Synthesis and in vitro anti-mycobacterial activity of 5-substituted pyrimidine nucleosides |
| |
Authors: | Johar Monika Manning Tracey Kunimoto Dennis Y Kumar Rakesh |
| |
Institution: | aDepartment of Laboratory Medicine and Pathology, 1-71 Medical Sciences Building, University of Alberta, Edmonton, AB, Canada T6G 2H7 bDepartment of Medicine, Faculty of Medicine and Dentistry, University of Alberta, Edmonton, AB, Canada T6G 2H7 |
| |
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 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. |
| |
Keywords: | Tuberculosis Heterocycle Anti-microbial agent |
本文献已被 ScienceDirect PubMed 等数据库收录! |
|