Article

Synthesis and in vitro anti-mycobacterial activity of 5-substituted pyrimidine nucleosides.

Department of Laboratory Medicine and Pathology, 1-71 Medical Sciences Building, University of Alberta, Edmonton, AB, Canada T6G 2H7.
Bioorganic & Medicinal Chemistry (impact factor: 2.92). 01/2006; 13(24):6663-71. DOI:10.1016/j.bmc.2005.07.046 pp.6663-71
Source: PubMed

ABSTRACT 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 (MIC90 = 1-5 microg/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.

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Keywords

2'-deoxyuridine series
 
2'-ribofluoro-2'-deoxyuridines
 
5-(C-1 Substituted)-2'-deoxyuridine derivatives
 
anti-mycobacterial activity
 
C-5 substituents
 
inhibitors
 
M. avium
 
M. bovis
 
mycobacterioses
 
Mycobacterium avium infections cause
 
potent inhibitors
 
Various 5-substituted 2'-deoxyuridines
 
vitro inhibitory activity