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

[ Vol. 2 , Issue. 3 ]

Author(s):

Rakesh Kumar, Dennis Y. Kunimoto, Tracey Manning and Naveen C. Srivastav   Pages 287 - 293 ( 7 )

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

Affiliation:

Department of LaboratoryMedicine and Pathology, 1-41, Medical Sciences Building, Faculty ofMedicine and Dentistry, University of Alberta, Edmonton, AB, Canada T6G2H7.



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