Synthesis and evaluation of thymidine-5′- O-monophosphate analogues as inhibitors of Mycobacterium tuberculosis thymidylate kinase

Abstract

A number of 2′- and 3′-modified thymidine 5′- O-monophosphate analogues were synthesized as potential leads for new anti-mycobacterial drugs. Evaluation of their affinity for Mycobacterium tuberculosis thymidine monophosphate kinase showed that a 2′-halogeno substituent and a 3′-azido function are the most favorable leads for further development of potent inhibitors of this enzyme.