Anti-trachoma activity of rifampicin and rifamycin SV derivatives

Yechiel Becker*, Yael Asher, Nehama Himmel, Zichriya Zakay-Rones

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

8 Scopus citations

Abstract

RIFAMPICIN effectively inhibits the replication of trachoma agents both in infected cell cultures in vitro1 and in embryonated eggs in vivo2. It acts during the initial developmental stages, characterized by active RNA synthesis3. The anti-trachoma inhibitory effect of rifampicin exceeded that of rifamycin SV1,2, indicating that the presence of a hydrazone sidechain in carbon 3 of the chromophoric part of rifamycin SV might be concerned in the activity. To determine the function of the side chain, we have compared the effect of four compounds synthesized by adding to the formyl-rifamycin derivative of rifamycin SV different side chains at carbon 3. We have found that the presence of a hydrazone side chain in the rifamycin SV molecule enhanced the anti-trachoma activity of the drug in vitro and was essential for the inhibition of trachoma agent in vivo.

Original languageEnglish
Pages (from-to)454-455
Number of pages2
JournalNature
Volume225
Issue number5231
DOIs
StatePublished - 1970

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