Antimycobacterial activities of 5-alkyl (or halo)-3'-substituted pyrimidine nucleoside analogs

Naveen C Srivastav; Neeraj Shakya; Sudha Bhavanam; Amogh Agrawal; Chris Tse; Nancy Desroches; Dennis Y Kunimoto; Rakesh Kumar

doi:10.1016/j.bmcl.2011.11.114

Antimycobacterial activities of 5-alkyl (or halo)-3'-substituted pyrimidine nucleoside analogs

Bioorg Med Chem Lett. 2012 Jan 15;22(2):1091-4. doi: 10.1016/j.bmcl.2011.11.114. Epub 2011 Dec 4.

Authors

Naveen C Srivastav¹, Neeraj Shakya, Sudha Bhavanam, Amogh Agrawal, Chris Tse, Nancy Desroches, Dennis Y Kunimoto, Rakesh Kumar

Affiliation

¹ Department of Laboratory Medicine and Pathology, 1-71 Medical Sciences Building, Edmonton, AB, Canada T6G 2H7.

PMID: 22178557
DOI: 10.1016/j.bmcl.2011.11.114

Abstract

Several 5-alkyl (or halo)-3'-azido (amino or halo) analogs of pyrimidine nucleosides have been synthesized and evaluated against Mycobacterium bovis, Mycobacterium tuberculosis and Mycobacterium avium. Among these compounds, 3'-azido-5-ethyl-2',3'-dideoxyuridine (3) was found to have significant antimycobacterial activities against M. bovis (MIC(50)=1μg/mL), M. tuberculosis (MIC(50)=10μg/mL) and M. avium (MIC(50)=10μg/mL).

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Anti-Bacterial Agents / chemical synthesis
Anti-Bacterial Agents / chemistry
Anti-Bacterial Agents / pharmacology*
Dose-Response Relationship, Drug
Microbial Sensitivity Tests
Molecular Structure
Mycobacterium / drug effects*
Pyrimidine Nucleosides / chemical synthesis
Pyrimidine Nucleosides / chemistry
Pyrimidine Nucleosides / pharmacology*
Stereoisomerism
Structure-Activity Relationship

Substances

Anti-Bacterial Agents
Pyrimidine Nucleosides