In vitro Anti-Mycobacterial Activities of Various 2-Deoxyuridine, 2- Arabinouridine and 2-Arabinofluoro-2-deoxyuridine Analogues: Synthesis and Biological Studies

Author(s): Rakesh Kumar, Dennis Y. Kunimoto, Tracey Manning, Naveen C. Srivastav

Journal Name: Medicinal Chemistry

Volume 2 , Issue 3 , 2006

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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

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Article Details

Year: 2006
Page: [287 - 293]
Pages: 7
DOI: 10.2174/157340606776930745
Price: $65

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