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

Autor: Ashraf Ali, Mohamed, Sanjeevi Lakshmipathi, Venu, Beevi, Farzana, Suresh Kumar, Raju, Ismail, Rusli, Soo Choon, Tan, Chee Wei, Ang, Keng Yoon, Yeong, Basiri, Alireza
Zdroj: Letters in Drug Design & Discovery; June 2013, Vol. 10 Issue: 5 p471-476, 6p
Abstrakt: 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 30M. 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 M.
Databáze: Supplemental Index