| Literature DB >> 17070048 |
Keith D Combrink1, Daniel A Denton, Susan Harran, Zhenkun Ma, Katrina Chapo, Dalai Yan, Eric Bonventre, Eric D Roche, Timothy B Doyle, Gregory T Robertson, Anthony S Lynch.
Abstract
A novel series of 3-morpholino rifamycins in which the C25 acetate group was replaced by a carbamate group were prepared and found to exhibit significantly improved antimicrobial activity than rifampin against Mycobacterium smegmatis. Further characterization of such compounds suggests that relatively large groups attached to the rifamycin core via a C25 carbamate linkage prevent inactivation via ribosylation of the C23 alcohol as catalyzed by the endogenous rifampin ADP-ribosyl transferase of M. smegmatis. SAR studies of the C25 carbamate rifamycin series against M. smegmatis and other bacteria are reported.Entities:
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Year: 2006 PMID： 17070048 DOI： 10.1016/j.bmcl.2006.10.016
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823