Bioorganic & Medicinal Chemistry Letters 2010-06-15

Biological activity of modified and exchanged 2-amino-5-nitrothiazole amide analogues of nitazoxanide.

T Eric Ballard, Xia Wang, Igor Olekhnovich, Taylor Koerner, Craig Seymour, Paul S Hoffman, Timothy L Macdonald

Index: Bioorg. Med. Chem. Lett. 20(12) , 3537-9, (2010)

Full Text: HTML

Abstract

Head group analogues of the antibacterial and antiparasitic drug nitazoxanide (NTZ) are presented. A library of 39 analogues was synthesized and assayed for their ability to suppress growth of Helicobacter pylori, Campylobacter jejuni, Clostridium difficile and inhibit NTZ target pyruvate:ferredoxin oxidoreductase (PFOR). Two head groups assayed recapitulated NTZ activity and possessed improved activity over their 2-amino-5-nitrothiazole counterparts, demonstrating that head group modification is a viable route for the synthesis of NTZ-related antibacterial analogues.Copyright 2010 Elsevier Ltd. All rights reserved.

Related Compounds

  • 5-Nitrothiazol-2-a...

Related Articles:

Evaluation of 2-amino-5-nitrothiazole as a hypoxic cell radiosensitizer.

1982-06-01

[Radiat. Res. 90(3) , 575-85, (1982)]

Platinum complexes with one radiosensitizing ligand [PtCl2(NH3) (sensitizer)]: radiosensitization and toxicity studies in vitro.

1987-11-01

[Radiat. Res. 112(2) , 273-82, (1987)]

2-amino-5-nitrothiazole.

1983-07-01

[IARC Monogr. Eval. Carcinog. Risk Chem. Hum. 31 , 71-7, (1983)]

Reaction of 2-amino-5-nitrothiazole with palladium salts. Farrell N and Carneiro TM.

[Inorganica Chim. Acta 126(2) , 137-139, (1987)]

Analysis of Oligonucleotide and Protein via Matrix-assisted Laser Desorption/Ionization Time-of-flight Mass Spectrometry Using 2-Amino-5-nitrothiazole as an Effective Matrix [J]. ZHOU LH, et al.

[Chem. Res. Chin. Univ. 12 , 012, (2004)]

More Articles...