Antimycobacterial activity: Synthesis and biological evaluation of novel substituted (3E,5E)-3,5-diarylidene-1-phenethylpiperidine-4-one derivatives

Mohamed Ashraf Ali, Venu Sanjeevi Lakshmipathi, Farzana Beevi, Raju Suresh Kumar, Rusli Ismail, Tan Soo Choon, Ang Chee Wei, Yeong Keng Yoon, Alireza Basiri

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Abstract

A series of 14-diarylidene-1-phenethylpiperidine-4-one derivatives were synthesized using Claisen-Schmidt condensation reactions. The synthesized compounds were screened for their antimycobacterial activity against Mycobacterium tuberculosis (MTB) H37Rv using High Throughput Screen (HTS) using an assay adapted from the microdilution alamarBlue (AB) broth assay reported by Collins and Franzblau and additionally an alternative method for end-point detection was assessed using the Promega reagent BacTiter-Glo™ Microbial Cell Viability (BTG). Most of the compounds showed low-to-moderate activity with MIC of less than 30μM. Compound (3d) (3E,5E)-3,5-bis (4- triflouromethylbenzyledene)- 1-phenethylpiperidin-4-one was found to be the most active with MIC of 27.00 μM.

Original languageEnglish
Pages (from-to)471-476
Number of pages6
JournalLetters in Drug Design and Discovery
Volume10
Issue number5
DOIs
Publication statusPublished - Jun 2013
Externally publishedYes

Keywords

  • Antimycobacterial activity
  • Antituberculosis
  • High Throughput Screening
  • Piperidone

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