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

An approach toward the synthesis of novel conjugates of 3,5-bis (arylidene)-4-piperidones (DAP) pharmacophore with amide-linkage has been developed  via  one-pot multicomponent reaction of aryl aldehydes, piperidinone and 2-chloro- N -phenylacetamide using [Et 3 NH][HSO 4 ] as a catalyst/medium. Both substitutions on arylidene rings and piperidinone nitrogen (substituted 2-chloro- N -phenylacetamide) were varied. The synthesized conjugates were evaluated for their  in vitro  antitubercular activity against  M. tuberculosis  H 37 Ra ( MTB ) and  M. bovis  BCG strains. Among the series, compounds  4f ,  4g, 4i  and  4j  showed remarkable broad spectrum antitubercular activity with low IC 50  values. Furthermore, computer docking simulations, for the most active conjugates were performed with the active site of mycobacterial enoyl-acyl carrier protein reductase (InhA) support the antitubercular activity. Lower cytotoxicity, high potency and promising activity against  MTB  and  M. Bovis  BCG suggest that amide linked DAP could serve as good leads for further modifications and development.

Amide-Linked Monocarbonyl Curcumin Analogues: Efficient Synthesis, Antitubercular Activity and Molecular Docking Study