Literature DB >> 19231179

Design, synthesis, and biological evaluation of novel 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted benzylamino-2-propanols.

Xiaoyun Chai1, Jun Zhang, Shichong Yu, Honggang Hu, Yan Zou, Qingjie Zhao, Zhigang Dan, Dazhi Zhang, Qiuye Wu.   

Abstract

Based on the results of computational docking to the active site of the cytochrome P450 14alpha-demethylase (CYP51), a series of 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted benzylamino-2-propanols as analogs of fluconazole were designed, synthesized, and evaluated as antifungal agents. Results of preliminary antifungal tests against eight human pathogenic fungi in vitro showed that all the title compounds exhibited excellent activities with broad spectrum.

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Year:  2009        PMID: 19231179     DOI: 10.1016/j.bmcl.2009.01.048

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  6 in total

1.  Chemoenzymatic Synthesis, Nanotization, and Anti-Aspergillus Activity of Optically Enriched Fluconazole Analogues.

Authors:  Shashwat Malhotra; Seema Singh; Neha Rana; Shilpi Tomar; Priyanka Bhatnagar; Mohit Gupta; Suraj K Singh; Brajendra K Singh; Anil K Chhillar; Ashok K Prasad; Christophe Len; Pradeep Kumar; Kailash C Gupta; Anjani J Varma; Ramesh C Kuhad; Gainda L Sharma; Virinder S Parmar; Nigel G J Richards
Journal:  Antimicrob Agents Chemother       Date:  2017-07-25       Impact factor: 5.191

2.  3,5-Bis(4-methoxy-phen-yl)-1H-1,2,4-triazole monohydrate.

Authors:  Hai-Ying Wang; Jian-Ping Ma; Ru-Qi Huang; Yu-Bin Dong
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2009-05-14

3.  Synthesis and Antifungal Activity of Novel Myrtenal-Based 4-Methyl-1,2,4-triazole-thioethers.

Authors:  Gui-Shan Lin; Wen-Gui Duan; Lin-Xiao Yang; Min Huang; Fu-Hou Lei
Journal:  Molecules       Date:  2017-01-24       Impact factor: 4.411

4.  N-Phenacyldibromobenzimidazoles-Synthesis Optimization and Evaluation of Their Cytotoxic Activity.

Authors:  Anna Kowalkowska; Konrad Chojnacki; Maciej Multan; Jan K Maurin; Edyta Łukowska-Chojnacka; Patrycja Wińska
Journal:  Molecules       Date:  2022-07-07       Impact factor: 4.927

5.  Triazole derivatives with improved in vitro antifungal activity over azole drugs.

Authors:  Shichong Yu; Xiaoyun Chai; Yanwei Wang; Yongbing Cao; Jun Zhang; Qiuye Wu; Dazhi Zhang; Yuanying Jiang; Tianhua Yan; Qingyan Sun
Journal:  Drug Des Devel Ther       Date:  2014-04-10       Impact factor: 4.162

6.  Synthesis, antimicrobial, and anti-inflammatory activity, of novel S-substituted and N-substituted 5-(1-adamantyl)-1,2,4-triazole-3-thiols.

Authors:  Ebtehal S Al-Abdullah; Hanadi H Asiri; Siham Lahsasni; Elsayed E Habib; Tarek M Ibrahim; Ali A El-Emam
Journal:  Drug Des Devel Ther       Date:  2014-05-12       Impact factor: 4.162

  6 in total

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