Tag: M.W=300-350

Wang, Shudong published the artcileSynthesis and evaluation of some substituted heterocyclic fluconazole analogues as antifungal agents, COA of Formula: C12H13F2N3O4S, the publication is Asian Journal of Chemistry (2014), 26(8), 2362-2364, database is CAplus.

A new series of fluconazole analogs I [R = 2-CH₃, 3,5-(NO₂)₂, 4-tert-Bu, etc.] were designed, synthesized and evaluated as antifungal agents. Most of the synthesized compounds showed moderate activity against eight human pathogenic fungi in vitro. Compounds I (R = 2-CH₃, 4-n-Pr) showed the best antifungal activity against Candida albicans with the value of MIC₈₀ = 0.5 μg/mL for both.

Asian Journal of 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 C4H6O3, COA of Formula: C12H13F2N3O4S.

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

Wang, Bao-Gang published the artcileDesign synthesis and biological evaluation of 3-substituted triazole derivatives, Recommanded Product: 1-((2-(2,4-Difluorophenyl)oxiran-2-yl)methyl)-1H-1,2,4-triazole methanesulfonate, the publication is Chinese Chemical Letters (2011), 22(5), 519-522, database is CAplus.

Based on the active site of lanosterol 14α-demethylase of azole antifungal agents, sixteen 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-(N-n-butyl-N-1-substituted-benzyl-4-methylene-1H-1,2,3-triazole)-2-propanols were designed, synthesized and evaluated as antifungal agents. Results of preliminary antifungal tests against eight human pathogenic fungi in vitro showed that some of the compounds exhibited excellent activities with broad spectrum.

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 C15H14N2, 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

Chai, Xiaoyun published the artcileSynthesis and biological evaluation of triazole derivatives as potential antifungal agent, Computed Properties of 86386-77-8, the publication is Chemical Biology & Drug Design (2012), 80(3), 382-387, database is CAplus and MEDLINE.

A series of triazole antifungal agents with piperidine side chains was designed and synthesized. Results of preliminary antifungal tests against eight human pathogenic fungi in vitro showed that all the title compounds exhibited excellent activities with broad spectrum. Moreover, a mol. model for the binding between compound I and the active site of CACYP51 was provided based on the computational docking results. The side chain of the compound I is oriented into substrate access channel 2 (FG loop) and forms hydrophobic and van der waals interactions with surrounding hydrophobic residues. The Ph group of the side chain can interact with the Ph group of Phe380 through the formation of π-π face-to-edge interaction.

Chemical Biology & Drug Design 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, Computed Properties of 86386-77-8.

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

Wu, Wei-feng published the artcileSynthesis and antifungal activity of 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-(N-cyclopropyl-N-benzyl-amino)-2-propanols, Safety of 1-((2-(2,4-Difluorophenyl)oxiran-2-yl)methyl)-1H-1,2,4-triazole methanesulfonate, the publication is Yaoxue Shijian Zazhi (2009), 27(4), 266-269, database is CAplus.

Design and synthesis of novel triazole antifungal derivatives, e.g. I, based on the structure of fluconazole are reported. The anti-fungal activities were also evaluated against the eight common pathogenic fungi. Some of the title compounds exhibited activity against fungi to some extent.

Yaoxue Shijian 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 C7H8BBrO3, 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

Chai, Xiaoyun published the artcileDesign, synthesis, and biological evaluation of novel 1, 2, 4-triazole derivatives as antifungal agent, Category: triazoles, the publication is Archives of Pharmacal Research (2012), 35(11), 1895-1901, database is CAplus and MEDLINE.

A series of novel 1,2,4-triazole derivatives have been designed and synthesized as potential antifungal agents. All compounds were characterized by ¹H-NMR, ¹³C-NMR, and LCMS. Their antifungal activities against seven human pathogenic fungi were evaluated in vitro by measuring the minimal inhibitory concentrations Most of the tested compounds were found to be more potent against Candida albicans than the control drug fluconazole.

Archives of Pharmacal Research 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, Category: triazoles.

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

Yan, Yongzheng published the artcileSynthesis and antifungal activity of novel triazole derivatives, SDS of cas: 86386-77-8, the publication is Archives of Pharmacal Research (2011), 34(10), 1649-1656, database is CAplus and MEDLINE.

A series of novel azoles, which are analogs of fluconazole, were designed and synthesized as potential antifungal agents by the click reaction. The click reaction approach toward the synthesis of novel 1,2,3-triazolyl linked triazole antifungal derivatives was achieved by Cu(I)-catalyzed 1,3-dipolar cycloaddition of 2-(2,4-difluorophenyl)-3-propargylamino-1-(1,2,4-triazol-1-yl)-2-propanol with substituted benzyl bromides and sodium azide. In addition, the target compounds tested can increase antifungal activity.

Archives of Pharmacal Research 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, SDS of cas: 86386-77-8.

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

Zhou, Yu published the artcileSynthesis and antifungal activity of 1-(1H-1, 2 ,4-triazole-1-yl)-2-(2, 4-difluorophenyl)-3-substituted-2-propanol, SDS of cas: 86386-77-8, the publication is Dier Junyi Daxue Xuebao (2011), 32(7), 754-758, database is CAplus.

To study the antifungal activity of triazole alcs. by introduction of Bu and triazole as side chains. A total of 16 compounds of 1-(1H-1, 2, 4-triazole-1-yl)-2-(2, 4-difluorophenyl)-3-substituted-2-propanol I(R = 2-F, 3-F, 4-F, 3-Cl, 4-Cl, 2-Br, 3-Br, 4-Br, 4-Me, 2-NO₂, 3-NO₂, 4-NO₂, 2-CN, 3-CN, 2,4-Cl₂, 2,6-CL₂) were synthesized and characterized by ¹HNMR and LC-MS. The in vitro antifungal activities of the compounds were determined by tests with 8 human pathogenic fungi. It was found that all the 16 title compounds exhibited antifungal activities, and compounds I(R = 3-F, 3-Cl, 4-Cl, 4-Me) had antifungal activities stronger than fluconazole, similar to itraconazole. Introduction of Bu and triazole side chain can confer antifungal activities to the compounds

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 Al2H32O28S3, SDS of cas: 86386-77-8.

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

Liao, Jun published the artcileSynthesis and biological evaluation of novel fluconazole analogues bearing 1,3,4-oxadiazole moiety as potent antifungal agents, Quality Control of 86386-77-8, the publication is Archives of Pharmacal Research (2015), 38(4), 470-479, database is CAplus and MEDLINE.

A novel series of fluconazole based mimics incorporating 1,3,4-oxadiazole moiety were designed and synthesized. All the title compounds were characterized by ¹H-NMR, ¹³C-NMR, and Q-TOF-MS. Preliminary results revealed that most of analogs exhibited significant antifungal activity against seven pathogenic fungi. Compound I [R = 2-Br, 3-OMe] (MIC₈₀ ≤ 0.125 μg/mL, resp.) were found more potent than the pos. controls itraconazole and fluconazole as broad-spectrum antifungal agents. The observed docking results showed that the 1,3,4-oxadiazole moiety enhanced the affinity binding to the cytochrome P 450 14α-demethylase (CYP51).

Archives of Pharmacal Research 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

Jiang, Zhigan published the artcileDiscovery of highly potent triazole antifungal derivatives by heterocycle-benzene bioisosteric replacement, Formula: C12H13F2N3O4S, the publication is European Journal of Medicinal Chemistry (2013), 16-22, database is CAplus and MEDLINE.

On the basis of the authors’ previously discovered triazole antifungal lead compounds, heterocycle-benzene bioisosteric replacement was used to improve their pharmacokinetic profile. The designed new triazole derivatives have good antifungal activity toward a wide range of pathogenic fungi. Their binding mode with the target enzyme was clarified by mol. docking. The MIC value of the highly potent compound 1-(4-(benzo[d]thiazol-2-yl-methyl)piperazin-1-yl)-2-(2,4-difluorophenyl)-3-(1H-1,2,4-triazol-1-yl)propan-2-ol against Candida albicans, Candida tropicalis, and Cryptococcus neoformans is 0.016 μg/mL, 0.004 μg/mL, and 0.016 μg/mL, resp. Moreover, preliminary pharmacokinetic studies revealed that it showed improved oral absorption as compared to the lead compound iodiconazole and deserved for further evaluations.

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 C12H13F2N3O4S, Formula: C12H13F2N3O4S.

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