Literature DB >> 25999204

Synthesis and antiprotozoal activity of mono- and bis-uracil isatin conjugates against the human pathogen Trichomonas vaginalis.

Kewal Kumar1, Nicole Liu2, Donald Yang2, Daniel Na2, John Thompson2, Lisa A Wrischnik2, Kirkwood M Land3, Vipan Kumar4.   

Abstract

A library of mono- and bis-uracil isatin conjugates were synthesized and subjected for the assessment of their in vitro activity against the protozoal pathogen Trichomonas vaginalis. The structure activity studies (SAR) revealed that the bis-uracil-isatin based conjugates were more effective than their corresponding mono conjugates in inhibiting the growth of T. vaginalis at approximately 10 μM with no visual effect on mammalian cells at the same concentration. Published by Elsevier Ltd.

Entities:  

Keywords:  Cytotoxicity; Structure activity relationship; Trichomonas vaginalis; Uracil-isatin conjugates

Mesh：

Substances：

Year:  2015        PMID： 25999204     DOI： 10.1016/j.bmc.2015.04.075

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  5 in total

1.  Auranofin inactivates Trichomonas vaginalis thioredoxin reductase and is effective against trichomonads in vitro and in vivo.

Authors:  Melissa Hopper; Jeong-Fil Yun; Bianhua Zhou; Christine Le; Katelin Kehoe; Ryan Le; Ryan Hill; Gregg Jongeward; Anjan Debnath; Liangfang Zhang; Yukiko Miyamoto; Lars Eckmann; Kirkwood M Land; Lisa A Wrischnik
Journal:  Int J Antimicrob Agents       Date:  2016-11-02       Impact factor: 5.283

2.  Synthesis and Preliminary Antimicrobial Analysis of Isatin-Ferrocene and Isatin-Ferrocenyl Chalcone Conjugates.

Authors:  Amandeep Singh; Grant Fong; Jenny Liu; Yun-Hsuan Wu; Kevin Chang; William Park; Jihwan Kim; Christina Tam; Luisa W Cheng; Kirkwood M Land; Vipan Kumar
Journal:  ACS Omega       Date:  2018-05-30

3.  Highly Potent 1H-1,2,3-Triazole-Tethered Isatin-Metronidazole Conjugates Against Anaerobic Foodborne, Waterborne, and Sexually-Transmitted Protozoal Parasites.

Authors:  Sumit Kumar; Trpta Bains; Ashley Sae Won Kim; Christina Tam; Jong Kim; Luisa W Cheng; Kirkwood M Land; Anjan Debnath; Vipan Kumar
Journal:  Front Cell Infect Microbiol       Date:  2018-10-30       Impact factor: 5.293

4.  Design, Synthesis and Preliminary Antimicrobial Evaluation of N-Alkyl Chain Tethered C-5 Functionalized Bis-Isatins.

Authors:  Amandeep Singh; Trpta Bains; Hye Jee Hahn; Nicole Liu; Christina Tam; Luisa W Cheng; Jong Kim; Anjan Debnath; Kirkwood M Land; Vipan Kumar
Journal:  Medchemcomm       Date:  2017-09-19       Impact factor: 3.597

Review 5.  Recent Advances in the Discovery of Novel Antiprotozoal Agents.

Authors:  Seong-Min Lee; Min-Sun Kim; Faisal Hayat; Dongyun Shin
Journal:  Molecules       Date:  2019-10-28       Impact factor: 4.411
  5 in total

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