101039-85-4Relevant articles and documents
Synthesis and in vitro anti-mycobacterial activity of 5-substituted pyrimidine nucleosides
Johar, Monika,Manning, Tracey,Kunimoto, Dennis Y.,Kumar, Rakesh
, p. 6663 - 6671 (2007/10/03)
Mycobacterium tuberculosis and Mycobacterium avium infections cause the two most important mycobacterioses, leading to increased mortality in patients with AIDS. Various 5-substituted 2′-deoxyuridines, uridines, 2′-O-methyluridine, 2′-ribofluoro-2′-deoxyuridines, 3′-substituted-2′,3′-dideoxy uridines, 2′,3′- dideoxyuridines, and 2′,3′-didehydro-2′,3′- dideoxyuridines were synthesized and evaluated for their in vitro inhibitory activity against M. bovis and M. avium. 5-(C-1 Substituted)-2′- deoxyuridine derivatives emerged as potent inhibitors of M. avium (MIC 90 = 1-5 μg/mL range). The nature of C-5 substituents in the 2′-deoxyuridine series appeared to be a determinant of anti-mycobacterial activity. This new class of inhibitors could serve as useful compounds for the design and study of new anti-tuberculosis agents.
