Abstract
M. tuberculosis, M. bovis and M. avium infections cause the most important mycobacterioses leading to increased mortality in patients with AIDS. Various 5-substituted 2-deoxyuridines, arabinouridines, arabinocytidines and 2-arabinofluoro-2-deoxyuridines were synthesized and evaluated for their in vitro inhibitory activity against M. bovis, M. tuberculosis and M. avium. 5-(C-1 Substituted)-2-deoxyuridine derivatives emerged as potent inhibitors of M. avium (MIC50 = 1-10 μg/mL range); 5-(1-azidovinyl)-2-deoxyuridine being the most active (MIC50 = 1-5 μg/mL range). The nature of C-5 substituents appeared to be a determinant of anti-mycobacterial activity.
Keywords: anti-microbial agent, heterocycle, Tuberculosis
Medicinal Chemistry
Title: In vitro Anti-Mycobacterial Activities of Various 2-Deoxyuridine, 2- Arabinouridine and 2-Arabinofluoro-2-deoxyuridine Analogues: Synthesis and Biological Studies
Volume: 2 Issue: 3
Author(s): Rakesh Kumar, Dennis Y. Kunimoto, Tracey Manning and Naveen C. Srivastav
Affiliation:
Keywords: anti-microbial agent, heterocycle, Tuberculosis
Abstract: M. tuberculosis, M. bovis and M. avium infections cause the most important mycobacterioses leading to increased mortality in patients with AIDS. Various 5-substituted 2-deoxyuridines, arabinouridines, arabinocytidines and 2-arabinofluoro-2-deoxyuridines were synthesized and evaluated for their in vitro inhibitory activity against M. bovis, M. tuberculosis and M. avium. 5-(C-1 Substituted)-2-deoxyuridine derivatives emerged as potent inhibitors of M. avium (MIC50 = 1-10 μg/mL range); 5-(1-azidovinyl)-2-deoxyuridine being the most active (MIC50 = 1-5 μg/mL range). The nature of C-5 substituents appeared to be a determinant of anti-mycobacterial activity.
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Cite this article as:
Kumar Rakesh, Kunimoto Y. Dennis, Manning Tracey and Srivastav C. Naveen, In vitro Anti-Mycobacterial Activities of Various 2-Deoxyuridine, 2- Arabinouridine and 2-Arabinofluoro-2-deoxyuridine Analogues: Synthesis and Biological Studies, Medicinal Chemistry 2006; 2 (3) . https://dx.doi.org/10.2174/157340606776930745
DOI https://dx.doi.org/10.2174/157340606776930745 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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