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