Literature DB >> 22579483

S-Adenosylhomocysteine hydrolase of the protozoan parasite Trichomonas vaginalis: potent inhibitory activity of 9-(2-deoxy-2-fluoro-β,D-arabinofuranosyl)adenine.

Ajit Shokar1, Aaron Au, Seung Hwan An, Elsie Tong, Gabriel Garza, Jessica Zayas, Stanislaw F Wnuk, Kirkwood M Land.   

Abstract

In the present study, we carried out a structure-activity analysis in Trichomonas vaginalis of a series of adenosine and uridine analogues. The most potent compounds were found to be 2' and 3' modified adenosine analogues some of which are potent inhibitors of S-adenosylhomocysteine hydrolase. The 9-(2-deoxy-2-fluoro-β,D-arabinofuranosyl)adenine compound was more potent than metronidazole, a current FDA approved and commonly prescribed drug for treatment of trichomoniasis. Its IC(50) was 0.09 μM compared to 0.72 μM for metronidazole.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID: 22579483     DOI: 10.1016/j.bmcl.2012.03.087

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


  4 in total

1.  Comprehensive characterization of purine and pyrimidine transport activities in Trichomonas vaginalis and functional cloning of a trichomonad nucleoside transporter.

Authors:  Manal J Natto; Yukiko Miyamoto; Jane C Munday; Tahani A AlSiari; Mohammed I Al-Salabi; Neils B Quashie; Anthonius A Eze; Lars Eckmann; Harry P De Koning
Journal:  Mol Microbiol       Date:  2021-11-20       Impact factor: 3.501

2.  Deazapurine Nucleoside Analogues for the Treatment of Trichomonas vaginalis.

Authors:  Manal J Natto; Fabian Hulpia; Eric R Kalkman; Susan Baillie; Amani Alhejeli; Yukiko Miyamoto; Lars Eckmann; Serge Van Calenbergh; Harry P de Koning
Journal:  ACS Infect Dis       Date:  2021-05-11       Impact factor: 5.578

3.  Hormopriming to Mitigate Abiotic Stress Effects: A Case Study of N 9-Substituted Cytokinin Derivatives With a Fluorinated Carbohydrate Moiety.

Authors:  Magdaléna Bryksová; Andrea Hybenová; Alba E Hernándiz; Ondřej Novák; Aleš Pěnčík; Lukáš Spíchal; Nuria De Diego; Karel Doležal
Journal:  Front Plant Sci       Date:  2020-12-10       Impact factor: 5.753

Review 4.  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

  4 in total

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