English (United Kingdom)

https://curated-unify.zendy.io/wp-json/zendy-region/v1/featured_content/oa?rat=en

https://curated-unify.zendy.io/wp-json/zendy-region/v1/highlighted_journal/

Global: Zendy Plus annual

Presents the access of premium content as premium feature

Premium Content

Presents the keyphrase highlighting as premium feature

Keyphrase Highlighting

Presents the summarisation as premium feature

Summarisation

Insights

Presents the pdf analysis as premium feature

PDF Analysis

Presents the zaia usage as premium feature

ZAIA

Global: Zendy Plus monthly

Global: Zendy Tools annual

Global: Zendy Tools monthly

Global: Zendy Free Plan

Background  Tuberculosis (TB) caused by  Mycobacterium tuberculosis  is the leading cause of death from a bacterial infection. The 4-aminopiperidine (PIP) series has been reported as having anti-bacterial activity against  M. tuberculosis . We explored this series for its potential to inhibit aerobic growth of  M. tuberculosis . We examined substitution at the N-1 position and C-4 position of the piperidine and modifications of the piperidine moiety systematically to delineate structure-activity relationships influencing potency. Compounds were tested for growth-inhibitory activity against virulent  M. tuberculosis . A selected set of compounds were also tested for its activity against  Staphylococcus aureus .    Results  The compound with a norbornenylmethyl substituent at the N-1 position and N-benzyl-N-phenethylamine at the C-4 position of the piperidine ( 1 ) was the only active compound with a minimum inhibitory concentration (MIC) of 10 μM against  M. tuberculosis . Compounds were not active against  S. aureus .    Conclusions  We were unable to derive any other analogs with MIC < 20 μM against  M. tuberculosis . Therefore we conclude that the lack of activity is a liability in this series precluding it from further development.

The 4-aminopiperidine series has limited anti-tubercular and anti-staphylococcus aureus activity