Synthesis and antimycobacterial evaluation of natural oridonin and its enmein-type derivatives.

Fitoterapia

State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, China; Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, China. Electronic address:

Published: December 2014

AI Article Synopsis

Article Abstract

A series of enmein-type derivatives were synthesized and assayed for their antimycobacterial effects. The structures of the synthesized compounds were established by (1)H NMR, (13)C NMR and mass spectral analysis. All the compounds were screened for their antimycobacterial properties against Mycobacterium phlei, Mycobacterium smegmatis and Mycobacterium marinum. Compounds 2, 6g and 6i were found to exhibit potent antimycobacterial activity against M. phlei at a concentration of 0.5 μg/mL, which was comparable to that of positive drug streptomycin. Furthermore, five compounds were tested against Mycobacterium tuberculosis H₃₇Rv based on the promising preliminary screening results. Among them, compound 10 showed potent activity with IC₅₀ value of 17.1 μg/mL against M. tuberculosis H₃₇Rv strain. Thus, compound 10 could emerge as a promising lead for further research work.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.fitote.2014.10.005DOI Listing

Publication Analysis

Top Keywords

enmein-type derivatives
8
tuberculosis h₃₇rv
8
synthesis antimycobacterial
4
antimycobacterial evaluation
4
evaluation natural
4
natural oridonin
4
oridonin enmein-type
4
derivatives series
4
series enmein-type
4
derivatives synthesized
4

Similar Publications

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!