifungal activities of fluconazole derivatives, Recommanded Product: 1-((2-(2,4-Difluorophenyl)oxiran-2-yl)methyl)-1H-1,2,4-triazole methanesulfonate, the publication is Youji Huaxue (2012), 32(5), 922-929, database is CAplus.

In search of more effective antifungal agents, twenty-two new fluconazole derivatives containing 4-Me phenol and thymine have been designed and synthesized based on the previous results of computer-aided drug design. All the derivatives retain the essential pharmacophore of fluconazole. Their structures are elucidated by ¹H NMR, elemental anal. and ESI-MS. Preliminary in vitro antifungal activities bioassay showed that compound I exhibits better in vitro antifungal activities against eight fungi except Aspergillus fumigatus (7544) than fluconazole. The introduction of propargyl group to nitrogen atom can enhance in vitro antifungal activities of this type derivative and it is worth of further research.

Youji Huaxue 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 C11H14O2, Recommanded Product: 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