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

doi:10.2174/1570180811310050015

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

Research output: Contribution to journal › Article › Research › peer-review

3 Citations (Scopus)

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 language	English
Pages (from-to)	471-476
Number of pages	6
Journal	Letters in Drug Design and Discovery
Volume	10
Issue number	5
DOIs	https://doi.org/10.2174/1570180811310050015
Publication status	Published - Jun 2013
Externally published	Yes

Keywords

Antimycobacterial activity
Antituberculosis
High Throughput Screening
Piperidone

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.2174/1570180811310050015

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Ali, M. A., Lakshmipathi, V. S., Beevi, F., Kumar, R. S., Ismail, R., Choon, T. S., Wei, A. C., Yoon, Y. K., & Basiri, A. (2013). Antimycobacterial activity: Synthesis and biological evaluation of novel substituted (3E,5E)-3,5-diarylidene-1-phenethylpiperidine-4-one derivatives. Letters in Drug Design and Discovery, 10(5), 471-476. https://doi.org/10.2174/1570180811310050015

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

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{\texttrademark} 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, Antituberculosis, High Throughput Screening, Piperidone",

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

year = "2013",

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doi = "10.2174/1570180811310050015",

language = "English",

volume = "10",

pages = "471--476",

journal = "Letters in Drug Design and Discovery",

issn = "1570-1808",

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Antimycobacterial activity: Synthesis and biological evaluation of novel substituted (3E,5E)-3,5-diarylidene-1-phenethylpiperidine-4-one derivatives. / Ali, Mohamed Ashraf; Lakshmipathi, Venu Sanjeevi; Beevi, Farzana et al.
In: Letters in Drug Design and Discovery, Vol. 10, No. 5, 06.2013, p. 471-476.

Research output: Contribution to journal › Article › Research › peer-review

TY - JOUR

T1 - Antimycobacterial activity

T2 - Synthesis and biological evaluation of novel substituted (3E,5E)-3,5-diarylidene-1-phenethylpiperidine-4-one derivatives

AU - Ali, Mohamed Ashraf

AU - Lakshmipathi, Venu Sanjeevi

AU - Beevi, Farzana

AU - Kumar, Raju Suresh

AU - Ismail, Rusli

AU - Choon, Tan Soo

AU - Wei, Ang Chee

AU - Yoon, Yeong Keng

AU - Basiri, Alireza

PY - 2013/6

Y1 - 2013/6

N2 - 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.

AB - 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.

KW - Antimycobacterial activity

KW - Antituberculosis

KW - High Throughput Screening

KW - Piperidone

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

Abstract

Keywords

UN SDGs

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