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.
Keywords: Antimycobacterial activity, Piperidone, Antituberculosis, High Throughput Screening
Letters in Drug Design & Discovery
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.
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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
DOI https://dx.doi.org/10.2174/1570180811310050015 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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