Antimycobacterial Activity: Synthesis and Biological Evaluation of Novel Substituted (3E,5E)-3,5-diarylidene-1-phenethylpiperidine-4-one Derivatives

Title:Antimycobacterial Activity: Synthesis and Biological Evaluation of Novel Substituted (3E,5E)-3,5-diarylidene-1-phenethylpiperidine-4-one Derivatives

Volume: 10 Issue: 5

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

Affiliation:

Keywords: Antimycobacterial activity, Piperidone, Antituberculosis, High Throughput Screening

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.

Cite this article as:

Ashraf Ali Mohamed, Sanjeevi Lakshmipathi Venu, Beevi Farzana, Suresh Kumar Raju, Ismail Rusli, Soo Choon Tan, Chee Wei Ang, Keng Yoon Yeong and Basiri Alireza, Antimycobacterial Activity: Synthesis and Biological Evaluation of Novel Substituted (3E,5E)-3,5-diarylidene-1-phenethylpiperidine-4-one Derivatives, Letters in Drug Design & Discovery 2013; 10 (5) . https://dx.doi.org/10.2174/1570180811310050015