89082-07-5Relevant academic research and scientific papers
Synthesis and Antimicrobial Activity of Novel 2-Substituted Phenoxy-N-(4-substituted Phenyl-5-(1H-1,2,4-triazol-1-yl)thiazol-2-yl)acetamide Derivatives
Liao, Guo-Ping,Zhou, Xia,Xiao, Wei,Xie, Yan,Jin, Lin-Hong
, p. 1506 - 1513 (2017/03/27)
A series of 2-substituted phenoxy-N-(4-substituted phenyl-5-(1H-1,2,4-triazol-1-yl)thiazole-2-yl)acetamide derivatives 8a, 8b, 8c, 8d, 8e, 8f, 8g, 8h, 8i, 8j, 8k, 8l, 8m, 8n, 8o, 8p, 8q, 8r, 8s, 8t was synthesized by the reaction of phenoxyacetyl chloride 7 with intermediate 4-substituted phenyl-5-(1H-1,2,4-triazol-1-yl)thiazol-2-amine 5. Their structures were confirmed by 1H NMR, 13C NMR, MS, IR, and elemental analyses. The synthesized compounds were also screened for their antimicrobial activity against three types of plant fungi (Gibberella zeae, Phytophthora infestans, and Paralepetopsis sasakii) and two kinds of bacteria [Xanthomonas oryzae pv. oryzae (Xoo) and Xanthomonas axonopodis pv. citri (Xac)] showing promising results. In particular, 8b, 8f, 8g, and 8h exhibited excellent antibacterial activity against Xoo, with 50% effective concentration (EC50) values of 35.2, 80.1, 62.5, and 82.1 μg/mL, respectively, which are superior to the commercial antibacterial agent bismerthiazol (89.9 μg/mL). The preliminary structure–activity relationship studies of these compounds are also briefly described.
Synthesis and antifungal activity of phenacyl azoles
Nelson, Ronald,Kesternich, Vctor,Perz-Fehrmann, Marcia,Salazar, Fernanda,Marcourt, Laurence,Christen, Philippe,Godoy, Patricio
, p. 549 - 552 (2014/12/11)
A new N-(4-methoxyphenacyl)imidazole and three new substituted N-(phenacyl)triazoles were prepared by reaction of the heterocycle with a phenacyl halide. The former ketone and one example of the latter were reduced to the corresponding alcohols. All six compounds were screened in vitro for antifungal activity against two pathogenic fungal strains, Candida albicans (fluconazole-resistant) and Aspergillus fumigatus. The results revealed that most of the compounds showed activity against both strains at 100 μg mL-1and 80 μg mL-1, some comparable with control compound fluconazole. The alcohols were less active than the corresponding ketones.
Synthesis and spectral characterization of some new thiazolyl-pyrazolines bearing 1,2,4-triazole moiety
Chen, Sheng-Qin,Zhang, Yi-Chao,Liu, Fang-Ming
body text, p. 319 - 325 (2011/04/26)
Chemical Equation Presented In this study, several new 1-(4-aryl-5- triazolyl-2-thiazolyl)-3,5-diaryl-2-pyrazolines (3a-r) were synthesized by reacting 3,5-diaryl1-thiocarbamoyl-2-pyrazolines (1) with 2-bromo-1-aryl-2-(1H- 1,2,4-triazol-1-yl) ethanones (2) in boiling ethanol. The chemical structures of the compounds were verified by IR, 1H NMR, ESI-MS spectroscopic data, and elemental analyses. Copyright Taylor & Francis Group, LLC.
Synthesis, structure, and biological activity of novel 1H-1,2,4-triazol-1- yl-thiazole derivatives
Ling, Shao,Xin, Zhou,Qing, Zhang,Jian-Bing, Liu,Zhong, Jin,Jian-Xin, Fang
, p. 199 - 207 (2007/10/03)
2-Amino-4-aryl-5-(1H-1,2,4-triazol-1-yl)thiazole derivatives were synthesized from the reaction of α-bromo substituted acetophenone and thiourea. The structures were confirmed by elemental analysis, 1H NMR and single crystal X-ray diffraction analysis. Biological evaluation showed that some of them possess antifungal and plant growth regulatory activities. Copyright Taylor & Francis Group, LLC.
Synthesis and QSAR studies of novel triazole compounds containing thioamide as potential antifungal agents
Wei, Qing-Li,Zhang, Shu-Sheng,Gao, Jun,Li, Wei-hua,Xu, Liang-Zhong,Yu, Zhi-Gang
, p. 7146 - 7153 (2007/10/03)
Eighteen novel triazole compounds containing thioamide were designed and synthesized. Their structures were confirmed by elemental analysis, 1H NMR, IR, and MS. The title compounds exhibited certain antifungal activity. And the geometry structures of the title compounds were optimized by means of the density functional theory (DFT) method at B3LYP/6-31G* level. The quantitative structure-activity relationship (QSAR) of the title compounds was systematically investigated. A correlative equation between FA and DELH, V was well established by using the multiple linear regression (MLR).
Synthesis and biological activities of new 1H-1,2,4-triazole derivatives containing ferrocenyl moiety
Liu, Jianbing,Li, Lichun,Dai, Hong,Liu, Zhun,Fang, Jianxin
, p. 2686 - 2690 (2007/10/03)
Some new 1H-1,2,4-triazole derivatives containing ferrocenyl moiety were synthesized in various yields by the condensation of ferrocenecarboxaldehyde with 1-(1H-1,2,4-triazol-1-yl)-3-aryl-2-one in toluene. Their structures of all these new compounds have been confirmed with 1H NMR, IR, MS and elemental analysis. Their results of bioassay showed that some title compounds exhibited some degree of antifungal and plant growth regulatory activities.
Synthesis and systemic fungicidal activity of silicon-containing azole derivatives
Itoh, Hiroyuki,Yoneda, Rieko,Tobitsuka, Junzo,Matsuhisa, Tadashi,Kajino, Hisaki,Ohta, Hiroshi,Hayashi, Noriki,Takahi, Yukiyoshi,Tsuda, Mikio,Takeshiba, Hideo
, p. 1148 - 1153 (2007/10/03)
A new series of azole derivatives containing silicon were synthesized and evaluated for fungicidal activity against rice sheath blight by submerged application. Among them, 2-(4-fluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-3-trimethylsilylpropan-2-ol (9a) exhibited satisfactory efficacy at 12.5 grams per 10 ares.
Characterization of the tautomeric equilibrium of triazolium ylids by NMR spectroscopy
Surpateanu, G.,Lungu, N. C.,Avarvari, N.,Lablache-Combier, A.,Grandclaudon, P.,Couture, A.
, p. 1648 - 1657 (2007/10/02)
The monitoring by 1H NMR of the kinetics of the tautomeric equilibrium between the triazolium ylids 1f-h and 2f-h confirms the existence of a dynamic equilibrium and corroborates the results obtained by the chemically induced perturbation of the equilibri
Synthesis and Antifungal Activity of a Series of Novel 1,2-Disubstituted Propenones
Ogata, Masaru,Matsumoto, Hiroshi,Kida, Shiro,Shimizu, Sumio,Tawara, Katsuya,Kawamura, Yoshimi
, p. 1497 - 1502 (2007/10/02)
To find an antifungal agent other than those of the imidazole and triazole series, a new class of 1,2-disubstituted propenones I and II was prepared and tested for antifungal activity.Comparison of the structure-activity relationships showed that the conjugated structure of carbonyl and exomethylene groups in I and II plays an important role in potent antifungal acivity.However, it is noteworthy that compounds 53, 54, and 56, which have a hydroxymethyl or methoxymethyl group instead of an exo-methylene group in I, also showed potent activity.Although many compounds exhibited strong antifungal activity in vitro, none showed activity in vivo of oral efficacy against subacute systemic candidiasis in mice. '
