Tag: M.W=300-350

He, Qiuqin’s team published research in Zhongguo Yaowu Huaxue Zazhi in 17 | CAS: 86386-77-8

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.

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’s team published research in Chinese Chemical Letters in 18 | CAS: 86386-77-8

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.

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

Wang, Nan’s team published research in Youji Huaxue in 32 | CAS: 86386-77-8

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.

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

Xia, Yajun’s team published research in Zhejiang Yike Daxue Xuebao in 24 | CAS: 86386-77-8

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.

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, Shengzheng’s team published research in European Journal of Medicinal Chemistry in 53 | CAS: 86386-77-8

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 C13H19Br2ClN2O, COA of Formula: C12H13F2N3O4S.

Wang, Shengzheng published the artcileDesign, synthesis and structure-activity relationships of new triazole derivatives containing N-substituted phenoxypropylamino side chains, COA of Formula: C12H13F2N3O4S, the publication is European Journal of Medicinal Chemistry (2012), 292-299, database is CAplus and MEDLINE.

It is highly desirable to develop novel azoles with improved biol. profiles. The structure-activity relationship (SAR) of the N-substitutions was investigated in this study. In vitro antifungal activities revealed that sterically large groups were not favored for the N-substitutions. The removal of the N-substitutions had little effect on the antifungal activity. Two compounds with free amine group, including 1-[[3-(4-bromophenoxy)propyl]amino]-2(2,4-difluorophenyl)-3-(1H-1,2,4-triazol-1-yl)propan-2-ol, showed excellent activity with broad antifungal spectrum. The SAR results were supported by mol. docking and the N-substitutions were found to be important for the conformation of the side chains. The SAR and binding mode of the azoles are useful for further lead optimization.

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 C13H19Br2ClN2O, COA of Formula: C12H13F2N3O4S.

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

Chen, Hai-Jiang’s team published research in Chinese Chemical Letters in 28 | CAS: 86386-77-8

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, Product Details of C12H13F2N3O4S.

Chen, Hai-Jiang published the artcileNew triazole derivatives containing substituted 1,2,3-triazole side chains: Design, synthesis and antifungal activity, Product Details of C12H13F2N3O4S, the publication is Chinese Chemical Letters (2017), 28(4), 913-918, database is CAplus.

A series of novel antifungal triazoles I (R = t-Bu, cyclopropyl, Ph) was designed and synthesized by reaction of azides with terminal alkynes. Synthesized compounds I were screened for their antifungal activity; results revealed that several target compounds showed good antifungal activity with a broad spectrum. In particular, compound I (R = cyclopropyl) was highly active against Candida albicans and Candida glabrata. Moreover, compound I (R = cyclopropyl) showed potent in vivo antifungal efficiency in the Caenorhabditis elegans-C. albicans infection model.

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, Product Details of C12H13F2N3O4S.

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

He, Xiaomeng’s team published research in MedChemComm in 6 | CAS: 86386-77-8

MedChemComm 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, HPLC of Formula: 86386-77-8.

He, Xiaomeng published the artcileDiscovery of highly potent triazole antifungal agents with piperidine-oxadiazole side chains, HPLC of Formula: 86386-77-8, the publication is MedChemComm (2015), 6(4), 653-664, database is CAplus.

Due to increasing incidence and mortality of invasive fungal infections, discovery and development of new generations of antifungal agents represents a challenging task. On the basis of the authors’ previously reported triazole-benzyloxypiperidinyl lead compound, a series of novel triazole antifungal agents containing piperidine-oxadiazole side chains were rationally designed and synthesized. Most of the target compounds showed excellent inhibitory activity against clin. important fungal pathogens. In particular, compounds 6g (MIC = 0.031 μg mL-1) and 11b (MIC = 0.016 μg mL-1) were highly active against Candida albicans including fluconazole-resistant strains. Moreover, they showed inhibitory activity against hyphal formation with low toxicity, which were promising leads for further development.

MedChemComm 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, HPLC of Formula: 86386-77-8.

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

Zhao, Qing-jie’s team published research in Dier Junyi Daxue Xuebao in 30 | CAS: 86386-77-8

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 C13H16O2, Quality Control of 86386-77-8.

Zhao, Qing-jie published the artcileSynthesis of 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-[(cyclopropyl)(benzyl)amino]-2-propanol derivatives and test of their antifungal activity, Quality Control of 86386-77-8, the publication is Dier Junyi Daxue Xuebao (2009), 30(2), 198-201, database is CAplus.

A method for the synthesis of the title compounds [i.e., α-[[(phenylmethyl)(cyclopropyl)amino]methyl]-α-(2,4-difluorophenyl)-1H-1,2,4-triazole-1-ethanol derivs] is reported here. A cyclopropyl group was introduced in order to study the antifungal activity of the compounds thus prepared The target compounds were characterized by NMR, MS, elemental anal. Eight fungi were used for in vitro anti-fungal test. The compounds thus prepared showed antifungal activity, especially to the deep infection fungi, and had an MIC value <0.125 μg/mL against Candida albicans (showing thus antifungal activity 4 times higher than that of fluconazole and similar to that of terconazole).

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 C13H16O2, Quality Control of 86386-77-8.

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

Zhao, Qing-Jie’s team published research in Chemistry & Biodiversity in 4 | CAS: 86386-77-8

Chemistry & Biodiversity 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 C13H12BClO3, Related Products of triazoles.

Zhao, Qing-Jie published the artcileDesign, synthesis, and antifungal activities of novel 1H-triazole derivatives based on the structure of the active site of fungal lanosterol 14α-demethylase (CYP51), Related Products of triazoles, the publication is Chemistry & Biodiversity (2007), 4(7), 1472-1479, database is CAplus and MEDLINE.

A series of fluconazole analogs I (R2 = H, R4 = H; R2 = Me, R4 = H; R2 = H, R4 = Me; R2 = F, R4 = H; R2 = H, R4 = F; R2 = Cl, R4 = H; R2 = H, R4 = Cl; R2 = Br, R4 = H; R2 = H, R4 = Br; R2 = H, R4 = CMe3; R2 = F, R4 = F) were prepared and assayed for antifungal activity. They were designed by computational docking experiments to the active site of the cytochrome P 450 14α-sterol demethylase (CYP51), whose crystal structure is known. Preliminary biol. tests showed that most of the target compounds exhibit significant activities against the eight most-common pathogenic fungi. Thereby, the most potent congener, 1-[(4-tert-butylbenzyl)(cyclopropyl)amino]-2-(2,4-difluorophenyl)-3-(1H-1,2,4-triazol-1-yl)propan-2-ol I (R2 = H, R4 = CMe3), was found to exhibit a broad antifungal spectrum, being more active against Candida albicans, Candida tropicalis, Cryptococcus neoformans, Microsporum canis, and Trichophyton rubrum (MIC80<0.125 μg/mL) than the standard clin. drug itraconazole. The observed affinities of the lead mols. towards CYP51 indicate that a cyclopropyl residue enhances binding to the target enzyme. These results may provide some guidance for the development of novel triazole-based antifungal lead structures.

Chemistry & Biodiversity 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 C13H12BClO3, Related Products of triazoles.

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

Jiang, Zhigan’s team published research in European Journal of Medicinal Chemistry in 82 | CAS: 86386-77-8

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, Recommanded Product: 1-((2-(2,4-Difluorophenyl)oxiran-2-yl)methyl)-1H-1,2,4-triazole methanesulfonate.

Jiang, Zhigan published the artcileDesign, synthesis and antifungal activity of novel triazole derivatives containing substituted 1,2,3-triazole-piperidine side chains, Recommanded Product: 1-((2-(2,4-Difluorophenyl)oxiran-2-yl)methyl)-1H-1,2,4-triazole methanesulfonate, the publication is European Journal of Medicinal Chemistry (2014), 490-497, database is CAplus and MEDLINE.

Due to increasing incidence of invasive fungal infections and severe drug resistance to triazole antifungal agents, a series of novel antifungal triazoles with substituted triazole-piperidine side chains was designed and synthesized. Most of the target compounds showed good inhibitory activity against a variety of clin. important fungal pathogens. In particular, compounds I (R = Ac or OCF3) were highly active against Candida albicans and Cryptococcus neoformans with MIC values in the range of 0.125 μg/mL to 0.0125 μg/mL. They represent promising leads for the development of new generation of triazole antifungal agents. Mol. docking studies revealed that the target compounds interacted with CACYP51 mainly through hydrophobic and Van der Waals interactions.

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, 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